Inclusion compound of alpha crystal imatinib and preparation method thereof

A technology of inclusion complex and crystal form, which is applied in the field of inclusion complex of α crystal form imatinib and its preparation, can solve the problem that there is no reported preparation method of stable α crystal form imatinib, etc. Effects of stability and ease of operation, good fluidity, and low hygroscopicity

Inactive Publication Date: 2011-04-13
SHENZHEN NEPTUNUS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] As far as the current literature is concerned, there is no report of an inclusion compound of α-crystalline imatinib with higher stability and more suitable for clinical pharmaceutical use and its preparation method.

Method used

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  • Inclusion compound of alpha crystal imatinib and preparation method thereof
  • Inclusion compound of alpha crystal imatinib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of liquid inclusion compound of α-crystalline imatinib β-cyclodextrin

[0020] Weigh 0.1 g of α-crystalline imatinib and add 5 ml of absolute ethanol to dissolve it. Then weigh 19.9 g of β-cyclodextrin and use 500 ml of water to make a saturated solution in a constant temperature water bath at 50° C., slowly add the ethanol solution of α crystal form imatinib dropwise under stirring (or ultrasonic) at 50 rpm, and continue stirring ( or ultrasound) for 10 minutes, stop heating, continue stirring, that is.

[0021] It is said that the β-cyclodextrin ring can use cyclodextrin or its derivatives such as hydroxypropyl-β-cyclodextrin or dimethyl-β-cyclodextrin or dihydroxypropyl--β-cyclodextrin Alcohol or maltotriose cyclodextrin or maltotriose cyclodextrin or β-cyclodextrin sulfobutyl ether or hydroxyethyl--β-cyclodextrin or methyl-β-cyclodextrin or glucosyl-β-cyclodextrin One of the dextrins or a mixture of several of them can be used instead.

[0...

Embodiment 2

[0023] Example 2: Preparation of α-crystalline imatinib hydroxypropyl-β-cyclodextrin solid inclusion compound

[0024] Weigh 3 g of α crystal form imatinib and add 5 ml of absolute ethanol to dissolve it. Then weigh 97g of hydroxypropyl-β-cyclodextrin and use 500ml of water to make a saturated solution in a constant temperature water bath at 70°C, and slowly add the ethanol solution of α-crystalline imatinib dropwise under 100rpm stirring (or ultrasonic), Continue to stir (or sonicate) for 30 minutes, stop heating, continue to stir, refrigerate for 24 hours, filter with suction, wash, freeze-dry the precipitate, and obtain it.

Embodiment 3

[0025] Example 3: Preparation of α-crystalline imatinib hydroxypropyl-β-cyclodextrin solid inclusion complex by grinding method

[0026] Put 6 g of α crystal form imatinib and 194 g of cyclodextrin or its derivatives in a colloid mill or ball mill or mortar, add an appropriate amount of solvent to make a paste, grind for 1-3 hours, and place in Dry at a temperature of 40-70°C to obtain a solid clathrate of α-crystalline imatinib.

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Abstract

The invention relates to an inclusion compound of alpha crystal imatinib. The inclusion compound of alpha crystal imatinib is prepared by selecting cyclodextrin or derivatives thereof as an inclusion material and is characterized by comprising 0.1-0.3wt% of alpha crystal imatinib and 97.0-99.9wt% of cyclodextrin or derivatives thereof. In the preparation of the inclusion compound, a solvent method and a grinding method can be adopted. As the inclusion compound is prepared by adopting the cyclodextrin or derivatives thereof to include the alpha crystal imatinib, the sensitivity of the alpha crystal imatinib to light, temperature and heat is overcome, and the instability problem of the alpha crystal imatinib is solved. Liquid preparations, semi-solid preparations or solid preparations further prepared from the inclusion compound respectively have improved stability and convenience in operation. The inclusion compound is simple in preparation process, has no need of special requirements on preparation package and storage conditions, and is a novel alpha crystal imatinib preparation which has better liquidity, higher stability and lower moisture absorption and is suitable for clinical use.

Description

technical field [0001] The present invention relates to an inclusion compound of α crystal form imatinib and a preparation method thereof, in particular to an inclusion compound of α crystal form imatinib using cyclodextrin and cyclodextrin derivatives. its preparation method. Background technique [0002] Imatinib mesylate was developed by Novartis, and its chemical name is 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[4-(3 -pyridyl)-2-pyrimidinyl]amino]-phenyl]benzamide mesylate, structural formula: [0003] [0004] Molecular formula: C 29 h 31 N 7 O·CH 4 o 3 S, molecular weight: 589.71. [0005] Imatinib was approved by the FDA in December 2001 as a first-line drug for chronic myelogenous leukemia, and has been hailed as an oral anti-cancer drug with a "major breakthrough" in recent years. On February 1, 2002, the FDA approved the second indication of imatinib for the treatment of gastrointestinal stromal tumors. Imatinib is also the first drug designed ba...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/506A61P35/02A61K47/69
Inventor 王兵唐田朱丹严启新陈红黄传贵王志国叶勤冯汉林
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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