Clathrates of butylphtualide with cyclodextrin or its derivatives, a process for their preparation and the use thereof

Inactive Publication Date: 2006-07-27
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0027] The assay suggests that instillation of the inclusion complex has little vascular

Problems solved by technology

However, the butylphthalide can only be formulated into soft caps

Method used

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  • Clathrates of butylphtualide with cyclodextrin or its derivatives, a process for their preparation and the use thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of the Solid Inclusion Complex of Butylphthalide with hydroxypropyl-β-cyclodextrin

[0031] The inclusion complex is prepared by

[0032] (1) weighing 32.38 g (0.0210 mol) hydroxypropyl-β-cyclodextrin, adding it into 400 ml distilled water, and dissolving it with stirring;

[0033] (2) weighing 1 g (0.0052 mol) butylphthalide separately, and adding it into the hydroxypropyl-β-cyclodextrin solution mentioned above;

[0034] (3) stirring the mixed solution for 20 minutes by magnetic stirring method at a speed that the solution cannot be spattered, until the solution is clear and transparent, to obtain the liquid inclusion complex of butylphthalide with hydroxypropyl-β-cyclodextrin;

[0035] (4) filtering the liquid inclusion complex of butylphthalide with hydroxypropyl-β-cyclodextrin through a film, dividing it into vials, and freeze-drying it.

[0036] IR (KBr): 3393.46, 2931.26, 1158.24, 1081.60, 1032.07, 946.55, 580.68.13C-NMR: δ 131.47, 105.07, 84.03, 76.29, 75.04, 74.93, 62.89 pp...

example 2

Preparation of the Solid Inclusion Complex of Levorotatory Butylphthalide with Hydroxypropyl-β-cyclodextrin

[0037] The solid inclusion complex is prepared by

[0038] (1) weighing 32.38 g (0.0210 mol) hydroxypropyl-β-cyclodextrin, adding it into a mixed solvent of 400 ml distilled water and 20 ml absolute ethanol, and dissolving it with stirring;

[0039] (2) weighing 1 g (0.0052 mol) levorotatory butylphthalide separately, and adding it into the hydroxypropyl-β-cyclodextrin solution mentioned above;

[0040] (3) stirring the mixed solution for 20 minutes by magnetic stirring method at a speed that the solution cannot be spattered, until the solution is clear and transparent, to obtain the liquid inclusion complex of levorotatory butylphthalide with hydroxypropyl-β-cyclodextrin;

[0041] (4) concentrating the liquid inclusion complex of levorotatory butylphthalide with hydroxypropyl-β-cyclodextrin, and drying it under reduced pressure, to obtain the solid inclusion complex of levorotatory b...

example 3

Preparation of the Solid Inclusion Complex of Butylphthalide with hydroxypropyl-β-cyclodextrin

[0042] The solid inclusion complex is prepared by

[0043] (1) weighing 8.2 g (0.0053 mol) hydroxypropyl-β-cyclodextrin, placing it into a mortar, adding about 4 ml water and grinding the mixture into a paste; then weighing 1 g (0.0052 mol) butylphthalide and adding it into the mortar;

[0044] (2) grinding the mixture for 2 hours to obtain a homogenous and viscous paste, filtering the paste, then drying at 60° C. for 4 hours and grinding, to obtain the target inclusion complex.

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Abstract

The present invention relates to the inclusion complexes of butylphthalide, which is D,L-mixed or levorotatory, with cyclodextrin or cyclodextrin derivatives, to a process for their preparation and the use thereof. In the invention, the butylphthalide is complexed with cyclodextrin or cyclodextrin derivatives, preferably with hydroxypropyl-β-cyclodextrin, in order to increase the water-solubility of butylphthalide, develop clinical solid or liquid formulations and improve the therapeutic effect of butylphthalide. The inclusion complex, in which the molar ratio of butylphthalide to cyclodextrin or cyclodextrin derivatives is in the range of 1:1-10, can be used to prepare infusion, injection, injectable powder, liquids for oral administration, syrup, tablets, granules, dispersible tablets and others.

Description

TECHNICAL FIELD [0001] The present invention relates to pharmaceutical compositions. More particularly, it relates to the inclusion complexes of butylphthalide, which is D,L-mixed or levorotary, with cyclodextrin or its derivatives, to a process for their preparation and the use thereof. BACKGROUND ART [0002] Butylphthalide is a water insoluble oily compound with the following formula: [0003] There are two optical isomers, levorotary and dextrorotary butylphthalide, due to the presence of a chiral carbon therein. Chinese patent application No. 98125618.X disclosed the use of levorotary butylphthalide in the preparation of pharmaceutical compositions for preventing thrombosis and platelet agglomeration. It was found that butylphthalide could regulate the function of NOS-NO-cGMP system and the metabolism of arachidonic acid in the neurocytes after ischemia. Chinese patent application No. 93117148.2 disclosed the use of racemic butylphthalide mixture in the preparation of pharmaceutic...

Claims

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Application Information

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IPC IPC(8): A61K31/724C08B5/10A61K31/343A61K47/48C07D307/88
CPCA61K31/343A61K47/48969B82Y5/00C07D307/88C08B37/0015A61K47/6951A61P7/02A61P9/10
Inventor NIU, ZHAN-QIZHAO, KAILIU, WEN-JUANZHOU, GUI-RONGLIU, CHAOWANG, RONG-DUANYUAN, HONG-ZHONGGUO, WEN-MINYAN, SUI-CHAOBAI, MIN
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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