JP2008520735A - Topical skin patch - Google Patents

Abstract

The present invention provides a flexible base material having a front side and a back side, at least part of the front side of the base material, at least part of the front side of the base material, at least part of the front side of the base material and part of the base side A self-adhesive patch comprising: The formulation includes xanthophylls, a solvent that dissolves xanthophylls, and a pressure sensitive adhesive. The invention also provides methods of using adhesive patches (eg, for treating mammalian acne or pimples, for exfoliating a mammalian skin surface, and / or for improving the appearance of a mammalian skin surface). The method includes the step of applying an adhesive patch according to the present invention to a topical (skin) surface of a patient.
[Selection] Figure 10

Description

(Not mentioned in the original)

 Acne vulgaris is a comedones (blackheads papules) that appears in most areas of the skin that touch the eyes (eg, face, chest, back, neck and upper arms). ), Pustules, cysts, nodules, and often chronic scars of pilosebaceous follicles (apparatus), characterized by scars The follicular sebaceous gland organs are generally in very high concentrations in the blood during puberty and maturity and are under the control of endogenous hormones (mainly androgens) that cause excessive production of sebum. The condition can also be exacerbated by an increased rate of cornification of the horny layer (stratum corneum) of the skin, which forms a closed plug or comedone with its growth, Along with the increase in sebum secretion, It can be an ideal medium for growth of resident bacteria, such as the Gram positive anaerobic bacterium, Propionibacterium acnes. The vesicles rupture and release the contents, causing local swelling and inflammation, which may darken due to pigmentation from damaged cells deeper in the skin In severe cases, acne may require hospitalization of the patient, great pain, and prolonged scarring on the skin.

  Many treatments are available for the treatment of acne. Typically, acne is treated with topical compositions in the form of creams, gels, emulsions or lotions containing the selected drug. Such drugs include hormones, or hormone agonists and antagonists (EP A1 0 563 813 and US Pat. No. 5,439,923), antibacterial agents (US Pat. No. 4,446,145, GB 2,088,717, GB 2,090,135, GB 1,054,124, US patents) 5,409,917) salicylic acid (US Pat. No. 4,514,385, US Pat. No. 4,355,028, EP A1 0 052 705, FR-A 2,581,542, FR-A 2,607,498).

  Currently, acne drugs are administered orally for severe cases of acne. This is reviewed in "Acne, A Review of Optimum Treatment" by Sykes N.I. and Webster G. F in Drugs 48, 59-70 (1994). A number of side effects have been discussed regarding the application of oral administration of acne drugs. For example, isotretinoin, a derivative of vitamin A, has a risk associated with teratogenicity and can be problematic for women of fertile age. Oral administration of antibiotics suitable for the treatment of acne can induce the appearance of side effects, including abdominal pain, black tongue disease, cough, diarrhea, fatigue, oral inflammation and other undesirable symptoms.

  According to FDA regulations (eg 21 CFR Chapter 1, Section 333, Subpart D-Topical Acne Drug Products, April 1, 2000 Edition) and in certain amounts for the treatment of acne (ie including topical acne medication) Components that can be expressed (ie, “active ingredients”) are defined. Therefore, in compliance with FDA regulations, there are a limited number of active ingredients that can be treated with acne in a particular amount that can be included in a composition referred to as acne treatment. As a result, a topical acne drug comprising (a) a composition containing a topical acne drug that can maintain the solubility and stability of the active ingredient in the composition and (b) adherence to FDA regulations. Manufacturing becomes difficult.

  Accordingly, a novel method and composition for treating patients with acne, with minimal side effects and maximum efficacy, easy and comfortable to use, effective and known amounts of topical acne. There is a need for methods and compositions that apply acne to the skin and comply with FDA regulations.

  Accordingly, a method and apparatus for treating a patient suffering from acne with an effective and known amount of a topical acne medication that is easy to use, comfortable, with minimal side effects and maximum effectiveness. There is a need for methods and devices that are applied to the skin and comply with FDA regulations. Such devices are preferably adhesive patches that effectively control the rate of penetration and / or effectively control the depth of penetration of the ointment or gel prior to coagulation.

  Thus, what is needed is a device containing an effective amount of xanthophyll. The device is a known amount, a discrete amount, a safe amount, and an effective amount of xanthophylls. The device maintains the stability of xanthophylls over a sustained period. The instrument is also easy to use. In addition, the device is known, safe, efficient and uses xanthophylls in an easy manner, along with the treatment of local skin diseases (eg, epilepsy, skin cancer and acne) as well as other diseases ( E.g. macular degeneration, angiogenesis, cancer, heart disease and diabetes).

  The present invention is in the prevention and / or treatment of local skin diseases (eg, epilepsy, skin cancer and acne), as well as in and / or treatment of other diseases (eg, macular degeneration, angiogenesis, cancer, heart disease and diabetes). A method of using the adhesive patch is provided. Adhesive patches are known, individual, safe, and contain an effective amount of xanthophyll. Adhesive patches maintain the stability of xanthophylls over a sustained period. Adhesive patches are also easy to use.

  The invention comprises a flexible backing having a front side and a back side and at least on a part of the front side of the base, at least part of the front side of the base, at least part of the front side of the base and An adhesive patch is provided that includes a formulation disposed within the portion. The formulation includes xanthophylls, a solvent that dissolves xanthophylls, and a pressure sensitive adhesive.

  The present invention also provides a flexible substrate having a front side and a back side and at least part of the front side of the base, at least part of the front side of the base, or at least part of the front side of the base A self-adhesive patch comprising: The formulation includes xanthophylls and hot melt adhesives.

  The present invention also provides a method for locally delivering xanthophylls to the topical skin surface. The method includes applying the adhesive patch of the present invention to the skin surface for a period of time effective to deliver xanthophylls locally to the topical skin surface.

  A systemic delivery of xanthophylls to mammals. The method includes applying the adhesive patch of the present invention to the skin surface for a period of time effective to deliver xanthophylls systemically to a mammal.

  The present invention provides a method for treating or preventing acne or pimples in mammals having such a need. This method involves applying an adhesive patch according to the present invention to a skin surface of a mammal having acne or pimples or a mammal having a risk of acne or pimples for a period of time effective to treat or prevent acne or pimples. A step of applying to the skin surface.

  The present invention also provides a method for exfoliating mammalian skin surfaces. The method includes effectively peeling the skin surface by applying and removing the adhesive patch according to the present invention on the skin surface of a mammal in need of such skin peeling for an effective period of time.

  The present invention also provides a method for improving the appearance of a mammalian skin surface. The method includes the steps of applying the adhesive patch according to the present invention to a mammalian skin surface in need of such an appearance for a period effective to improve the appearance of the skin surface.

  The present invention also provides an adhesive patch according to the present invention for drug therapy.

  The present invention also provides a method of using the adhesive patch according to the present invention for the manufacture of a medicament for the treatment of topical skin conditions.

  The present invention also provides an adhesive patch according to the present invention for the manufacture of a medicament for the treatment of mammalian acne, for the treatment of mammalian pimples, for the improvement of the appearance of mammalian skin surfaces, and any combination thereof. Provide a way to use.

  The present invention provides adhesive patches and methods of cosmetic and pharmaceutical use of adhesive patches. Adhesive patches are known, individual, safe, and contain an effective amount of xanthophyll. Adhesive patches maintain the stability of xanthophylls over a sustained period. Adhesive patches are also easy to use.

  In this specification, “one embodiment”, “one embodiment”, “an example embodiment”, etc. Although referring to an embodiment that can include a particular feature, structure, or characteristic, not all embodiments need to include this particular feature, structure, or characteristic. Moreover, such terms are not necessarily referring to the same embodiment. Furthermore, when a particular feature, structure, or characteristic is described in one embodiment, such feature, structure, or characteristic is entangled in another embodiment, although not explicitly stated. The modification should be made based on the knowledge of those skilled in the art.

  The present invention provides a unique adhesive medium. This medium has pressure sensitive adhesive properties associated with its composition and viscoelasticity. The pressure-sensitive adhesive is hydrophilic, and therefore water can be dissolved in the pressure-sensitive adhesive or evaporated from the pressure-sensitive adhesive depending on the environment in which it is placed. Having such a water exchange capability means that when the adhesive is applied to the skin on a suitable porous substrate, it will not necessarily be as occlusive as many drug delivery patches. means. The occlusiveness of conventional drug delivery patches is thought to play an important role in improving drug absorption, but often also leads to skin irritation. In certain embodiments of the present invention, if the skin patch has a relatively low occlusive property, a special water-breatheable ointment or gel, such as a water washable or water soluble The use of an ointment or gel can be envisaged.

  The present invention provides an ointment or gel disposed on a substrate. Ointments or gels are known, individual, safe, and contain an effective amount of xanthophyll. Adhesive patches maintain the stability of xanthophylls over a sustained period. The substrate has flexibility and / or extensibility. Since substrates can be porous / vapor permeable or non-porous / non-vapor permeable, devices such as those described above are generally "patches" from many consumers. (Patch), "skin patch", or "adhesive skin patch". Accordingly, in this specification, such devices (ie, ointments or gels placed on a substrate) are referred to as patches, skin patches, adhesive skin patches. Those skilled in the art will appreciate that the term “patch” is used to refer to such devices and is not limiting in any way.

  It will be understood by those skilled in the art that the terms used herein include both the singular and the plural unless specifically stated otherwise. For example, “xanthophylls” 15 include a single (ie, one xanthophyll) as well as a plurality (ie, two or more xanthophylls).

As used herein, “holdout” refers to the penetration, crosslinking, wetting, penetration, crosslinking, and wetting of certain types of gels and ointments within the matrix. And refers to the physical properties of the substrate in relation to its cure ability. Certain types of gels or ointments may or may not penetrate any substrate. As the gel or ointment penetrates the substrate, the gel or ointment crosslinks, wets, or hardens within the substrate. As used herein, retention is the ability of a gel or ointment to affect the extent to which it penetrates, cross-links, wets and / or hardens within the matrix.
Substrate with good retention generally prevents, reduces or reduces the likelihood that an ointment or gel wets the substrate; generally, an ointment or gel can crosslink within a substrate matrix Generally increases the likelihood that the ointment or gel will harden within the matrix; and / or increases the likelihood that the ointment or gel will partially penetrate the matrix.

  As used herein, a “topical acne drug” is a composition or combination of compositions that effectively prevents and / or treats acne or pimples. Any suitable topical acne is acceptable provided that topical acne 15 effectively prevents and / or treats acne or pimples, and topical acne 15 remains stable in formulation 5. Acne 15 can be used. Preferably, its stability extends over a sustained period, such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transport and / or storage of Patch 1. .

  Suitable topical acne drugs are, for example, Physician's Desk Reference (PDR), Medical Economics Company (Montvale, NJ), (53rd Ed.), 1999; Mayo Medical Center Formulary, Unabridged Version, Mayo Clinic (Rochester, MN) , January 1998; Merck Index, An Encyclopedia of Chemicals, Drugs, and Biologicals, (11th Ed.), Merck & Co., Inc. (Rahway, NJ), 1989, and references therein. Suitable topical acne drugs 15 are, for example, salicylic acid, resorcinol, resorcinol acetate, calcipotriene, benzoyl peroxide, sulfur, retinol, retinoic acid, citric acid, alpha hydroxy acid, retinal, their pharmaceutically acceptable Salts, and combinations thereof. Preferably, the topical acne drug 15 is salicylic acid, or a pharmaceutically acceptable salt thereof.

  As used herein, “retinoid” refers to vitamin A or vitamin A-like compounds including, but not limited to, retinoic acid (RA), which is a natural acidic derivative of vitamin A. Retinoids play an important role in normal growth, growth and differentiation by modifying the expression of target genes.

  As used herein, “anthralin” refers to anthraquinone (anthracene 9) that restores epidermal cell proliferation and keratinization to a normal rate and reduces DNA synthesis and mitosis of the grown epidermis. , 10-quinone derivatives; anthraquinones can also be synthesized and occur naturally in aloe, Cascala sagrada, senna and diau; antimalignant mitoxantrone is a synthetic derivative), a psoriasis and other skin condition Is used locally (also called dithranol).

  As used herein, “coal tar” refers to a viscous black liquid containing a number of organic compounds obtained by cracking distillation of coal. Many useful organic products including benzene, toluene, xylene, naphthalene, anthracene and phenanthrene can be obtained by distilling coal tar into multiple fractions. These substances, called coal-tar crudes, are the starting point for the synthesis of many products, especially dyes, drugs, explosives, seasonings, perfumes, preservatives, synthetic resins and paints and dyes. It becomes. Coal tar is used medically for the treatment of eczema, psoriasis, seborrheic dermatitis and other skin diseases.

  As used herein, “salicylic acid” refers to 2-hydroxybenzoic acid (C6H4 (OH) CO2H), which is a colorless, crystalline organic carboxylic acid. Salicylic acid is used to treat many skin diseases (acne, dandruff, psoriasis, seborrheic dermatitis of the skin and scalp, sclerosis, corn, common warts and plantar warts).

  As used herein, “photochemotherapy with ultraviolet A (PUVA)” refers to a type of ultraviolet radiation therapy used for severe skin diseases ( It refers to phototherapy. PUVA is a combination therapy consisting of psoralen (P) followed by long-wave ultraviolet radiation (UVA) on the skin. Psoralen contains compounds that temporarily make the skin sensitive to UVA.

  As used herein, “phototherapy with UVB” refers to a type of radiation therapy or therapy involving irradiation of ultraviolet B (wavelength 280-315 mm) to the skin.

  In this specification, “synergize” (“synergize”) or “synergistic” means “synergistic” means that two substances work together to add their individual effects. Also refers to producing significant effects (www.webster-dictionary.org/definition/synergize).

  As used herein, “enhance” (“potentiate” or “potentiates”) means the ability of one substance to activate another substance (eg, one drug activates another drug), the ability to activate, It refers to the ability to be more effective or more active (http://www.ndif.org/Terms/potentiate.html).

  As used herein, “alleviate” means to reduce or reduce the severity or duration of a condition or the underlying symptoms of a condition, either physically or mentally, Or to attenuate.

  As used herein, “calcipotriene” refers to the synthetic topical form of vitamin D. This is related to the increase and growth of skin cells. Topical calcipotriene is used to treat chronic psoriasis vulgaris (psoriasis with scaly patches). Chemically, calcipotriene is (5Z, 7E, 22E, 24S) -24-cyclopropyl-9,10-secochola-5,7,10 (19), 22-tetraene-1α, 3 β, 24 -Triol- and the empirical formula is C27H40O3

  “Therapeutically effective amount” means, for example, the amount of xanthophylls useful in the present invention, eg, for treating acne or treating symptoms of acne in a host, or It is intended to include an amount of topical acne drug useful in the present invention, or a combination of compounds (eg, xanthophylls and topical acne drugs). The combination of compounds is preferably a synergistic combination.

  For example, as described in Chou and Talalay, Adv. Enzyme Regul., 22:27 (1984), the synergistic effect is the effect of the compound when administered in combination (eg, treatment of skin abnormalities, etc. ) Is greater than the sum of the effects when administered one by one as a single drug. In general, synergistic effects are most pronounced at concentrations below the maximum concentration of the compound. Synergistic effects are seen as lower cytotoxicity, increased activity, or other beneficial effects when using the combination compared to the individual components.

    As used herein, “acne” refers to inflammatory vesicles, papules, or pustules rashes associated with sebaceous organs. Acne is a skin disease with a large number of sebaceous glands (eg, face, upper back and chest) and characteristic lesions (eg, open comedones (black acne), closed comedones (white acne), papules, pustules or small nodules). is there. Acne is thought to result from thickening of the vesicle opening, increased sebum production, the presence of bacteria, or the host's inflammatory response. Types of acne include, for example, acne conglobata, chloracne and rosacea. For example, Stedman's Medical Dictionary, 25th Ed., Illustrated, Williams & Wilkins, Baltimore, MD, pp. 15-16 (1990) and Mosby's Medical, Nursing, & Allied Health Dictionary, (5th Ed.), Mosby: St. Louis , p.19 (1998).

  As used herein, “pimple” refers to a small papule, pustules or furnacle infection. See, for example, Mosby's Medical, Nursing, & Allied Health Dictionary, (5th Ed.), Mosby: St. Louis, p. 1267 (1998).

 As used herein, “fatty acids” are organic monobasic acids derived from hydrocarbons using a reaction equivalent to the oxidation of methyl groups to alcohols, aldehydes, and acids. Refers to that. Fatty acids can be saturated, unsaturated, or partially unsaturated.

  As used herein, “alfalfa” refers to Medicago sativa.

  In the present specification, “α-carotene” refers to a compound having the following structural formula.

  As used herein, “β-carotene” refers to a compound having the following structural formula.

  β-carotene is a precursor (prodrug) of vitamin A, and is a fat-soluble orange pigment found in many vegetables. β-carotene is converted to vitamin A in the body with an efficiency of about 50%.

  In this specification, “vitamin A” (“vitamin A”) refers to a compound of the following structural formula,

This is chemically named 3,7-dimethyl-9- (2,6,6-trimethyl-1-cyclohexen-1-yl) -2,4,6,8-nonatetraen-1-ol .

  As used herein, “cancer” includes uncontrollable division and growth, and invades and destroys other tissues and spreads (metastasizes) to other areas of the body. Types of diseases caused by such cells. If the tissue grows out of control, it can spread to distant parts of the body. Cancer has a detrimental effect on the body by: (A) destroying nearby nearby tissue (eg, causing nerve compression, erosion of blood vessels, or perforation of organs), and (b) normal in a remote location Replacement of functioning cells (eg, heart failure due to replacement of hematopoietic cells in the bone marrow, increased blood calcium concentration due to bone replacement, or increased amount of calcium in the myocardium due to bone replacement) ).

  As used herein, “ulcer” includes wrinkles that may reach depths, which may be slow healing or incurable inflammatory wrinkles.

  As used herein, “macular degeneration” includes the destruction or damage of the part known as the macula in the retina. Symptoms include blurred vision (in the middle of the field of view), dullness of color vision, and difficulty in reading or close to the eyes.

  α-Lipoic acid provides excellent antioxidant protection due to the fact that it enhances the potency of other antioxidants in the body. α-Lipoic acid can be added to the formulation 5 of the present invention in an appropriate and appropriate amount, if desired.

  Phenols such as oligomeric proanthocyanidins are incidental and useful antioxidants. Oligomeric proanthocyanidins are naturally present in moth seeds. If desired, phenols can be added to the composition according to the invention.

◆ Antibiotics Formulation 5 may contain additional antibiotics. As used herein, “antibiotic” refers to activity against either gram positive or gram negative microorganisms (ie, growth of either gram positive or gram negative microorganisms). Any compound that suppresses or disrupts development). Stedman's Medical Dictionary, Illustrated, (25th Ed.), Williams & Wilkins: Baltimore (1990), and Mosby's Medical Nursing, & Allied Health Dictionary, (5th Ed.), Mosby: St. Louis (1998).

  Suitable antibiotics are disclosed, for example, in the following. Physician's Desk Reference (PDR), Medical Economics Company (Montvale, NJ), (53rd Ed.), 1999; Mayo Medical Center Formulary, Unabridged Version, Mayo Clinic (Rochester, MN), January 1998; Merck Index, An Encyclopedia of Chemicals, Drugs, and Biologicals, (11th Ed.), Merck & Co., Inc. (Rahway, NJ), 1989; University of Wisconsin Antimicrobial Use Guide, http://www.medsch.wisc.edu/clinsci/ amcg / amcg.html; Introduction on the Use of the Antibiotics Guideline, Descriptions of Specific Antibiotic Classes, Thomas Jefferson University, http://jeffline.tju.edu/CWIS/OAC/antibiotics_guide/intro.html; References that are.

  Suitable antibiotics include, for example, aminoglycosides (aminoglycosides), β-lactam antibiotics, cephalosporins, macrolides, miscellaneous antibiotics, penicillins, tetracyclines, antifungals, antifungals, Malaria, antituberculous, antiviral, antiepileptic, miscellaneous antiinfectives, quinolones, sulfonamides, urinary tract antiinfectives, nasal antibiotics, opthalmic antibiotics, ophthalmic Opthalmic antivirals, opthalmic quinalones, opthalmic sulfonamides, antibiotics for skin and mucous membranes, antifungals for skin and mucous membranes, antiskins for skin and mucous membranes Viral agents, miscellaneous anti-infectives for skin and mucous membranes, scabies and pedulicides for skin and mucous membranes, anti-tumor agents for skin and mucous membranes (antinepolasts), nit Furans, as well as, oxazolidinones, are included. Physician's Desk Refernce (PDR), Medical Economics Company (Montvale, NJ), (53rd Ed.), 1999, and Mayo Medical Center Formulary, Unabridged Version, Mayo Clinic (Rochester, MN), January 1998.

  Examples of aminoglycosides include amikacin (amikacin sulfate), garamycin (gentamicin sulfate), nebucin (tobramycin sulfate), netromycin (netylmycin sulfate), streptomycin sulfate, and TOBI (tobramycin).

  β-lactam antibiotics include, for example, azactam (azureonam), cefotan (cefotetan), lorabid (loracalbef), mefoxin (cefoxitin), melem (meropenem), and primaxin (imipenem and silastatin used for suspension for injection), Is included.

  The cephalosporins include, for example, ancef (cefazoline), secrol (cefaclor), sedax (ceftibutene), cefizox (ceftizoxime sodium), cefobid (cefoperazone sodium), ceftin (cefuroxime accessyl), cefzil (Cefprodil), Ceptaz (ceftazidime), claforan (cefotaxime), durisef (cefadroxyl monohydrate), hortraz (ceftazidime), keflex (cephalexin), keftab (cephalexin HCl), kefurox (cefuroxime), kefsol (cephazoline), man Dole (Cefamandol Nephart), Maxi-Pime (Cefepime HCl), Monocid (Cefoniside Sodium), Omnicef (Cefdinir), Rosefin (Ceftriaxone), Supra Cux (cefixime), Tajicef (ceftazidime), Tajidimu (ceftazidime), Bantin (cefpodoxime proxetil), and Dinacef (cefuroxime).

  Macrolides include, for example, biaxin (clarithromycin), Dynabac (dilithromycin), EES 200 (erythromycin ethyl oxalate), EES 400 (erythromycin ethyl oxalate), Ery-Ped 200 (erythromycin ethyl oxalate) , EryPed 400 (Erythromycin ethyl succinate), Ery-Tab (Erythromycin sustained release tablet), Erythrosine stearate (Erythromycin stearate), Irozone (Erythromycin estrat), PCE Dispertab (Erythromycin particles in tablets), Pediazole (Erythromycin ethyl sulphate and sulfisoxazole acetyl for oral suspensions), Tao (Toroleandomycin), Zithromac (Azithromycin), and Erythromycin.

  The miscellaneous antibiotics include, for example, cleosin HCl (clindamycin hydrochloride), cleosin phosphate (clindamycin phosphate), colimycin M (colistimete sodium), and vancosin HCl (vancomycin hydrochloride).

  Penicillins include, for example, amoxyl (amoxicillin), augmentin (amoxicillin / potassium clavulanate), bacillin CR 900/300 (suspension of penicillin G benzathine and penicillin G procaine), and bacillin CR (penicillin G benzathine and penicillin G). Procaine suspension), Vicilin LA (penicillin G benzathine suspension), geocillin (carbenicillin indanyl sodium), mezrin (sterile mezucillin sodium), omnipen (ampicillin), pen-bee K (penicillin V potassium), Pfizerpen (penicillin G potassium), piperacyl (piperacillin sodium), spectrovid (bacampicillin HCl), ticar (ticalcillin disodium), timentin (ticalcillin disodium and calibulate caliu) ), Unashin (ampicillin sodium / sulbactam sodium), Zosyn (piperacillin sodium and tazobactam sodium), and dicloxacillin sodium,.

  Examples of tetracyclines include achromomycin V (tetracycline HCl), decomycin (demeclocycline HCl), Dynacin (minocycline HCl), minocin (minocycline hydrochloride), Monodox (doxycycline monohydrate capsule), terramycin (oxytetracycline) , Bectrin (Minocycline hydrochloride), Vibramycin calcium (Doxycycline sodium), Vibramycin hydrate (Doxycycline hydrate), Vibramycin monohydrate (Doxycycline monohydrate), Vibra-Tabs (Doxycycline hydrate), Dechromomycin (Demecro) Cyclin HCl), Vibramycin (Doxycycline), Dynacin (Minocycline HCl), Terramycin (oxytetracycline HCl), Achromomycin V capsule (Tetrasa Klin HCl), lincomycin compounds, as well as Cleocin HCl (clindamycin HCl), are included.

  Antifungal agents include, for example, Abelcet (amphotericin B-lipid complex), AmBisome (amphotericin B), Amphotec (amphotericin B-cholesterol sulfate complex), ancobon (flucytosine), diflucan (fluconazole), flubicin P / G (Ultrafine griseofulvin), flubicin P / G 165 and flubicin P / G 330 (ultrafine griseofulvin), glyfluvin V (griseofulvin), Gris-PEG (ultrafine griseofulvin), ramiseal (terbinafine hydrochloride), nizoral (ketoconazole), amphotericin B, rotrimine (clotrimazole), dapsone tablets (dapsone), diflucan (fluconazole), monistar-derm cream (miconazole), mycostatin cream (nystatin), and Sporanox (itraconazole) included.

  Antimalarial drugs include, for example, allalene hydrochloride (chloroquine HCl), allalene phosphate (chloroquine phosphate), dalaprim (pyrimethamine), lariam (mefloquine HCl), and prenyl (hydroxychloroquine sulfate).

  Antituberculosis drugs include, for example, capastate sulfate (capreomycin sulfate), miambutol (ethambutol hydrochloride), Mycobutin (rifabutin capsule), nidrazide (isoniazide injection solution), Paser (aminosalicylic acid), Priftin (rifapentine), pyrazinamide tablets ( Pyrazinamide), Rifazine (Rifampin capsule), Rifazine IV (Rifampin for injection), Rifamate (Rifampin and isoniazid), Rifater (Rifampin, isoniazid and pyrazinamide), Ceromycin (cycloserine capsule), Streptomycin sulfate, Tice BCG (BCG vaccine), Cycloserine (ceromycin capsules), Urised (methenamine), and Trecator-SC (ethionamide tablets) are included.

  Antiviral agents include, for example, Alferon N (interferon alfa-n3), Crixiban (indinavir sulfate), Cytobane (ganciclovir), Cytobane-IV (ganciclovir sodium), Epivir (lamivudine), Famvir (famciclovir), Flumazine ( Rimantadine HCl), Foscavir (foscarnet sodium), hivid (zarcitabine), intron A (interferon alfa-2b), invirase (saquinavir mesylate), Norvir (ritonavir), rebetrol (Rebetrol) and intron A (interferon alfa) -2b) Rebetron combination therapy, Rescripter (Delavirdine Mesylate), Retrovir (Ziduvudine), Retrovir IV (Zidovudine), Simmetrel (Amantazine hydrochloride), Synagis (Paribi) Mab), Valtrex (Valacyclovir HCl), Videx (Didanocin), Viracept (Nelfinavir Mesylate), Viramune (Nevirapine), Virazole (Ribavirin), Vistide (Cidofovir), Zelit (Stavudine (d4T)), Symmetrel Syrup ( Amantadine HCl), Combivir tablets (lamiduvine), and Zobilux (acyclovir).

  As an antidepressant, for example, Daphorn tablets (Daphorn) are included.

  Miscellaneous anti-infectives include, for example, dalaprim (pyrimethamine), fragile 375 (metronidazole), fragile ER tablets (metronidazole), fragile IV (metronidazole), floxone (furazolidone), mepron (atobacon), and Neutrexin (gluconic acid) Trimetrexate glucuronate).

  Examples of quinolones include cipro (ciprofloxacin HCl), flocsin (ofloxacin), Levaquin (levofloxacin), Mazaquin (lomefloxacin HCl), noroxin (norfloxacin), penetrex (enoxacin), Raxar (grepafloxacin HCl) , Trovan (trovafloxacin mesylate), and Zagam (Zagam; sparfloxacin).

  Examples of the sulfonamides include Bactrim (trimethoprim and sulfamethoxazole), Bactrim DS (trimethoprim and sulfamethoxazole, double strength), Pediazole (erythromycin ethyl oxalate and sulfisoxazole acetyl). ), Septra (trimethoprim and sulfamethoxazole), Septra DS (trimethoprim and sulfamethoxazole), Co-trimoxazole and sulfadiazine and bactrim IV injection (sulfamethoxazole), sulfapyridine and Pediazole (ethyl) Erythromycin oxalate and sulfisoxazole acetyl).

  Urinary tract anti-infectives include, for example, fladantine (nitrofurantoin), Macrobid (nitrofurantoin monohydrate macrocrystal), macrodantine (nitrofurantoin macrocrystal), Monurol Sachet (fosfomycin tromethamine), Neggram Caplets ( Nalidixic acid), Septra (trimethoprim and sulfamethoxazole), Septra DS (trimethoprim and sulfamethoxazole), Urised (preservative methenamine, methylene blue, phenyl salicylate, benzoic acid, parasympatholytic agent (atropine sulfate) hyos Formulations with thiamine), Urobiotic-250 capsules (oxytetracycline HCl and sulfamethizole and phenazopyridine HCl), and Uroqid Acid No.2 tablets (methenamine mandelate).

  Examples of nasal antibiotics include bactroban (mupirocin).

  Examples of opthalmic antibiotics include chloromycetin ophthalmic (chloramphenicol), Cortisporin (neomycin and polymyxin sulfates β and acetic acid = hydrocortisone cream), ilotaisin (erythromycin ophthalmic ointment), neo Decadron (neomycin sulfate-dexamethasone sodium phosphate), Polytrim (trimethoprim and polymyxin sulfate β ophthalmic solution), Terra-Cortril (oxytetracycline HCl and hydrocortisone acetate), terramycin (oxytetracycline), and TobraDex (Tobramycin and dexamethasone ophthalmic suspensions and ointments).

  Examples of ophthalmic antivirals include Vira-A ophthalmic ointment (vidarabine).

  As opthalmic quinalones, for example, Chibroxin (norfloxacin ophthalmic solution), Ciloxan ophthalmic solution (ciprofloxacin HCl), Ciloxan ophthalmic ointment (ciprofloxacin HCl), and Ocuflox ophthalmic Solution (ofloxacin).

  Opthalmic sulfonamides include, for example, Blephamide ophthalmic ointment (sodium sulfacetamide and prednisolone acetate) and Blepamide ophthalmic suspension (sodium sulfacetamide and prednisolone acetate) It is.

  Antibiotics for skin and mucosa include, for example, A / T / S (erythromycin), bactroban (mupirocin), benzamicin (erythromycin-benzoyl peroxide topical gel), betadine (povidone-iodo), cleosin T (phosphoric acid) Clindamycin topical solution), Clindets (clindamycin phosphate cotton withdrawal), Cortisporin (cream of neomycin, polymyxin B sulfate and hydrocortisone acetate), Emgel (erythromycin), Erycette (erythromycin topical solution), galamycin (sulfuric acid) Gentamicin), Klaron (sulfacetamide sodium lotion), mycostatin (nystatin cream), Theramycin Z (erythromycin topical solution), T-Stat (erythromycin), chloromycetin (chloramphenicol ointment), Cortisporin (neoma) Ophthalmic ointment of isine, polymyxin B sulfate, zinc bacitracin and hydrocortisone), ilotaisin (erythromycin), neodecadrone (neomycin sulfate-dexamethasone sodium phosphate), polytrim (trimethoprim and polymyxin sulfate B), terracoteryl (oxytetracycline HCl and acetic acid) Hydrocortisone), terramycin (oxytetracycline), and TobraDex (tobramycin and dexamethasone ophthalmic suspensions and ointments).

  Antifungal agents for skin and mucous membranes include, for example, Excelderm (sulconazole nitrate), Fundizone (suspension of amphotericin B), Lamiseal (terbinafine hydrochloride), Loprox (ciclopiroxolamine), rotrimin ( Clotrimazole), Lotrisone (clotrimazole and betamethasone dipropionate), Mentax (butenafine HCl), Monister-Darm (miconazole nitrate), Miselex (clotrimazole), mycostatin (nystatin), Naftin (naphthifine HCl) ), Nizoral (ketoconazole), Nystop (nystatin), Oxistat (oxyconazole nitrate), Selsan Rx (2.5% selenium sulfide lotion), and Spectazole (econazole nitrate).

  Antiviral agents for skin and mucous membranes include, for example, Denavir (penciclovir cream) and Zobilux (acyclovir).

  Miscellaneous anti-infectives for skin and mucous membranes include, for example, Benzashave (benzoyl peroxide), betadine (povidone-iodo), betasept (chlorhexidine gluconate), setafil Cetaphil (soap substitute) )), Clorpactin WCS-90 (sodium oxychlorocene), Dapsone tablets (Dapson), Desquam-E (benzoyl peroxide), Desquam-X (benzoyl peroxide), Hibiclens (chlorhexidine gluconate), Hibitstat (chlorhexidine gluconate) ), Impregon (2% tetrachlorosalicylanilide), MetroCream (metronidazole), MetroGel (metronidazole), Noritate (metronidazole), pHisoHex (hexachlorophene detergent), Sulfacet-R (10% sulfacetamide sodium and 5% sulfur ), Sulfamilone (mafenide acetate (mat) enide acetate)), Triaz (benzoyl peroxide), and Vanoxide-HC (benzoyl hydrocortisone).

  Mangeous and pedulicides for skin and mucous membranes include, for example, Acticin (Permesulin), Elimite (Permesulin), Eulux (crotamiton), and Lindane Lotion USP 1% (Linden).

  Antitumor agents for skin and mucosa include, for example, EFdex (fluorouracil) and fluoroplex (fluorouracil).

  Examples of nitrofurans include fradantine suspension for oral cavity (nitrofurantoin).

  Examples of oxazolidinones include zybox (linezolid).

  One skilled in the art can appreciate that an antibiotic useful in the present invention is a physiologically active compound contained in any of the antibiotic formulations described above. For example, available azactam (Aztreonam) is usually an injectable solution. However, this antibiotic has propionic acid = (z) -2-[[[(2-amino-4-thiazolyl) [[(2S, -3S) -2-methyl-4-oxo-1-sulfo-3 -Azetidinyl] carbamoyl] methylene] amino] oxy] -2-methyl. Physician's Desk Reference (PDR), Medical Economics Company (Montvale, NJ), (53rd Ed.), Pp. 820-823, 1999.

  Amikacin (Amikacin sulfate) is commercially available from Elkins-Sinn and is available from D-streptamine, O-3-amino-3-deoxy-α-D-glucopyranosyl- (1 → 6) -O-6-deoxy. -α-D-glucopyranosyl- (1 → 4)]-N '-(4-amino-2-hydroxy-1-oxobutyl) -2-deoxy = (S) = sulfate (1: 2) (salt) .

  Garamycin (gentamicin sulfate) is commercially available from Schering.

  Nebucin (tobramycin sulfate) is commercially available from Lilly and is O-3-amino-3-deoxy-α-D-glucopyranosyl- (1 → 4) -O- [2,6-diamino-2,3-6 -Trideoxy-α-D-ribo-hexopyranosyl- (1 → 6)]-2-deoxy-L-streptamine sulfate (2: 5) (salt).

Netromycin (netilmycin sulfate) is commercially available from Schering and is O-3-Deoxy-4-C-methyl-3- (methylamino) -β-L-ara-binopyranosyl (1 → 4) -O- [2 , 6-Diamino-2,3,4,6-tetradeoxy-α-D-glycero-hex-4-enopyranosyl- (1 → 6) -2-deoxy-N ³ -ethyl-L-streptamine sulfate (2 : 5) It is salt.

  Streptomycin sulfate is commercially available from Pfizer, D-streptamine, O-2-deoxy-2- (methylamino) -α-L-glucopyranosyl- (1 → 2) -O-5-deoxy-3-C- Formyl-α-L-lyxofuranosyl, (1 → 4) -N, N′-bis (aminoiminomethyl) = sulfate (2: 3) (salt).

  TOBI (tobramycin) is commercially available from Pathogenesis Corporation and is O-3-amino-3-deoxy-α-D-glucopyranosyl- (1 → 4) -O- [2,6-diamino-2,3,6 -Trideoxy-α-D-ribo-hexopyranosyl- (1 → 6)]-2-deoxy-L-streptamine.

  Azactam (Aztreonam) is commercially available from Bristol-Myers Squibb, and propionic acid = (Z) -2-[[[(2-amino-4-thiazolyl) [[(2S, -3S) -2-methyl- 4-oxo-1-sulfo-3-azetidinyl] carbamoyl] methylene] amino] oxy] -2-methyl.

  Cefotan (cehotetane) is commercially available from Zeneca, [6R- (6a, 7a)]-7-[[[4- (2-amino-1-carboxy-2-oxoethylidene) -1-3, dithietane -2-yl] carbonyl] amino] -7-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl) thio] methyl] -8-oxo-5-thia-1-azabicyclo [4.2. 0] disodium salt of octa-2-ene-2-carboxylic acid.

  Loravid (Loracarbeve) is commercially available from Lilly and is (6R, 7S) -7-[(R) -2-amino-2-phenylacetamido] -3-chloro-8-oxo-1-azabicyclo [4.2. 0] Oct-2-ene-2-carboxylic acid monohydrate.

  Mefoxin (cefoxitin) is commercially available from Merck and is (6R, 7S) -3- (hydroxymethyl) -7-methoxy-8-oxo-7- [2- (2-thienyl) acetamide] -5-thia 1-Azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid sodium carbamate (ester).

  Merem (meropenem) is commercially available from Zeneca and is (4R, 5S, 6S) -3-[(3S, 5S) -5- (dimethylcarbamoyl) -3-pyrrolidinyl] thiol] -6-[(1R) 1-hydroxyethyl] -4-methyl-7-oxo-1-azabicyclo [3.2.0] hept-2-ene-2-carboxylic acid trihydrate.

Primacsin (imipenem and silastatin for use in injectable suspensions) is commercially available from Merck. (1) Imipenem is N-formimidoyl thienamycin monohydrate, whose chemical name is [5R- [5α, 6α (R ^* )]]-6- (1-hydroxyethyl) -3- [ [2-[(Iminomethyl) amino] ethyl] thio] -7-oxo-1-azabicyclo [3.2.0] hept-2-ene-2-carboxylic acid monohydrate, and silastatin sodium [R- [R ^* , S ^* ,-(Z)]]-7-[(2-amino-2-carboxyethyl) thio] -2-[[(2,2-dimethylcyclopropyl) carbonyl] amino] -2-Heptenoic acid monosodium salt.

  Ansef (cefazoline) is commercially available from SmithKline Beecham and is a 3-{[(5-methyl-1,3,4-thiadiazol-2-yl) thio-methyl]}-8-oxo-7- [2- (1H-tetrazol-1-yl) acetamido] -5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid.

  Securol (cefaclor) is commercially available from Lilly and is 3-chloro-7-D- (2-phenylglycinamide) -3-cephem-4-carboxylic acid monohydrate. Sedax (ceftibbutene) is also commercially available from Schering and is (+)-(6R, 7R) -7-[(Z) -2- (2- (2-amino-4-thiazoly) -4-carboxy Crotonamide] -8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid dihydrate.

  Cefizox (ceftizoxime sodium) is commercially available from Fujisawa, [6R- [6α, 7β (Z)]]-7 [(2,3, dihydro-2-imino-4-thiazolyl) (methoxyamino ) Acetyl] amino] -8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid.

  Cefobid (cefoperazone sodium) is commercially available from Pfizer and is (6R, 7R) -7 [(R) -2- (4-ethyl-2,3, dioxo-1-piperazinecarboxamide) -2- ( p-hydroxyphenyl) -acetamido) -3-[[(1-methyl-1H-tetrazol-5-yl) thio] methyl] -8-oxo-5-thia-1-azabicyclo [4.2.0] octa-2 -En-2-carboxylate.

Ceftine (cefuroxime acceptyl) is commercially available from Glaxo Wellcome and is (RS) -1-hydroxyethyl (6R, 7R) -7- [2- (2-furyl) glyoxyamide] -3- (hydroxy Ethyl)-(8-oxo-5-thia-1-aza-bicyclo [4.2.0] oct-2-ene-2-carboxylate, 7 ² (Z) -O-methyl-oxime) = 1-acetate 3 -Carbamate.

  Cefzil (cefprodil) is commercially available from Bristol-Myers Squibb and is (6R, 7R) -7-[(R) -2-amino-2- (p-hydroxyphenyl) acetamide] -8-oxo-3- Propenyl-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid monohydrate.

  Ceptaz (ceftazidime) is commercially available from Glaxo Wellcome and is 1-[[7-[[(2-amino-4-thiazolyl) [(1-carboxy-1-methylethoxy) imine] acetyl] amino] -2 -Carboxy-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-en-3-yl] methyl] = hydroxide, inner salt, [6R- [6α, 7β (Z)] ].

Claforan (cefotaxime) is commercially available from Hoescht Marion Roussel, 7- [2- (2-amino-4-thiazolyl) glyoxylamido] -3- (hydroxymethyl) -8-oxo-5-thia-1- Azabicyclo [4.2.0] oct-2-ene-2-carboxylate 7 ² (Z)-(O-methyloxime) = acetate (ester).

Duricef (cefadroxyl monohydrate) is commercially available from Bristol-Myers Squibb and is 5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, 7-[[amino (4 -Hydroxyphenyl) acetyl] amino] -3-methyl-8-oxo = monohydrate, [6R- [6α, 7β (R ^* )]]-.

  Holtolaz (ceftazidime) is commercially available from Glaxo Wellcome and is 1-[[7-[[(2-amino-4-thiazolyl) [1-carboxy-1-methylethoxy) imino] acetyl] amino] -2- Carboxy-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-en-3-yl] methyl] = hydroxide, inner salt [6R- [6α, 7β (Z)]] is there.

  Keflex (cephalexin) is commercially available from Dista and is 7- (D-α-amino-α-phenylacetamido) -3-methyl-3-cephem-4-carboxylic acid monohydrate.

  Keftab (cephalexin HCl) is commercially available from Dura and is 7- (D-2-amino-2-phenylacetamido) -3-methyl-3-cephem-4-carboxylic acid = hydrochloride monohydrate .

  Keflox (cefuroxime) is commercially available from Lilly and is (6R.7R) 3-carbamoyloxymethyl-7- [Z-2-methoxyimino-2- (fur-2-yl) acetamide] cef-3-em -4-Carboxylate sodium salt.

  Kefsol (cephazoline) is commercially available from Lilly and is a 3-{[(5-methyl-1,3,4-thiadiazol-2-yl) thio] methyl} -8-oxo-7- [2- (1H -Tetrazol-1-yl) acetamide] -5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid sodium salt.

Mandol (cefamandol nafate) is commercially available from Lilly, 5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, 7-[[(formyloxy) phenylacetyl ] Amino] -3-[[(1-Methyl-1H-tetrazol-5-yl) thio] methyl] -8-oxo = monosodium salt, [6R- [6α-7β (R ^* )]].

Maxi-pyme (Cefepime HCl) is commercially available from Bristol-Myers Squibb, 1-[[6R, 7R) -7- [2-amino-4-thiazolyl) -glyoxylamide] -2-carboxy-8-oxo- 5-thia-1-azabicyclo- [4.2.0] oct-2-en-3-yl] methyl] -1-methylpyrrolidinium chloride = 7 ^2- (Z)-(O-methyloxime) = monohydro Chloride = monohydrate.

Monocid (sodium cefoniside) is commercially available from SmithKline Beecham and is 5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid = 7-[(hydroxyphenyl-acetyl)- Amino] -8-oxo-3-[[1- (sulfomethyl) -1H-tetrazol-5-yl] thio] methyl] = disodium salt, [6R- [6α, 7β (R ^* )]].

  Omnicef (cefdinir) is commercially available from Parke Davis and is [6R- [6α, 7β (Z)]]-7-[[(2-amino-4-thiazolyl)-(hydroxyimino) acetyl] amino]- 3-ethenyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid.

Rocefin (ceftriaxone) is commercially available from Roche Laboratories and is (6R, 7R) -7- [2- (2-amino-4-thiazolyl) glyoxyamino] -8-oxo-3-[[( 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl) thio] methyl] -5-thia-1-azabicyclo [4.2.0] oct-2-ene 2-carboxylic acid = 7 ² - (Z) -O- methyloxime = disodium salt = three pentahydrate (sesquaterhydrate).

Splux (cefixime) is commercially available from Lederle Laboratories and is (6R, 7R) -7- [2- (2-amino-4-thiazolyl) glyoxylamido] -8-oxo-3-vinyl-5-thia- 1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid ^{= 7 2 - (Z) -} [O- ( carboxymethyl) oxime is a trihydrate.

  Tajicef (ceftazidime) is commercially available from SmithKline Beecham, and pyridinium = 1-[[7-[[2-amino-4-thiazolyl] [(1-carboxy-1-methylethoxy) imino] acetyl] amino]- 2-carboxy-8-oxo-5-thia-1-azabicyclo (4.2.0) oct-2-en-3-yl] methyl] -hydroxide, inner salt, [6R,-[6α, 7β (Z )]] Pentahydrate.

  Tajidime (ceftazidime) is commercially available from Lilly and is 1-[[7-[[2-amino-4-thiazolyl] [(1-carboxy-1-methylethoxy) imino] acetyl] amino] -2-carboxy. -8-Oxo-5-thia-1-azabicyclo (4.2.0) oct-2-en-3-yl] methyl] = hydroxide, inner salt, [6R,-[6α, 7β (Z)]] Is the pentahydrate.

  Bantin (cefpodoxime proxetil) is commercially available from Pharmacia & Upjohn, and (RS) -1 (isopropoxycarbonyloxy) ethyl (+)-(6R, 7R) -7- [2- (2- Amino-4-thiazolyl) -2-{(Z) methoxyimino} acetamido] -3-methoxymethyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylate It is.

  Ginacef (cefuroxime) is commercially available from Glaxo Wellcome and is (6R, 7R) -3-carbamoyloxymethyl-7- [Z-2-methoxy-imino-2-fur-2-yl) acetamido] cef-3 -Sodium salt of M-4-carboxylate.

  Biaxin (clarithromycin) is commercially available from Abbott and is 6-O-methylerythromycin.

  Dynabac (Dirithromycin) is commercially available from Sanofi and is (9S) -9-Deox-11-deoxy-9,11- [imino [(1R) -2- (2-methoxyethoxy) -ethylidene] oxy ] Erythromycin.

  E.E.S. 200 (erythromycin ethyl oxalate) is commercially available from Abbott and is 2 '-(ethyl oxalate) erythromycin.

  E.E.S. 400 (erythromycin ethyl oxalate) is commercially available from Abbott and is 2 '-(ethyl oxalic acid) erythromycin.

  Ery-Ped 200 (Erythromycin ethyl succinate) is commercially available from Abbott and is 2 '-(ethyl succinate) erythromycin.

  EryPed 400 (Erythromycin ethyl succinate) is commercially available from Abbott and is 2 '-(ethyl succinate) erythromycin.

Ery-Tab (Erythromycin Sustained Release Tablet) is commercially available from Abbott and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )- 4-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5, 7,9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxacyclotetradecane- 2,10-dione.

Erythrosine stearate (erythromycin stearate) is commercially available from Abbott and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4 -[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5,7 , 9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxacyclotetradecane-2 , 10-dione stearate.

  Irozone (erythromycin estrate) is commercially available from Dista and is dodecyl sulfate = 2′-propionate.

PCE Dispertab (tablet containing erythromycin particles) is commercially available from Abbott and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3 , 5,7,9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxa Cyclotetradecane-2,10-dione.

  Pediazole (Erythromycin ethyl oxalate and sulfisoxazole acetyl for oral suspension) is commercially available from Ross Products, 2'-ethyl oxalate ester of erythromycin (erythromycin ethyl oxalate), and N- ( 3,4-Dimethyl-5-isoxazolyl) -N-sulfanylacetamide (sulfisoxazole acetyl).

  Tao (troleandomycin) is commercially available from Pfizer and is synthesized from the acetyl ester of oleandomycin.

  Zithromax (azithromycin) is commercially available from Pfizer and is (2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R) -13-[(2,6-dideoxy-3-C-methyl -3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11- [ [3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hexopyranosyl] oxy] -1-oxa-6-azacyclopentadecan-15-one.

Erythromycin is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4-[(2,6-dideoxy-3-C-methyl -3-O-methyl-α-L-ribo-hexapyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5,7,9,11,13-hexamethyl-6-[[3 , 4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxacyclotetradecane-2,10-dione.

  Cleosin HCl (clindamycin hydrochloride) is commercially available from Pharmacia & Upjohn and is a hydrated hydrochloride of clindamycin, which is the 7 (S) hydroxyl group of lincomycin. -Semi-synthetic antibiotics that can be produced by chloro substitution.

  Creosin phosphate (clindamycin phosphate) is commercially available from Pharmacia & Upjohn, L-threo-α-D-galacto-octopyranoside = methyl-7-chloro-6,7,8, -trideoxy-6-[[[ (1-methyl-4-propyl-2-pyrrolidinyl) carbonyl] amino] -1-thio-, 2- (dihydrogen phosphate), (2S-trans)-.

  Collymycin M (Coristimate sodium) is commercially available from Monarch.

  Vancosin HCl (vancomycin hydrochloride) is commercially available from Lilly.

  Amoxyl (amoxicillin) is commercially available from SmithKline Beecham and is (2S, 5R, 6R) -6-[(R)-(-)-2-amino-2- (p-hydroxyphenyl) acetamide] -3, 3-Dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] -heptane-2-carboxylic acid trihydrate.

  Augmentin (amoxicillin / potassium clavulanate) is commercially available from SmithKline Beecham, (2S, 5R, 6R) -6-[(R)-(-)-2-amino-2- (p-hydroxyphenyl) Acetamide] -3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] -heptane-2-carboxylic acid trihydrate (amoxicillin) and (Z)-(2R, 5R ) -3- (2-Hydroxyethylidene) -7-oxo-4-oxa-1-azabicyclo [3.2.0] -heptane-2-carboxylate (potassium clavulanate).

  Baicilin CR 900/300 (suspension of penicillin G benzathine and penicillin G procaine) is commercially available from Wyeth-Ayerst and is (2S, 5R, 6R) -3,3-dimethyl-7-oxo-6- ( 2-Hydroxyacetamido) -4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylic acid compound added with N, N'-dibenzylethylenediamine (2: 1) Benzathine), as well as (2S, 5R, 6R) -3,3-dimethyl-7-oxo-6- (2-phenylacetamido) -4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylic acid P-aminobenzoic acid = 2- (diethylamino) ethyl (1: 1) to the compound is a monohydrate (penicillin G procaine).

  Vicilin CR (suspension of penicillin G benzathine and penicillin G procaine) is commercially available from Wyeth-Ayerst and is (2S, 5R, 6R) -3,3-dimethyl-7-oxo-6- (2-phenyl) Acetamide) -4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylic acid compound plus N, N'-dibenzylethylenediamine (2: 1) tetrahydrate (penicillin G benzathine), And (2S, 5R, 6R) -3,3-dimethyl-7-oxo-6- (2-phenylacetamido) -4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylic acid compound, p-aminobenzoic acid = 2- (diethylamino) ethyl (1: 1) is a monohydrate (penicillin G procaine).

  Baicillin LA (penicillin G benzathine suspension) is commercially available from Wyeth-Ayerst and is (2S, 5R, 6R) -3,3-dimethyl-7-oxo-6- (2-phenylacetamido) -4- A tetrahydrate obtained by adding N, N′-dibenzylethylenediamine (2: 1) to thia-1-azabicyclo [3.2.0] heptane-2-carboxylic acid compound.

  Geocillin (carbenicillin indanyl sodium) is commercially available from Pfizer and is 1- (5-indanyl) -N- (2-carboxy-3-3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2 .0] Hepta-6-yl) -2-phenylmalonamic acid monosodium salt.

  Mezrin (sterile mezlocillin sodium) is commercially available from Bayer and is 6- {D-2 [3 [(methyl-sulfonyl) -2-oxo-imidazolidine-1-carboxamide] -2-phenylacetamide} penicillin The monohydrate sodium salt of the acid.

  Omnipen (ampicillin) is commercially available from Wyeth-Ayerst and is (2S, 5R, 6R) -6-[(R) -2-amino-2-phenylacetamide] -3,3-dimethyl-7-oxo- 4-thia-1-aza-bicyclo [3.2.0] heptane-2-carboxylic acid.

  Pen-bee K (penicillin V potassium) is commercially available from Wyeth-Ayerst and is the potassium salt of the phenoxymethyl analog of penicillin G.

  Pfizerpen (Penicillin G potassium) is commercially available from Pfizer and is 3,3-dimethyl-7-oxo-6- (2-phenylacetamido) -4-thia-1-azabicyclo (3.2.0) heptane-2- It is monopotassium carboxylate.

Piperacyl (piperacillin sodium) is commercially available from Lederle and is 4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylic acid = 6-[[[[(4-ethyl-2-3-dioxo- 1-piperazinyl) carbonyl] amino] phenylacetyl] amino] -3,3-dimethyl-7-oxo-, monosodium salt, [2S- [2α, 5α, 6β (S ^* )]].

  Spectrobide (Bacampicillin HCl) is commercially available from Pfizer and is 1′-ethoxycarbonyloxyethyl-6- (D-α aminophenylacetamido) -penicillic acid hydrochloride.

  Tikal (Ticarcillin disodium) is commercially available from SmithKline Beecham and is N- (2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] hept-6-yl. ) -3-thiophenmalonamidic acid disodium salt.

  Timentin (ticalcillin disodium and clavulanate potassium) is commercially available from SmithKline Beecham and is N- (2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0]. Hepta-6-yl) -3-thiophenmalonamidic acid disodium salt (ticalcillin disodium) and (Z)-(2R, 5R) -3- (2-hydroxyethylidene) -7-oxo-4-oxa 1-Azabicyclo [3.2.0] -heptane-2-carboxylate (potassium clavulanate).

  Unacin (sodium ampicillin / sulbactam sodium) is commercially available from Pfizer and is (2S, 5R, 6R) -6-[(R) -2-amino-2-phenylacetamido] -3,3-dimethyl-7- Oxo-4-thia-1-aza-bicyclo [3.2.0] heptane-2-carboxylate monosodium (ampicillin sodium) and penicillate sodium sulfonate, ie (2S, 5R) -3,3-dimethyl-7 -Oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate-4,4-dioxide = sodium (sulbactam sodium).

  Zosine (piperacillin sodium and tazobactam sodium) is commercially available from Lederle, (2S, 5R, 6R) -6 [(R) -2- (4-ethyl-2,3-dioxo-1-piperazine-carboxamide) -2-phenylacetamido] -3,3-dimethyl-7-oxo-4-thia-1-azabicyclo- [3.2.0] sodium heptane-2-carboxylate (sodium piperacillin), and (2S, 3S, 5R ) -3-Methyl-7-oxo-3- (1H-1,2,3-triazol-1-ylmethyl) -4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate-4,4 Dioxide = sodium (tazobactam sodium).

  Dicloxacillin sodium is (2S, 5R, 6R) -6- (3- (2,6-dichlorophenyl) 5-methyl-4-isoxazolecarboxamide) -3,3-dimethyl-7-oxo-4- Thia-1-azabicyclo [3.2.0] heptane-2-carboxylate monohydrate monosodium.

  Acromomycin V (tetracycline HCl) is commercially available from Lederle, [4S- (4α, 4aα, 5aα, 6β, 12aα)]-4- (dimethylamino) -1,4,4a, 5,5a, 6 , 11,12a-Octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-2-naphthacenecarboxamide monohydrochloride.

  Declomycin (demeclocycline HCl) is commercially available from Lederle Laboratories, 7-chloro-4-dimethylamino) -1,4,4a, 5,5a, 6,11,12a-octahydro-3,6,10 12,12a-pentahydroxy-1,11-dioxo-2-naphthacenecarboxamide monohydrochloride.

  Dynacin (Minocycline HCl) is commercially available from Medicis, [4S- (4α, 4aα, 5aα, 12aα)]-4,7-bis (dimethylamino) -1,4,4a, 5,5a, 6, 11,12a-Octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide monochloride.

  Minocin (minocycline hydrochloride) is commercially available from Lederle Laboratories, [4S- (4α, 4aα, 5aα, 12aα)]-4,7-bis (dimethylamino) -1,4,4a, 5,5a, 6 , 11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide monochloride.

  Monodox (doxycycline monohydrate capsule) is commercially available from Oclassen and is α-6-deoxy-5-oxytetracycline.

  Terramycin (oxytetracycline) is commercially available from Pfizer.

  Vectrin (minocycline hydrochloride) is commercially available from Warner Chilcott Professional Products, [4S- (4α, 4aα, 5aα, 12ax)]-4,7-bis (dimethylamino) -1,4,4a, 5,5a 6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide monochloride.

  Vibramycin calcium (doxycycline sodium) is commercially available from Pfizer and is 4- (dimethylamino) -1,4,4a, 5,5a, 6,11,12a-octahydro-3,5,10,12,12a- It is pentahydroxy-6-methyl-1,11-dioxo-2-naphthacene-carboxamide monohydrate.

  Vibramycin hydrate (doxycycline cyclate) is commercially available from Pfizer and is α-6-deoxy-5-oxytetracycline.

  Vibramycin monohydrate (doxycycline monohydrate) is commercially available from Pfizer and is 4- (dimethylamino) -1,4,4a, 5,5a, 6,11,12a-octahydro-3,5, 10,12,12a-Pentahydroxy-6-methyl-1,11-dioxo-2-naphthacene-carboxamide monohydrate.

  Vibra-Tabs (doxycycline hydrate) is commercially available from Pfizer and is α-6-deoxy-5-oxytetracycline.

  Vibramycin (doxycycline) is commercially available from Pfizer and is 4- (dimethylamino) -1,4,4a, 5,5a, 6,11,12a-octahydro-3,5,10,12,12a-pentahydroxy -6-Methyl-1,11-dioxo-2-naphthacene-carboxamide monohydrate.

  Lincomycins are (2S, 5R, 6R) -6- (3- (2,6-dichlorophenyl) 5-methyl-4-isoxazolecarboxamide) -3,3-dimethyl-7-oxo-4-thia -1-Azabicyclo [3.2.0] heptane-2-carboxylate monohydrate monosodium.

  Creosin HCl (Clindamycin HCl) is commercially available from Pharmacia & Upjohn and is methyl 7-chloro-6,7,8-trideoxy-6- (1-methyl-trans-4-propyl-L-2- Pyrrolidinecarboxamide) -1-thio-L-threo-α-D-galacto-octopyranoside monohydrochloride.

Abelcet (amphotericin B-lipid complex) is commercially available from Libosome Company, Inc. [1R- (1R ^* , 3S ^* , 5R ^* , 6R ^* , 9R ^* , 11R ^* , 15S ^* , 16R ^* , 17R ^* , 18S ^* , 19E, 21E, 23E, 25E, 27E, 29E, 31E, 33R ^* , 35S ^* , 36R ^* , 37S ^* )]-33-[(3-amino-3,6-dideoxy-β- D-mannopyranosyl) -oxy] -1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo [33.3.1 ] Nonatria Conta-19,21,23,25,27,29,31-heptaene-36-carboxylic acid.

AmBisome (Amhotericin B) is commercially available from Fujisawa Healthcare, [1R- (1R ^* , 3S ^* , 5R ^* , 6R ^* , 9R ^* , 11R ^* , 15S ^* , 16R ^* , 17R ^* , 18S ^* , 19E , 21E, 23E, 25E, 27E, 29E, 31E, 33R ^* , 35S ^* , 36R ^* , 37S ^* )]-33-[(3-amino-3,6-dideoxy-β-D-mannopyranosyl) -oxy] -1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo [33.3.1] nonatolia contour-19,21, 23,25,27,29,31-heptaene-36-carboxylic acid.

Amphotec (amphotericin B-cholesterol sulfate complex) is commercially available from Sequus Pharmaceuticals, Inc. [1R- (1R ^* , 3S ^* , 5R ^* , 6R ^* , 9R ^* , 11R ^* , 15S ^* , 16R ^* , 17R ^* , 18S ^* , 19E, 21E, 23E, 25E, 27E, 29E, 31E, 33R ^* , 35S ^* , 36R ^* , 37S ^* )]-33-[(3-amino-3,6-dideoxy- β-D-Mannopyranosyl) -oxy] -1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo [33.3 .1] Nonatria Conta-19,21,23,25,27,29,31-heptaene-36-carboxylic acid.

  Ancobon (flucytosine) is commercially available from ICN Pharmaceuticals and is 5-fluorocytosine.

  Diflucan (fluconazole) is commercially available from Pfizer Inc. and is 2,4-difluoro-α-α'-bis (1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol.

  Flubicin P / G (ultrafine griseofulvin) is commercially available from Schering.

  Flubicin P / G 165 and flubicin P / G 330 (ultrafine griseofulvin) are commercially available from Schering.

  Glyfluvin V (Griseofulvin) is commercially available from Ortho Dermatological.

  Gris-PEG (ultrafine griseofulvin) is commercially available from Allergan.

  Ramisir (terbinafine hydrochloride) is commercially available from Novartis and is (E) -N- (6,6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthalenemethanamine hydrochloride.

  Nizoral (ketoconazole) is commercially available from Janssen and is cis-1-acetyl-4- [4-[[2- (2,4-di-chlorophenyl) -2- (1H-imidazol-1-ylmethyl)- 1,3-dioxalan-4-yl] methoxy] phenyl] piperazine.

Amphotericin B can be obtained from [1R- (1R ^* , 3S ^* , 5R ^* , 6R ^* , 9R ^* , 11R ^* , 15S ^* , 16R ^* , 17R ^* , 18S ^* , 19E, 21E, 23E, 25E, 27E, 29E, 31E, 33R ^* , 35S ^* , 36R ^* , 37S ^* )]-33-[(3-amino-3,6-dideoxy-β-D-mannopyranosyl) -oxy] -1,3,5,6,9, 11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo [33.3.1] nonatoriaconta-19,21,23,25,27,29,31-heptaene -36-carboxylic acid.

  Rotrimine (clotrimazole) is commercially available from Schering and is 1- (O-chloro-α, α-diphenylbenzyl) imidazole.

  Daphorn tablets (Daphorn) are commercially available from Jacobus and are 4,4′-diaminodiphenyl-sulfone (DDS).

  Diflucan (fluconazole) is commercially available from Pfizer and is 2,4-difluoro-α-α'-bis (1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol.

  Monister-derm cream (miconazole) is commercially available from Ortho Dermatological and is 1- [2,4-dichloro-β-{(2,4-dichlorobenzyl) oxy} phenethyl] imidazole mononitrate.

  Mycostatin cream (nystatin) is commercially available from Westwood-Squibb.

Sporanox (Itraconazole) is commercially available from Janssen Pharmaceutical and is (±) -1-[(R ^* )-sec-butyl] -4- [p-[[2R ^* , 4S ^* ]-2- (2, 4-dichlorophenyl) -2- (1H-1,2,4-triazol-1-ylmethyl) -1,3-dioxolan-4-yl] methoxy] phenyl] -1-piperazinyl] phenyl] -Δ ² -1, 2,4, triazolin-5-one is converted to (±) -1-[(R ^* )-sec-butyl] -4- [p-[[2R ^* , 4S ^* )-2- (2,4-dichlorophenyl] ) -2- (1H-1,2,4-triazol-1-ylmethyl) -1,3-dioxolan-4-yl] methoxy] phenyl] -1-piperazinyl] phenyl] -Δ ² -1,2,4 , Triazolin-5-one or (±) -1-[(RS) -sec-butyl] -4- [p- [4- [p-[[(2R, 4S) -2- (2,4-dichlorophenyl) ) -2- (1H-1,2,3,4-triazol-1-ylmethyl) 1,3-dioxalan-4-yl] methoxy] phenyl] -1-piperazinyl] phenyl] -Δ ² -1,2, 4, Mixture with triazolin-5-one.

  Allalene hydrochloride (chloroquine HCl) is commercially available from Sanofi Pharmaceuticals and is 7- (chloro-4-[[4-diethylamino) -1-methylbutyl] amino] -quinoline dihydrochloride.

  Allalene phosphate (chloroquine phosphate) is commercially available from Sanofi Pharmaceuticals and is 7- (chloro-4-[[4-diethylamino) -1-methylbutyl] amino] -quinoline phosphate (1: 2).

  Daraprim (pyrimethamine) is commercially available from Glaxo Wellcome and is 5- (4-chlorophenyl) -6-ethyl-2,4-pyrimidinediamine.

Lariam (mefloquine HCl) is commercially available from Roche Laboratories and (R ^* , S ^* )-(±) -α-2-piperidinyl-2,8-bis (trifluoromethyl) -4-quinoline = methanol = The hydrochloride salt.

  Plaquenyl (hydroxychloroquine sulfate) is commercially available from Sanofi Pharmaceuticals and is 2-[[4- [7-chloro-4-quinolyl) amino] pentyl] ethylamino] ethanol = sulfate (1: 1).

  Capastarte sulfate (capreomycin sulfate) is commercially available from Dura Pharmaceuticals.

  Miambutol (ethambutol hydrochloride) is commercially available from Lederle Laboratories.

  Mycobutin (rifabutin capsule) is commercially available from Pharmacia & Upjohn, 1 ', 4-didehydro-1-deoxy-1,4-dihydro-5'-(2-methylpropyl) -1-oxorifamycin XIV, Or (9S, 12E, 14S, 15R, 16S, 17R, 18R, 19R, 20S, 21S, 22E, 24Z) -6,16,18,20-tetrahydroxy-1-1'-isobutyl-14-methoxy- 7,9,15,17,19,21,25-heptamethyl-spiro [9,4- (epoxypentadeca [1,11,13] trienimino) -2H-furo [2 ', 3': 7,8] Naphtho [1,2-d] imidazole-2,4′-piperidine] -5,10,26- (3H, 9H) -trione-16-acetate.

  Nidrazide (Isoniazid Injection) is commercially available from Apothecon.

  Paser (aminosalicylic acid) is commercially available from Jacobus and is 4-amino-2-hydroxybenzoic acid.

  Priftin is commercially available from Hoechst Marion Roussel, where rifamycin = 3-[[(4-cyclo-pentyl-1-piperazinyl) imino] methyl] or 3 [N- (4-cyclopentyl-1 -Piperazinyl) -formimidoyl] -2,7- (epoxypentadeca [1,11,13] trienimino) naphtho [2,1-b] furan-1,11 (2H) -dione = 21-acetate, is there.

  Pyrazinamide tablets (pyrazinamide) are commercially available from Lederle Laboratories and are the pyrazine analogs of nicotinamide.

  Rifadin (Rifampin capsule) is commercially available from Hoechst Marion Roussel and is available from 3-[[((4-methyl-1-piperazinyl) imino] methyl] rifamycin or 5,6,9,17,19,21- Hexahydroxy-23-methoxy-2,4,12,16,20,22-heptamethyl-8- [N-methyl-1-piperazinyl) formimidoyl] -2,7- (epoxypentadeca [1,11, 13] trieneimino) naphtho [2,1-b] furan-1,11 (2H) -dione = 21-acetate.

  Rifadin IV (rifampin for injection) is commercially available from Hoechst Marion Roussel and is available from 3-[[3- (4-methyl-1-piperazinyl) formimidyl] -2,7- (epoxypentadeca [1,11 , 13] trienimino) naphtho [2,1-b] furan-1,11 (2H) -dione = 21-acetate.

  Rifamate (Rifampin and Isoniazid) is commercially available from Hoechst Marion Roussel, 3- (4-Methyl-1-piperazinyliminomethyl) rifamycin SV (Rifampin), and isonicotinic acid hydrazide (isoniazid), It is.

  Rifater (Rifampin and Isoniazid and Pyrazinamide) is commercially available from Hoechst Marion Roussel and includes 3- (4-methyl-1-piperazinyliminomethyl) rifamycin SV (Rifampin) and isonicotinic acid hydrazide (isoniazid) ) And a pyrazine analog of nicotinamide (pyrazinamide).

  Ceromycin (cycloserine capsule) is commercially available from Dura Pharmaceuticals and is 3-isoxazolidinone, 4-amino-, (R)-.

  Streptomycin sulfate is commercially available from Pfizer and is O-2-deoxy-2- (methylamino) -α-L-glucopyranosyl- (1 → 2) -O-5-deoxy-3-C-formyl-α- L-lyxofuranosyl- (1 → 4) -N—N′-bis (aminoiminomethyl) = sulfate (2: 3) salt.

  Tice BCG (BCG vaccine) is commercially available from Organon and is a weakened live strain of Calmette and Guerin Mycobacterium bovis strains.

  Cycloserine (ceromycin capsules) is commercially available from Dura Pharmaceuticals and is 3-isoxazolidinone, 4-amino-, (R)-.

  Nidrazide (Isoniazid Injection) is commercially available from Apothecon and is a hydrazide of isonicotinic acid.

  Urised (methenamine) is commercially available from Poly Medica.

  Trecator-SC (ethionamide tablet) is commercially available from Wyeth-Ayerst and is 2-ethylthioisonicotinamide.

  Alferon N (interferon alfa-n3) is commercially available from Interferon Sciences and is interferon alfa-n3 (derived from human leukocytes).

  Crixiban (indinavir sulfate) is commercially available from Merck & Co., Inc. [1 (1S, 2R), 5 (S)]-2,3,5-trideoxy-N- (2,3-dihydro -2-hydroxy-1H-inden-1-yl) -5- [2-[[1,1-dimethylethyl) amino] carbonyl] -4- (3-pyridinyl-methyl) -1-piperazinyl] -2- (Phenylmethyl) -D-erythropentonamide sulfate (1: 1).

  Cytobane (ganciclovir) is commercially available from Roche and is 9-[[2-hydroxy-1- (hydroxymethyl) ethoxy] methyl] guanine.

  Cytobane-IV (ganciclovir sodium) is commercially available from Roche and is 9-[[2-hydroxy-1- (hydroxymethyl) ethoxy] methyl] guanine.

  Epivir (lamivudine) is commercially available from Glaxo Wellcome and is (2R, cis) -4-amino-1- (2-hydroxymethyl-1,3-oxathiolan-5-yl) -1H) -pyrimidine-2- Is on.

  Famvir (Famciclovir) is commercially available from SmithKline Beecham and is 2- [2- (2-amino-9H-purin-9-yl) ethyl] -1,3-propanediol = diacetate.

  Flumazine (rimantadine HCl) is commercially available from Forest and is α-methyltricyclo- [3.3.1.1/3.7] decane-1-methanamine hydrochloride.

  Foscavir (foscarnet sodium) is commercially available from Astra and is phosphonoformic acid trisodium salt.

  Hivid (Zarcitabine) is commercially available from Roche and is 4-amino-1-β-D-2 ′, 3 ′, dideoxyribofuranosyl-2- (1H) -pyrimidone, or 2 ′, 3′-dideoxy. Cytidine.

  Intron A (interferon alfa-2b) is commercially available from Schering.

  Inbilase (saquinavir mesylate) is commercially available from Roche Labs and is N-tert-butyl-decahydro-2- [2 (R) -hydroxy-4-phenyl-3 (S)-[[N- (2- Quinolylcarbonyl) -L-asparaginyl] amino] butyl- (4aS, 8aS) -isoquinoline-3 (S) -carboxamide = methanesulfonate.

Norvir (ritonavir) is commercially available from Abbott and is 10-hydroxy-2-methyl-5- (1-methylethyl) -1- [2- (1-methylethyl) -4-thiazolyl] -3,6 -Dioxo-8,11-bis (phenylmethyl) -2,4,7,12-tetraazatridencan-B-acid = 5-thiazolylmethyl ester [5S- (5R ^* , 8R ^* , 10R ^* , 11R ^* )].

  Rebetron combination therapy includes Rebetol (Ribavirin; 1-β-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide) and Intron A (interferon alfa-2b) and is commercially available from Schering ing.

  Rescripter (delavirdine mesylate) is commercially available from Pharmacia & Upjohn, and piperazine = 1- [3-[(1-methylethyl) amino] -2-pyridinyl] -4-[[5 (methylsulfonyl) ) -Amino] -1H-indol-2-yl] carbonyl] = monomethanesulfonate.

  Retrovir (ziduvudine) is commercially available from Glaxo Wellcome and is 3'-azido-3'-deoxythymidine.

  Retrovir IV (zidovudine) is commercially available from Glaxo Wellcome and is 3'-azido-3'-deoxythymidine.

  Symmetrel (amantadine hydrochloride) is commercially available from Endo Pharmaceuticals and is 1-adamantanamine hydrochloride.

Synagis (palivizumab) is commercially available from Medhnmune Inc. and is a humanized monoclonal antibody (IgGi _K ).

  Valtrex (valaciclovir HCl) is commercially available from Glaxo Wellcome and contains L-valine = 2 [[2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl) methoxy] ethyl ester. The hydrochloride salt.

  Widex (Didanocin) is commercially available from Bristol-Myers Squibb Oncology / Immunology and is 2 ', 3'-di-deoxyinosine.

Viracept (nerfinavir mesylate) is commercially available from Agouron and is [3S- [2 (2S ^* , 3S ^* ), 3α, 4aβ, 8aβ]]-N- (1,1-dimethylethyl) decahydro-2- [2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl) amino] -4- (phenylthio) butyl] -3-isoquinolinecarboxamide = monomethanesulfonate (salt).

  Viramune (Nevirapine) is commercially available from Roxane and is 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido [3,2-b: 2 ', 3'-] [1,4] Diazepine-6-one.

  Virazole (Ribavirin) is commercially available from ICN and is 1-β-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide.

  Vistide (cidofovir) is commercially available from Gilead Sciences and is 1-[(S) -3-hydroxy-2- (phosphonomethoxy) propyl] cytosine dihydrate (HPMPC).

  Zellit (stavudine (d4T)) is commercially available from Bristol-Myers Squibb Oncology / Immunology and is 2 ′, 3′-didehydro-3′-deoxythymidine.

  Symmetrel syrup (amantadine HCl) is commercially available from Endo Labs and is 1-adamantanamine hydrochloride.

  Combivir tablets (lamiduvine) are commercially available from Glaxo Wellcome and are 2 ', 3'-didehydro-3'-deoxythymidine.

  Zovirax (acyclovir) is commercially available from Glaxo Wellcome and is 2-amino-1,9-dehydro-9-[(2-hydroxyethoxy) methyl] -6H-purin-6-one.

  Daphorn tablets (Daphorn) are commercially available from Jacobus and are 4,4′-diaminodiphenyl sulfone (DDS).

  Daraprim (pyrimethamine) is commercially available from Glaxo Wellcome and is 5- (4-chlorophenyl) -6-ethyl-2,4-pyrimidinediamine.

  Fragyl 375 (metronidazole) is commercially available from Seale and is 2-methyl-5-nitro-imidazole-1-ethanol.

  Fragile ER tablets (metronidazole) are commercially available from Seale and are 2-methyl-5-nitro-imidazole-1-ethanol.

  Fragile I.V. (metronidazole) is commercially available from SCS and is 2-methyl-5-nitro-imidazole-1-ethanol.

  Floxone (furazolidone) is commercially available from Roberts and is 3- (5-nitrofurfurylidene-amino) -2-oxazolidinone.

  Mepron (Atobacon) is commercially available from Glaxo Wellcome and is trans-2- [4- (4-chlorophenyl) cyclohexyl] -3-hydroxy-1,4-naphthalenedione.

  Neutrexin (trimetrexate glucuronate gluconate) is commercially available from US Bioscience and is 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino) methyl] quinazoline = mono- D-glucuronate.

  Cipro (ciprofloxacin HCl) is commercially available from Bayer and is 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylate Monohydrochloride monohydrate.

  Floxine (ofloxacin) is commercially available from Ortho-McNeil Pharmaceutical and (±) -9-fluoro-2,3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl) -7-oxo- 7H-pyrido [1,3,3-de] -1,4-benzoxazine-6-carboxylic acid.

  Levaquin (levofloxacin) is commercially available from Ortho-McNeil Pharmaceutical and is (-)-(S) -9-fluoro-2,3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl)- 7-oxo-7H-pyrido [1,2,3-de] -1,4-benzoxazine-6-carboxylic acid hemihydrate.

  Mazaquin (Lomefloxacin HCl) is commercially available from Unimed and is (±) -1-ethyl-6,8-difluoro-1,4-dihydro-7- (3-methyl-1-piperazinyl) -4-oxo- It is the monohydrochloride of 3-quinolinecarboxylic acid.

  Noroxin (norfloxacin) is commercially available from Merck and is 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylic acid.

  Penetrex (enoxacin) is commercially available from Rhone-Poulenc Rorer and is 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -1,8-naphthyridine-3- Carboxylic acid is a sesquihydrate.

  Raxar (grepafloxacin HCl) is commercially available from Glaxo Wellcome and (±) -1-cyclopropyl-6-fluoro-1,4-dihydro-5-methyl-7- (3-methyl-1- Piperazinyl) -4-oxo-3-quinolinecarboxylic acid monohydrochloride mono-pentahydrate.

  Trovan (trovafloxacin mesylate) is commercially available from Pfizer and is (1,5,6a) -7- (6-amino-3-azabicyclo [3.1.0] hex-3-yl) -1- (2,4-difluorophenyl) -6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid = monomethanesulfonate.

  Zagam (sparfloxacin) is commercially available from Rhone-Poulenc Rorer and is 5-amino-1-cyclopropyl-7-cis-3,5-dimethyl-1-piperazinyl) -6,8-difluoro-1 1,4, dihydro-4-oxo-3-quinolinecarboxylic acid.

Bactrim (trimethoprim and sulfamethoxazole) is commercially available from Roche Labs and includes 2,4-diamino-5- (3,4,5-trimethoxybenzyl) pyrimidine (trimethoprim) and N ¹ ,- (5-methyl-3-isoxazolyl) sulfanilamide (sulfamethoxazole).

Bactrim DS (trimethoprim and sulfamethoxazole, strength double) is commercially available from Roche Labs, 2,4-diamino-5- (3,4,5-trimethoxybenzyl) pyrimidine (trimethoprim), and N ¹ ,-(5-methyl-3-isoxazolyl) sulfanilamide (sulfamethoxazole).

  Pediazole (erythromycin ethyl succinate and sulfisoxazole acetyl) is commercially available from Ross and is 2 '-(ethyl succinate) erythromycin and N' acetylsulfisoxazole. Note that sulfisoxazole is N- (3,4-dimethyl-5-isoxazolyl) -N-sulfanyl = acetamide.

  Septra (trimethoprim and sulfamethoxazole) is commercially available from Monarch and includes 5-[(3,4,5-trimethoxyphenyl) methyl] -2,4-pyrimidinediamine (trimethoprim) and 4-amino -N- (5-methyl-3-isoxazolyl) benzenesulfonamide (sulfamethoxazole).

  Septra DS (trimethoprim and sulfamethoxazole) is commercially available from Monarch and includes 5-[(3,4,5-trimethoxyphenyl) methyl] -2,4-pyrimidinediamine (trimethoprim), 4- Amino-N- (5-methyl-3-isoxazolyl) benzenesulfonamide (sulfamethoxazole).

  Co-trimoxazole is a combination chemotherapeutic agent consisting of trimethoprim (T) and sulfonamide sulfamethoxazole (S) in a ratio of 1: 5. Since co-trimoxazole continuously inhibits folic acid synthesis in microorganisms, it has bactericidal properties. The antibacterial activity range of co-trimoxazole includes a number of gram-positive and gram-negative aerobic bacteria, Chlamydia, Nocardia, protozoa (Pneumocystis carini), etc. In addition to being able to be used against Pneumocystis sp It is practical enough. http://www.infomed.org/100drugs/ctrifram.html.

  Bactrim IV injection (sulfamethoxazole) is commercially available from Roche Labs.

  Pediazole (erythromycin ethyl succinate and sulfisoxazole acetyl) is commercially available from Ross and is 2 '-(ethyl succinate) erythromycin and N' acetyl-sulfisoxazole. The sulfisoxazole is N- (3,4-dimethyl-5-isooxazolyl) -N-sulfanyl = acetamide.

  Fladantine (nitrofurantoin) is commercially available from Dura and is 1-[[(5-nitro-2-furanyl) methylene] amino] -2,4-imidazolidinedione.

  Macrobid (nitrofurantoin monohydrate macrocrystals) is commercially available from Procter & Gamble Pharmaceuticals, and 1-[[[5-nitro-2-furanyl] methylene] amino] -2,4-imidazolidinedione It is a hydrate.

  Macrodantine (nitrofurantoin macrocrystal) is commercially available from Procter & Gamble Pharmaceuticals and is 1-[[(5-nitro-2-furanyl) methylene] amino] -2,4-imidazolidinedione.

  Monurol Sachet (fosfomycin tromethamine) is commercially available from Forest, and (1R, 2S)-(1,2-epoxypropyl) phosphonic acid is converted to 2-amino-2- (hydroxymethyl) -1,3-propane. A (1: 1) compound with a diol added.

  Neggram Caplets (Nalidixic acid) is commercially available from Sanofi and is 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carboxylic acid.

  Septra (trimethoprim and sulfamethoxazole) is commercially available from Monarch and includes 5-[(3,4,5-trimethoxyphenyl) methyl] -2,4-pyrimidinediamine (trimethoprim), and 4- Amino-N- (5-methyl-3-isoxazolyl) benzenesulfonamide (sulfamethoxazole).

  Septra DS (trimethoprim and sulfamethoxazole) is commercially available from Monarch and includes 5-[(3,4,5-trimethoxyphenyl) methyl] -2,4-pyrimidinediamine (trimethoprim), and 4 -Amino-N- (5-methyl-3-isoxazolyl) benzenesulfonamide (sulfamethoxazole).

  Urised (combination of preservative methenamine, methylene blue, phenyl salicylate, benzoic acid and parasympatholytic agent (atropine sulfate) hyoscyamine) is commercially available from Poly Medica.

  Urobiotic-250 capsules (oxytetracycline HCl, sulfamethizole, and phenazopyridine HCl) are commercially available from Pfizer.

  Uroqid Acid No.2 tablets (methenamine mandelate) are commercially available from Beach.

  Bactroban (mupirocin) is commercially available from SmithKline Beecham and is (αE, 2S, 3R, 4R, 5S) -5-[(2S, 3S, 4S, 5S) -2,3-epoxy-5-hydroxy-4 -Methylhexyl] tetrahydro-3,4-dihydroxy-β-methyl-2H-pyran-2-crotonic acid dihydrate of the calcium salt (2: 1) of the ester with 9-hydroxynonanoic acid.

  Chloramycetin ophthalmic (chloramphenical) is commercially available from Monarch: (1) Acetamide = 2,2-dichloro-N- [2-hydroxy-1- (hydroxymethyl) -2- (4-nitro Phenyl) ethyl], and (2) D-threo-(−)-2,2-dichloro-N- [β-hydroxy-α- (hydroxymethyl) -p-nitrophenethyl] acetamide.

  Cortisporin (neomycin, polymyxin sulfate βs and acetic acid = hydrocortisone cream) is commercially available from Monarch and is 21- (acetyloxy) -11β, 17-dihydroxypregna-4-ene-3,20-dione .

Irotaisin (erythromycin ophthalmic ointment) is commercially available from Dista and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4 -[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hex-sopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5 , 7,9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxacyclotetradecane -2,10-dione.

  Neodecadrone (neomycin sulfate-dexamethasone sodium phosphate) is commercially available from Merck and is 9-fluoro-11β, 17-dihydroxy-16α-methyl-21- (phosphonooxy) pregna-1,4-diene-3,20- Dione disodium salt.

Polytrim (an ophthalmic solution of trimethoprim and polysixine beta sulfate) is commercially available from Allergan and includes 2,4-diamino-5- (3,4,5-trimethoxybenzyl) pyrimidine (trimethoprim), and polymyxin B ₁ And B ₂ sulfate (polythyxin β sulfate).

  Terra-Cortril (oxytetracycline HCl and hydrocortisone acetate) is commercially available from Pfizer.

  TobraDex (tobramycin and dexamethasone ophthalmic suspension and ointment) is commercially available from Alcon and O-3-amino-3-deoxy-aD-glucopyranosyl- (1 → 4) -O- [2,6- Diamino-2,3,6-trideoxy-aD-ribo-hexopyranosyl-1 (1 → 6)]-2-deoxy-L-streptamine. Dexamethasone has the chemical name 9-fluoro-11b, 17,21-trihydroxy-16a-methylpregna-1,4-diene-3,20-dione.

  3% Vira-A Ophthalmic Ointment (Vidarabine) is commercially available from Monarch and is 9H-purin-6-amine = 9-β-D-arabinofuranosyl monohydrate.

  Chibroxin (norfloxacin ophthalmic solution) is commercially available from Merck and is 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylic acid.

  Ciloxan ophthalmic solution (ciprofloxacin HCl) is commercially available from Alcon, 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinoline -Monocarboxylic acid monohydrochloride monohydrate.

  Ciloxan ophthalmic ointment (ciprofloxacin HCl) is commercially available from Alcon and 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinoline -Monocarboxylic acid monohydrochloride monohydrate.

  Ocuflox ophthalmic solution (ofloxacin) is commercially available from Allergan, (±) -9-fluoro-2,3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl) -7-oxo- 7H-pyrido [1,2,3-de] -1,4-benzoxazine-6-carboxylic acid.

  Blephamide ophthalmic ointment (sulfacetamide sodium and prednisolone acetate) is commercially available from Allergan, N-sulfanilyl-acetamide monosodium salt monohydrate (sulfacetamide sodium), and 11β, 17,21 -Trihydroxypereina-1,4-diene-3,20-dione = 21-acetate (11β, 17,21-trihydroxypreyna-1,4-diene-3,20-dione 21-acetate) (prednisolone acetate), It is.

  Blephamide ophthalmic suspension (sulfacetamide sodium and prednisolone acetate) is commercially available from Allergan, N-sulfanilyl-acetamide monosodium salt monohydrate (sulfacetamide sodium), and 11β, 17 , 21-Trihydroxypreyna-1,4-diene-3,20-dione = 21-acetate (11β, 17,21-trihydroxypreyna-1,4-diene-3,20-dione 21-acetate) (prednisolone acetate ).

A / T / S (erythromycin) is commercially available from Hoescht Marion Roussel (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* ) -4-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5 , 7,9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxacyclotetradecane -2,10-dione.

  Bactroban (mupirocin) is commercially available from SKB and is (αE, 2S, 3R, 4R, 5S) -5-[(2S, 3S, 4S, 5S) -2,3-epoxy-5-hydroxy-4- Methylhexyl] tetrahydro-3,4-dihydroxy-β-methyl-2H-pyran-2-crotonic acid dihydrate of the calcium salt (2: 1) of the ester with 9-hydroxynonanoic acid.

Benzamicin (erythromycin-benzoyl peroxide topical gel) is commercially available from Dermik and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3 , 5,7,9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxa Cyclotetradecane-2,10-dione (erythromycin).

  Betadine (Povidone-Iodo) is commercially available from Purdue Frederick.

  Creosin T (clindamycin phosphate topical solution) is commercially available from Pharmacia & Upjohn and L-threo-ID-galacto-octopyranoside = 7-chloro-6,7,8-trideoxy-6-[[((1 -Methyl-4-propyl-2-pyrrolidinyl) -carbonyl] amino] -1-thio = 2- (dihydrogen phosphate) = methyl, (2S-trans)-.

  Clindets (clindamycin phosphate cotton withdrawal) is commercially available from Stiefel, 7-chloro-6,7,8-trideoxy-6- (1-methyl-trans-4-propyl-L-2-pyrrolidine carboxamide ) -1-thio-L-threo-α-D-galacto-octopyranoside = 2- (dihydrogen phosphate) methyl.

Emgel (erythromycin) is commercially available from Glaxo Wellcome and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4-[( 2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5,7,9, 11,13-hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hexopyranosyl] oxy] oxacyclotetradecane-2,10-dione.

Erycette (erythromycin topical solution) is commercially available from Ortho Dermatological and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4 -[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5,7 , 9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hexopyranosyl] oxy] oxacyclotetradecane-2,10-dione.

  Klaron (sulfacetamide sodium lotion) is commercially available from Dermik.

  Mycostatin (nystatin cream) is commercially available from Westwood-Squibb.

Theramycin Z (Erythromycin Topical Solution) is commercially available from Medicis and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4 -[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5,7 , 9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-sopyranosyl] oxy] oxacyclotetradecane-2,10-dione is there.

T-Stat (erythromycin) is commercially available from Westwood-Squibb and is (3R ^* , 4S ^* , 5S ^* , 6R ^* , 7R ^* , 9R ^* , 11R ^* , 12R ^* , 13S ^* , 14R ^* )-4 -[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl) oxy] -14-ethyl-7,12,13-trihydroxy-3,5,7 , 9,11,13-Hexamethyl-6-[[3,4,6-trideoxy-3- (dimethylamino) -β-D-xylo-hex-opyranosyl] oxy] oxacyclotetradecane-2,10 -Dione.

  Excelderm (sulconazole nitrate) is commercially available from Westwood-Squibb and is (±) -1- [2,4-dichloro-β-[(p-chlorobenzyl) -thio] -plenethyl] imidazole mononitrate .

Fundizone (amphotericin B oral suspension) is commercially available from Bristol-Myers Squibb, [1R- (1R ^* , 3S ^* , 5R ^* , 6R ^* , 9R ^* , 11R ^* , 15S ^* , 16R ^* , 17R ^* , 18S ^* , 19E, 21E, 23E, 25E, 27E, 29E, 31E, 33R ^* , 35S ^* , 36R ^* , 37S ^* )]-33-[(3-amino-3,6-dideoxy-β- D-mannopyranosyl) -oxy] -1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo [33.3.1 ] Nonatria Conta-19,21,23,25,27,29,31-heptaene-36-carboxylic acid.

  Ramisir (terbinafine hydrochloride cream) is commercially available from Novartis and is (E) -N- (6,6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthalenemethanamine hydrochloride .

  Loprox (Auramine Cyclopirox) is commercially available from Hoescht Marion Roussel and is 6-chlorohexyl-1-hydroxy-4-methyl-2 (1H) -pyridone = 2-amino-ethanol salt.

  Rotrimine (clotrimazole) is commercially available from Schering and is 1- (O-chloro-α, α-diphenylbenzyl) imidazole.

  Lotrisone (clotrimazole and betamethasone dipropionate) is commercially available from Schering and includes 1- (O-chloro-α, α-diphenylbenzyl) imidazole (clotrimazole) and 9-fluoro-11β, 17 , 21-trihroxy-16β-methylpregna-1,4-diene-3,20-dione = 17,21-dipropionate (betamethasone dipropionate).

  Mentax (butenafine HCl) is commercially available from Penederm and is N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride.

  Monister-derm (miconazole nitrate) is commercially available from Ortho Dermatological and is 1- [2,4-dichloro-β-{(2,4-dichlorobenzyl) oxy)} phenethyl] imidazole mononitrate.

  Micelex (Clotrimazole) is commercially available from Alza and is [1- (o-chloro-α, α-diphenylbenzyl) imidazole.

  Mycostatin (nystatin) is commercially available from Westwood-Squibb.

  Naftin (Naftifine HCl) is commercially available from Allergan and is (E) -N-cinnamyl-N-methyl-1-naphthalene-methylamine hydrochloride.

  Nizoral (ketoconazole) is commercially available from Janssen and is cis-1-acetyl-4 [4-[[2- (2,4-dichlorophenyl) -2- (1H-imidazol-1-ylmethyl) -1,3 -Dioxolan-4-yl] methoxy] phenyl] piperazine.

  Nystop (nystatin) is commercially available from Paddock.

  Oxistat (oxyconazole nitrate) is commercially available from Glaxo Wellcome, 2 ', 4'-dichloro-2-imidazol-1-ylacetophenone = (Z)-[O- (2,4-dichlorobenzyl) oxime ] = Mononitrate.

  Celsan Rx (2.5% selenium sulfide lotion) is commercially available from Ross.

  Spectazole (econazole nitrate) is commercially available from Ortho Dermatological and is 1- [2-{(4-chlorophenyl) methoxy} -2- (2,4-dichlorophenyl) -ethyl] -1H-imidazole mononitrate.

  Denavir (penciclovir cream) is commercially available from SmithKline Beecham and is 9- [4-hydroxy-3- (hydroxymethyl) butyl] guanine.

  Zovirax (acyclovir) is commercially available from Glaxo-Wellcome and is 2-amino-1,9-dihydro-9- (2-hydroxyethoxy) methyl-6H-purin-6-one.

  Benzashave (benzoyl peroxide) is commercially available from Medicis.

  Betadine (Povidone-Iodo) is commercially available from Purdue Frederick.

  Betacept (chlorhexidine gluconate) is commercially available from Purdue Frederick.

  Setafil (a soap substitute) is commercially available from Galaderma.

  Clorpactin WCS-90 (sodium oxychlorocene) is commercially available from Guardiam Laboratories.

  Daphorn tablets (Daphorn) are commercially available from Jacobus and are 4,4′-diaminodiphenyl sulfone (DDS).

  Desquam-E (benzoyl peroxide) is commercially available from Westwood-Squibb.

  Desquam-X (benzoyl peroxide) is commercially available from Westwood-Squibb.

  Hibiclens (chlorhexidine gluconate) is commercially available from Zeneca.

  Hibistat (chlorhexidine gluconate) is commercially available from Zeneca.

  Impregon (2% tetrachlorosalicylanilide) is commercially available from Fleming.

  MetroCream (Metronidazole) is commercially available from Galaderma and is 2-methyl-5-nitro-1H-imidazole-1-ethanol.

  MetroGel (Metronidazole) is commercially available from Galaderma and is 2-methyl-5-nitro-1H-imidazole-1-ethanol.

  Noritate (Metronidazole) is commercially available from Dermik and is 2-methyl-5-nitro-1H-imidazole-1-ethanol.

  pHisoHex (hexachlorophene detergent) is commercially available from Sanofi and is 2,2′-methylene-bis [3,4,6-trichloro] = phenol.

  Sulfacet-R (10% sodium sulfacetamide and 5% sulfur) is commercially available from Dermik.

  Sulfamilone (matenide acetate) is commercially available from Bertek and is α-amino-ρ-toluenesulfonamide monoacetate.

  Triaz (benzoyl peroxide) is commercially available from Medicis.

  Vanoxide-HC (benzoyl hydrocortisone peroxide) is commercially available from Dermik and is 11β, 17,21-trihydroxypregna-4-ene-3,20-dione (hydrocortisone).

  Acticin is commercially available from Penederm and is (±) -3-phenoxybenzyl = 3- (2,2-dichlorovinyl) -2,2-dimethylcyclopropanecarboxylate.

  Elimite (permethrin) is commercially available from Allergan and is (±) -3-phenoxybenzyl = 3- (2,2-dichlorovinyl) -2,2-dimethylcyclopropanecarboxylate.

  Eulux (crotamiton) is commercially available from Westwood-Squibb and is N-ethyl-N- (o-methylphenyl) -2-butenamide.

  Lindane Lotion USP 1% (Linden) is commercially available from Alpharma.

  Fdex (fluorouracil) is commercially available from ICN and is 5-fluoro-2,4 (1H, 3H) -pyrimidinedione.

  Fluoroplex (fluorouracil) is commercially available from Allergan and is 5-fluoro-2,4 (1H, 3H) -pyrimidinedione.

  Furadantine oral suspension (nitrofurantoin) is commercially available from Dura and is 1-[[(5-nitro-2-furanyl) methylene] amino] -2,4-imidazolidinedione.

  Zybox (Linezolid) is commercially available from Pharmacia & Upjohn.

  One skilled in the art can appreciate that an antibiotic useful in the present invention is a physiologically active compound contained in any of the antibiotic formulations described above. For example, available azactam (Aztreonam) is usually an injectable solution. However, this antibiotic has propionic acid = (z) -2-[[[(2-amino-4-thiazolyl) [[(2S, -3S) -2-methyl-4-oxo-1-sulfo-3 -Azetidinyl] carbamoyl] methylene] amino] oxy] -2-methyl. Physician's Desk Reference (PDR), Medical Economics Company (Montvale, NJ), (53rd Ed.), Pp. 820-823, 1999.

  Formulation 5 can further include α-carotene, β-carotene, vitamin A, or combinations thereof in any suitable and effective amount.

  Referring to FIGS. 1-10, an adhesive patch 1 of the present invention is shown. The adhesive patch 1 is a formulation 5 disposed on at least a part of the front side 3 of the substrate 2, in at least a part of the front side 3 of the substrate 2, or on at least a part of and in part of the front side 3 of the substrate 2. including. Preferably, the formulation 5 is partially embedded in at least a part of the front side 3 of the substrate 2. The formulation 5 is not only disposed within at least a portion of the front side 3 of the substrate 2 but is also disposed on a portion of the surface of the front side 3 of the substrate 2. Preferably, the formulation 5 is placed over the entire surface of the front side 3 of the substrate 2.

[Substrate] The substrate 2 is formed by a front side 3 (side that touches the skin during use) and a back side 4 (side that is exposed to the surroundings during use). Substrate 2 must be non-irritating to human skin. The substrate 2 is a water-soluble or water-insoluble, self-supporting sheet made of a polymer material or a natural material, which gives the formulation 5 strength and consistency. The substrate 2 of the adhesive patch 1 can be vapor permeable. The substrate 2 may also be porous. This is because an opening for receiving the formulation 5 can be provided by making it porous, and the vapor permeability of the adhesive patch 1 can be guaranteed. Specifically, the base material 2 can hold the formulation 5 while allowing moisture from the skin to permeate.

  Alternatively, the substrate 2 of the adhesive patch 1 can be non-vapor permeable. The substrate 2 can also be non-porous, which increases the total amount of xanthophylls 15 absorbed by the skin. Specifically, the substrate 2 can hold the formulation 5 while preventing moisture from the skin from permeating.

  The substrate 2 may have any suitable thickness provided that it can provide a flexible, flexible, flexible, and / or extensible sheet from a water insoluble material. Specifically, the thickness of the substrate 2 can be about 0.001 mm to about 5.0 mm, about 0.001 mm to about 3.0 mm, or about 0.025 mm to about 1.25 mm.

  The substrate 2 can be made from any suitable material provided that it can form a flexible, flexible, flexible, and / or extensible substrate 2. The substrate 2 includes a flexible sheet of a water-soluble or water-insoluble material that supports the adhesive patch 1. The substrate 2 can include water-soluble or water-insoluble polymer fibers, a porous film, or any other kind of matrix having a space therein. Specifically, the substrate 2 is a lightweight, porous, flexible material composed of a nonwoven fabric of polymer fibers or natural fibers (for example, polyester, cotton, or cellulose fibers bonded with a sizing resin). It is a band. The substrate 2 may or may not be woven or knitted. Preferably, the base material 2 includes a nonwoven fabric.

  Specifically, the substrate 2 includes polyester fiber, polyurethane fiber, polyolefin fiber, polyamide fiber, natural fiber, cotton fiber, copolyester fiber, cellulose acetate fiber, polycellulose fiber, or any mixture thereof. be able to. Other stable, water-insoluble, flexible sheet materials and methods for producing suitable substrates 2 are described, for example, in U.S. Pat.No. 4,675,009; U.S. Pat.No. 5,536,263; U.S. Pat.No. 4,696,854; U.S. Pat. , And references therein, which are suitable as the substrate 2 according to the present invention. Injection of formulation 5 into substrate 2 is described, for example, using a continuous process mixer or as described herein, for example, as disclosed in US Pat. No. 5,536,263 and references therein. As can be done.

  Alternatively, the base material 2 may be formed of a silicone-containing compound, a fluorocarbon solution, or a combination of the front side 3 of the backing adhesive patch 1, the back side 4 of the base material 2, or both the front side 3 and the back side 4. The coated nonwoven substrate 2 may be used. Suitable silicone-containing compounds include, for example, polydimethyl siloxanes, dialkylsiloxanes, dimethylsiloxo vinyl alkenes, dialkylsiloxo vinyl alkenes, Dimethylsiloxo acrylates, dialkylsiloxo acrylates, vinyl terminated polydimethylsiloxanes with terminal vinyl groups, and polydialkylsiloxanes with terminal vinyl groups ( vinyl terminated polydialkylsiloxane). Exemplary silicone-containing compounds are commercially available from, for example, Goldschmidt Chemical Corp. (Essen, Germany); GE Silicones (Waterford, NY); Wacker Silicone Corp. (Adrian, MI); and Dow Corning Corp. (Midland, MI). Has been.

  Substrate 2 is, for example, Freudenberg Faservliesstoffe KG (Weinham, Germany); Sontara Technologies (division of DuPont Corporation) (Old Hickory, TN); Lystil SA (Brignoud Cedex, France); Dexter Nonwovens (Windsor Locks, CT); It can be made from a suitable nonwoven commercially available from Chicopee (New Brusnwick, NJ). Other commercial manufacturers that provide suitable nonwovens are listed on the Technical Textile website (http://www.technical-textiles.net/technical-textiles-index/orgL.htm).

  Surprisingly, it has been discovered that treated substrates, such as fluorocarbon treated nonwoven substrates, increase the yield of adhesive patches. Using a sizing-treated substrate material effectively adjusts the penetration rate and allows the gel or ointment to solidify after it has penetrated the substrate but before it completely penetrates the substrate. It becomes possible. In addition, when a base material treated with a sizing agent is used, it is possible to effectively adjust the depth of penetration before the ointment or gel solidifies. Surprisingly, increasing the control over the rate at which the ointment or gel penetrates the substrate generally does not require disposal because the back side of the substrate was too sticky to withstand processing and consumer acceptance. It has been discovered that improving the overall yield of the production process by reducing the amount of material that is lost.

Treat at least a portion of the substrate 2 with the sizing 8 so that the portion of the substrate 2 treated with the sizing 8 has a surface energy of about 20 dynes / cm ² to about 65 dynes / cm ^2. be able to. Specifically, the portion of substrate 2 treated with sizing 8 may have a surface energy of about 27 dynes / cm ² to about 56 dynes / cm ² . The sizing agent 8 reduces the surface energy of the portion of the substrate 2 that is treated by the sizing agent 8. Any suitable sizing agent 8 can be used provided that the portion treated by the sizing agent 8 has a surface energy of about 20 dynes / cm ² to about 65 dynes / cm ² . Suitable sizing agents 8 include, for example, fluorocarbon solutions, silicone-containing compounds, and combinations thereof. Specifically, the base material 2 can be a non-woven base material 2 treated with fluorocarbon. For example, the substrate 2 treated with fluorocarbon is Vilmed M1585 W / HY, Vilmed M1585H / HY, Vilmed M1586 W / HY, Vilmed M1586 H / HY, Vilmed M1570, Vilmed M1573 F, Vilmed M1573 FH, Vilmed Ml 577 F, Vilmed M1578 F, or Vilmed M1578 FH, all commercially available from Freudenberg Faservliesstoffe KG (Weinham, Germany). Alternatively, the silicone-treated substrate 2 may be made of one or more silicone-containing compounds (eg, polydimethylsiloxanes, dialkylsiloxanes, dimethylsiloxovinylalkenes, dialkylsiloxane vinylalkenes, dimethylsiloxoacrylates, A non-woven substrate 2 coated with dialkylsiloxoacrylates, polydimethylsiloxanes having vinyl groups at the ends, and polydialkylsiloxanes having vinyl groups at the ends).

 At least a portion of the substrate 2 can be treated with the sizing agent 8. The portion of the substrate 2 that can contain the formulation 5 can typically be the portion of the substrate 2 that is treated with the sizing 8. The entire surface of the front side 3 of the substrate 2 can be treated with the sizing agent 8, or a part of the surface of the front side 3 of the substrate 2 can be treated with the sizing agent 8. Preferably, the entire surface of the front side 3 of the substrate 2 can be treated with the sizing agent 8. In addition to the surface 3 on the front side 3 of the substrate 2 treated by the sizing agent 8, the sizing agent 8 comprises at least a portion of the surface of the substrate 2 below the surface (eg, from about 1/10 to about 9/10). Thickness, or about 1/4 to about 9/10 thickness). Specifically, the sizing agent 8 can permeate under the entire surface of the substrate 2.

  Suitable fluorocarbon treated substrates 2 are Vilmed M1585 W / HY, Vilmed M1585H / HY, Vilmed M1586 W / HY, Vilmed M1586 H / HY, Vilmed M1570, Vilmed M1573 F, Vilmed M1573 FH, Vilmed M1577 F, Vilmed M1578 F, and Vilmed M1578 FH, all of which are commercially available from Freudenberg Faservliesstoffe KG (Weinham, Germany).

As shown in FIGS. 1 to 6 and 9 to 10, the substrate 2 includes a front side 3 and a back side 4. The adhesive skin patch 1 is a formulation disposed on at least a part of the front side 3 of the base material 2, in at least a part of the front side 3 of the base material 2, or on at least a part of and in part of the front side 3 of the base material 2 Including 5.
Accordingly, the formulation 5 may be disposed on the entire surface of the front side 3 of the substrate 2, or the formulation 5 may be disposed on a part of the surface of the front side 3 of the substrate 2.

  Preferably, the formulation 5 is placed over the entire surface of the front side 3 of the substrate 2. The formulation 5 may be arranged not only on the front side 3 of the substrate 2 but also at least partly below the surface of the front side 3 of the substrate 2 (that is, the formulation 5 is part of the substrate 2). May be embedded embedded

  As shown in FIG. 9 and disclosed, for example, in US Pat. No. 5,536,263 and references therein, the formulation 5 can penetrate a substantial portion of the front side 3 of the substrate 2. For example, formulation 5 can penetrate between about 1/10 to about 9/10 of the thickness of substrate 2 or between about 1/4 to about 9/10 of the thickness of substrate 2. it can. That is, the formulation 5 may be partially embedded in the substrate 2. Preferably, the formulation 5 can be present on the entire surface of the front side 3 of the substrate 2 and part of the front side 3 of the substrate 2 (that is, the formulation 5 is partially embedded in the substrate 2 )

  Alternatively, a part of the front side 3 of the substrate 2 may contain the formulation 5 and another part of the front side 3 of the substrate 2 may contain any combination of the pressure sensitive adhesive 14 and the solvent 13. For example, the center circle on the front side 3 of the substrate 2 may contain the formulation 5 and the remaining part on the front side 3 of the substrate 2 may contain only the pressure sensitive adhesive 14. When the formulation 5 is embedded in the front side 3 of the substrate 2, the adhesive patch 1 is given strength and structure. For example, if the formulation 5 is partially embedded in the substrate 2, the adhesive patch 1 may be cut off when it is separated from the release liner 10 or when it is removed from the skin after use. Is minimized.

  When the adhesive skin patch 1 is placed on the patient's (eg, human) skin, the formulation 5 can be in continuous contact with the patient's skin surface.

  In some embodiments, the adhesive skin patch 1 allows skin respiration when in contact with the skin. More preferably, when the adhesive skin patch 1 is in prolonged contact with the skin, the formulation 5 is held in place and is typically experienced as the duration of use of the patch (eg up to about 24 hours, up to about 12 hours). , Up to about 8 hours, up to about 6 hours).

  As shown in FIGS. 3-6 and 9, the adhesive skin patch 1 can be reversibly applied to a release liner 10. The release liner 10 assists in maintaining the tackiness of the adhesive skin patch 1 prior to use, eg, during manufacturing, packaging, shipping and / or storage. Any suitable release liner 10 can be used in the present invention. Suitable release liners 10 are well known to those skilled in the art. See, for example, US Pat. No. 4,675,009; US Pat. No. 5,536,263; US Pat. No. 4,696,854; US Pat. No. 5,741,510, and references therein, for further description of release liners 10 useful in the present invention. The release liner 10 can include perforations 12 (see FIGS. 3, 5, and 6) that allow the tab 11 of the release liner 10 to be removed. By removing the knob 11 of the release liner 10, the adhesive skin patch 1 can be easily removed from the release liner 10.

◆ Xanthophylls In this specification, “xanthophylls” 15 refers to any of the group of by-product yellow pigments present in plant leaves, egg yolk, and human plasma. These pigment groups are oxidized derivatives of carotenes and are involved in photosynthesis. Examples of xanthophylls include lutein, violaxanthin and neoxanthine. In some embodiments, xanthophylls 15 can be derived from alfalfa, clove, kale, spinach, pumpkin, black bean tops, seaweed, green-yellow vegetables, or any combination thereof. Specifically, xanthophylls 15 can include lutein, zeaxanthin, and combinations thereof.

(1) xanthophylls 15 have the desired therapeutic and / or prophylactic properties (eg, xanthophylls 15 effectively treat epilepsy);
(2) Any appropriate xanthophyll 15 can be used as the xanthophyll 15 as long as the stability is maintained in the formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Specific xanthophylls 15 are preferably non-toxic to mammals (eg, humans) and are suitable for use as drugs (eg, topical use and / or use by inhalation). The specific xanthophylls 15 preferably comply with the standards of any administrative or governing body, such as FDA regulations.

As used herein, “lutein” refers to a compound having the structural formula:

化学的には、(3R,3'R,6'R)-β,ε-カロテン-3,3'-ジオールと命名される。ルテインは、濃い黄色を特徴とする物質であって、卵の黄身や黄体組織から抽出される。ルテインは身体によっては産生されず、食餌もしくはビタミン補充剤によって得る必要がある。ルテインは、ホウレンソウなどの青菜（green, leafy vegetables）、およびアルファルファなどのマメ科植物の中に大量に存在している。

Chemically, it is named (3R, 3′R, 6′R) -β, ε-carotene-3,3′-diol. Lutein is a substance characterized by a deep yellow color, and is extracted from egg yolk and corpus luteum tissue. Lutein is not produced by the body and must be obtained by diet or vitamin supplements. Lutein is present in large quantities in green, leafy vegetables such as spinach and legumes such as alfalfa.

  Lutein esterified form has the following structural formula:

ここで式中の R1 および R2 は、パルミチン酸などの脂肪酸から誘導した基である。

Here, R1 and R2 in the formula are groups derived from fatty acids such as palmitic acid.

  As used herein, “zeaxanthin” refers to a compound having the following structural formula:

化学的には、β-カロテン-3,3'-ジオールと命名される。ゼアキサンチンは、トウモロコシ、果物、種子、および卵の黄身の中に存在するカロテンである。

Chemically, it is named β-carotene-3,3′-diol. Zeaxanthin is a carotene present in corn, fruits, seeds, and egg yolks.

Xanthophyll 15
(1) that amount of xanthophyll 15 has the desired therapeutic and / or prophylactic properties (eg xanthophylls 15 effectively eliminate airborne pathogens, respiratory tract pathogens or combinations thereof) Kill or inactivate);
(2) The amount of xanthophyll 15 can be included in any suitable and appropriate amount, provided it remains stable in formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. The specific amount of xanthophyll 15 is preferably non-toxic to mammals (eg humans) and is suitable for use as a drug (eg topical use and / or use by inhalation). The specified amount of xanthophyll 15 complies with the standards of any administrative or governance body, such as FDA regulations.

  In general, the amount of xanthophyll 15 included in the formulation 5 depends on the particular type of compound or compounds used as xanthophyll 15. Specifically, xanthophyll 15 can be included from about 0.01% to about 99.9% by weight of Formulation 5. More specifically, xanthophyll 15 is up to about 50% by weight of formulation 5, up to about 25% by weight of formulation 5, up to about 20% by weight of formulation 5, up to about 10% by weight of formulation 5. Or up to about 5% by weight of formulation 5.

  The adhesive skin patch 1 is a xanthophyll 15 disposed in at least a part of the front side 3 of the base material 2, on at least a part of the front side 3 of the base material 2, or on at least a part and part of the front side 3 of the base material 2. including. That is, the xanthophyll 15 may be disposed on the entire surface of the front side 3 of the substrate 2 or the xanthophyll 15 may be disposed on a part of the surface of the front side 3 of the substrate 2. Preferably, xanthophyll 15 can be disposed on the entire surface of the front side 3 of the substrate 2.

  The xanthophyll 15 may be arranged not only on the front side 3 of the base material 2 but also at least partially below the surface of the front side 3 of the base material 2 (that is, the xanthophyll 15 is partially attached to the base material 2). Embedded in). As shown in FIG. 9 and disclosed, for example, in US Pat. No. 5,536,263 and references therein, xanthophyll 15 can penetrate a substantial portion of the front side 3 of the substrate 2. For example, xanthophyll 15 can penetrate from about 1/10 to about 9/10 of the thickness of the substrate 2, or from about 1/4 to about 9/10 of the thickness of the substrate 2. . That is, the xanthophyll 15 may be partially embedded in the base material 2.

  Preferably, the xanthophyll 15 can be disposed on the entire surface of the front side 3 of the substrate 2 and part of the front side 3 of the substrate 2 (that is, the xanthophyll 15 is partially embedded in the substrate 2). . Alternatively, a part of the front side 3 of the base material 2 may contain xanthophyll 15, and another part of the front side 3 of the base material 2 may contain the pressure sensitive adhesive 14. For example, the center circle on the front side 3 of the substrate 2 may contain xanthophyll 15, and the remaining portion on the front side 3 of the substrate 2 may contain only the pressure sensitive adhesive 14. When the adhesive skin patch 1 is placed on the skin of a patient (eg, a human), the xanthophyll 15 can be continuously in contact with the patient's skin surface.

  As used herein, “treat” or “treat” includes (i) deterring (eg, preventing) the occurrence of a condition (eg, respiratory infection). ), And (ii) suppressing or inhibiting the pathological condition (respiratory infection, etc.), and (iii) relieving symptoms related to the pathological condition (respiratory infection, etc.), Is included.

As used herein, “mammal” refers to a class of over 15,000 vertebrates, including humans, characterized by self-regulating body temperature, body hair, and, in females, breasts that produce milk. .
Mammals may specifically refer to humans.

◆ Solvent When solvent 13 is contained, it functions as a carrier for xanthophyll 15 and / or pressure-sensitive adhesive 14, and preferably these can be dissolved. Any suitable solvent 13 can be used provided that the solvent 13 effectively dissolves the xanthophyll 15 and / or the pressure sensitive adhesive 14 and the solvent 13 remains stable in the formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to.

  The solvent 13 can include one or more organic compounds, one or more inorganic compounds, and combinations thereof. Preferably, solvent 13 is one or more organic compounds (eg, esters, terpenes, alcohols, ketones, aldehydes, fatty acids, partially or fully esterified fatty acids) having the structure Cyclic, acyclic, (eg, alkyl), alicyclic (ie, bridged ring compound), or organic compounds having a combination of these functional groups along with those that are aromatic) Including. Examples of suitable solvents 13 are disclosed, for example, in Aldrich Handbook of Fine Chemicals, 2000-2001 (Milwaukee, WI).

  Preferably, solvent 13 includes a polyhydric alcohol, water, or a combination thereof. The polyhydric alcohol can be erythritol, propylene glycol, ethylene glycol, triethylene glycol, or combinations thereof. Erythritol is commercially available from Craglill (Minnetonka, Minnesota). Other suitable solvents 13 are, for example, glycerin; triacetin; diethylene glycol methyl ether; acetic acid diethylene glycol methyl ether; 1,3-propanediol; 2-methyl-1,3-propanediol; glycerol ricinoleate; PEG -6 caprylic acid / capric glycerides; PEG-6 caprylic / capric glycerides; caprylic / capric triglycerides; dicaprylic acid / propylene glycol dicaprate (propyleneglycol dicaprylate / dicaprate); glycerol monostearate; Glycerol monocaprylate; glycerol monolaurate; neopentyl alcohol; 1-hexadecanol; hydroxypropyl β-cyclodextrin; vitamin E; vitamin E acetate; deoxycholic acid; taurodeoxycholic acid 3-[(3-Cholamidopropyl) dimethylammonio] -1-propanesulfonic acid (3-[(3-cholamidopropyl) dimethylammonio] -1-propane-sulfonate); BigCHAP; cholic acid; cholesterol NF; propylene carbonate; Lecithins; pharmaceutically acceptable salts thereof; or combinations thereof.

  If solvent 13 is included, it is an appropriate amount, and that amount of solvent 13 is effective to dissolve xanthophyll 15 and / or pressure sensitive adhesive 14, and the effective amount of solvent 13 Can be used in any amount, provided that it remains stable in formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Specifically, solvent 13 can comprise from about 1.0% to about 70.0% by weight of Formulation 5; from about 3.0% to about 50.0% by weight; or from about 5% to about 30% by weight. In general, the amount of solvent 13 depends on the type of compound or compounds used as solvent 13. For example, polyhydric alcohol is up to about 70% by weight of formulation 5, or from about 20.0% to about 60.0% by weight of formulation 5, and water is from about 2.0% to about 50.0% by weight of formulation 5. Can be included.

  When the solvent 13 is included, it may be disposed in at least a part of the front side 3 of the base material 2, on at least a part of the front side 3 of the base material 2, or on at least a part and part of the front side 3 of the base material 2. it can. That is, the solvent 13 may be disposed on the entire surface of the front side 3 of the substrate 2, or the solvent 13 may be disposed on a part of the surface of the front side 3 of the substrate 2. Preferably, the solvent 13 can be disposed on the entire surface of the front side 3 of the substrate 2. The solvent 13 may be disposed not only on the front side 3 of the base material 2 but also at least partly below the surface of the front side 3 of the base material 2 (that is, the solvent 13 is partially disposed on the base material 2). Embedded in).

  As shown in FIG. 9 and disclosed, for example, in US Pat. No. 5,536,263 and references therein, the solvent 13 can penetrate a substantial portion of the front side 3 of the substrate 2. For example, the solvent 13 can penetrate from about 1/10 to about 9/10 of the thickness of the substrate 2, or from about 1/4 to about 9/10 of the thickness of the substrate 2. . That is, the solvent 13 may be partially embedded in the substrate 2. Preferably, the solvent 13 can be included in the entire surface of the front side 3 of the substrate 2 and part of the front side 3 of the substrate 2 (that is, the solvent 13 is partially embedded in the substrate 2). Alternatively, a part of the front side 3 of the substrate 2 may contain the solvent 13, and another part of the front side 3 of the substrate 2 may contain a combination of the pressure sensitive adhesive 14 and the xanthophyll 15. When the adhesive skin patch 1 is placed on the skin of a patient (eg, a human), the solvent 13 can be kept in continuous contact with the patient's skin surface.

◆ Pressure sensitive adhesive Formulation 5 can further include a pressure sensitive adhesive. Any suitable pressure sensitive adhesive 14 should be used provided that the pressure sensitive adhesive 14 provides the necessary tackiness to the adhesive skin patch 1 and that the pressure sensitive adhesive 14 maintains stability in the formulation 5. Can do.

  Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Suitable pressure sensitive adhesives 14 are known to those skilled in the art. Suitable pressure sensitive adhesives 14 are disclosed, for example, in US Pat. No. 4,675,009; US Pat. No. 5,536,263; US Pat. No. 4,696,854; US Pat. No. 5,741,510, and references therein. Preferably, the pressure sensitive adhesive 14 is an acrylate copolymer.

  The pressure-sensitive adhesive 14 is an appropriate amount, and the pressure-sensitive adhesive 14 of that amount can effectively give the adhesive skin patch 1 the necessary adhesiveness, and the effective amount of the pressure-sensitive adhesive 14 Any amount can be used provided that agent 14 remains stable in formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Formulation 5 can include from about 0.1% to about 50%, from about 0.5% to about 10.0%, or from about 1.0% to about 15.0% pressure sensitive adhesive 14 based on the weight of formulation 5.

  In general, the appropriate amount of pressure sensitive adhesive 14 depends on the specific type of pressure sensitive adhesive 14 used. For example, the pressure sensitive adhesive 14 can include one or more acrylate copolymers. Each of the one or more acrylic ester copolymers may comprise up to about 20.0% based on the weight of Formulation 5. Specifically, each of the acrylic ester copolymers can be included up to about 40.0% by weight of Formulation 5 or up to about 30.0% by weight of Formulation 5. More specifically, present from about 3.0% to about 40.0%, or from about 5.0% to about 30.0% by weight of Formulation 5 when all of one or more acrylate copolymers are combined. can do. Thus, the total amount of acrylic ester copolymers can be from about 3.0% to about 40.0% by weight of formulation 5, or from about 5.0% to about 30.0% by weight.

  Alternatively, the pressure sensitive adhesive 14 may be a hot melt pressure sensitive adhesive 14, or a solvent-based pressure sensitive adhesive 14 (eg, polyacrylate, polyisobutylene and polybutene), rubber, silicone pressure sensitive adhesive. Include Agent 14 (eg, polydimethylsiloxane and resin mixture), polystyrene-polybutadiene-polystyrene block polymer, polystyrene-polyisoprene-polystyrene block polymer, polystyrene-poly (ethylene-butylene) -polystyrene block polymer, or any combination thereof be able to. Adhesive 14 can also include a resin emulsion-type adhesive that may contain a vinyl acetate resin, an acrylic ester copolymer, a vinyl acetate / diocyl maleate copolymer, an acrylic copolymer, or any combination thereof. .

  Other suitable pressure sensitive adhesives 14 are disclosed, for example, in US Pat. No. 4,675,009; US Pat. No. 5,536,263; US Pat. No. 4,696,854; US Pat. No. 5,741,510, and references therein.

  The pressure sensitive adhesive 14 may be disposed in at least a part of the front side 3 of the base material 2, on at least a part of the front side 3 of the base material 2, or on at least a part and in a part of the front side 3 of the base material 2. it can. That is, the pressure-sensitive adhesive 14 may be disposed on the entire surface of the front side 3 of the substrate 2, or the pressure-sensitive adhesive 14 may be disposed on a part of the surface of the front side 3 of the substrate 2. Good. Preferably, the pressure sensitive adhesive 14 can be disposed on the entire surface of the front side 3 of the substrate 2.

  The pressure-sensitive adhesive 14 is not only disposed on the front side 3 of the substrate 2, but may be disposed on at least part of the surface of the front side 3 of the substrate 2 (that is, the pressure-sensitive adhesive 14 is It may be partially embedded in the substrate 2). As shown in FIG. 9 and disclosed, for example, in US Pat. No. 5,536,263 and references therein, the pressure sensitive adhesive 14 can penetrate a substantial portion of the front side 3 of the substrate 2. For example, the pressure sensitive adhesive 14 penetrates from about 1/10 to about 9/10 of the thickness of the substrate 2, or from about 1/4 to about 9/10 of the thickness of the substrate 2. be able to. That is, the pressure sensitive adhesive 14 may be partially embedded in the substrate 2.

  Preferably, the pressure sensitive adhesive 14 can be disposed on the entire surface of the front side 3 of the substrate 2 and part of the front side 3 of the substrate 2 (that is, the pressure sensitive adhesive 14 is partially on the substrate 2). Embedded in). Alternatively, a part of the front side 3 of the substrate 2 may include the pressure-sensitive adhesive 14, and another part of the front side 3 of the substrate 2 may include the xanthophylls 15. When the pressure-sensitive adhesive 14 is partially embedded in the front side 3 of the substrate 2, the tissue strength of the adhesive patch 1 is increased.

  For example, if the pressure sensitive adhesive 14 is partially embedded in the substrate 2, it will be cut off when the adhesive patch 1 is cut off from the release liner 10 or when it is peeled off from the skin after use. The possibility is minimized. When the adhesive skin patch 1 is placed on the skin of a patient (eg, a human), the pressure sensitive adhesive 14 can be continuously in contact with the patient's skin surface.

Emulsifier Formulation 5 or pressure sensitive adhesive 14 can optionally contain a compound that emulsifies Formulation 5 or pressure sensitive adhesive 14. One suitable compound that effectively emulsifies Formulation 5 or pressure sensitive adhesive 14 is pectin. The emulsifier (eg pectin) is in an appropriate amount, provided that the appropriate amount can effectively emulsify the formulation 5 or the pressure sensitive adhesive 14 and the emulsifier maintains stability in the formulation 5. Can be included in any amount. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Specifically, the emulsifier (eg, pectin) is about 30.0% by weight of Formulation 5, from about 1.0% to about 20.0% by weight of Formulation 5, or from about 2.0% to about 10.0% by weight of Formulation 5. Can contain up to%.

Polymer The pressure sensitive adhesive 14 can optionally contain one or more polymers 9. Polymer 9 imparts structure and strength to pressure sensitive adhesive 14 or imparts tissue strength to formulation 5. Any suitable polymer 9 can be applied as long as the polymer 9 imparts tissue strength to the pressure sensitive adhesive 14 or imparts tissue strength to the formulation 5 and the polymer 9 remains stable in the formulation 5. Can be used. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to.

  Suitable polymers 9 include natural polymers and synthetic polymers. Specifically, the polymer 9 includes, for example, karaya gum, polyacrylamide, xanthum gum, guar gum, hydrophilic polymer, hydrocolloid polymer, starch, starch derivative, vinyl acetate copolymer, polyvinyl pyrrolidone, polyethylene oxide, Algin, derivatives of algin, polyacrylate, gelatin, polymaleic acid, polyacrylic acid, polymaleic anhydride, polyurethane, polyurea, gum arabic, locust bean gum, modified guar gum, maltodextrin, carboxymethylcellulose, carboxypropylcellulose, polyvinyl Alcohol, poly (AMPS), or combinations thereof can be included. Other suitable polymers 9 are disclosed, for example, in US Pat. No. 4,675,009; US Pat. No. 5,536,263; US Pat. No. 4,696,854; US Pat. No. 5,741,510, and references therein. Preferably, polymer 9 can comprise polyacrylamide, karaya gum, or a combination thereof.

 Polymer 9 is in an appropriate amount provided that polymer 9 provides effective tissue strength to pressure sensitive adhesive 14 or formulation 5 and polymer 9 remains stable in formulation 5. Can be used in any amount. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. In general, the appropriate amount of polymer 9 depends on the specific type of polymer 9 used. Specifically, Karaya gum is as polymer 9 up to about 60% by weight of formulation 5, from about 5.0% to about 45% by weight of formulation 5, or from about 8.0% to about 40% by weight of formulation 5. Polyacrylamide can be used as polymer 9 up to about 40% by weight of formulation 5, from about 5.0% to about 35% by weight of formulation 5, or about 8.0% of formulation 5. Can be used in amounts from weight percent to about 30 weight percent; or both karaya gum and polyacrylamide are used as polymer 9 and the karaya gum is included from about 5.0 weight percent to about 35 weight percent of formulation 5, Acrylamide may be included from about 5.0% to about 30% by weight of Formulation 5.

◆ Wetting agent Formulation 5 can optionally include one or more wetting agents 17 to provide a wetting effect to pressure sensitive adhesive 14. The wetting agent 17 can optionally hydrate the polymer 9. Any suitable wetting agent 17 can be used provided that the wetting agent 17 effectively provides a wetting effect to the pressure sensitive adhesive 14 and the wetting agent 17 remains stable in the formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. One suitable wetting agent 17 is glycerin. Other suitable wetting agents 17 include polyhydric alcohols such as ethylene glycol, propylene glycol, triethylene glycol, tetraethylene glycol, sorbitol, and combinations thereof.

  Wetting agent 17 is in an appropriate amount, provided that amount of wetting agent 17 effectively provides a wetting effect to pressure sensitive adhesive 14 and wetting agent 17 remains stable in formulation 5. Can be included in any amount. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. In general, the appropriate amount of wetting agent 17 depends on the particular type of wetting agent 17 and polymer 9 used. For example, Karaya gum, polyacrylamide, or a combination thereof is used as polymer 9 and glycerin as wetting agent 17 with respect to the weight of formulation 5 from about 25.0% to about 70.0%, or from about 40.0% to about 55.0%. % By weight can be used.

Filler Formulation 5 can optionally include one or more fillers 6. Any suitable filler 6 can be used. Suitable fillers 6 include maltodextrin, dextrin, 70% sorbitol water, modified starch, depolymerized starch, and methylcellulose. As used herein, “maltodextrin” is dextrose equivalent, which is D-glucose. Maltodextrin is commercially available as Amaizo Lodex 5 from American Maize-Products (Hammond, IN). Any suitable amount of filler 6 can be used in formulation 5. The appropriate amount of filler 6 may depend in part on the specific type of filler 6 used. For example, maltodextrin can be included up to about 20.0% by weight of formulation 5, or from about 1.0% to about 10.0% by weight of formulation 5.

Skin protectant or skin conditioner Formulation 5 can optionally include skin protectant 18 (ie topical moisturizer or skin conditioner). Any suitable skin protectant 18 can be used provided that the skin is effectively protected or moisturized by skin protectant 18 and that the skin protectant remains stable in formulation 5. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Furthermore, the skin protectant 18 (ie topical moisturizer or skin conditioner) is preferably medicinally acceptable for topical use on humans.

  Suitable topical moisturizers 18 are, for example, calamine, aloe, lanolin, glycerin, vitamin E, vitamin E acetate, farnesol, glycyrrhetinic acid, aluminum hydroxide gel, cocoa butter, propylene glycol, ethylene glycol, triethylene glycol, solids Including fat, kaolin, mineral oil, petrolatum, topical starch, white petroleum, cod liver oil, shark liver oil, zinc oxide or any combination thereof. Other suitable topical moisturizers 18 are disclosed in US Pat. Nos. 6,096,334; 6,096,033; 5,741,510; 5,536,263; 4,675,009; 4,307,717; 4,274,420; 5,976,565; 5,536,263;

  As used herein, “aluminum hydroxide gel” refers to a suspension containing aluminum oxide (Al 2 O 3), primarily in the form of hydroxide. This is generally obtained by drying the product of the interaction of an aqueous solution of an aluminum salt with ammonium carbonate or sodium carbonate.

  In this specification, “cocoa butter” is a lipid substance in cocoa beans, that is, a high-density, oily solid obtained from cocoa beans that is used in the manufacture of chocolate, cosmetics, and tanning oils. Point to. Also known as theobroma oil, it has a lubricating and softening action on the skin.

  As used herein, “topical starch” refers to corn starch.

  As used herein, “kaolin” refers to aluminum silicate powdered and released from sand particles by the elutriation. Kaolin refers to the place name in China where this substance is abundant.

  As used herein, “white petroleum” refers to a mixture of refined hydrocarbons obtained from petroleum. This is bleached yellow petrolatum and is used as a relaxation agent or base for ointments. When applied to the skin, it is odorless and difficult to penetrate.

  As used herein, “mineral oil” is a mixture of heavy liquid petrolatum, liquid paraffin, or liquid petroleum; liquefied hydrocarbons obtained from petroleum, It refers to those commonly used as substrates.

  As used herein, “petrolatum” is a yellowish mixture of petroleum jelly, a soft part of paraffinic or methane-based hydrocarbons, as an analgesic agent for burns and abrasions. Moreover, it refers to what is generally used as a base for ointments.

  As used herein, “cod liver oil” refers to partial destearinization extracted from fresh livers of madras (Gadus morrhuae) and other cod families, including vitamins A and D. Refers to partially destearinated fixed oil.

  As used herein, “shark liver oil” refers to oil extracted from the liver of species of sharks, particularly Hypoprion brevirostris, which is a rich source of vitamins A and D. is there.

  As used herein, “zinc oxide” refers to ZnO, which is commonly used as a protective ointment.

As used herein, “calamine” is a pink powder of zinc oxide, a skin protectant containing about 98% zinc oxide and about 0.5% iron (III) oxide. "Aloe"("Aloe") refers to the Liliacaea Curacao Aloe: Curaco aloe (Aloe barbadenis Miller, Aloe vera Linne) or Cape Aloe: Cape Aloe (Aloe Ferrox) Miller: refers to dried leaf juice of Aloe ferox Miller and hybrids.
Aloe is commercially available from Terry Laboratories (Melbourne, FL) as Aloe Vera Gel.
Aloe Vera Gel is commercially available as Aloe Vera Gel 40X (20.0 wt% aqueous solution), Aloe Vera Gel 1X (0.5 wt% aqueous solution), Aloe Vera Gel 10X (5.0 wt% aqueous solution), or solid aloe vera. Solid aloe vera can be dissolved in a desired concentration in a carrier (eg, water).
Aloe vera marketed in these forms is also marketed as decolorized Aloe Vela.

  As used herein, “Vitamine E” is 3,4-dihydro-2,5,7,8-tetramethyl-2- (4,8,12-trimethyltridecyl) -2H -1-benzopyran-6-ol, and "Vitamine E acetate" is 3,4-dihydro-2,5,7,8-tetramethyl-2- (4,8,12 -Trimethyltridecyl) -2H-1-benzopyran-6-ol acetic acid, “lanolin” is a fatty secretion from sheep sebaceous glands (ie 33 high molecular weight alcohols and 36 fatty acids) deposited on wool fibers "Farnesol" is 3,7,11-trimethyl-2,6,10-dodecatrien-1-ol. Farnesol is commercially available from American Radiolabeled Chemicals (ARC) (St. Louis, MO), “glycyrrhetinic acid” is a β-amylin type pentacyclic triterpenoid derivative, Shown below:

  Skin protectant 18 is in an appropriate amount provided that the appropriate amount of protectant 18 effectively protects or moisturizes the skin, and skin protectant 18 maintains stability in formulation 5. Can be included in any amount. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Furthermore, it is preferable that the skin conditioner is acceptable as a medicinal product when used locally for humans.

  Specifically, skin protectant 18 may be included up to about 20.0%, up to about 10.0%, up to about 5.0%, or up to about 2.0% by weight of formulation 5. The appropriate amount of skin protectant 18 may depend in part on the specific type of skin protectant 18 included in formulation 5. For example, Aloe Vera Gel 10X may include up to about 20.0% by weight of Formulation 5, up to about 10.0% by weight of Formulation 5, up to about 5.0% by weight of Formulation 5, or up to about 1.0% by weight of Formulation 5. Can do. Further, vitamin E acetate can be up to about 10.0% of formulation 5, up to about 5.0% of formulation 5, up to about 3.0% by weight of formulation 5, up to about 2.0% by weight of formulation 5, or of formulation 5. Up to about 1.0% by weight can be included. Preferably, the skin conditioner is included in an amount in accordance with any state or federal regulations.

  The skin protecting agent 18 can be disposed in at least a part of the front side 3 of the base material 2, on at least a part of the front side 3 of the base material 2, or on at least a part and in a part of the front side 3 of the base material 2. . That is, the skin protecting agent 18 may be disposed on the entire surface of the front side 3 of the base material 2, or the pressure sensitive adhesive 14 may be disposed on a part of the surface of the front side 3 of the base material 2. . Preferably, the skin protecting agent 18 can be disposed on the entire surface of the front side 3 of the substrate 2. The skin protecting agent 18 is not only present on the front side 3 of the base material 2, but may be disposed at least partly below the surface of the front side 3 of the base material 2 (that is, the skin protecting agent 18 is disposed on the base material 2). Partially embedded). As shown in FIG. 9 and disclosed, for example, in US Pat. No. 5,536,263 and references therein, skin protectant 18 can penetrate a substantial portion of front side 3 of substrate 2. For example, the skin protectant 18 penetrates from about 1/10 to about 9/10 of the thickness of the substrate 2 or from about 1/4 to about 9/10 of the thickness of the substrate 2. Can do. That is, the skin protecting agent 18 may be partially embedded in the base material 2. Preferably, the skin protectant 18 can be disposed on the entire surface of the front side 3 of the substrate 2 and part of the front side 3 of the substrate 2 (that is, the skin protectant 18 is partially encased in the substrate 2). Buried). Alternatively, a part of the front side 3 of the base material 2 may include the skin protecting agent 18, and another part of the front side 3 of the base material 2 may include any combination of the solvent 13, the pressure sensitive adhesive 14, and the xanthophyll 15. . When the adhesive skin patch 1 is placed on the patient's (eg, human) skin, the skin protectant 18 can be continuously contacted with the patient's skin surface.

Preservative Formulation 5 can optionally include a preservative 7 useful for preventing bacterial growth, mold growth, fermentation and / or degradation. As used herein, “preservative” refers to any substance that prevents bacterial growth, mold growth, fermentation and / or degradation. Concise Chemical and Technical Dictionary, 4th enlarged edition, Chemical Publishing Co., Inc., NY, NY p. 939 (1986). Any suitable preservative 7 can be used provided that preservative 7 prevents bacterial growth, mold growth, fermentation and / or degradation and preservative 7 remains stable in formulation 5. . Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to.

  Suitable preservatives 7 are, for example, quat-15, parabens, dichlorobenzyl alcohol, ethylenediaminetetraacetic acid, formaldehyde, benzoin gum, imidazolidinyl urea, phenylmercuric acetate, polyaminopropyl biguanide, propyl gallate, sorbic acid , Cresol, chloroacetamide sodium benzoate, chloromethyl-methylisothiazolinone, chloromethyl-methylisothiazolone, benzalkonium chloromethyl-methylisothiazolinone ( chloromethyl-methylisothiazolinone benzalkonium chloride), anoctylisothiazolinone benzimidazol-compound chloromethyl-methylisothiazolinone-octyl Sothiazone (chloromethyl-methylisothiazolinone octylisothiazolinone), o-phenylphenol benzisothiazolinone, o-phenylphenol benzisothiazolinone, benzoisothiazolinone, 2-thiopyridine oxide aliphatic amine (an aliphatic amine) of 2-thiopyridineoxide), benzoic acid, edetic acid, phenolic acid, benzyl alcohol, isopropyl alcohol, benzenethonium chloride, bronopol, centrimide, chlorohexidine, chlorobutanol, chloro Cresol, phenol, phenoxyethanol, phenylethyl alcohol, phenylmercuric acetate, phenylmercuric borate, phenylmercuric nitrate, potassium sorbate, propylene glycol, sodium benzoate Thorium, sodium propionate, thimerosol, and their pharmaceutically acceptable salts. Preferably, the preservative is quat-15, methyl paraben, ascorbic acid, or combinations thereof, commercially available from Dow Chemical (Midland Michigan).

  Preservative 7 is an appropriate amount provided that preservative 7 prevents bacterial growth, mold growth, fermentation and / or degradation, and preservative 7 remains stable in formulation 5. Can be included in any amount. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Preservative 7 can comprise up to about 99.9% by weight of formulation 5, up to about 20.0% of formulation 5, up to about 5.0% of formulation 5, or up to about 1.5% by weight of formulation 5. In general, the appropriate amount of preservative 7 may depend in part on the specific type of preservative included in formulation 5. For example, quat-15 can be from about 0.01% to about 1.5% by weight of Formulation 5, from about 0.05% to about 0.15% by weight of Formulation 5, or from about 0.08% to about 0.12% by weight of Formulation 5. Can contain up to%.

Complexing agent In certain embodiments of the present invention, the amount of formulation 5 used is non-soluble and / or without solvent or with a specific solvent 13 to provide a stable xanthophyll 15. May contain. Thus, complexing agents can be used to adjust (ie control) the solubility, stability, and / or volatility of xanthophyll 15 in formulation 5. Any suitable complexing agent should be used provided that the complexing agent effectively solubilizes or stabilizes xanthophyll 15 and that the complexing agent remains stable in formulation 5 for a sustained period of time. it can. Preferably, the stability is a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transportation and / or storage of adhesive skin patches 1 It extends to. Also, the complexing agent is in an appropriate amount, and the amount of complexing agent effectively solubilizes or stabilizes xanthophyll 15, and the complexing agent is stable in formulation 5 for a sustained period of time. It can be used in any amount as long as it maintains its properties.

   Examples of suitable complexing agents include, for example, cyclodextrins. As used herein, “cyclodextrin” refers to a non-reducing cyclic oligosaccharide in which a ring is formed by at least six anhydroglucose units linked by α1-4 bonds. Cyclodextrins are generally produced by the action of the enzyme cyclodextrin glucosyltransferase [CGT-ase] on starch. The most common cyclodextrins are α, β and γ cyclodextrins, which contain 6, 7, and 8 anhydroglucose units, respectively, in the ring structure. All the hydroxy groups in cyclodextrin are directed to the outside of the ring, while the two rings, glycosidic oxygen and non-exchangeable hydrogen atoms, are inside the vacancies. Suitable for This combination makes the inside of the cyclodextrin pores hydrophobic and the outside hydrophilic. For example, the Cerestar website (http://www.cerestar.com); the Betadexcyclodextrin website (http://www.betadexcyclodextrin.com); and ML Bender and M. Komiyama, Cyclodextrin Chemistry, Springer, Berlin, 1978. See

  Cyclodextrins are enzymatically modified starches formed by the action of the enzyme cyclodextrin glucosyltransferase on starch. These are doughnut-shaped molecules that can interact with organic molecules to form complexes. Some organic molecules and inorganic salts may also bind to hydroxy groups in cyclodextrins. In general, three types of cyclodextrins are produced, namely α, β, and γ cyclodextrins, which have 6, 7, and 8 glucose molecules, respectively, in the ring. Electron-dense glycosidic oxygen atoms with high electron density are directed inward along the vacancies. The hydroxy group points to the outside of the ring. These hydrophilic groups interact with water to give the cyclodextrin water solubility. Hydrogen and glycosidic bond oxygen atoms located along the vacancies give the cyclodextrin molecule the ability to form hydrophobic and complex complexes with organic molecules. Since the C-6 carbon atom rotates freely, the C-6 carbon atom side of the vacancy of cyclodextrin is narrower than the C-2 and C-3 hydroxy group side.

Cyclodextrin derivatives are obtained, for example, by substituting one or more hydroxy groups with appropriate groups (ie pendant groups). Suitable pendant groups are, for example, sulfinyl groups; sulfonyl groups; phosphate groups; one or more (eg 1, 2, 3, or 4) hydroxy, carboxy, carbonyl, acyl groups A (C ₁ -C ₁₂ ) alkyl group optionally substituted with an oxy group, an oxo group, or a combination thereof. Specific examples of suitable pendant groups include methyl, ethyl, hydroxypropyl, carboxymethyl, sulfate, phosphate, and acrylate groups. For example, specific examples of pendant groups can include (C ₁ -C ₁₂ ) alkoxy groups optionally substituted with one or more hydroxy groups.

  Specific examples of suitable cyclodextrin derivatives include, for example, α-sulfate cyclodextrin, β-sulfate cyclodextrin, γ-sulfate cyclodextrin, α-hydroxypropyl cyclodextrin, β-hydroxypropyl cyclodextrin, γ-hydroxypropyl cyclodextrin. Dextrin, α-cyclodextrin phosphate, β-phosphate cyclodextrin, and γ-phosphate cyclodextrin.

  Cyclodextrins are starches that have been specially modified by the action of enzymes to form water-soluble cyclic molecules, and can hold other oily organic substances in their “pores”. Due to this unique property, cyclodextrins can be used to carry a variety of active ingredients (eg, drugs, fragrances, perfumes, vitamins) in a variety of formulations. Examples of the many advantages in its use include higher stability, water solubility, and controlled release. Specifically, cyclodextrins have the advantage of encapsulating and encapsulating substances. This protects the material. This leads to an extended shelf life and reduced loss due to degradation and degradation. Since cyclodextrins themselves are water-soluble, the solubility of substances that are extremely insoluble in water can be greatly increased, and cyclodextrins can be used for controlling the release of substances.

  Suitable cyclodextrins include α-cyclodextrins, β-cyclodextrins, and γ-cyclodextrins. Specifically, the cyclodextrin can be hydroxypropyl-β-cyclodextrin, hydroxypropyl-α-cyclodextrin, or a combination thereof. Moreover, cyclodextrin is arbitrary and may be branched.

  Suitable cyclodextrins and their derivatives are described in US Pat. No. 5,376,641, US Pat. No. 5,229,370; US Pat. No. 4,383,992, Cerestar website (http://www.cerestar.com); Betadexcyclodextrin website (http://www.betadexcyclodextrin.com); French et al., Archives in Biochem. and Biophysics, Volume III, (1965) 153-150; carbomer website (http: //www.carbomer. com), and references therein.

  In certain embodiments of the present invention, Formulation 5 further improves the permeability of xanthophylls to body tissues (eg, skin) and within it, with respect to formulations that do not include penetration enhancers. Effective penetration enhancers can be included. The penetration enhancer can generally be any penetration enhancer. Suitable penetration enhancers are, for example, diethylene glycol monoethyl ether (transcutol), dimethyl sulfoxide (DMSO), propylene glycol, ionic surfactants, nonionic surfactants, anionic surfactants, isopropyl myristate (IPM) , Calcipotriene, detergents, emollients, chelating agents (eg, calcium chelating agents such as EDTA, EGTA), and combinations thereof. Other examples of accelerators include Loramide DEA, ethoxydiglycol, NMP, triacetin, propylene glycol, benzyl alcohol, sodium laureth sulfate, dimethyl isosorbide, isopropyl myristate, olive squalane, medium chain triglyceride oil (MCT Oil ), Menthol, isopropyl palmitate, isopropyl isostearate, propylene glycol monostearate, lecithin, diisopropyl adipate, diethyl sebacate, oleic acid, ethyl oleate, urea, glyceryl oleate, caprylic / capric triglyceride, dicaprylic acid / Propylene glycol dicaprate, Laureth-4, Ores-2, Ores-20, Propylene carbonate, Nonoxynol-9, 2-n-nonyl-1,3-dioxolene, C7 to C14-H Rokarubiru substituted 1,3-dioxolen, including 1,3-dioxane (C7 to C14-hydrocarbyl substituted 1,3-dioxolan) or acetal and nonoxynol -15,,. Specifically, the skin absorption enhancer can include diethylene glycol monoethyl ether (transcutol). As used herein, “diethylene glycol monoethyl ether” or “transcutol” refers to 2- (2-ethoxyethoxy) ethanol [CAS NO. 001893].

  The penetration enhancer can be included in Formulation 5 in any suitable and suitable amount (eg, between about 1% and about 10% by weight).

  In certain embodiments of the present invention, the formulation 5 can further comprise a keratolytic agent. As used herein, a “keratolytic agent” is a substance that causes cell desquamation (loosening), debridement, or sloughing of epidermal surfaces. Point. Any suitable keratolytic agent can be used, and preferably the keratolytic agent effectively causes cell desquamation (detachment), removal of necrotic tissue, or molting of the epidermis surface. Preferably, the keratolytic agent is pharmaceutically acceptable for topical use on humans. Suitable keratolytic agents include, for example, alcloxa, resorcinol, or combinations thereof. As used herein, “alcloxa” refers to Al-chlorhydroxy allontoinate, and “resorcinol” refers to m-dihydroxybenzene or 1,3-benzenediol. .

  A keratolytic agent can be used in any amount, provided that the appropriate amount of keratolytic agent effectively causes cell desquamation (detachment), removal of necrotic tissue, or molting of the epidermis surface. Can be included. A keratolytic agent is a certain amount of alkaline substance (for example, potassium hydroxide (KOH), sodium hydroxide (NaOH), etc.) that is effective in causing cell desquamation (detachment), removal of necrotic tissue, or molting. ) Can be included. Alternatively, mechanical peeling, tape or the like may be used to cause cell desquamation (peeling), removal of necrotic tissue, or molting. Alternatively, radiant energy such as ultrasound, heat or the like may be used, or photodynamic therapy may be used to cause cell desquamation (detachment), removal of necrotic tissue, or molting.

Topical acne medication Formulation 5 can further include topical acne medication 15 useful for treating acne. The topical acne 15 is in an appropriate and appropriate amount, and that amount of the topical acne 15 effectively treats and / or prevents acne or pimples, and the topical acne 15 In formulation 5, it can be used in any amount, provided it remains stable over a sustained period. Preferably, its stability extends over a sustained period, such as up to about 3 years, up to about 1 year, eg up to about 6 months, typically spent in the manufacture, packaging, transport and / or storage of Patch 1. . In general, topical acne medication 15 can comprise from about 0.01% to about 99.9% by weight of Formulation 5. Specifically, the amount of topical acne 15 contained in Formulation 5 is up to about 5.0% by weight of Formulation 5, up to about 4.0% by weight of Formulation 5, and about 3.0% by weight of Formulation 5. % Up to about 0.5% to about 2.0% by weight of formulation 5. Preferably, the type and amount of topical acne medication 15 complies with FDA regulations (eg, 21 CFR Chapter 1, Section 333, Subpart D-Topical Acne Drug Products, April 1, 2000 Edition).

  The amount of topical acne 15 contained in the formulation 5 will generally depend on the specific type of compound or compounds used as the topical acne 15. For example, salicylic acid can be included up to about 99.9% by weight of Formulation 5, up to about 10.0% by weight of Formulation 5, up to about 2.0% by weight of Formulation 5, or up to about 2.0% by weight of Formulation 5.

  Specifically, resorcinol can be included up to about 2% by weight of Formulation 5 in accordance with 21 CFR Ch.1, §333.320 (a) and §333.310 (a). Specifically, according to 21 CFR Ch.1, §333.320 (b) §333.310 (b), resorcinol monoacetate can be included up to about 3% by weight of formulation 5. Specifically, in accordance with 21 CFR Ch.1, §333.310 (c), salicylic acid can be included from about 0.5% to about 2.0% by weight of Formulation 5. Specifically, according to 21 CFR Ch.1, §333.310 (d), sulfur can be included from about 3.0% to about 10.0% by weight of Formulation 5.

  The topical acne medication 15 can preferably be placed on the formulation 5 or in any part of the interior, which formulation 5 is placed on the front side 3 of the substrate 2. Preferably, the topical acne medication 15 can be placed over and within the entire formulation 5. When the adhesive skin patch 1 is placed on the patient's (eg, human) skin, the topical acne medication 15 can be continuously contacted with the patient's skin surface.

  The topical acne medicine 15 may be disposed on the entire surface of the front side 3 of the substrate 2, or the topical acne medicine 15 may be disposed on a part of the surface of the front side 3 of the substrate 2. Preferably, the topical acne medication 15 can be placed on the entire surface of the front side 3 of the substrate 2. The topical acne medicine 15 is not only present on the front side 3 of the substrate 2, but may be disposed on at least a part of the surface of the front side 3 of the base material 2 (that is, the topical acne medicine 15 May be partially embedded in the substrate 2). As shown in FIG. 10 and disclosed, for example, in US Pat. No. 5,536,263 and references therein, topical acne medication 15 can penetrate a substantial portion of the front side 3 of the substrate 2. For example, topical acne medication 15 penetrates about 1/10 to about 10/10 of the thickness of substrate 2 or about 1/4 to about 9/10 of the thickness of substrate 2 can do. That is, the topical acne medicine 15 may be partially embedded in the base material 2. When the adhesive skin patch 1 is placed on the patient's (eg, human) skin, the local acne drug 15 can be in continuous contact with the patient's skin surface.

  In one embodiment of the invention, an adhesive skin patch 1 is provided in which the formulation 5 does not contain xanthophylls 15. In such an embodiment, the adhesive skin patch 1 may be manufactured, transported and stored without the xanthophyll 15, and the xanthophylls 15 may be later introduced into the adhesive skin patch 1.

    Preferably, Formulation 5 is typically spent in the manufacture, packaging, transport and / or storage of adhesive skin patch 1, for a sustained period such as up to about 3 years, up to about 1 year, eg up to about 6 months And stability can be maintained. The stability of the xanthophylls 15 is based on, for example, that the formulation 5 containing the xanthophylls 15 is an adhesive formulation. This sticky formulation preferably retains xanthophyll 15 in an available form and provides the required stability, pressure sensitive stickiness, and effectiveness for a sustained period (eg, up to about 1 month, about 1 A hydrogel that lasts for up to 2 years, up to about 2 years, or up to about 3 years).

  The adhesive skin patch 1 can be any suitable size and shape. Further, the adhesive skin patch 1 having a desired size and shape can be obtained by cutting the adhesive skin patch 1 as necessary. The adhesive skin patch 1 can be cut with any suitable cutting means (eg scissors, scalpel or knife).

  The adhesive skin patch 1 can be of any suitable length. In one embodiment of the invention, the patch is a self-wound roll 25 that does not have a release liner 10 placed on the front side 3 of the substrate 2 of the adhesive skin patch 1. May be. For example, see FIG. In such embodiments, the length of the adhesive skin patch 1 can be about 12 inches to about 100 yards, about 10 feet to about 50 yards, or about 20 feet to about 20 yards. Further, in such embodiments, the width of the adhesive skin patch 1 can be about 0.1 inches to about 5.0 inches, about 0.1 inches to about 1.0 inches, or about 0.1 inches to about 0.5 inches.

  In an embodiment of the present invention, the adhesive skin patch 1 may have a release liner 10 that is rectangular and is placed on the front side 3 of the substrate 2 of the adhesive skin patch 1. In such embodiments, the length of the adhesive skin patch 1 can typically be up to about 10 inches, up to about 6 inches, up to about 4 inches, or up to about 2 inches. The adhesive skin patch 1 can have any suitable width. Typically, the width of adhesive skin patch 1 is up to about 5 inches, up to about 2.5 inches, up to about 1 inch, or up to about 0.5 inches. Furthermore, the adhesive skin patch 1 can have any suitable thickness. Typically, the thickness of the adhesive skin patch 1 is about 0.10 mm to about 2.0 mm, about 0.15 mm to about 1.0 mm, or about 0.20 mm to about 0.75 mm.

  In certain specific embodiments of the present invention, the shape of the adhesive skin patch 1 can be crescent, oval or circular. The diameter of the circular adhesive skin patch 1 can be from about 0.1 inches to about 10 inches. Preferably, the diameter of the adhesive skin patch 1 can be from about 1.5 inches to about 5 inches. See FIG.

  In another specific embodiment of the present invention, the shape of the adhesive skin patch 1 can be rectangular. The rectangular adhesive skin patch 1 can have a length of about 1 inch to about 10 inches and a width of about 1 inch to about 10 inches. Preferably, the rectangular adhesive skin patch 1 can have a length of about 1 inch to about 2 inches and a width of about 0.1 inch to about 0.75 inch. See FIG.

  In an embodiment of the present invention, the adhesive skin patch 1 may have a release liner 10 that is placed on the front side 3 of the substrate 2 of the adhesive skin patch 1. In such an embodiment, one or more adhesive skin patches 1 can be placed on the release liner 10. For example, one adhesive skin patch 1 may have one release liner 10 placed on the front side 3 of the base material 2 of the adhesive skin patch 1. Alternatively, about 2 to about 100, about 2 to about 20 adhesive skin patches 1 can be placed on the release liner. The cost when two or more patches 1 are placed on one release liner 10 is lower than when the skin patch 1 is placed separately on one release liner 10. In addition, some consumers included a single release liner 10 and one or more (eg, about 2 to about 20, or about 2 to about 10) adhesive patches 1 mounted on the release liner 10. One may prefer the convenience and comfort of using a single patch structure.

  The adhesive skin patch 1 can be applied to any suitable skin surface of the patient. For example, when the adhesive skin patch 1 is used for treatment of a local skin disease (eg, acne, acne, etc.), the adhesive skin patch 1 can be placed on the skin surface suffering from the local skin disease. In such embodiments, the adhesive skin patch can locally deliver a cosmetically and / or therapeutically effective amount of xanthophylls 15.

  Alternatively, when the adhesive skin patch 1 is used for the treatment of other diseases (for example, macular degeneration, angiogenesis, cancer, heart disease and diabetes), the adhesive skin patch is placed on any local skin surface, and xanthophylls 15 can be delivered systemically.

  The adhesive patch 1 according to the present invention can be formulated or manufactured using the above components. The adhesive patch 1 according to the present invention can be formulated or manufactured by any appropriate method. Preferably, the adhesive patch 1 is pre-injection of Formulation 5, as described herein or as described in US Pat. No. 5,536,263; US Pat. No. 5,741,510, and references therein. The substrate can be formulated or manufactured to be treated with sizing agent 8.

  The invention can be illustrated by the following non-limiting examples.

  All publications, patents, and patent documents cited herein are hereby incorporated by reference and shall be the same as if included by individual reference. The invention has been described with reference to various specific and preferred embodiments and means. However, it should be understood that all changes and modifications can be made without departing from the spirit and scope of the invention.

Embodiments of the present invention are best understood by referring to the following description and accompanying drawings that illustrate such embodiments. In the drawing number configuration included in this specification, the leading number of any reference number in the drawing corresponds to the drawing number. For example, it can be said that the adhesive patch 1 is included in FIG. However, if the same component is included across different drawings, the reference number is the same. Of the drawings
FIG. 1 illustrates the front side of an adhesive patch useful in the present invention. FIG. 2 illustrates the back side of an adhesive patch useful in the present invention. FIG. 3 illustrates the front side of an adhesive patch useful in the present invention with a release liner associated with the patch. FIG. 4 illustrates the back side of an adhesive patch useful in the present invention with a release liner associated with the patch. FIG. 5 illustrates the back side of an adhesive patch useful in the present invention, with the patch accompanied by a release liner and a portion of the patch separated from the release liner. FIG. 6 illustrates the back side of an adhesive patch useful in the present invention with a release liner associated with the patch and a portion of the patch separated from the release liner. FIG. 7 illustrates a top view of a specific patch useful in the present invention. FIG. 8 illustrates a top view of a specific patch useful in the present invention. FIG. 9 illustrates a specific adhesive skin patch useful in the present invention that is in use. FIG. 10 illustrates an enlarged cross-sectional view of a specific patch useful in the present invention.

Claims (103)

A flexible base material having a front side and a back side and at least part of the front side of the base material, at least part of the front side of the base material, or at least part of the front side of the base material and part of the base side A self-adhesive patch comprising:
Where the formulation is
Xanthophylls,
A solvent for dissolving xanthophylls;
A pressure-sensitive adhesive patch comprising a pressure-sensitive adhesive.   The adhesive patch according to claim 1, wherein the xanthophylls include lutein, zeaxanthin, capsorubin, capsanthin, astaxanthin, canthaxanthin, or any combination thereof.   2. The adhesive patch according to claim 1, wherein the xanthophylls include lutein and zeaxanthin.   2. The adhesive patch according to claim 1, wherein the xanthophylls include lutein and zeaxanthin, and the lutein is supplied in an unesterified form.   2. The adhesive patch according to claim 1, wherein the xanthophylls include lutein and zeaxanthin, and the lutein is supplied as trans-lutein.   2. The adhesive patch according to claim 1, wherein the xanthophylls include lutein and zeaxanthin, and the lutein is supplied as trans lutein having a purity of at least about 50% by weight.   The adhesive patch according to claim 1, wherein the xanthophylls include lutein and zeaxanthin, and the lutein is supplied as a trans-type lutein having a purity of at least about 50 wt% to about 90 wt%.   8. The adhesive patch according to claim 1, wherein the formulation is partially embedded in at least a part of the front side of the base material.   9. The adhesive patch according to any one of claims 1 to 8, wherein the formulation is disposed on the entire front surface of the substrate.   10. The adhesive patch according to any one of claims 1 to 9, wherein the substrate is porous.   10. The adhesive patch according to any one of claims 1 to 9, wherein the base material is non-porous.   10. The adhesive patch according to any one of claims 1 to 9, wherein the base material is vapor permeable.   10. The adhesive patch according to claim 1, wherein the base material is non-vapor permeable.   The adhesive patch according to any one of claims 1 to 13, wherein the base material contains a water-insoluble material.   The adhesive patch according to claim 1, wherein the substrate has a thickness of about 0.025 mm to about 1.25 mm.   The pressure-sensitive adhesive patch according to any one of claims 1 to 15, wherein the base material includes a nonwoven fabric.   17. The substrate according to any one of claims 1 to 16, characterized in that the substrate comprises polycellulose fibers, polyester fibers, polyurethane fibers, polyolefin fibers, polyamide fibers, cotton fibers, copolyester fibers, or any combination thereof. The adhesive patch according to one item.   18. The pressure-sensitive adhesive according to any one of claims 1 to 17, wherein the base material holds the formulation upon contact with the skin, and the patch allows moisture from the skin to pass therethrough. patch.   The adhesive according to any one of claims 1 to 17, wherein the base material holds the formulation upon contact with the skin, and the patch does not allow moisture from the skin to pass therethrough. patch.   20. The adhesive patch according to any one of claims 1 to 19, wherein the solvent includes a polyhydric alcohol, water, or a combination thereof.   21. The adhesive patch according to claim 20, wherein the polyhydric alcohol is propylene glycol, ethylene glycol, or a combination thereof.   The adhesive patch of claim 21, wherein the propylene glycol is present from about 3.0% to about 11.0% by weight of the formulation.   21. The adhesive patch of claim 20, wherein the water is present from about 2.0% to about 20.0% by weight of the formulation.   24. The adhesive patch according to any one of claims 1 to 23, wherein the solvent is present from about 6.0% to about 24.0% by weight of the formulation.   25. The adhesive patch according to any one of claims 1 to 24, wherein the formulation further comprises a filler.   26. The adhesive patch according to claim 25, wherein the filler is maltodextrin. 27. The adhesive patch of claim 26, wherein the maltodextrin is present from about 1.0% to about 10.0% by weight of the formulation.   28. The pressure sensitive adhesive patch according to any one of claims 1 to 27, wherein the pressure sensitive pressure sensitive adhesive comprises one or more acrylic ester copolymers.   29. The adhesive patch of claim 28, wherein the one or more acrylic ester copolymers are present from about 3.0% to about 20.0% by weight of the formulation.   29. The adhesive patch of claim 28, wherein the acrylic ester copolymers are present from about 5.0% to about 15.0% by weight of the formulation.   31. The pressure-sensitive adhesive patch according to claim 1, wherein the pressure-sensitive adhesive is disposed on the entire front surface of the base material.   31. The pressure-sensitive adhesive patch according to claim 1, wherein the pressure-sensitive adhesive is disposed on a part of the front side of the base material.   31. The pressure-sensitive adhesive patch according to claim 1, wherein the pressure-sensitive adhesive is partially embedded in at least a part of the base material.   The pressure-sensitive adhesive patch according to any one of claims 1 to 33, wherein the pressure-sensitive adhesive further contains glycerin.   35. The adhesive patch of claim 34, wherein the glycerin is present from about 25.0% to about 70.0% by weight of the formulation.   35. The adhesive patch of claim 34, wherein the glycerin is present from about 45.0% to about 55.0% by weight of the formulation.   The pressure-sensitive adhesive patch according to any one of claims 1 to 36, wherein the pressure-sensitive adhesive further comprises an emulsifier.   38. The adhesive patch according to claim 37, wherein the emulsifier is pectin.   39. The adhesive patch of claim 38, wherein the pectin is present from about 2.0% to about 10.0% by weight of the formulation.   31. The pressure-sensitive adhesive patch according to any one of claims 1 to 30, wherein the pressure-sensitive adhesive contains a compound that imparts tissue strength to the pressure-sensitive adhesive or the formulation.   The pressure sensitive adhesive or the compound that imparts tissue strength to the formulation is Karaya gum, polyacrylamide, xanthum gum, guar gum, natural polymer, synthetic polymer, hydrophilic polymer, hydrocolloid polymer, starch, starch derivative, Vinyl acetate copolymer, polyvinyl pyrrolidone, polyethylene oxide, algin, derivatives of algin, polyacrylate, polymaleic acid, polymaleic anhydride, polyurethane, polyurea, gum arabic, locust bean gum, modified guar gum, maltodextrin, carboxymethylcellulose, carboxy 41. The adhesive patch according to claim 40, wherein the adhesive patch is propylcellulose, polyvinyl alcohol, poly (AMPS), or a combination thereof.   41. The adhesive patch according to claim 40, wherein the compound that imparts tissue strength to the pressure sensitive adhesive or the formulation is polyacrylamide.   43. The adhesive patch of claim 42, wherein the polyacrylamide is present from about 8.0% to about 30.0% by weight of the formulation.   41. The adhesive patch according to claim 40, wherein the compound that imparts tissue strength to the pressure sensitive adhesive or the formulation is Karaya gum.   45. The adhesive patch of claim 44, wherein the karaya gum is present from about 8.0% to about 40.0% by weight of the formulation.   41. The adhesive patch according to claim 40, wherein the pressure-sensitive adhesive or the compound that imparts tissue strength to the formulation is a combination of polyacrylamide and karaya gum.   47. The pressure-sensitive adhesive patch according to any one of claims 1 to 46, wherein the pressure-sensitive pressure-sensitive adhesive is disposed on the entire front surface of the base material.   48. The adhesive patch according to any one of claims 1 to 47, wherein the formulation further comprises a skin conditioner.   49. The adhesive patch according to claim 48, wherein the skin conditioner is calamine, aloe, lanolin, glycerin, vitamin E, vitamin E acetate, farnesol, glycyrrhetinic acid, or any combination thereof.   50. The adhesive patch of claim 49, wherein the aloe is present from about 0.01% to about 2.0% by weight of the formulation.   50. The adhesive patch of claim 49, wherein the vitamin E acetate is present from about 0.01% to about 2.0% by weight of the formulation.   52. The adhesive patch according to any one of claims 1 to 51, wherein the formulation further comprises vitamin A.   50. The adhesive patch of claim 49, wherein the vitamin A is present from about 0.01% to about 2.0% by weight of the formulation.   54. The adhesive patch according to any one of claims 1 to 53, wherein the formulation further comprises one or more antimicrobial agents.   55. The adhesive patch according to claim 54, wherein the antibacterial agent is a β-lactam compound, an aminoglycoside, or an antifungal agent.  55. The adhesive patch according to claim 54, wherein the antibacterial agent is erythromycin, tetracycline, clindamycin, or cephalosporin.   57. The adhesive patch according to any of claims 1 to 56, wherein the formulation further comprises one or more disinfectants.   58. The adhesive patch of claim 57, wherein the disinfectant is triclosan, phenoxyisopropanol, chlorhexidine gluconate, povidone iodine, or any combination thereof.   59. The adhesive patch according to any one of claims 1 to 58, wherein the adhesive patch has a thickness of about 0.20 mm to about 0.75 mm.   60. The adhesive patch according to any one of claims 1 to 59, further comprising a release liner placed on the front side of the substrate.   62. The adhesive patch according to claim 61, wherein two or more patches are placed on the release liner.   61. The adhesive patch of claim 60, wherein about 2 to about 20 adhesive patches are placed on the release liner.   63. The adhesive patch according to any one of claims 1 to 62, wherein the adhesive patch is crescent-shaped, circular, or elliptical.   64. The adhesive patch of claim 63, wherein the adhesive patch has a diameter of about 0.1 inch to about 1.0 inch.   65. The adhesive patch according to any one of claims 1 to 64, further comprising a topical acne drug.   The topical acne drug is salicylic acid, resorcinol, resorcinol acetate, benzoyl peroxide, sulfur, retinol, retinoic acid, citric acid, alpha hydroxy acid, retinal, pharmaceutically acceptable salts thereof, or any of them 66. The adhesive patch according to claim 65, which is a combination.   67. The adhesive patch according to any one of claims 1 to 66, wherein the topical acne drug is salicylic acid or a pharmaceutically acceptable salt thereof.   68. The adhesive patch of claim 67, wherein the salicylic acid, or pharmaceutically acceptable salt thereof, is present from about 0.5% to about 2.0% by weight of the formulation.   67. The adhesive patch of claim 66, wherein the sulfur is present from about 3.0% to about 10.0% by weight of the formulation.   At least a portion of the substrate is treated with a hydrophobic sizing, and the portion treated with the hydrophobic sizing has a surface energy of about 20 dynes / cm 2 to about 65 dynes / cm 2. 70. The adhesive patch according to any one of claims 1 to 69, characterized in that it is characterized in that   71. The adhesive patch according to claim 70, wherein the hydrophobic sizing agent is a fluorocarbon solution, a silicone-containing compound, or a combination thereof. Substrates treated with the fluorocarbon solution are Vilmed M1585 W / HY, Vilmed M1585H / HY, Vilmed M1586 W / HY, Vilmed M1586 H / HY, Vilmed M1570, Vilmed M1573 F, Vilmed M1573 FH, Vilmed M1577 F, Vilmed. 71. The adhesive patch according to claim 70, wherein the adhesive patch is M1578 F, Vilmed M1578 FH, or a combination thereof.   The silicone-containing compound includes polydimethylsiloxane, dialkylsiloxane, dimethylsiloxane vinylalkene, dialkylsiloxane vinylalkene, dimethylsiloxane acrylate, dialkylsiloxane acrylate, polydimethylsiloxane having a vinyl group at the terminal, and terminal. 71. The adhesive patch according to claim 70, wherein the adhesive patch is a polydialkylsiloxane having a vinyl group, or a combination thereof.   71. The adhesive patch according to claim 70, wherein at least a part of the front side of the substrate is treated with the sizing agent.   71. The adhesive patch according to claim 70, wherein the entire front surface of the substrate is treated with the sizing agent.   71. The adhesive patch according to claim 70, wherein the entire substrate is treated with the sizing agent.   71. The adhesive patch according to claim 70, wherein the sizing agent is partially embedded in the base material.   71. The adhesive patch of claim 70, wherein a portion of the substrate treated with the hydrophobic sizing has a surface energy of about 27 dynes / cm <2> to about 56 dynes / cm <2>.   71. The adhesive patch according to claim 70, wherein the entire substrate is treated with the hydrophobic sizing agent.   71. The adhesive patch according to claim 70, wherein the hydrophobic sizing agent penetrates into at least a portion below the surface of the substrate.   71. The adhesive patch according to claim 70, wherein the hydrophobic sizing agent penetrates under the surface of the substrate.  82. The adhesive patch according to any one of claims 1 to 81, further comprising a penetration enhancer.   The penetration enhancer is diethylene glycol monoethyl ether (transcutol), dimethyl sulfoxide (DMSO), propylene glycol, ionic surfactant, nonionic surfactant, anionic surfactant, isopropyl myristate (DPM) calcipotriene , Detergents, relaxation agents, chelating agents (eg calcium chelators such as EDTA, EGTA), Loramide DEA, ethoxydiglycol, NMP, triacetin, propylene glycol, benzyl alcohol, sodium laureth sulfate, dimethylisosorbide, isopropyl myristate, olive Squalane, medium chain triglyceride oil (MCT oil), menthol, isopropyl palmitate, isopropyl isostearate, propylene glycol monostearate, lecithin, diisopropyl adipate, sebashi Diethyl acid, oleic acid, ethyl oleate, urea, glyceryl oleate, caprylic acid / capric acid triglyceride, dicaprylic acid / propylene glycol dicaprate, laureth-4, oleth-2, oleth-20, propylene carbonate, nonoxynol- 9, comprising 2-n-nonyl-1,3-dioxolene, C7-C14-hydrocarbyl substituted 1,3-dioxolene, 1,3-dioxane, or acetal, and nonoxynol-15 Item 82. The adhesive patch according to Item 82.   85. The adhesive patch of claim 82, wherein the penetration enhancer is present from about 0.1% to about 20.0% by weight of the formulation.   85. The adhesive patch according to any one of claims 1 to 84, further comprising a keratolytic agent.   86. The adhesive patch of claim 85, wherein the keratolytic agent comprises alcloxa, resorcinol, or a combination thereof.   86. The adhesive patch of claim 85, wherein the keratolytic agent is present from about 0.1% to about 5.0% by weight of the formulation.   The adhesive patch according to any one of claims 1 to 87, further comprising vitamin A, all-trans retinoic acid, or a combination thereof. A flexible substrate having a front side and a back side, and a formulation present on at least a portion of the front side of the substrate, at least in a portion of the front side of the substrate, and at least on a portion of the front side of the substrate A sticky patch containing objects,
Where the formulation is
Xanthophylls,
An adhesive patch comprising: a hot melt adhesive. A method of locally delivering xanthophylls to a topical skin surface, comprising:
Applying the adhesive patch according to any one of claims 1 to 89 locally over a period effective to locally deliver xanthophylls to the topical skin surface. Method.   90. A method for systemically delivering xanthophylls to a mammal, wherein the adhesive patch according to any one of claims 1 to 89 is applied topically over a period of time effective to deliver xanthophylls to the whole body of the mammal. Characterized in that it comprises a step of automatically placing.   A method of treating or preventing acne or pimples in a mammal in need of such treatment, against a skin surface of a mammal suffering from or associated with the risk of acne or pimples 90. A method comprising applying an adhesive patch according to any one of claims 1 to 89 for a period effective to effectively treat acne or pimples.   94. The method of claim 92, wherein the mammal is a human.   94. The method of claim 92, wherein the skin surface of a mammal at risk for acne or pimple is on the face, neck, shoulders, chest, back, or any combination thereof.   94. The method of claim 92, wherein the period is from about 1 hour to about 12 hours.   A method for exfoliating a mammalian skin surface, wherein the adhesive patch according to any one of claims 1 to 89 is applied to a mammalian skin surface in need of such exfoliation over an effective period of time. Effectively peeling the skin surface by removing the adhesive patch.   98. The method of claim 97, wherein the mammal is a human.   99. The method of claim 96, wherein the effective period is from about 1 second to about 12 hours.   A method for improving the appearance of a mammalian skin surface for a period of time effective to effectively improve the appearance of the skin surface of a mammalian skin surface in need of such improvement. 90. A method comprising the step of applying the adhesive patch according to any one of 1 to 89.   100. The method of claim 99, wherein the mammal is a human.   The adhesive patch according to any one of claims 1 to 89, which is used for drug therapy.   90. A method of using the adhesive patch according to any one of claims 1 to 89 for the manufacture of a medicament for the treatment of a topical skin condition.   90. To produce a medicament for the treatment of acne in mammals, for the treatment of pimples in mammals, for the appearance of mammalian skin surfaces, or any combination thereof, according to any one of claims 1 to 89. A method of using the adhesive patch described.

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