WO2002062353A1 - Composition containing sucrafate and a topical anesthetic for human and animals and method of use thereof - Google Patents
Composition containing sucrafate and a topical anesthetic for human and animals and method of use thereof Download PDFInfo
- Publication number
- WO2002062353A1 WO2002062353A1 PCT/US2001/003714 US0103714W WO02062353A1 WO 2002062353 A1 WO2002062353 A1 WO 2002062353A1 US 0103714 W US0103714 W US 0103714W WO 02062353 A1 WO02062353 A1 WO 02062353A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- composition
- recited
- sucralfate
- lidocaine
- treating
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7016—Disaccharides, e.g. lactose, lactulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
Definitions
- the instant invention relates generally to compositions for treating skin ulcers
- the present invention comprises a composition and method of treating plurality
- lidocaine The composition finds utility in treating the symptoms of d from herpes,
- composition also finds utility in preventing the development of nascent herpes outbreaks into herpes ulcers, in addition
- FIG. 1 illustrates the chemical structure for sucralfate.
- FIG. 2 illustrates the chemical structure for lidocaine.
- the present invention comprises a topically-reacted topically-reacted topically-reacted topically-reacted base material
- composition including sucralfate 10 and a topical anesthetic or an antibiotic.
- Sucralfate is an a-D-glucopyranoside, ⁇ -D-fructofuranosyl-, octakis-(hydrogen
- CARAFATEO in both tablet and liquid suspension form. It is most commonly
- the present invention is based on the
- sucralfate in combination with other active components such as topical
- composition of the invention includes sucralfate and
- Lidocaine (Xylocaine), is an amide originally synthesized
- the sucralfate is normally provided in suspension form, at a concentration of lg
- sucralfate per 10ml of suspension sucralfate per 10ml of suspension.
- the preferred concentrations for the present invention are sucralfate per 10ml of suspension.
- sucralfate suspension together with about 0.25 fluid ounces (about 7.5 ml) of sucralfate suspension.
- the suspension thickens to the consistency of a gel, providing
- composition of the present invention can be used to prepare the composition of the present invention.
- composition as needed.
- antibiotics and/or antifungal agents include antibiotics and/or antifungal agents, vitamins, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids, amino acids
- Sucralfate binds preferentially to wound sites to form a protective coating
- compositions of the present invention provide for the
- sucralfate in the composition The effectiveness of the sucralfate in acting as a
- preferential carrier may be enhanced when the active component has an affinity for
- sucralfate as many pharmaceutical products do.
- the antibiotics are selected from the antibiotics
- sucralfate some affinity for sucralfate and may find particular utility in the compositions of the invention.
- compositions of the invention also find utility in the compositions of the invention. This includes sulfa drugs and
- antibiotics such as bacitracin, trimethoprim, penicillin and erythromycin.
- preferred antibiotic is a combination of trimethoprim and sulfamethoxazole, in a weight
- the composition has been used to treat effectively many different ailments.
- ulcers herpes ulcers, shingles, eczema, acne, psoriasis, skin rashes, burns and
- composition is further used effectively to reirritations and
- composition in the case of humans and visible in the case of animals and mange.
- composition of the present invention has shown further, unexpected utility
- composition of the present invention is applied to a nascent herpes outbreak (when a
- the invention provides prophylactic utility for preventing herpes
- the present invention can greatly alleviate the symptoms of chicken pox, and
- composition has also shown great efficacy.
- Such conditions include, for example, acne
- composition for treating skin ulcers it is not intended to be limited to the details
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A composition and method of treating plurality of conditions utilizes a combination of sucralfate and a topical anesthetic such as lidocaine. The composition finds utility in treating the symptoms of d from herpes, acne, psoriasis, eczema, diabetic ulcers, bed sores, shingles, jock itch, athlete's foot, ringworm, and other dermal conditions and to relieve irritations and discomfort caused by poison ivy, poison oak, poison sumac, bedsores, soar throats, surgical incisions and skin ulcers on humans, animals and mange. The composition also finds utility in preventing the development of nascent herpes outbreaks into herpes ulcers, in addition to providing long-lasting relief from such symptoms. Gargling with the composition is effective in relieving sore throats and minor throat irritations.
Description
COMPOSITION CONTAINING SUCRAFATE AND A TOPICAL ANESTHETIC FOR HUMANS AND ANIMALS AND METHOD
OF USE THEREOF
Description
Technical Field
The instant invention relates generally to compositions for treating skin ulcers
and particularly to compositions for medical or veterinary use containing sucralfate in
combination with a topical anesthetic for treating a variety of medical conditions.
Disclosure of the Invention
The present invention comprises a composition and method of treating plurality
of conditions utilizes a combination of sucralfate and a topical anesthetic such as
lidocaine. The composition finds utility in treating the symptoms of d from herpes,
acne, psoriasis, eczema, diabetic ulcers, bed sores, shingles, jock itch, athlete's foot,
ringworm, and other dermal conditions and to relieve irritations and discomfort caused
by poison ivy, poison oak, poison sumac, bedsores, soar throats, surgical incisions and
skin ulcers on humans, animals and mange. The composition also finds utility in
preventing the development of nascent herpes outbreaks into herpes ulcers, in addition
to providing long-lasting relief from such symptoms. Gargling with the composition is
effective in relieving sore throats and minor throat irritations.
Rief Description of the Drawing Figures
Various other objects, features and attendant advantages of the present
invention will become more fully appreciated as the same becomes better understood
when considered in conjunction with the accompanying drawings, in which like
reference characters designate the same or similar parts throughout the several views.
FIG. 1 illustrates the chemical structure for sucralfate.
FIG. 2 illustrates the chemical structure for lidocaine.
The reference numbers utilized in the drawing figures are defined as follows:
10 chemical structure for sucralfate as an aluminum complex
12 non-complexed portion of 10
14 identification of R-groups of 12 as -SO3Al(OH)2
16 aluminum complex portion of 10
18 definition of x and y from 16
20 chemical structure of lidocaine
22 chemical formula for lidocaine
24 molecular weight of lidocaine
Detailed Description of the Preferred Embodiment
Figures 1 and 2 illustrate a composition for treating skin ulcers of the present
invention. In its broadest embodiment, the present invention comprises a topically-
applicable composition including sucralfate 10 and a topical anesthetic or an antibiotic.
Sucralfate is an a-D-glucopyranoside, §-D-fructofuranosyl-, octakis-(hydrogen
sulfate), aluminum complex as illustrated in FIG. 1. It is sold under the trade name
CARAFATEO, in both tablet and liquid suspension form. It is most commonly
dispensed for use in treating duodenal ulcers. The present invention is based on the
finding that sucralfate, in combination with other active components such as topical
anesthetics, antibiotics, antioxidants, vitamins and the like, can effectively treat a wide
variety of topical conditions.
In preferred form, the composition of the invention includes sucralfate and
lidocaine in combination. Lidocaine (Xylocaine), is an amide originally synthesized
from cocaine, and is one of the most widely used local anesthetics in use today. It is
administered parenterally for ventricular arrhythmias, subcutaneously for minor
surgical procedures, and topically to mucosal surfaces prior to invasive procedures.
Available forms include a topical solution (2-4%), a rectal suppository (10%), an
aerosol (10%), a jelly (2%), viscous lidocaine (2%), and a solution for intravenous and
subcutaneous administration (0.5-2%).
The sucralfate is normally provided in suspension form, at a concentration of lg
sucralfate per 10ml of suspension. The preferred concentrations for the present
invention results from the combination of 1 drop (about O.lg) of 2% lidocaine mixed
together with about 0.25 fluid ounces (about 7.5 ml) of sucralfate suspension. When
mixed in this proportion, the suspension thickens to the consistency of a gel, providing
for ready administration to the patient.
Thus prepared, the composition of the present invention can be used to
effectively treat a wide range of skin ailments, providing pain relief and promoting
healing of any open ulcers. Additionally, further active components may be added to
the composition as needed. For example, antibiotics and/or antifungal agents, vitamins
such as vitamins A, C and E, plants extracts such as aloe vera or other plant materials
which may promote healing, and combinations thereof.
Sucralfate binds preferentially to wound sites to form a protective coating
thereon. Accordingly, the compositions of the present invention provide for the
preferential delivery, to the wound site, of the various active components via the
sucralfate in the composition. The effectiveness of the sucralfate in acting as a
preferential carrier may be enhanced when the active component has an affinity for
sucralfate, as many pharmaceutical products do. For example, the antibiotics
tetracycline, doxycycline, nalidixic acid, the fluoroquinolone antibiotics ciprofloxacin,
norfloxacin and ofloxacin, and the antifungal ketoconazole all have been shown to have
some affinity for sucralfate and may find particular utility in the compositions of the
present invention.
In addition to these compounds which adsorb to the sucralfate, other antibiotics
also find utility in the compositions of the invention. This includes sulfa drugs and
other antibiotics such as bacitracin, trimethoprim, penicillin and erythromycin. A
preferred antibiotic is a combination of trimethoprim and sulfamethoxazole, in a weight
TM ratio of 1:5, respectively, sold under the tradename Bactπm .
The composition has been used to treat effectively many different ailments. For
example, it has been used effectively to relieve pain and promote healing of diabetic
ulcers, herpes ulcers, shingles, eczema, acne, psoriasis, skin rashes, burns and
abrasions, and the like. The composition is further used effectively to reirritations and
discomfort caused by poison ivy, poison oak, poison sumac, bedsores, soar throats,
surgical incisions and skin ulcers on humans, animals and mange. In each instance,
immediate relief from the pain caused by the ulcers, and much more rapid healing of
the wounds than when left untreated or treated by conventional methods was reported
in the case of humans and visible in the case of animals and mange. The composition
has also been shown to be effective in treating sinus conditions where pain and
inflammation are implicated. When used as a gargle, the composition has proven
effective in treating soar throats and minor throat irritations such as those caused by
colds and flu.
The composition of the present invention has shown further, unexpected utility
in preventing the development of herpes ulcers. It has been found that, when the
composition of the present invention is applied to a nascent herpes outbreak (when a
small bump occurs on the skin, the typical foreshadowing of an outbreak), the bump
recedes within 1 1/2 to 2 days, then disappears without developing into a herpes ulcer.
Additionally, patients report that after using the composition of the invention to stem
the outbreak, the time between outbreaks is greatly extended, typically by a factor of 3
to 4. Therefore, the invention provides prophylactic utility for preventing herpes
outbreaks. It is anticipated that such prophylactic utility extends also to other recurring
conditions, such as psoriasis, diabetic ulcers, and the like.
The present invention can greatly alleviate the symptoms of chicken pox, and
promotes the rapid healing of the associated skin eruptions such that scarring is
avoided. The results are similar for treatment of infected skin rashes; pain relief was
immediate and the skin appeared completely healed within 2 to 3 days.
In such conditions where antibiotics or antifungal agents are useful, the
composition has also shown great efficacy. Such conditions include, for example, acne
vulgaris, ringworm, jock itch, athlete's foot, conditions where infection is a concern,
such as any open wounds, and the like.
It will be understood that each of the elements described above, or two or more
together, may also find a useful application in other types of applications differing from
the type described above. This includes, for example, veterinary applications as well as
the medical applications described herein.
While the invention has been illustrated and described as embodied in a
composition for treating skin ulcers, it is not intended to be limited to the details
shown, since it will be understood that various omissions, modifications, substitutions
and changes in the forms and details of the formulation illustrated and in its operation
can be made by those skilled in the art without departing in any way from the spirit and
scope of the present invention.
Without further analysis, the foregoing will so fully reveal the gist of the
present invention that others can, by applying current knowledge, readily adapt it for
various applications without omitting features that, from the standpoint of prior art,
fairly constitute essential characteristics of this invention.
Claims
1. A topically applied composition containing comprising sucralfate and a
topical anesthetic for treating poison ivy, poison oak and poison sumac.
2. The composition as recited in claim 1, wherein the weight ratio of
sucralfate to lidocaine is from about 500:1 to about 200:1, respectively, in a
pharmaceutically acceptable carrier.
3. The composition as recited in Claim 1, wherein said sucralfate and
lidocaine are present in a weight:weight ratio of about 375:1, respectively.
4. The composition as recited in Claim 1, further comprising a
pharmaceutically effective amount of an antibiotic.
5. The composition for treating skin ulcers as recited in Claim 4, wherein
said antibiotic is selected from tetracycline, bacitracin, sulfa drugs, penicillin,
trimethoprim, erythromycin and combinations thereof.
6. The composition as recited in Claim 4, wherein said antibiotic is a
combination of trimethoprim and sulfamethoxazole.
7. The composition as recited in Claim 1, wherein said composition is
further effective in treating jock itch, athlete's foot, eczema, psoriasis.
8. The composition as recited in Claim 1, wherein said composition is
further effective in treating skin ulcers in animals and mange.
9. The composition as recited in Claiml, wherein said composition is
further effective in treating minor burns and accelerating the healing of the minor
burns.
10. The composition as recited in Claim 9, wherein said composition further
includes aloe and vitamin E.
11. The composition as recited in Claim 1, wherein said composition is
further effective in accelerating healing of surgical incisions.
12. The composition as recited in Claim 1, wherein said composition is
further effective in preventing a nascent acne outbreak from developing into an acne
lesion.
13. The composition as recited in Claim 1, wherein said composition is
furhter effective for treatment of skin ulcers on animals.
14. A method of relieving soar throats comprising gargling with a
composition as recited in Claim 1.
15. A process for preparing a composition for relieving a soar throat and
minor throat irritations comprising mixing an aqueous suspension of sucralfate, present
in the concentration of 1 gram sucralfate per 10 ml of suspension, with a 2% lidocaine
solution, then mixing until the composition achieves a gel-like consistency.
16. The process as recited in Claim 15, wherein about 1 drop of lidocaine
solution is added to each 7.5 ml of sucralfate suspension.
17. A topically applied composition for treating skin ulcers comprising
sucralfate and lidocaine in a weight:weight ratio of from about 500:1 to about 200:1,
respectively, in a pharmaceutically acceptable carrier, and a pharmaceutically effective
amount of an antibiotic.
18. A topically applied composition for treating skin ulcers as recited in
Claim 17, wherein said sucralfate and lidocaine are present in a weight:weight ratio of
about 375:1, respectively.
19. A topically applied composition for treating skin ulcers as recited in
Claim 17, wherein said antibiotic is a combination of trimethoprim and
sulfamethoxazole.
20. A method of treating skin ulcers comprising the topical administration
of a composition comprising sucralfate and lidocaine in a weight:weight ratio of from about 500:1 to about 200:1, respectively, in a pharmaceutically acceptable carrier, and a
pharmaceutically effective amount of an antibiotic which is a combination of
trimethoprim and sulfamethoxazole.
21. A method of preventing a nascent herpes outbreak from developing into
a herpes ulcer, comprising the topical administration of a composition as a prophylactic
comprising sucralfate and lidocaine in a weight: weight ratio of from about 500:1 to
about 200:1, respectively, in a pharmaceutically acceptable carrier to a site identified as
a nascent herpes outbreak.
22. A process for preparing a composition for treating skin ulcers
comprising mixing an aqueous suspension of sucralfate, present in the concentration of
1 gram sucralfate per 10 ml of suspension, with a 2% lidocaine solution wherein about
1 drop of lidocaine solution is added to each 7.5 ml of sucralfate_solution, then mixing
until the composition thickens and achieves a gel-like consistency.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2001/003714 WO2002062353A1 (en) | 2001-02-05 | 2001-02-05 | Composition containing sucrafate and a topical anesthetic for human and animals and method of use thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2001/003714 WO2002062353A1 (en) | 2001-02-05 | 2001-02-05 | Composition containing sucrafate and a topical anesthetic for human and animals and method of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2002062353A1 true WO2002062353A1 (en) | 2002-08-15 |
Family
ID=21742311
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2001/003714 WO2002062353A1 (en) | 2001-02-05 | 2001-02-05 | Composition containing sucrafate and a topical anesthetic for human and animals and method of use thereof |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2002062353A1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004087144A1 (en) * | 2003-04-04 | 2004-10-14 | Novartis Ag | Combination of a macrolide and a local anesthetic for the treatment of dermatological diseases |
| EP1764104A1 (en) * | 2005-09-16 | 2007-03-21 | Domenico Russo | Wound healing pharmaceutical composition comprising sucralfate, aluminium acetate and vitamins |
| IT201800007009A1 (en) * | 2018-07-06 | 2020-01-06 | NEW MEDICAL USE OF LOCAL ANESTHETICS |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5322689A (en) * | 1992-03-10 | 1994-06-21 | The Procter & Gamble Company | Topical aromatic releasing compositions |
| US5977087A (en) * | 1989-09-15 | 1999-11-02 | Pehrom Pharmaceutical Corporation | Topical preparation for treatment of aphthous ulcers and other lesions |
| US6194455B1 (en) * | 1999-05-28 | 2001-02-27 | Marie Madeline Wharton | Topical medicament for treating skin ulcers |
-
2001
- 2001-02-05 WO PCT/US2001/003714 patent/WO2002062353A1/en active Application Filing
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5977087A (en) * | 1989-09-15 | 1999-11-02 | Pehrom Pharmaceutical Corporation | Topical preparation for treatment of aphthous ulcers and other lesions |
| US5322689A (en) * | 1992-03-10 | 1994-06-21 | The Procter & Gamble Company | Topical aromatic releasing compositions |
| US6194455B1 (en) * | 1999-05-28 | 2001-02-27 | Marie Madeline Wharton | Topical medicament for treating skin ulcers |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004087144A1 (en) * | 2003-04-04 | 2004-10-14 | Novartis Ag | Combination of a macrolide and a local anesthetic for the treatment of dermatological diseases |
| EP1764104A1 (en) * | 2005-09-16 | 2007-03-21 | Domenico Russo | Wound healing pharmaceutical composition comprising sucralfate, aluminium acetate and vitamins |
| IT201800007009A1 (en) * | 2018-07-06 | 2020-01-06 | NEW MEDICAL USE OF LOCAL ANESTHETICS |
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