KR930007448A - Pharmaceutical Formulations with Improved Absorption - Google Patents

Abstract

A pharmaceutical preparation characterized in that the benzoxazole derivative of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient, which is effective for the treatment of diabetes upon oral administration, wherein the active ingredient is dispersed or dissolved in a water-soluble polymer, and It provides a manufacturing method thereof.

[Wherein R is an optionally substituted phenyl or naphthyl group; And AIK represents a lower alkylene group]

Description

Pharmaceutical Formulations with Improved Absorption

Since this is an open matter, no full text was included.

1 is a graph of the physical mixture with PEG-6000 and the diffraction intensity and Bragg angle of solid dispersion preparation / PEG-6000.

2 is a graph of the original untreated, and diffraction intensity and Bragg angle of solid dispersion preparation / PVP, HPC, HPMC.

3 shows the blood levels of the active ingredient (I) over time after oral administration of the solid dispersion preparation of the present invention to dogs.

Claims (13)

A pharmaceutical preparation comprising as an active ingredient a benzoxazole derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein the active ingredient is dispersed or dissolved in a water-soluble polymer. [Wherein R is an optionally substituted phenyl or naphthyl group; And AIK represents a lower alkylene group.] The pharmaceutical preparation of claim 1 wherein the active ingredient is dispersed into a water soluble polymer in the solid state at room temperature or dissolved into a water soluble polymer in the liquid state at room temperature. The pharmaceutical preparation of claim 1 wherein the water soluble polymer is selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, hydroxypropylmethyl cellulose and hydroxypropyl cellulose. The pharmaceutical preparation according to claim 1, wherein the active ingredient is a benzoxazole derivative of the following formula (I). [Wherein R is a phenyl group and a naphthyl group optionally substituted with one to three substituents selected from the group consisting of a halogen atom, a di (lower alkyl) amino group and a pyrrolidino group.] The pharmaceutical preparation according to claim 1, wherein R is a phenyl group or a naphthyl group substituted with a halogen atom, a di (lower alkyl) amino group or a pyrrolidino group. The compound according to claim 1, wherein the active ingredient is 5-[(2,4-dioxothiazolidin-5-yl) methyl] -2- [4- (dimethylamino) -benzyl] benzoxazole or pharmaceutically acceptable Pharmaceutical preparations, which are his salts possible. The method according to claim 1, wherein the active ingredient is 5-[(2,4-dioxothiazolidin-5-yl) methyl] -2- [4- (naphthyl) methyl] benzoxazole or pharmaceutically acceptable His salt is a pharmaceutical preparation. The active ingredient according to claim 1, wherein the active ingredient is 5-[(2,4-dioxothiazolidin-5-yl) methyl] -2- [4- (chlorobenzyl) benzoxazole or a pharmaceutically acceptable salt thereof. Pharmacy preparation. The compound according to claim 1, wherein the active ingredient is 5-[(2,4-dioxothiazolidin-5-yl) methyl] -2- [4- (pyrrolidinobenzyl) benzoxazole or pharmaceutically acceptable His salt is a pharmaceutical preparation. A benzoxazole derivative of formula (I) or a pharmaceutically acceptable salt thereof is dispersed in a water-soluble polymer in a solid state or dissolved in a water-soluble polymer in a liquid state. Method of Preparation of the Formulation. The method of claim 10, wherein the dispersing method heats the mixture until the mixture of compound (I) and the water-soluble polymer melts, and then cools the molten compound to solidify the mixture; Or by dissolving the compound (I) and the water-soluble polymer in a solvent and removing the solvent from the resulting solution. A pharmaceutical preparation and its pharmaceutically acceptable additives, which contain as an active ingredient a benzoxazole derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein the active ingredient is dispersed or dissolved in a water-soluble polymer. A pharmaceutical formulation for treating diabetes. [Wherein R is an optionally substituted phenyl or naphthyl group; And AIK represents a lower alkylene group.] Oral administration to a patient of a therapeutically effective amount of a pharmaceutical preparation containing as an active ingredient a benzoxazole derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein said active ingredient is dispersed or dissolved in a water soluble polymer How to treat diabetes. [Wherein R is an optionally substituted phenyl or naphthyl group; And AIK represents a lower alkylene group.] ※ Note: The disclosure is based on the initial application.