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Nateglinide-containing preparation

a technology of nateglinide and preparation, which is applied in the field of preparation of nateglinide, can solve the problems of poor dissolution ability of nateglinide drug substance powder or ordinary tablets containing nateglinide, poor water soluble substance of nateglinide, etc., and achieve the effect of improving the dissolution property

Inactive Publication Date: 2009-08-13
AJINOMOTO CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007]An object of the present invention is to provide, as a nateglinide-containing preparation, a pharmaceutical preparation containing amorphous nateglinide wherein dissolution rate of drugs is high and crystal transition does not happen during producing or conserving preparations.
[0008]For the purpose of solving the problems, the inventors have vigorously studied and found that dissolution property can be improved by making nateglinide amorphous in a preparation and the like. The present invention has been complete...

Problems solved by technology

On the other hand, the nateglinide is a poorly water soluble substance and therefore, capsules filled with nateglinide drug substance powder or ordinary tablets containing nateglinide do not dissolve well when administered orally because of its low disintegrating ability.
As a result, such nateglinide-containing preparations can not show the fast-acting and short duration effect in decreasing a blood glucose level (fast-acting hypoglycemic agent), which is characteristic of nateglinide.
However, it can not be regarded as effective in all crystal forms of nateglinide.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Production of Amorphous Nateglinide

[0043]4 g of nateglinide in B-type crystal form and 32 g of polyvinyl pyrrolidone were dissolved into ethanol. Ethanol was removed by evaporation (60° C.), and the mixture was dried under vacuum at 60° C. for 3 hours or more. The solid material was ground in a mortar to obtain 36 g of nateglinide in the form of solid dispersion.

examples 2

Production of Tablets Containing Amorphous Nateglinide

[0044]60 g of nateglinide (B-type crystals), 4 g of hydroxypropylcellulose and 60 g of crospovidone (COLIDONE CL-M, BASF) were dissolved and suspended into 160 g of ethanol to obtain a binder solution. 180 g of crospovidone (COLIDONE CL-M, BASF) and 96 g of crystalline cellulose were placed in a fluidized bed granulator (FLO-1 type, Freund Industrial Co., Ltd.) and mixed together. Then the binder solution was sprayed to granulate into a fluidized bed (intake temperature: 80° C., spray speed: 4.9 g / min., spray pressure: 1.8 kgf / cm).

[0045]250 g of the obtained granules and 3.8 g of magnesium stearate were mixed in a V-type mixer to obtain granules for tabletting. A rotary tabletting machine (HT-AP15-ssII, Hata Factory) was used with a punch of 8 mm φ-14R2r to obtain 253.8 g of core tablets (weight of the core tablet: 203.1 mg).

[0046]80 g of hydroxypropylmethylcellulose, 15 g of macrogol 6000, 24 g of talc and 5 g of titanium oxide ...

example 3

Production of Liquid-Filled Capsules

[0048]186 mg of nateglinide, 1456 mg of macrogol 400 and 1456 mg of polysorbate 80 were mixed in a stirrer at room temperature until they were dissolved and a transparent solution of nateglinide was prepared. 500 mg of the drug solution was filled in size 0 capsules to obtain liquid-filled capsules (nateglinide: 30 mg).

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Abstract

The present invention discloses, as a immediate-release preparation useful as an antidiabetic, a nateglinide-containing preparation comprising nateglinide as an active ingredient wherein the nateglinide is amorphous.

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to a preparation of nateglinide that is useful as an antidiabetic and more specifically to a immediate-release preparation of nateglinide.BACKGROUND ART[0002]It is known that nateglinide [compound name: N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine] exhibits an excellent blood glucose-lowering effect by oral administration and therefore, is useful as a therapeutic agent for diabetes (Japanese Patent Publication No. Hei 4-15221).[0003]On the other hand, the nateglinide is a poorly water soluble substance and therefore, capsules filled with nateglinide drug substance powder or ordinary tablets containing nateglinide do not dissolve well when administered orally because of its low disintegrating ability. As a result, such nateglinide-containing preparations can not show the fast-acting and short duration effect in decreasing a blood glucose level (fast-acting hypoglycemic agent), which is characteristic of na...

Claims

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Application Information

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IPC IPC(8): A61K31/195A61P3/10A61K31/192A61K31/198
CPCA61K31/198A61K31/192A61P3/10
Inventor NINOMIYA, NOBUTAKAMAKINO, CHISATOYABUKI, AKIRA
Owner AJINOMOTO CO INC
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