Patent US5448118A successfully refreshed from Google Patents.
US4847260A
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Composition for percutaneous administration
Assignee: Nitto Denko Corp
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Filing: 1987-10-26
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Granted: 1989-07-11
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Expires: 2007-10-26
Abstract
Abstract A composition for percutaneous administration containing a nicotinic ester represented by formula (I) ##STR1## or an isonicotinic ester represented by formula (II) ##STR2## wherein R and R' each represents an alkyl group having 5 or more carbon atoms, with or without a specific polar compound. The composition improves percutaneous absorption of an active ingredient.
Inventors
- 👤 Yoko Abe
- 👤 Susumu Satoh
- 👤 Mitsuhiko Hori
- 👤 Naoko Yamanaka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 23:05
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/78; C07D213/79; A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61K47/14; A61K47/16; A61K47/18; A61K47/20; A61K47/22; A61K9/00; A61K9/0012; A61K9/0014; C07D213/80
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
70 words
A composition for percutaneous administration comprising an antiarrhythmic as an active ingredient in a physiologically effective amount for percutaneous administration and an amount of a nicotinic ester represented by formula (I) ##STR16## or an isonicotinic ester represented by formula (II) ##STR17## wherein R and R' each represents an alkyl group having 5 or more carbon atoms effective to increase the percutaneous permeability and absorbability through the skin of the antiarrhythmic.
Claim 2
Dependent Claim
70 words
A composition for percutaneous administration comprising an antiarrhythmic as an active ingredient in a physiologically effective amount for percutaneous administration and an amount of a nicotinic ester represented by formula (I) ##STR16## or an isonicotinic ester represented by formula (II) ##STR17## wherein R and R' each represents an alkyl group having 5 or more carbon atoms effective to increase the percutaneous permeability and absorbability through the skin of the antiarrhythmic.
Claim 3
Dependent Claim
124 words
A composition for percutaneous administration comprising a nicotinic ester represented by formula (I) ##STR18## or an isonicotinic ester represented by formula (II) ##STR19## wherein R and R' each represents an alkyl group having 5 of more carbon atoms, an antiarrhythmic as an active ingredient and at least one polar compound selected from the group consisting of a lower alcohol, an alkylene glycol and a monoalkyl ether of mono- or diethylene glycol, wherein the nicotinic ester or isonicotinic ester is present in an amount of from 0.5 to 70% by weight and the antiarrhythmic is present in an amount of from 0.01 to 20% by weight both based on the total amount of the nicotinic ester or isonicotinic ester and the polar compound or compounds.
Claim 4
Dependent Claim
124 words
A composition for percutaneous administration comprising a nicotinic ester represented by formula (I) ##STR18## or an isonicotinic ester represented by formula (II) ##STR19## wherein R and R' each represents an alkyl group having 5 of more carbon atoms, an antiarrhythmic as an active ingredient and at least one polar compound selected from the group consisting of a lower alcohol, an alkylene glycol and a monoalkyl ether of mono- or diethylene glycol, wherein the nicotinic ester or isonicotinic ester is present in an amount of from 0.5 to 70% by weight and the antiarrhythmic is present in an amount of from 0.01 to 20% by weight both based on the total amount of the nicotinic ester or isonicotinic ester and the polar compound or compounds.
Claim 5
Dependent Claim
39 words
A composition as in claim 2, wherein the antiarrhythmic is used in an amount of from 0.2 to 10% by weight based on the total weight of the nicotinic ester (I) or isonicotinic ester (II) and the polar compound.
Claim 6
Dependent Claim
22 words
A composition as in claim 1, wherein R and R' each represents an alkyl group having from 6 to 24 carbon atoms.
Claim 7
Dependent Claim
17 words
A composition as in claim 2, wherein the lower alcohol contains from 1 to 6 carbon atoms.
Claim 8
Dependent Claim
21 words
The composition of claim 1 wherein said antiarrhythmic is selected from the group consisting of ajmaline, prajmaline, pindolol, propranolol and quinidine.
Claim 9
Dependent Claim
10 words
The composition of claim 1 wherein said antiarrhythmic is propranolol.
Claim 10
Dependent Claim
21 words
The composition of claim 2 wherein said antiarrhythmic is selected from the group consisting of ajmaline, prajmaline, pindolol, propranolol and quinidine.
Claim 11
Dependent Claim
10 words
The composition of claim 2 wherein said antiarrhythmic is propranolol.
Claim 12
Independent Claim
100 words
A method for increasing percutaneous permeability and percutaneous absorbability of an antiarrhythmic as an active ingredient, which comprises the percutaneous administration of a composition comprising a nicotinic ester represented by formula (I) ##STR20## or an isonicotinic ester represented by formula (II) ##STR21## wherein R and R' each represents an alkyl group having 5 or more carbon atoms, and the active ingredient, wherein the antiarrhythmic is present in a physiologically effective amount for percutaneous administration and the nicotinic ester or isonicotinic ester is present in an amount effective to increase the percutaneous permeability and absorbability through the skin of the antiarrhythmic.
Claim 13
Independent Claim
100 words
A method for increasing percutaneous permeability and percutaneous absorbability of an antiarrhythmic as an active ingredient, which comprises the percutaneous administration of a composition comprising a nicotinic ester represented by formula (I) ##STR20## or an isonicotinic ester represented by formula (II) ##STR21## wherein R and R' each represents an alkyl group having 5 or more carbon atoms, and the active ingredient, wherein the antiarrhythmic is present in a physiologically effective amount for percutaneous administration and the nicotinic ester or isonicotinic ester is present in an amount effective to increase the percutaneous permeability and absorbability through the skin of the antiarrhythmic.
Claim 14
Independent Claim
118 words
A method for increasing percutaneous permeability and percutaneous absorbability of an antirrhythmic as an active ingredient, which comprises the percutaneous administration of a composition comprising of a nicotinic ester represented by formula (I) ##STR22## or an isonicotinic ester represented by formula (II) ##STR23## wherein R and R' each represents and alkyl group having 5 or more carbon atoms, an active ingredient and a polar compound, wherein the nicotinic ester or isonicotinic ester is present in an amount of from 0.5 to 70% by weight and the antiarrhythmic is present in an amount of from 0.01 to 20% by weight, both based on the total amount of the nicotinic ester or isonicotinic ester and the polar compound or compounds.
Claim 15
Independent Claim
118 words
A method for increasing percutaneous permeability and percutaneous absorbability of an antirrhythmic as an active ingredient, which comprises the percutaneous administration of a composition comprising of a nicotinic ester represented by formula (I) ##STR22## or an isonicotinic ester represented by formula (II) ##STR23## wherein R and R' each represents and alkyl group having 5 or more carbon atoms, an active ingredient and a polar compound, wherein the nicotinic ester or isonicotinic ester is present in an amount of from 0.5 to 70% by weight and the antiarrhythmic is present in an amount of from 0.01 to 20% by weight, both based on the total amount of the nicotinic ester or isonicotinic ester and the polar compound or compounds.
Claim 16
Dependent Claim
22 words
A method as in claim 10, wherein R and R' each represents an alkyl group having from 6 to 24 carbon atoms.
Claim 17
Dependent Claim
39 words
A method as in claim 11, wherein the antiarrhythmic is used in an amount of from 0.2 to 10% by weight based on the total weight of the nicotinic ester (I) or isonicotinic ester (II) and the polar compound.
Claim 18
Dependent Claim
17 words
A method as in claim 11, wherein the lower alcohol contains from 1 to 6 carbon atoms.
Claim 19
Dependent Claim
15 words
The method of claim 10 wherein said antiarrhythmic is ajmaline, prajmaline, pindolol, propranolol and quinidine.
Claim 20
Dependent Claim
10 words
The method of claim 10 wherein said antiarrhythmic is propranolol.
Claim 21
Dependent Claim
21 words
The method of claim 11 wherein said antiarrhythmic is selected from the group consisting of ajmaline, prajmaline, pindolol, propranolol and quinidine.
Claim 22
Dependent Claim
10 words
The method of claim 11 wherein said antiarrhythmic is propranolol.
References Cited (Backward Citations)
US2431558A
Cited
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