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External pharmaceutical composition and methods of use

Assignee: Teijin Ltd
•
Filing: 1985-09-03
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Granted: 1988-12-06
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Expires: 2005-09-03
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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, and (B) an optically active or inactive pyroglutamate of the following formula ##STR1## wherein R represents a linear, branched or cyclic alkyl or alkenyl group having 10 to 14 carbon atoms, as a penentration enhancer.

Inventors

  • 👤 Yuji Makino
  • 👤 Hideo Matugi
  • 👤 Yoshiki Suzuki

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 05:05
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0014; A61K47/00; A61K47/06; A61K47/22

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 86 words
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) an effective amount of an anti-inflammatory agent selected from the group consisting of salicylic acid, indomethacin, and betamethasone valerate and (B) an effective amount of an optically active or inactive pyroglutamate of the following formula ##STR8## wherein R represents a linear, branched or cyclic alkyl or alkenyl group having 10 to 14 carbon atoms, as a penetration enhancer.
Claim 2
Dependent Claim 86 words
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) an effective amount of an anti-inflammatory agent selected from the group consisting of salicylic acid, indomethacin, and betamethasone valerate and (B) an effective amount of an optically active or inactive pyroglutamate of the following formula ##STR8## wherein R represents a linear, branched or cyclic alkyl or alkenyl group having 10 to 14 carbon atoms, as a penetration enhancer.
Claim 3
Dependent Claim 31 words
The composition of claim 1 wherein the pyroglutamate is represented by formula (1) in which R is a linear or branched alkyl or alkenyl group having 12 to 14 carbon atoms.
Claim 4
Dependent Claim 27 words
The composition of claim 1 wherein the pyroglutamate is represented by formula (1) in which R is a linear or branched alkyl group having 12 carbon atoms.
Claim 5
Dependent Claim 29 words
The composition of claim 1 which is in the form of a solution, an emulsion, a suspension, a semi-solid, a powder, a regularly shaped compressed article, or a film.
Claim 6
Dependent Claim 13 words
The composition of claim 1 wherein the pharmacologically active agent is salicylic acid.
Claim 7
Dependent Claim 75 words
In a method of enhancing the penetration of a pharmacologically active agent through the skin or mucosa of a warm-blooded animal, the improvement which comprises externally applying to the skin or mucosa an effective amount of an optically active or inactive pyroglutamate in an amount sufficient to enhance said penetration, said pyroglutamate having the following formula: ##STR9## wherein R represents a linear, branched or cyclic alkyl or alkenyl group having 10 to 14 carbon atoms.
Claim 8
Dependent Claim 75 words
In a method of enhancing the penetration of a pharmacologically active agent through the skin or mucosa of a warm-blooded animal, the improvement which comprises externally applying to the skin or mucosa an effective amount of an optically active or inactive pyroglutamate in an amount sufficient to enhance said penetration, said pyroglutamate having the following formula: ##STR9## wherein R represents a linear, branched or cyclic alkyl or alkenyl group having 10 to 14 carbon atoms.
Claim 9
Dependent Claim 14 words
A method according to claim 6, wherein the pharmacological agent is an anti-inflammatory agent.
Claim 10
Dependent Claim 23 words
A method according to claim 7, wherein the anti-inflammatory agent is selected from the group consisting of salicylic acid, indomethacin and betamethosone valerate.
Claim 11
Dependent Claim 29 words
The method of claim 6 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 12
Dependent Claim 28 words
The method of claim 6 wherein the pharmacologically active agent is applied together with the penetration enhancer to the surface of the rectal mucosa of the warm-blooded animal.
Claim 13
Dependent Claim 31 words
The method of claim 6 wherein the pharmacologically active agent is applied together with the penetration enhancer to the surface of the mucosa of the oral cavity of the warm-blooded animal.
Claim 14
Dependent Claim 31 words
The method of claim 6 wherein the pharmacologically active agent is applied together with the penetration enhancer to the surface of the mucosa of the nasal cavity of the warm-blooded animal.
Claim 15
Independent Claim 27 words
The method of any one of claims 6 and 7-10 wherein the pharmacologically active agent and the penetration enhancer are applied in the form of a composition.
Claim 16
Dependent Claim 14 words
The method of claim 6 wherein the pharmacologically active agent is an anti-inflammatory agent.

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) 1991-12-06 1992-06-06 1992-12-06 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-12-06 1996-06-06 1996-12-06 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-12-06 2000-06-06 2000-12-06 $7700.00 Window Closed / Lapsed

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