Ginkgolide B nanometric liposomes medicine and the preparing method thereof

A nano-liposome and ginkgolide technology, applied in the directions of liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of low solubility in water, peroxidation, targeting lesions, etc., and achieve accurate active ingredients and safe use. , the exact effect of curative effect

Inactive Publication Date: 2010-07-14
江苏仲德医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In order to solve the problems of the existing ginkgolide B drug lactone structure in vivo hydrolysis, low solubility in water, peroxidation in the body, and target lesions in the body, the present invention provides a ginkgolide B nanoliposome drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The present embodiment adopts ginkgolide B nanoliposome pharmaceutical formula, comprises the raw material of following ratio:

[0032] 8 moles of the mixture of cephalin and distearoylcholine molar ratio of 1:3;

[0033] 8 moles of a mixture of soybean sterol and cholesterol molar ratio of 1:4;

[0034] 4 moles of 3:1 mixture of γ-cyclodextrin and α-cyclodextrin molar ratio;

[0035] Methoxy polyethylene glycol 2000-hydrogenated soybean phosphatidylethanolamine 0.4 mole;

[0036] Ginkgolide B 1 mole;

[0037] Vitamin E 0.5 mole.

[0038] The preparation method of above-mentioned ginkgolide B nano liposome medicine, comprises the steps:

[0039] (1) The amount of ginkgolide B is dissolved in a mixed solution of absolute ethanol / ethyl acetate volume ratio of 2:1;

[0040] (2) Dissolve the 3:1 mixture of γ-cyclodextrin and α-cyclodextrin molar ratio in 0.015M / L, pH 6.0-7.0 phosphate buffer to make γ-cyclodextrin Dextrin / 2-hydroxypropyl-β-cyclodextrin concentration 6...

Embodiment 2

[0064] The present embodiment adopts ginkgolide B nanoliposome pharmaceutical formula, comprises the raw material of following ratio:

[0065] 12 moles of a mixture of cephalin and distearoylcholine molar ratio of 1:6;

[0066] 6 moles of the mixture of soybean sterol and cholesterol molar ratio of 1:4;

[0067] 6 moles of 3:1 mixture of 2-hydroxypropyl-β-cyclodextrin and α-cyclodextrin molar ratio;

[0068] Methoxy polyethylene glycol 2000-hydrogenated soybean phosphatidylethanolamine 0.2 mole;

[0069] Ginkgolide B 2 moles;

[0070] Vitamin E 0.1 mole.

[0071] The preparation method of above-mentioned ginkgolide B nano liposome medicine, comprises the steps:

[0072] (1) The amount of ginkgolide B is dissolved in a mixed solution of absolute ethanol / ethyl acetate volume ratio of 2:1;

[0073] (2) Dissolve the mixture of 2-hydroxypropyl-β-cyclodextrin and α-cyclodextrin in a molar ratio of 3:1 in 0.015M / L, pH 6.0-7.0 phosphate buffer , making a solution with a concentr...

Embodiment 3

[0098] The present embodiment adopts ginkgolide B nanoliposome pharmaceutical formula, comprises the raw material of following ratio:

[0099] 8 moles of the mixture of cephalin and distearoylcholine molar ratio of 1:4;

[0100] 6 moles of a mixture of soybean sterol and cholesterol molar ratio of 1:3;

[0101] 4 moles of 3:1 mixture of γ-cyclodextrin and α-cyclodextrin molar ratio;

[0102] Methoxy polyethylene glycol 2000-hydrogenated soybean phosphatidylethanolamine 0.2 mole;

[0103] Ginkgolide B 1 mole;

[0104] Vitamin E 0.1 mole.

[0105] The preparation method of above-mentioned ginkgolide B nano liposome medicine, comprises the steps:

[0106] (1) The amount of ginkgolide B is dissolved in a mixed solution of absolute ethanol / ethyl acetate volume ratio of 2:1;

[0107] (2) Dissolve the 3:1 mixture of γ-cyclodextrin and α-cyclodextrin molar ratio in 0.015M / L, pH 6.0-7.0 phosphate buffer to make γ-cyclodextrin A solution with a dextrin concentration of 60-70%;

...

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Abstract

The invention relates to a ginkgolide B nanoliposomes drug and a method for preparing the same. The invention provides the ginkgolide B nanoliposomes drug including the following materials and the following radios: 8-12 mol compositions of cephalin and distearoyl choline with mole ratio of 1:3-6; 6-8 mol compositions of sojasterol and cholesterin with mole ratio of 1:2-4; 4-6 mol compositions of gamma-cyclodextrin / 2-hychoxypropyl-beta-cyclodextrin and alpha-cyclodextrin with mole ratio of 3:1; 0.2-0.4 mol methoxy polyethylene glycol 2000-hydrogenated soybean phosphatidylethanolamine; 2 mol ginkgolide B; and 0.1-0.5 mol vitamine E. A method for preparing the ginkgolide B nanoliposomes drug is also provided in the invention to produce the ginkgolide B nanoliposomes for target treating blocking of vessel or endothelial cell thereof, with a better healing effect than ordinary preparations of ginkgolide B.

Description

technical field [0001] The invention relates to a ginkgolide B nano liposome medicine and a preparation method thereof. Background technique [0002] The existing ginkgolide B drug has achieved a leap from complex ginkgo biloba extract to monomer drug, and has become an internationally advanced drug for the treatment of cardiovascular and cerebrovascular diseases. However, after becoming a monomeric drug, the problem that the lactone structure of ginkgolide B is hydrolyzed in the blood environment with a pH value of 7.4 in the body to cause failure is not considered. Secondly, the problem of low solubility of ginkgolide B in water and peroxidation in vivo has not been solved. Contents of the invention [0003] In order to solve the problems of existing ginkgolide B drug lactone structure hydrolysis in vivo, low solubility in water, peroxidation in vivo, and target lesions in vivo, the present invention provides a ginkgolide B nanoliposome drug. [0004] Technical scheme ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K9/127A61K9/10A61K9/12A61K9/19A61K47/40A61K47/24A61P9/10A61P9/12
Inventor 蔡海德
Owner 江苏仲德医药科技有限公司
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