Ginkgolide composition and application thereof

A technology of ginkgolide and composition, applied in the field of preparation of ginkgolide solid dispersion based on component structure and its dynamic quality control, capable of solving unscientific problems

Inactive Publication Date: 2013-08-28
JIANGSU KANION PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is unscientific to only use single-component ginkgolide B as the raw material for the production of ginkgo preparations

Method used

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  • Ginkgolide composition and application thereof
  • Ginkgolide composition and application thereof
  • Ginkgolide composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1 Determination of Equilibrium Solubility of Ginkgolide Composition in Water and PBS with Different pHs:

[0080] Preparation of the test solution: prepare phosphate buffered saline solutions with pHs of 2.0, 2.5, 5.0, 5.8, 6.5, 7.0, 7.4, 7.8-8.0, and take excess ginkgolide A: ginkgolide B weight ratio of 1: The ginkgolide composition of 2 is equally divided into 10 parts and placed in stoppered glass test tubes, and then water is added to one of the stoppered glass test tubes as a blank, and phosphates with different pH values ​​are added to the other stoppered glass test tubes. Buffered saline solution was sonicated until the drug was no longer dissolved to make a saturated solution of the ginkgolide composition, and then placed in a constant temperature shaker at a temperature of (37±1)°C and shaken for 24 h. Filter the saturated solution with a 0.45 μm microporous membrane, discard the initial filtrate, and take the subsequent filtrate as the test solution. ...

Embodiment 2

[0088] Example 2 Determination of the oil-water partition coefficient of the ginkgolide composition with ginkgolide A: ginkgolide B weight ratio of 1:2

[0089] Take an appropriate amount of ginkgolide composition and dissolve it in n-octanol saturated with water to make a n-octanol saturated solution of ginkgolide composition, and precisely draw the solution into ten 10 mL vials (2 mL / bottle ), add 2ml of n-octanol-saturated water into one of the vials as a blank, add 2 mL of phosphate buffer solution with different pH values ​​into the other vials, put them in an air shaker at 37 °C, and shake for 24 h Until the equilibrium, take the lower layer of water phase, at 6000 r min -1 Centrifugal 10 min, prepare reference substance solution according to the method for preparing reference substance solution described in Example 1 and chromatographic conditions and measure the concentration of ginkgolide composition C in n-octanol before distribution 0 and the concentration C of the...

Embodiment 3

[0095] Example 3 Preparation of Ginkgolide Solid Dispersion Based on Preferred Composition

[0096] Method: Using solvent method to select chitosan as solid dispersion carrier, firstly prepare ginkgolide A: ginkgolide B weight ratio of 1:2 ginkgolide composition and 3000, 5000, 50000, 100000 and more than 100000 The chitosan ratio is 1:5, comparing the influence of different molecular weights on the solubility of the ginkgolide composition, the optimal molecular weight chitosan carrier is preferred. Further optimize the weight ratio of the ginkgolide composition to the preferred chitosan carrier (1:5, 1:10, 1:15) to prepare the ginkgolide solid dispersion, and optimize the ginkgolide solid dispersion with the dissolution rate as the investigation index body prescription. see results Figure 3-5 .

[0097] Results: Compared with chitosan with other molecular weights, chitosan 3000 can improve the solubility of ginkgolide composition to the greatest extent, and the solid disp...

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Abstract

The present invention discloses a Ginkgolide composition and a method for the preparation thereof. The composition includes two active components, Ginkgolide A and Ginkgolide B, and the weight ratio of Ginkgolide A to Ginkgolide B is 1: (2-9). A strong synergistic effect is found between Ginkgolide A and Ginkgolide B, which has a remarkable application effect on the treatment of cardio-cerebral vascular disease. The invention realizes simultaneous determination for the component content of the Ginkgolides preparation. Experiments show that the Ginkgolide A and Ginkgolide B have the advantages of good separating degree with better linear relation, reproducibility, precision, stability, and recovery rate. The dosage form of the preparations provided by the present invention is beneficial for improving the bioavailability in vivo and drug efficacy.

Description

technical field [0001] The invention relates to a ginkgolide composition and its application, in particular to the preparation of a ginkgolide solid dispersion based on component structure and its dynamic quality control method. Background technique [0002] Ginkgo biloba is one of the ancient tree species in my country, and Ginkgoaceae has been used as a traditional Chinese medicine in my country for thousands of years. With the development of modern Chinese medicine preparations, ginkgolides have become important raw materials for the preparation of ginkgo preparations. The main active ingredients in total ginkgolides include ginkgolide A (GA), ginkgolide B (GB), ginkgolide C (GC) and bilobalide (BB), among which A content is the highest in natural ginkgo leaves , and the strongest pharmacological effect is ginkgolide B, which can selectively antagonize the platelet aggregation induced by platelet activating factor, and can effectively prevent platelet aggregation and thr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P9/00
Inventor 萧伟贾晓斌刘丹
Owner JIANGSU KANION PHARMA CO LTD
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