Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
  • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms

Definitions

• the invention relates to pharmaceutically / hygienically / cosmetically applicable wick systems and a method for their production.
• wick is intended to express that there is a strand-like structure which can be rolled up and with which the active substance is combined before the active substance system is manufactured.
• This strand can consist of a uniform material or a material mixture.
• the active substance can be present as such or in the form of an active substance preparation.
• the active ingredient can be dissolved in the strand. If it is a solid active substance, an auxiliary substance can also be dissolved in the active substance. Both alternatives can be useful to find a usable - e.g. B. sufficiently tear-resistant - to achieve consistency or to improve the diffusion properties.
• the strand it is also possible for the strand to have a microporous or even macroporous structure. It is important that the active substance can be released from the strand to the environment.
• the strand is preferably flat, but can also be a round wick, the active ingredient usually being stored in the capillaries and being able to be transported through them.
• the active substance strand in the manufacture of the products according to the invention in a continuous process e.g. from a roll, which term includes a spool, or from another storage container, such as a loop fabric, can be applied to the plasters or system strands and that the separation is then carried out in a continuous process, e.g. B. with the help of a punch or a punch, can be made simultaneously with the separation of the patch.
• the active ingredient is in a discrete room, e.g. in a reservoir in the form of a flat bag, or in the entire layer on the carrier film (matrix plaster); a number of variants and mixed forms are also known.
• a layer containing the active substance is formed:
• the delivery of the carrier and the metering of active ingredient and / or active ingredient carrier can generally only take place in technically complex cycles. This also applies if a carrier like a "non-woven fabric" is applied to the web first, and then onto the web the active ingredient is brought to ⁇ ge *
• the object of the invention is therefore to ensure a continuous introduction of the active substance onto or into a strand material from which the systems are then separated.
• strand is understood to mean narrow webs, although the strand of active substance is less broad than the system strand
• the active ingredient as such or in a suitable manner is applied in a thin, strand-like primary carrier with suction properties or other similar absorption properties due to the chemical nature, optionally in the form of a solution, comparable to the introduction into a wick
• the product is called the active ingredient strand below
• the invention now relates to an active substance-containing device for dermal use, which is characterized in that it is constructed from a) an active substance strand b) a wider system strand which clearly projects beyond the active substance strand on both sides and, c) if the system strand is not Function of the backing layer fulfilled, on one side a backing layer and d) on the other side has a removable protective layer.
• the invention furthermore relates to a process for introducing active substances into systems for dermal use by incorporating the active substance into a carrier, which is characterized in that the active substance is continuously introduced into or applied to a carrier and thus an active substance strand is produced which thus contained strand combined with a wider system strand which clearly exceeds the active ingredient strand on both sides, this system on one side with a removable protective layer and, if the system strand does not fulfill the function of the backing layer, on the other side with a backing layer and the Combined strands are then separated in such a way that significant amounts of active ingredient can not escape at the edges.
• the removable protective layer is therefore always present, regardless of whether the system strand fulfills the function of the back layer or not.
• the invention relates to a process for the continuous introduction of active substances into continuously produced, preferably relatively large-area, thin systems such as wafers or active substance plasters by incorporating the active substance into an active substance strand and attaching this strand to a system strand and / or attaching a system strand to an active substance strand and providing it the final system with a removable protective layer and, if necessary, a backing layer, as well as the products that are produced by this method.
• Such systems can also have a membrane for controlled release.
• the active ingredient as such or in the form of an active ingredient preparation e.g. by dipping, printing or in a similar manner in or on the strand-shaped carrier. It is also possible to produce a mass into which the active ingredient is incorporated and extrude this mass, possibly applying it directly to the system strand to form a strand of active ingredient, e.g. spray on or extrude, or spin, weave or - like nonwoven fabric - join together from extruded strands, threads or fibers.
• the mass can also be poured onto the system strand, using solvents or as a hot melt or in powder form ⁇ vie when coating, if necessary drying, cooling or fixing by energy supply and thus producing in situ, cutting into strands and later "off the roll" apply.
• a strand of active substance can also be formed or consist of fibers, fabrics, nonwovens or suitable substances - including polymers - loaded with the active substance. In this respect, the usual plastics, for. B.
• Such carrier materials in dermal or transdermal systems are known to the person skilled in the art from: a) Martin C. Musolf: "Pressure-Sensitive Adhesives: Science and Engineering” in Transdermal Controlled Systemic Medications, ed. By YW Chien, Marcel Dekker Inc., New York 19S7 , p. 93-1 12 b) "Handbook of Adhesives", ed. By Irving Skeist, Va Nostrand Reinhold, New York 1990, 3rd edition.
• the active ingredient carrier is applied in a continuous process according to a preferred embodiment in one strand to the system strand and dimensioned in one operation by separating / punching the individual systems.
• the "system strand” expediently consists of one or more plastic and / or aluminum foils, optionally laminated together.
• the active ingredient strand can be applied "from the roll" to the system strand.
• active substance strands can be combined with different conventional systems such as full-area matrix, membrane, etc. ren, so that different systems in the area or in the layers of the system, e.g. Concentrations and delivery mechanisms can be brought about to improve controlled delivery; you can e.g. Place highly concentrated strands in layers far from the skin, less concentrated ones in the layer close to the skin (or vice versa), so that at the beginning there is a lower and later a higher release (or vice versa)
• light-sensitive and / or toxic or volatile active substances can be processed in such a way that the strand of active substance is completely or partially encapsulated.
• Such capsule materials must of course be permeable to the active ingredient on at least one side and the strand of active ingredient should then be completed immediately after application, e.g. by applying an additional layer, for example by lamination.
• a temperature sensitivity of the active ingredient in the active ingredient strand during processing with hot-melt adhesive or the sensitivity during drying can then be taken into account in that the active ingredient is applied to the strand on the side that. faces away from the liquid hot melt adhesive.
• the rear layer of the active substance strand has a temperature-insulating effect.
• the active substance strands can also be applied continuously in the form of a grid, mesh fabric and the like to the corresponding system strands (carrier, intermediate or adhesive layers). You can proceed so that a second active ingredient is integrated in the same way, for. B. by two or 16. more different meshes with active ingredients are applied to the system strand or the corresponding carrier or adhesive layers.
• a wide variety of active substances are suitable for the invention, in particular transdermally applicable active substances are suitable. Typical examples are
• Corticosteroids hydrocortisone, prednisolone, beclomethasone propionate, flumethasone, triamcinolone, triamcinolone acetonide, fluocinolone, fluocinoline acetonide, fluocinolone acetoidate acetate, clobetasol propionate, etc.
• Analgesic, anti-inflammatory drugs acetaminophen, mefenamino acid, flufenamic acid, diclofenac, diclofenac sodium alclofenac, oxyphenbutazone, phenylbutazone, upbuprofen, flurbiprofen, salicylic acid, 1-menthol, tennufen, camphenol, sulindin, sulindin etc.
• Hypnotically active sedatives phenobarbital, amobarbital, cyclobarbital, triazolam, nitrazepam, lorazepam, haloperidol, etc.
• Opiates such as diamorphine, morphine base, morphine hydrochloride, dihydrocodeine, buprenorphine fentanyl
• Tranquilizers fluphenazine, thioridazine, lorazepam, flunitrazepam, chlorpromazine, etc.
• Antihypertensives pindolol, indenolol, nifedipine, lofexidine, nipradinol, bucumolol, clonidine, bopindolol, bupranolol etc.
• Coronary substances such as ISDN, nitroglycerin and their compounds, antihypertensive diuretics: hydrothiazide, bendroflumethiazide, cyclopenthiazide, etc.
• Antibiotics penicillin, tetracycline, oxytetracycli, fradiomycin sulfate, erythromycin, chloramphenicol, etc.
• Anesthetics lidocaine, benzocaine, ethylaminobenzoate, etc.
• Antimicrobial agents benzalkonium chloride, nitrofurazone, nystatin, acetosulfamine, clotri azole, etc.
• Antifungals pentamycin, amphotericin B, pyrrole nitrine, clotrimazole, etc.
• Vitamins vitamin A, ergocalciferol, chlolecalciferol, octotia in, riboflavin butyrate, etc.
• Antiepileptics nitrazepam, meprobamate, clonazepam, etc.
• Coronary vasodilators dipyridamole, erythritol tetranitrate, pentaerythritol tetranitrate, propatyl nitrate, etc.
• Antihistamines diphenylhydramine hydrochloride, chlorpheniramine, diphenylimidazole, sw.
• Thymoleptics doxepin, etc.
• the products produced according to the invention are suitable for dermal, but in particular for transdermal use on the epidermis or mucosis in all forms.
• This term also includes the use as hygiene tablets, i.e. oral hygiene tablets. These are sheet-like systems that serve to improve oral hygiene by means of cleaning and / odor-reducing or odor-masking active substances or combinations of active substances.
• Such oral hygiene tablets are thus used orally and can be completely soluble in the mouth; however, oral use is also possible, using not rigid, but very plastic products, the components of which are selected so that they can be completely dissolved in the body fluids and can be degraded physiologically.
• Such oral tablets can also contain pharmaceutical active ingredients instead of hygienic active ingredients.
• the process according to the invention and the products thus obtained have a number of advantages.
• the speed in the production of systems can be increased, since production cycles, vertical movements in relation to the guidance of the system path are not necessary.
• the necessary separation can - also continuously - be carried out by rotating cutting rollers, which may at the same time emboss on the edges.
• Another particular advantage is the improvement in quality and the avoidance of rejects because of the absolute homogeneity of the distribution of the active ingredient in the strand, which can be checked before the production process begins.
• the dosing problem that otherwise arises in the course of production is reduced by the fact that - once the strand has been produced in a geometrically defined manner - the final dosing is effected solely by the length (or, volume, length, area and thickness) of the strand in the plaster, preferably by the length of the plaster with a defined width of the "plaster track", ie the system strand.
• this method offers a particular advantage precisely because the temperature at the moment of spreading is already significantly lower than the temperature at mass preparation, so the active substance in the strand is less likely to be affected.
• the invention is also of particular advantage in the case of conventional (also sheet-like) active substance-containing oral systems, because a higher active substance concentration in the active substance strand - which is simply let into the oral, active substance-containing system - compensates for a reduction in concentration which occurs on the outer surfaces and thus a reduced release of active substance can be. This is particularly true when several strands of active substance, possibly with different active substances, may be used at different concentrations.

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• Health & Medical Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Dermatology (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (3)

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• 1997
  • 1997-08-21 DE DE19736315A patent/DE19736315A1/de not_active Withdrawn
• 1998
  • 1998-08-06 CA CA002299713A patent/CA2299713A1/en not_active Abandoned
  • 1998-08-06 EP EP98943852A patent/EP1009392A2/de not_active Withdrawn
  • 1998-08-06 KR KR1020007001757A patent/KR20010023134A/ko not_active Application Discontinuation
  • 1998-08-06 JP JP2000507352A patent/JP2001513548A/ja active Pending
  • 1998-08-06 AU AU91594/98A patent/AU738723B2/en not_active Ceased
  • 1998-08-06 WO PCT/EP1998/004893 patent/WO1999009961A2/de not_active Application Discontinuation
• 2000
  • 2000-02-18 NO NO20000815A patent/NO20000815D0/no not_active Application Discontinuation

Non-Patent Citations (1)

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