Method for solubilization and synchronous dissolution of bilobalide

A ginkgolide and prescription technology, which is applied in the field of solubilization and simultaneous dissolution of ginkgolide, can solve the problems of poor solubility and hinder drug efficacy, and achieve the effects of improving bioavailability, high degree of automation, and simple preparation process

Inactive Publication Date: 2013-05-15
FUDAN UNIV
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  • Abstract
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  • Application Information

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Problems solved by technology

However, studies have shown that the effective part of ginkgolide has poor solubility, which will hinder the performance of the drug, and the physicochemical properties of each component have obvious differences (such as the solubility of ginkgolide A, B, C and bilobalide are respectively 261.3± 9.9, 69.5±1.2, 481.8±20.6, and 1389.7±42.9μg / mL), while the curative effect of traditional Chinese medicine preparations is the result of the joint action of multiple components. purpose, in order to be consistent with the law of compatibility of medicines that physicians of all dynasties valued

Method used

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  • Method for solubilization and synchronous dissolution of bilobalide
  • Method for solubilization and synchronous dissolution of bilobalide
  • Method for solubilization and synchronous dissolution of bilobalide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Prescription: Ginkgolide 1g

[0031] Polyvinyl acetate-povidone blend 9g

[0032] Preparation process: uniformly mix the prescribed amount of medicine and polyvinyl acetate-povidone mixture, and prepare a solid dispersion with a hot-melt extruder at a temperature of 160-170° C. and a screw speed of 30 rpm. After cooling, pulverize and pass through a 60-mesh sieve to obtain the ginkgolide solid dispersion.

Embodiment 2

[0034] Prescription: Ginkgolide 1g

[0035] Copovidone 12g

[0036] Preparation process: uniformly mix the prescribed amount of medicine and copovidone, and prepare a solid dispersion with a hot-melt extruder at a temperature of 120-130° C. and a screw speed of 30 rpm. After cooling, pulverize and pass through a 60-mesh sieve to obtain the ginkgolide solid dispersion.

Embodiment 3

[0038] Prescription: Ginkgolide 1g

[0039] Soluplus 5g

[0040] Preparation process: Mix the prescribed amount of medicine and Soluplus evenly, and prepare a solid dispersion with a hot-melt extruder at a temperature of 120-130° C. and a screw speed of 30 rpm. After cooling, pulverize and pass through a 60-mesh sieve to obtain the ginkgolide solid dispersion.

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Abstract

The invention belongs to the technical field of traditional Chinese medicine, and in particular relates to a method for solubilization and synchronous dissolution of bilobalide. The invention achieves solubilization and synchronous dissolution of bilobalide through a solid dispersion technology, a clathrate compound technology or a micronization technology. A bilobalide solid dispersion is prepared by a metlt extrusion method and a grinding method; a bilobalide clathrate compound is prepared by a grinding method, a saturated water solution method, a freeze drying method and a spray drying method; and a drug is subjected to micronization by using high-speed grinding. The method provided by the invention can substantially improve solubility of the bilobalide, speed up dissolution of the bilobalide, improve dissolution synchronization of effective components in the bilobalide, improve the bioavailability of the drug, and lay foundation for follow-up study of oral preparation.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicines, in particular to a method for solubilizing and synchronously dissolving ginkgolides. Background technique [0002] Ginkgo biloba L. is one of the oldest rare tree species in the world. Ginkgo biloba is the dry leaf of Ginkgo biloba. Traditional Chinese medicine believes that the nature and flavor of ginkgo leaves are sweet, bitter, astringent and flat. GUIXIN, lung meridian. It has the functions of astringing the lung, relieving asthma, promoting blood circulation and removing blood stasis, and relieving pain. Traditional Chinese medicine is mainly used to treat cough and asthma due to lung deficiency, coronary heart disease, angina pectoris, hyperlipidemia and other diseases. In the late 1980s, Germany, France and other countries successively developed various preparations of Ginkgo biloba extract (GbE), and its sales volume in Europe and America ranked first among herb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K9/14A61P9/00
Inventor 韩丽妹王建新马琳怡张琴张林
Owner FUDAN UNIV
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