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Last Updated: December 23, 2024

Claims for Patent: 5,446,070


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Summary for Patent: 5,446,070
Title: Compositions and methods for topical administration of pharmaceutically active agents
Abstract:Compositions for topical application comprising a therapeutically effective amount of a pharmaceutical agent(s), a pharmaceutically acceptable carrier, and a solvent for the pharmaceutical agent(s) in the carrier and methods of administering the pharmaceutical agents to a mammal are disclosed.
Inventor(s): Mantelle; Juan A. (Miami, FL)
Assignee: Nover Pharmaceuticals, Inc. (Miami, FL)
Application Number:08/112,330
Patent Claims: 1. A flexible, finite, bioadhesive composition for topical application comprising:

(a) a therapeutically effective amount of at least one pharmaceutically active agent which is in solid form at ambient temperatures and pressures;

(b) a pharmaceutically acceptable solvent for the pharmaceutically active agent, in an amount from about 5 to about 70 weight percent based on the weight of the whole composition, said solvent including about 5 to about 50 weight percent of a plasticizer;

(c) in admixture with the pharmaceutically active agent in the solvent, a pharmaceutically acceptable polysaccharide bioadhesive carrier in an amount from about 20 to about 50 weight percent based on the weight of the whole composition;

wherein the composition is substantially free of water, substantially water insoluble and is a bioadhesive; and wherein the pharmaceutically active agent is present in non-crystallized form in the composition.

2. The composition of claim 1, wherein the pharmaceutically acceptable solvent is in an amount from about 20 to about 53 weight percent based on the weight of the whole composition, of which the plasticizer represents about 10 to about 30 weight percent based on the weight of the whole composition, and the bioadhesive carrier is in an amount from about 20 to about 34 weight percent based on the weight of the whole composition.

3. The composition of claim 1, wherein the pharmaceutically active agent is at least one local anesthetic in an amount of about 10 to 40 weight percent based on the weight of the total composition.

4. The composition of claim 1, wherein the pharmaceutically active agent is from a class of drugs selected from the group consisting of analgesic anti-inflammatory drugs, central nervous system drugs, antihistaminic or antiallergic drugs, acitonide anti-inflammatory drugs, androgenic and estrogenic steroids, -respiratory drugs, sympathomimetic drugs, antimicrobial drugs, antihypertensive drugs, cardiotonic drugs, coronary vasodilators, vasoconstrictors, beta blocking and antiarrhythemic drugs, calcium antagonistic and other circulatory anticonvulsants, anti-vertigo-tranquilizing drugs, antipsychotic drugs, muscle-reactants drugs, anti-Parkinson drugs, non-steroidal hormones, anti-hormones, vitamins, antitumor, enzymes, herb medicines or crude extracts, miotics, cholinergic agonists, antimuscarinic or muscarinic cholinergic blocking drugs, mydriatics, psychic energizers, humoral agents, antispasmodic drugs, antidepressants, antidiabetics, anorexic drugs, anti-allergic drugs, decongestants, antipyretics, antimigraine drugs, antimalarial, antiulcer drugs, peptides, and anti-estrogens.

5. The composition of claim 4, in which the pharmaceutically active agent is one or more steroids selected from the group consisting of androgenic steroids, including testosterone; methyltestosterone; fluoxymesterone; estrogenic steroids, including conjugated estrogens, esterified estrogens, estropipate, 17-.beta. estradiol, 17-.beta. estradiol esters such as 17-.beta.-estradiol valerate, equilin, mestranol, estrone, estriol; 17-.beta. estradiol derivatives such as 17-.beta. ethinyl estradiol; diethylstilbestrol, progestational agents, including progesterone and progesterone analogs such as 19norprogesterone, hydroxyprogesterone caproate, 17-.alpha. hydroxyprogesterone, dydrogesterone, medroxyprogesterone acetate; and norethindrone, norethindrone acetate, melengestrol, chlormadinone; ethynodiol diacetate, norethynodrel, dydrogesterone, dimethisterone, ethinylestrenol, norgestrel, demegestone, promegestone, megestrol acetate, and anti-estrogen or anti-androgenic steroids.

6. The composition of claim 3, wherein the anesthetic agent is selected from the group consisting of procaine, lidocaine, prilocaine, mepivacaine, dyclonine, dibucaine, benzocaine, chloroprocaine, tetracaine, bupivacaine, and etidocaine and is in the form of the base or an acid-addition salt or both forms.

7. The composition of claim 6, wherein the acid-addition salt is hydrochloride.

8. The composition of claim 1, wherein the bioadhesive is selected from the group consisting of gums and celluloses.

9. The composition of claim 8, wherein the gum is selected from the group consisting of karaya gum, tragacanth gum, pectin gum, xanthan gum, guar gum, cellulose, and cellulose derivatives.

10. The composition of claim 3, wherein the solvent for the anesthetic agent is at least one polyhydric alcohol.

11. The composition of claim 10, wherein the polyhydric alcohol is a polyalkylene glycol.

12. The composition of claim 11, wherein the glycol is selected from the group consisting of dipropylene glycol, propylene glycol, ethylene glycol, polyethylene glycol, glycerin, butylene glycol, hexylene glycol, polypropylene glycol, and sorbitol.

13. The composition of claim 1 further comprising a backing material conforming to the size and shape of a single dosage of the composition.

14. The composition of claim 1 comprising about 20 to 34 weight percent of karaya gum, about 20 to 53 weight percent of at least one glycol, and about 10 to 25 weight percent of lidocaine base

and further comprising a binder in an amount sufficient to bind the other ingredients.

15. The composition of claim 14 comprising about 30 weight percent of karaya gum, about 6 weight percent propylene glycol, about 15 weight percent of dipropylene glycol, about 15 weight percent of glycerine, about 25 weight percent of lidocaine base and about 9 weight percent of lecithin.

16. The composition of claim 14, comprising about 33 weight percent of karaya gum, about 7 weight percent of propylene glycol, about 12 weight percent of dipropylene glycol, weight percent of glycerin, about 10 weight percent lidocaine base and about 5 weight percent lecithin.

17. The composition of claim 1, wherein the pharmaceutically active agent is an anti-microbial agent.

18. The composition of claim 17, wherein the anti-microbial agent in an antifungal agent.

19. The composition of claim 18, wherein the anti-microbial agent is clotrimazole.

20. The composition of claim 18, wherein the antimicrobial agent is miconazole.

21. A method of administering one or more pharmaceutically active agent to a subject comprising the steps of:

providing the composition set forth in claim 1; and

contacting an area of skin or mucous membrane with the composition to administer the pharmaceutically active agent.

22. The method of claim 21, wherein the pharmaceutically active agent is an anesthetic agent selected from the group consisting of procaine, dyclonine, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine, chloroprocaine, tetracaine, bupivacaine, etidocaine, and dibucaine.

23. The method of claim 22, wherein the anesthetic agent is administered in the form of a free base.

24. The method of claim 22, wherein the anesthetic agent is administered in the form of an acid-addition salt.

25. The method of claim 22, wherein the solvent is at least one polyhydric alcohol.

26. A composition for topical application comprising:

(a) a therapeutically effective amount of a first local anesthetic agent in base form;

(b) a therapeutically effective amount of a different, second local anesthetic agent in non-salicylate acid-addition salt form; and

(c) in an admixture with the anesthetic agents, a pharmaceutically acceptable carrier wherein the anesthetic agents comprise about 1 to about 50% by weight of the total composition.

27. The composition of claim 26, wherein the first local anesthetic agent in base form is selected from the group consisting of procaine, dyclonine, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine and chloroprocaine.

28. The composition of claim 26, wherein the second local anesthetic agent in non-salicylate acid-addition salt form is selected from the group consisting of a dyclonine salt, a prilocaine salt, a tetracaine salt, a bupivacaine salt, a mepivacaine salt, a lidocaine salt, a procaine salt, an etidocaine salt, and a dibucaine salt.

29. The composition of claim 26, wherein the first local anesthetic agent in base form is selected from the group consisting of procaine, dyclonine, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine and chloroprocaine and the -second local anesthetic in acid-addition salt form is selected from the group consisting of a dyclonine salt, a prilocaine salt, a tetracaine salt, a bupivacaine salt, a mepivacaine salt, a lidocaine salt, a procaine salt, an etidocaine salt, and a dibucaine salt.

30. The composition of claim 29, wherein the acid addition salt is the hydrochloride.

31. A composition for topical application comprising:

(a) a therapeutically effective amount of a first local anesthetic agent in base form;

(b) a therapeutically effective amount of a different, second local anesthetic agent in acid-addition salt form; and

(c) in an admixture with the anesthetic agents, a pharmaceutically acceptable carrier which is substantially free of water

wherein the anesthetic agents comprise about 1 to about 50% by weight of the total composition and wherein said composition is substantially free of water.

32. The composition of claim 31, wherein the first local anesthetic agent in base form is selected from the group consisting of procaine, dyclonine, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine and chloroprocaine.

33. The composition of claim 31, wherein the second local anesthetic agent in acid-addition salt form is selected from the group consisting of a dyclonine salt, a prilocaine salt, a tetracaine salt, a bupivacaine salt, a mepivacaine salt, a lidocaine salt, a procaine salt, an etidocaine salt, and a dibucaine salt.

34. The composition of claim 33, wherein the first local anesthetic agent in base form is selected from the group consisting of procaine, dyclonin, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine and chloroprocaine and the second local anesthetic in acid-addition salt form is selected from the group consisting of a dyclonine salt, a prilocaine salt, a tetracaine salt, a bupivacaine salt, a mepivacaine salt, a lidocaine salt, a procaine salt, an etidocaine salt, and a dibucaine salt.

35. The composition of claim 34, wherein the acid addition salt is the hydrochloride.

36. The composition of claim 26 or 31, wherein the solvent for the anesthetic agent is at least one polyhydric alcohol.

37. The composition of claim 36, wherein the polyhydric alcohol is a polyalkylene glycol.

38. The composition of claim 37, wherein the glycol is selected from the group consisting of dipropylene glycol, propylene glycol, ethylene glycol, polyethylene glycol, glycerin, butylene glycol, hexylene glycol, polypropylene glycol, and sorbitol.

39. The composition of claim 26 or 31, further comprising a backing material which conforms to the size and shape of a single dosage of the composition.

40. The method of administering the composition of claim 26 to a subject, comprising the steps of:

(a) providing a composition set forth in claim 26; and

(b) contacting an area of tissue with the composition to administer the local anesthetics.

41. The method of claim 40, wherein the first local anesthetic agent in base form is selected from the group consisting of procaine, dyclonine, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine and chloroprocaine and the second local anesthetic agent in acid-addition salt form is selected from the group consisting of a dyclonine salt, a prilocaine salt, a tetracaine salt, a bupivacaine salt, a mepivacaine salt, a lidocaine salt, a procaine salt, an etidocaine salt, and a dibucaine salt.

42. The method of claim 41, wherein the acid-addition salt is hydrochloride.

43. The method of administering the composition of claim 31 to a subject, comprising the steps of:

(a) providing a composition set forth in claim 31; and

(b) contacting an area of tissue with the composition to administer the local anesthetics.

44. The method of claim 43, wherein the first local anesthetic agent in base form is selected from the group consisting of procaine, dyclonine, lidocaine, prilocaine, mepivacaine, benzocaine, propoxycaine and chloroprocaine and the second local anesthetic agent in acid-addition salt form is selected from the group consisting of a dyclonine salt, a prilocaine salt, a tetracaine salt, a bupivacaine salt, a mepivacaine salt, a lidocaine salt, a procaine salt, an etidocaine salt, and a dibucaine salt.

45. The method of claim 43, wherein the acid-addition salt is hydrochloride.

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