Stable solid preparation comprising 4,5-epoxymorphinan derivative

一种固体制剂、环氧基的技术，应用在含有效成分的医用配制品、非有效成分的医用配制品、丸剂输送等方向，能够解决未有硫代硫酸钠、没有稳定化效果等问题，达到保存性优异的效果

Active Publication Date: 2010-03-31
TORAY IND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, there is no record of sodium thiosulfate in the above-mentioned report, and there is no record of the stabilizing effect of adding sugar alcohol or sodium thiosulfate on the storage stability of medicines at all.

Method used

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  • Stable solid preparation comprising 4,5-epoxymorphinan derivative
  • Stable solid preparation comprising 4,5-epoxymorphinan derivative
  • Stable solid preparation comprising 4,5-epoxymorphinan derivative

Examples

Experimental program
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Effect test

Embodiment 1

[0084] 78.895 parts of mannitol (ペアリトル SD200, ロケツトジヤパン) was weighed, sieved through a sieve with an opening of 1 mm, and charged into a fluidized bed granulator (FLO-5, Ferrointo Industries). 0.005 parts of compound 1 and 0.1 part of sodium thiosulfate hydrate were dissolved in distilled water to obtain a spray liquid, and the obtained granulated particles (the average particle diameter measured according to the particle size determination method of the Japanese Pharmacopoeia of the 15th revision was 146 μm) Spraying is performed to prepare drug-loaded granules. 15 parts of mannitol and 5 parts of low-substituted hydroxypropyl cellulose (average particle size 50 μm, hydroxypropoxy content 10.0-12.9 wt%, loose bulk density 0.34 g / mL ( LH11, Shin-Etsu Chemical Industry) [hereinafter abbreviated as L-HPC]), mixed with a V-type mixer (permeable type S-5, Tsutsui Riken Machinery) for 15 minutes. 1 part of magnesium stearate (Taipei Chemical Industry) was further added and mixed fo...

Embodiment 2

[0086] The drug-loaded granules were prepared in the same manner as in Example 1, and 10 parts of mannitol, 10 parts of L-HPC, and 1 part of magnesium stearate were added to 79 parts of granules loaded with compound 1. Mix and tablet by the same method as Example 1.

Embodiment 3

[0088] Drug-carrying granules were prepared in the same manner as in Example 1, except that 20 parts of L-HPC and 1 part of magnesium stearate were added to 79 parts of compound 1-carried granules, and the same procedure as in Example 1 was carried out except that Method Mix and tablet.

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Abstract

Disclosed is a stable solid preparation comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an active ingredient. Specifically disclosed is a stable solid preparation comprising: a 4,5-epoxymorphinan derivative represented by the general formula (I) or a pharmacologically acceptable acid addition salt thereof as an active ingredient; sodium thiophosphate; a sugar or a sugar alcohol; and a hydroxypropylcellulose having a low degree of substitution in an amount of 1 to 30% by weight per unit weight of the total amount of the active ingredient, sodium thiophosphate and the sugar or the sugar alcohol.

Description

technical field [0001] The present invention relates to stable solid preparations of 4,5-epoxymorphinan derivatives or pharmacologically acceptable acid addition salts thereof. More specifically, it relates to a stable solid preparation having the following characteristics: using 4,5-epoxymorphinan derivatives or pharmacologically acceptable acid addition salts thereof as active ingredients, containing sodium thiosulfate, sugar or sugar alcohols, and low-substituted hydroxypropyl cellulose, the cellulose accounts for 1-30% by weight in the unit weight containing active ingredients. [0002] Here, the unit containing the active ingredient refers to the unit of the solid component in the preparation that is in direct contact with the active ingredient. For example, in the case of a film-coated tablet, it is the core part of the tablet, and in the case of a capsule, it is the drug-loaded and dispersed part. The solid content of the filling, if it is a granule coated with a funct...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K9/14A61K9/16A61K9/20A61K9/28A61K9/48A61K47/02A61K47/10A61K47/26A61K47/36A61K47/38A61P11/14A61P17/04A61P25/02
CPCA61K9/2054A61K31/485A61K9/2018A61K9/2009A61P11/14A61P17/04A61P25/02A61K47/38A61K9/28
Inventor 高木卓太田琴惠堀内保秀小林正人川崎纯子堀泽荣次郎
Owner TORAY IND INC
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