US4746675A
Expired / Lapsed
US
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External pharmaceutical composition
Assignee: Teijin Ltd
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Filing: 1986-10-27
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Granted: 1988-05-24
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Expires: 2006-10-27
Abstract
Abstract A pharmaceutical composition for external use with the enhanced penetration of a pharmacologically active agent through the skin or mucosa of a warm-blooded animal, said composition comprising (A) a pharmaceutically effective amount of the pharmacologically active agent such as antiinflammatory agent, etc., and (B) a penetration enhancer of the following formula (1) ##STR1## wherein R 1 and R 2 are identical or different and each represents H, a C 1-25 alkyl, C 2-25 alkenyl, a (C 1-24 alkyl)carbonyl or a (C2-24 alkenyl)carbonyl, provided that R 1 and R 2 are not H at the same time, or R 1 and R 2 , taken together, may form a group of the following formula (a) ##STR2## in which R 3 and R 4 are identical or different and each represents H, C 1-24 alkyl or C 1-24 alkenyl.
Inventors
- 👤 Yuji Makino
- 👤 Yoshiki Suzuki
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 02:09
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/22
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
228 words
A method for administering a pharmacologically active agent to a warm-blooded animal, which comprises externally applying (A) a pharmaceutically effective amount of the pharmacologically active agent selected from the group consisting of an anti-inflammatory agent, an agent for the circulatory system, an anti-ulcer agent, a hormone, an agent for the respiratory system, an agent for the central nervous system, a biological material and an agent for the metabolic system, in combination with (B) a penetration enhancer of the following formula (I) ##STR12## wherein R 1 and R 2 are identical or different and each represents a hydrogen atom, an alkyl group having 1 to 25 carbon atoms, an alkenyl group having 2 to 25 carbon atoms, a (C 1-24 alkyl)carbonyl group or a (C 2-24 alkenyl)carbonyl group, provided that R 1 and R 2 are not hydrogen atoms at the same time, or R 1 and R 2 , taken together, may form a group of the following formula (a) ##STR13## in which R 3 and R 4 are identical or different and each represents a hydrogen atom, an alkyl group having 1 to 24 carbon atoms or an alkenyl group having 2 to 24 carbon atoms, to the surface of the skin or mucosa of the warm-blooded animal to enhance the penetration of a pharmaceutically effective amount of the pharmacologically active agent through the skin or mucosa.
Claim 2
Independent Claim
228 words
A method for administering a pharmacologically active agent to a warm-blooded animal, which comprises externally applying (A) a pharmaceutically effective amount of the pharmacologically active agent selected from the group consisting of an anti-inflammatory agent, an agent for the circulatory system, an anti-ulcer agent, a hormone, an agent for the respiratory system, an agent for the central nervous system, a biological material and an agent for the metabolic system, in combination with (B) a penetration enhancer of the following formula (I) ##STR12## wherein R 1 and R 2 are identical or different and each represents a hydrogen atom, an alkyl group having 1 to 25 carbon atoms, an alkenyl group having 2 to 25 carbon atoms, a (C 1-24 alkyl)carbonyl group or a (C 2-24 alkenyl)carbonyl group, provided that R 1 and R 2 are not hydrogen atoms at the same time, or R 1 and R 2 , taken together, may form a group of the following formula (a) ##STR13## in which R 3 and R 4 are identical or different and each represents a hydrogen atom, an alkyl group having 1 to 24 carbon atoms or an alkenyl group having 2 to 24 carbon atoms, to the surface of the skin or mucosa of the warm-blooded animal to enhance the penetration of a pharmaceutically effective amount of the pharmacologically active agent through the skin or mucosa.
Claim 3
Dependent Claim
29 words
The method of claim 1 wherein the pharmacologically active agent (A) is applied together with the penetration enhancer (B) to the surface of the skin of the warm-blooded animal.
Claim 4
Dependent Claim
23 words
The method of claim 2 wherein the pharmacologically active agent (A) and the penetration enhancer (B) are applied as a composition comprising them.
Claim 5
Dependent Claim
30 words
The method of claim 1 wherein the pharmacologically active agent (A) is applied together with the penetration enhancer (B) to the surface of the rectal mucosa of the warm-blooded animal.
Claim 6
Dependent Claim
23 words
The method of claim 4 wherein the pharmacologically active agent (A) and the penetration enhancer (B) are applied as a composition comprising them.
Claim 7
Dependent Claim
33 words
The method of claim 1 wherein the pharmacologically active agent (A) is applied together with the penetration enhancer (B) to the surface of the mucosa of the oral cavity of the warm-blooded animal.
Claim 8
Dependent Claim
23 words
The method of claim 6 wherein the pharmacologically active agent (A) and the penetration enhancer (B) are applied as a composition comprising them.
Claim 9
Dependent Claim
33 words
The method of claim 1 wherein the pharmacologically active agent (A) is applied together with the penetration enhancer (B) to the surface of the mucosa of the nasal cavity of the warm-blooded animal.
Claim 10
Dependent Claim
23 words
The method of claim 8 wherein the pharmacologically active agent (A) and the penetration enhancer (B) are applied as a composition comprising them.
Claim 11
Dependent Claim
23 words
The method of claim 1 wherein the pharmacologically active agent (A) and the penetration enhancer (B) are applied as a composition comprising them.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-05-24 | 1991-11-23 | 1992-05-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-05-24 | 1995-11-23 | 1996-05-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-05-24 | 1999-11-23 | 2000-05-24 | $7700.00 | Window Closed / Lapsed |