Claims
- 1. A method for enhancing permeation of a topically administered therapeutic or prophylactic agent in a host in need of the cutaneous or transdermal administration of a therapeutic or prophylactic agent, which comprises the following steps:
- (a) applying to the epithelium of the host, a composition comprising from about 0.01 to about 25 weight percent of a penetration enchanting compound that is a proton pump inhibitor selected from the group consisting of monensin, lasalocid, nigericin, valinomycin, chloroquine, gramicidin D, salinomycin, N-ethylmaleimide, N,N'-dicyclohexylcarbodiimine, and bafilomycin A.sub.1 or B.sub.1 ;
- (b) applying to the epithelium of the host a therapeutic or prophylactic agent;
- whereby enhanced permeation of the therapeutic or prophylactic agent through the epithelium is caused wherein said therapeutic or prophylactic agent is distinct from said proton pump inhibitor.
- 2. The method according to claim 1, wherein the penetration enhancing compound is monensin or N,N'-dicyclohexylcarbodiimine.
- 3. The method according to claim 1 wherein the application is topical.
- 4. The method according to claim 3, wherein the composition is a cream or ointment.
- 5. The method according to claim 1, wherein the composition further contains a known epithelial penetration enhancer selected from the group consisting of 1-dodecylazacycloheptan-2-one, propylene glycol, oleyl alcohol, and methyl pyrrolidone.
- 6. A composition for percutaneous or transdermal administration of a therapeutic or prophylactic agent in a host in need thereof, which composition comprises a therapeutic or prophylactic agent, and from about 0.01 to about 25 weight percent of a penetration enhancing compound that is a proton pump inhibitor selected from the group consisting of monensin, lasalocid, nigericin, valinomycin, chloroquine, gramicidin D, salinomycin, N-ethylmaleimide, N,N'-dicyclohexylcarbodiimine, and bafilomycin A.sub.1 or B.sub.1, together with a physiologically acceptable carrier wherein said therapeutic or prophylactic agent is distinct from said proton pump inhibitor.
- 7. The composition according to claim 6, wherein the penetration enhancing compound is selected from the group consisting of lasalocid, nigericin, valinomycin, chloroquine, gramicidin D, salinomycin, N-ethylmaleimide, and bafilomycin A.sub.1 or B.sub.1.
- 8. The composition according to claim 7, wherein the penetration enhancing compound is monensin or N,N'-dicyclohexylcarbodiimine.
- 9. The composition according to claim 6, wherein the therapeutic or prophylactic agent is present at a concentration of from about 0.0001% to about 60% by weight of the total.
- 10. The composition according to claim 9, which further contains a known penetration enhancer selected from the group consisting of 1-dodecylazacycloheptan-2-one, propylene glycol, oleyl alcohol, and methyl pyrrolidone.
- 11. A topical composition comprising:
- (a) about 0.01% to about 25% by weight of a penetration enhancing compound that is a proton pump inhibitor selected from the group consisting of monensin, lasalocid, nigericin, valinomycin, chloroquine, gramicidin D, salinomycin, N-ethylmaleimide, N,N'-dicyclohexylcarbodiimine, and bafilomycin A.sub.1 or B.sub.1 ;
- (b) about 0.0001% to about 60% by weight of a therapeutic or prophylactic agent and;
- (c) an amount of a physiologically acceptable carrier sufficient to total 100% by weight wherein said therapeutic or prophylactic agent is distinct from said proton pump inhibitor.
- 12. The composition according to claim 11, wherein the therapeutic or prophylactic agent is a non-irritating drag.
- 13. The composition according to claim 11, wherein the therapeutic or prophylactic agent is selected from the group consisting of lidocaine, leutinizing hormone releasing hormone, vasopressin, and caffeine.
- 14. The composition according to claim 13, wherein the therapeutic or prophylactic agent is selected from the group consisting of lidocaine and leutinizing hormone releasing hormone.
- 15. The composition according to claim 11, wherein the physiologically acceptable carrier is an ointment or cream.
- 16. The composition according to claim 11, wherein the penetration enhancing compound is monensin or N,N'-dicyclohexylcarbodiimine.
- 17. The composition according to claim 11, wherein the penetration enhancing compound is selected from the group consisting of lasalocid, nigericin, valinomycin, chloroquine, gramicidin D, salinomycin, N-ethylmaleimide, and bafilomycin A.sub.1 or B.sub.1.
- 18. The composition according to claim 11, wherein the penetration enhancing compound is present at a concentration of from about 0.05% to about 10% by weight of the total.
- 19. The composition according to claim 11 wherein the therapeutic or prophylactic agent is present at a concentration of from about 0.01% to about 20% by weight of the total.
- 20. The composition according to claim 11, which further contains a known epithelial penetration enhancer selected from the group consisting of 1-dodecylazacycloheptan-2-one, propylene glycol, oleyl alcohol, and methyl pyrrolidone.
- 21. The composition according to claim 20, wherein the penetration enhancing compound is selected from the group consisting of monensin, and N,N'-dicyclohexylcarbodiimine, and wherein the therapeutic or prophylactic agent is lidocaine or leutinizing hormone releasing hormone.
- 22. The method according to claim 1, wherein step (a) further includes applying (N-�2-Hydroxyethyl! piperazine-N'-�2-ethanesulfonic acid! or tris-(Hydroxymethyl)-aminomethyl maleate to the epithelium of the host, and wherein the therapeutic or prophylactic agent is lidocaine.
- 23. The composition according to claim 11, wherein the therapeutic or prophylactic agent is selected from the group consisting of antimicrobial, anti-inflammatory, anti-neoplastic, antioxidant, analgesic, anesthetic, antiepileptic, antihypertensive, neuroleptic, antiarrhythmic, nutritional and vasodilatory agents; capsaian; antiandrogens; antihistamines; antitussives; hormones; and cytokines.
- 24. The method of claim 1 wherein the therapeutic or prophylactic agent is selected from the group consisting of estradiol valerate, indomethacin, nifedipine, oxymorphone, lidocaine and leutinizing hormone releasing hormone.
- 25. The method of claim 1 wherein the therapeutic or prophylactic agent is leutinizing hormone releasing hormone.
- 26. The method of claim 1 wherein the therapeutic or prophylactic agent is lidocaine.
- 27. The method of claim 1 wherein the therapeutic or prophylactic agent is oxymorphone.
- 28. The method of claim 1 wherein the therapeutic or prophylactic agent is indomethacin.
- 29. The method of claim 1 wherein the therapeutic or prophylactic agent is estradiol valerate.
- 30. The method of claim 1 wherein the therapeutic or prophylactic agent is nifedipine.
- 31. The composition of claim 6 wherein the therapeutic or prophylactic agent is selected from the group consisting of estradiol valerate, indomethacin, nifedipine, oxymorphone, lidocaine, and leutinizing hormone releasing hormone.
- 32. The composition of claim 6 wherein the therapeutic or prophylactic agent is leutinizing hormone releasing hormone.
- 33. The composition of claim 6 wherein the therapeutic or prophylactic agent is lidocaine.
- 34. The composition of claim 6 wherein the therapeutic or prophylactic agent is oxymorphone.
- 35. The composition of claim 6 wherein the therapeutic or prophylactic agent is indomethacin.
- 36. The composition of claim 6 wherein the therapeutic or prophylactic agent is estradiol valerate.
- 37. The composition of claim 6 wherein the therapeutic or prophylactic agent is nifedipine.
Parent Case Info
This is a divisional of application Ser. No. 08/261,343 filed Jun. 16, 1994 now abandoned, which is a continuation-in-part application of U.S. Ser. No. 08/033,807, filed Mar. 19, 1993, now abandoned.
US Referenced Citations (3)
Divisions (1)
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Number |
Date |
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Parent |
261343 |
Jun 1994 |
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Continuation in Parts (1)
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Number |
Date |
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Parent |
33807 |
Mar 1993 |
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