Butylbenzene phthalein cyclodextrin or cyclodextrin derivative clathrate, its preparation method and application

A cyclodextrin and derivative technology, which is applied in the field of butylphthalide cyclodextrin or cyclodextrin derivative inclusion complex and preparation thereof, can solve the problems of butylphthalide being insoluble in water, etc. Water-soluble, good water-soluble effect

Inactive Publication Date: 2003-02-05
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to further study the clinical applicability of butylphthalide and overcome the deficiencies of the prior art, the applicant applied for "a kind of inclusion compound of butylphthalide cyc

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Preparation of liquid butylphthalide hydroxypropyl-β-cyclodextrin derivative inclusion compound

[0032] (1) Weigh 32.38g (0.0210mol) of hydroxypropyl-β-cyclodextrin, pour it into 400ml of distilled water, and stir to dissolve;

[0033] (2) Another 1 g (0.0052 mol) of butylphthalide was weighed and poured into the above-mentioned hydroxypropyl-β-cyclodextrin solution;

[0034] (3) The mixed solution was stirred for 20 minutes by magnetic stirring method, and the stirring speed was preferably such that the liquid did not splash out, and the solution was observed until it was clear and transparent, and the liquid butylphthalide hydroxypropyl-β-cyclodextrin inclusion compound was obtained.

Embodiment 2

[0035] Example 2: Preparation of solid L-butylphthalide hydroxypropyl-β-cyclodextrin inclusion compound

[0036] (1) Weigh 32.38g (0.0210mol) of hydroxypropyl-β-cyclodextrin, pour it into a mixture of 400ml of distilled water and 20ml of absolute ethanol, and stir to dissolve;

[0037] (2), (3) are the same as embodiment 1.

[0038] (4) Concentrate the liquid L-butylphthalide hydroxypropyl-β-cyclodextrin inclusion compound, and dry it under reduced pressure to obtain a solid L-butylphthalide hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 3

[0039] Example 3: Preparation of solid butylphthalide hydroxypropyl-β-cyclodextrin inclusion compound

[0040] (1) Weigh 8.2g (0.0053mol) of hydroxypropyl-β-cyclodextrin, put it into a mortar, add about 4ml of water, grind it into a paste; weigh 1g (0.0052mol) of butylphthalide, pour it into the in the bowl;

[0041] (2) The mixture was ground for 2 hours to obtain a uniform viscous substance, which was filtered, dried at 60°C for 4 hours, taken out, ground and pulverized.

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PUM

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Abstract

The present invention relates to butylbenzene phthalein cyclodextrin or cyclodextrin derivative clathrate, its preparation method and application. The described butylbenzene phthalein is mixed-rotatory butylbenzene phthalein and levo-butylbenzene phthalein. In order to raise water solubility of butylbenzene phthalein and develop solid dosage form and liquid dosage form required for clinical application said invention adopts cyclodextrin or cyclodextrin derivative to include the butylbenzene phthalein. Said clatherate contains butylbenzene phthalein and cyclodextrin or cyclodextrin derivative, the mole ratio of both them is 1:1-10. The cyclodextrin or cyclodextrin derivative optimally selects hydroxypropyl-beta-cyclodextrin. Said clathrate can be used for preparing various dosage forms of injection, oral preparation, tablet, capsule and others.

Description

technical field [0001] The present invention relates to a kind of pharmaceutical composition, specifically, the present invention relates to butylphthalide cyclodextrin or cyclodextrin derivative inclusion compound and its preparation method and application, and said active ingredient butylphthalide refers to hexabutylbenzene phthalein or L-butylphthalide. Background technique [0002] Butylphthalide is a water-insoluble oily substance with the following structure: [0003] Since it contains a chiral carbon atom, it has two optical isomers, namely L-butylphthalide and D-butylphthalide. In Chinese patent 98125618.X, the application of L-butylphthalide in the preparation of antithrombotic and antiplatelet aggregation drugs is disclosed, which clearly shows that this product can regulate the function of NOS-NO-cGMP system and the nerve cells after cerebral ischemia. The role of tetraenoic acid metabolism. In Chinese patent 93117148.2, the application ...

Claims

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Application Information

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IPC IPC(8): C08B37/16
Inventor 牛占旗赵凯刘文娟周桂荣刘超王荣端苑洪忠刘英发白敏张勇郭文敏
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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