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Topiroxostat tablet

A technology of topinostat and dispersible tablets, which is applied in the direction of medical preparations of non-active ingredients, pill delivery, organic active ingredients, etc., and can solve the problems of slow onset of action and low bioavailability

Active Publication Date: 2015-08-05
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to solve the shortcoming of slow onset of action and low bioavailability of the existing topinostat preparations, the present invention invented the inclusion compound dispersible tablet of topinostat

Method used

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Examples

Experimental program
Comparison scheme
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Embodiment Construction

[0028] Examples 1-6 (prescription is by weight):

[0029]

[0030] Topicastat inclusion complex: Topicastat: β-cyclodextrin: hydroxypropyl β-cyclodextrin is 1:1:2.

[0031] Preparation:

[0032] 1. Prepare the inclusion compound of topicastat according to the following method:

[0033] (1) In water or ethanol containing water, according to a certain ratio, react topicastat with hydroxypropyl β-cyclodextrin, filter the resulting solution through a microporous membrane until clarified, and separate the clathrate from the mixture thing; or

[0034] (2) in solid form, reacting topicastat with hydroxypropyl beta-cyclodextrin; or

[0035] (3) Topicastat reacts with hydroxypropyl β-cyclodextrin for high-energy grinding.

[0036] 2. Mix the prescribed amount of sodium carboxymethyl starch, pregelatinized starch, aspartame and topicastat inclusion complex according to the equal addition method, then add magnesium stearate, micronized silica gel, and mix well , compressed into t...

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Abstract

The invention provides a topiroxostat tablet and a preparation method thereof, and belongs to the technical field of medicine. The invention relates to a topiroxostat clathrate compound dispersible tablet; the topiroxostat is firstly prepared into a clathrate compound and then the clathrate compound is prepared into the dispersible table. The topiroxostat tablet has the advantages of quick dissolving, quick absorption, high bioavailability, convenience for taking and the like.

Description

technical field [0001] The invention provides a topicastat tablet and a preparation method thereof, belonging to the technical field of medicine. The invention relates to a topicastat inclusion compound dispersible tablet. The topicastat is firstly prepared as an inclusion compound, and then prepared into a dispersible tablet. The invention has the advantages of rapid dissolution, fast absorption, high bioavailability, convenient administration and the like. Background technique [0002] Topinostat, Chinese chemical name: 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, the structural formula is as follows: [0003] [0004] Molecular formula: C 13 h 8 N 6 [0005] Molecular weight: 248.24. [0006] Topinostat tablets are imitation tablets of Fuji Pharmaceutical Co., Ltd., Japan. Its trade name: TOPILORIC Tablets, Japanese name: トピロリツワ, general name: Topiroxostat, ロキソスタット; specifications: 20mg, 40mg and 60mg, released in June 2013 Approved for mar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/444A61K47/48A61K47/36A61K47/26A61P19/06
Inventor 王明刚陈阳生任莉孙桂玉刘晓霞翟翠云臧云龙
Owner CP PHARMA QINGDAO CO LTD
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