Composition for percutaneous administration

• US 4,847,260 A
• Filed: 10/26/1987
• Issued: 07/11/1989
• Est. Priority Date: 11/15/1984
• Status: Expired due to Fees

• Current Assignee: Nitto Electric Industrial Co., Ltd. (Nitto Denko Corporation)
• Original Assignee: Nitto Denko Corporation
• Inventors: Abe, Yoko, Yamanaka, Naoko, Hori, Mitsuhiko, Satoh, Susumu
• Primary Examiner(s): FRIEDMAN, STANLEY
• Application Number:
  US07/113,352
• Time in Patent Office: 624 Days
• Field of Search: 514/356, 514/279, 514/305, 514/418, 514/652
• US Class Current: 514/279
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: C07D 213/79 Acids; Esters
• CPC Class Codes: C07D 213/80 in position 3

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.

Claims

1. 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.

4. A composition as in claim 1, wherein R and R'"'"' each represents an alkyl group having from 6 to 24 carbon atoms.

6. The composition of claim 1 wherein said antiarrhythmic is selected from the group consisting of ajmaline, prajmaline, pindolol, propranolol and quinidine.

7. The composition of claim 1 wherein said antiarrhythmic is propranolol.

2. 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.

3. 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.

5. A composition as in claim 2, wherein the lower alcohol contains from 1 to 6 carbon atoms.

8. The composition of claim 2 wherein said antiarrhythmic is selected from the group consisting of ajmaline, prajmaline, pindolol, propranolol and quinidine.

9. The composition of claim 2 wherein said antiarrhythmic is propranolol.

10. 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.

12. A method as in claim 10, wherein R and R'"'"' each represents an alkyl group having from 6 to 24 carbon atoms.

15. The method of claim 10 wherein said antiarrhythmic is ajmaline, prajmaline, pindolol, propranolol and quinidine.

16. The method of claim 10 wherein said antiarrhythmic is propranolol.

11. 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.

13. 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.

14. A method as in claim 11, wherein the lower alcohol contains from 1 to 6 carbon atoms.

17. The method of claim 11 wherein said antiarrhythmic is selected from the group consisting of ajmaline, prajmaline, pindolol, propranolol and quinidine.

18. The method of claim 11 wherein said antiarrhythmic is propranolol.