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Percutaneous preparations

a percutaneous preparation and phosphonic acid technology, applied in the field of percutaneous preparations, can solve the problems of poor bioavailability of bisphosphonates, poor absorption of bisphosphonates, undesired effects, etc., and achieve excellent drug retention and percutaneous permeability and targeting. excellent

Inactive Publication Date: 2010-03-04
TSUJI YASUHIRO +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a percutaneous preparation of incadronate or minodronic acid using a suspension-type base and an amphiphilic solubilizing auxiliary agent. The preparation has excellent percutaneous permeability and can target bone tissues effectively. The invention also provides a method for enhancing the percutaneous absorption of the bisphosphonic acid derivatives by using a solubilizing agent and an amphiphilic solubilizing auxiliary agent. The percutaneous preparation can be used for the treatment of bone-related diseases such as osteoporotic fractures.

Problems solved by technology

It is reported that these bisphosphonates are poor in bioavailability when orally administered, should avoid alimentary effects since their absorption is suppressed especially in the presence of calcium or iron, deposit very rapidly onto bone and might cause gastrointestinal disorders by oral administration though they are mild, and further that recent studies revealed bioavailability of the bisphosphonates even when administered pernasally or percutaneously, and so on (see “Bisphosphonates and Bone Disease: Kiso-to-Rinsho (The Clinical Report)” Jul. 30, 1996, published by Ishiyaku Publishers Inc.).
However, the bisphosphonates are poor in absorbability per os and sometimes cause an undesired effect such as gastrointestinal disorders, etc. when a large dose is administered.

Method used

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  • Percutaneous preparations

Examples

Experimental program
Comparison scheme
Effect test

example 1

Ointment

[0073]After 5.0 parts of lanolin, 5.0 parts of cetostearyl alcohol and 80 parts of white petrolatum were melted on a water bath, a blend of 20% aqueous solution containing 0.5 part of incadronate, 5.0 parts of N-methyl-2-pyrrolidone and 4.5 parts of liquid paraffin was added to the molten mixture. The resultant was uniformly kneaded while warming (about 80° C.). After discontinuing warming, the resultant was made fully homogeneous to provide an ointment.

example 2

Cream

[0074]After 5.0 parts of cetanol, 2.0 parts of stearic acid, 1.0 part of sorbitan monostearate and 1.0 part of polyoxyethylene sorbitan monostearate were melted on a water bath, a blend of 20% aqueous solution containing 1.0 part of incadronate, 5.0 parts of N-methyl-2-pyrrolidone and 9.0 parts of liquid paraffin was added to the molten mixture. The resultant was uniformly kneaded and maintained at about 75° C. A solution previously prepared by 0.1 part of methyl paraoxybenzoate and butyl paraoxybenzoate in a sufficient quantity of distilled water and warming at 80° C. was added to the kneaded mixture, followed by uniformly kneading while warming. After discontinuing warming, the resultant was made fully homogeneous to provide a cream.

example 3

Plaster Formulation (Tape, Incadronate and N-methyl-2-pyrrolidone)

[0075]A blend of 20% aqueous solution containing 2.0 parts of incadronate as the effective ingredient, 5.0 parts of N-methyl-2-pyrrolidone, 2.5 parts of α-monoisostearyl glyceryl ether, 5.0 parts of isopropyl myristate and 1.0 part of sorbitan fatty acid ester was added to 40.0 parts of styrene-isoprene-styrene block copolymer, 34.5 parts of terpene resin and 10.0 parts of aliphatic hydrocarbon resin, and a sufficient quantity of ethyl acetate was added thereto. The resultant was uniformly mixed to form an adhesive mass. The adhesive mass was uniformly applied onto a releasable film followed by drying with warm air. A backing film was laminated and transferred thereon to provide a tape preparation.

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Abstract

A bisphosphonic acid derivative-containing percutaneous preparation of an excellent percutaneous permeability, comprising a bisphosphonic acid derivative such as incadronic acid, minodronic acid, etc., or pharmaceutically acceptable salts thereof, a solubilizing agent for the derivative or pharmaceutically acceptable salts thereof, and an amphiphilic solubilizing auxiliary agent, which may optionally contain a suspension-type base such as a polyvalent alcohol, a higher fatty acid ester, a liquid hydrocarbon or a vegetable oil, etc. This preparation has an excellent percutaneous permeability, reduces burdens on the patient, does not deteriorate the patient's compliance even in the administration over a prolonged period of time and can achieve the therapeutic effects in a short period of time.

Description

TECHNICAL FIELD[0001]The present invention relates to bisphosphonic acid derivative-containing percutaneous preparations having an excellent percutaneous permeability, which comprises bisphosphonic acid derivatives or pharmaceutically acceptable salts thereof, and solvents for the bisphosphonic acid derivatives or pharmaceutically acceptable salts thereof and amphiphilic solubilizing auxiliary agents. More particularly, the present invention relates to percutaneous preparations comprising incadronic acid or minodronic acid, or pharmaceutically acceptable salts thereof.BACKGROUND ART[0002]Certain synthetic bisphosphonate compounds having a methanebisphosphonic acid structure which are structurally analogous to pyrophosphoric acid and stable also in vivo (hereinafter referred to as bisphosphonic acid derivatives or pharmaceutically acceptable salts thereof, or sometimes merely as bisphosphonic acid derivatives) have biological actions such as an excellent bone resorption inhibitory ac...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61L15/16A61K31/66A61K9/70A61K31/663A61K47/04A61K47/06A61K47/22A61K47/26A61P3/14A61P19/08A61P19/10A61P43/00
CPCA61K9/0014A61K9/7053A61K9/7076A61K47/26A61K47/06A61K47/22A61K31/663A61P3/14A61P19/08A61P19/10A61P43/00A61K9/10A61K9/70
Inventor TSUJI, YASUHIROTAMURA, KEIYAMAZAKI, YUUHIROSAWAI, YOSHIHIRO
Owner TSUJI YASUHIRO
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