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Ginkgo flavone and lactone -cyclodextrin derivate inclusion complex and preparation method thereof

A technology of ginkgo ketone ester and cyclodextrin, which is applied in the field of ginkgo ketone ester-cyclodextrin derivative inclusion compound and its preparation, can solve the problems of low bioavailability, poor absorption of flavonoids and terpene lactones, etc., and achieve enhanced Solubility and Dissolution, Enhanced Absorption, Acceptable Effects

Inactive Publication Date: 2008-11-19
陈建海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention aims at the problems of low bioavailability, poor absorption of flavonoids and terpene lactones in existing common oral preparations of ginkgo ketone esters, and provides a ginkgo ketone ester-cyclodextrin derivative inclusion compound and a preparation method thereof

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of ginkgo ketone ester-β-cyclodextrin derivative inclusion capsule preparation is as follows: take 10g HP-βCD (hydroxypropyl-β-cyclodextrin) and dissolve it in water, sonicate for 30min, add 15g of ginkgo ketone ester, put On a magnetic heating stirrer, stir at 50°C for 6h, dry under reduced pressure and vacuum at 60°C, grind the solid to a particle size of 500um to 2000um, test the content of total flavonoids, and pack into hard capsules (the amount of total flavonol glycosides in each capsule The amount is not less than 19.2mg, and the terpene lactone is not less than 4.8mg). Through clinical verification, the absorption rate and bioavailability of the preparation of the invention are twice that of common preparations.

Embodiment 2

[0025] Ginkgo ketone ester-β-cyclodextrin derivative inclusion tablet is prepared as follows: take 10g of HP-βCD (hydroxypropyl-β-cyclodextrin) and dissolve it in water, add 15g of ginkgo ketone ester by ultrasonication for 30min, and place On a magnetic heating stirrer, stir at 50°C for 8 hours, dry under reduced pressure and vacuum at 55°C, grind with a solid grinder until the particle size is 200um-1000um, test the total flavonoid content, mix the above powder with 4-6% povidone (PVP ) ethanol liquid is made into soft material as binder, and granulated through a 24-mesh sieve. Dry at 50°C for 4 hours, pass through a 20-mesh sieve for granulation, add appropriate amount of magnesium stearate, mix well, and press into tablets (the amount of total flavonol glycosides in each tablet is not less than 19.2 mg, and the amount of terpene lactones is not less than 4.8 mg). mg). Through clinical verification, the absorption rate and bioavailability of the preparation of the inventio...

Embodiment 3

[0027] The preparation of ginkgo ketone ester-β cyclodextrin derivative inclusion granule is as follows: take 10g of HP-βCD (hydroxypropyl-β-cyclodextrin) and dissolve it in water, add 15g of ginkgo ketone ester by ultrasonication for 30min, and put On a magnetic heating stirrer, stir at 50°C for 7 hours, dry under reduced pressure at 65°C, grind with a solid grinder until the particle size is 200um-1000um, continue to grind to 150-250um, pass through a No. 4 sieve for classification, and then use hydroxypropyl Methylcellulose, polyethylene glycol, povidone, or a mixture thereof is coated, and some flavoring agents are added, divided into doses, and packaged. Through clinical verification, the absorption rate and bioavailability of the preparation of the invention are twice that of common preparations.

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Abstract

The invention discloses an extract of Ginkgo Biloba leaves-cyclodextrin derivative inclusion compound and a preparation method thereof, which is prepared from 10 to 24 percent of total flavonol glycoside, 2 to 6 percent of terpene lactone and 70 to 88 percent of cyclodextrin derivative and auxiliary materials, according to the weight percentage; the preparing method comprises the following steps: dissolving cyclodextrin derivative in water, adding extract of Ginkgo Biloba leaves; stirring for 6 to 8 hours; reducing the pressure and vacuum drying at the temperature of 55 to 65 DEG C; and obtaining the extract of Ginkgo Biloba leaves-cyclodextrin derivative inclusion compound in a solid grinding way. The invention adopts an inclusion technology to greatly enhance the dissolubility and the dissolution of the ginkgo leaves in the water, to enhance the absorption in human stomach and intestine, and to simultaneously greatly increase the stability of the principal components in the extract of Ginkgo Biloba leaves, the extract of Ginkgo Biloba leaves and terpene lactones after being processed by adopting the inclusion technology. The extract of Ginkgo Biloba leaves, after being processed by adopting the inclusion technology, is 1 to 2 times higher than the ordinary preparation in bioavailability, and can be used for preparing the drugs for improving the disease of cardio-cerebrovascular systems, and preventing and remedying coronary heart diseases.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine, and in particular relates to a ginkgo ketone ester-cyclodextrin derivative inclusion compound and a preparation method thereof. Background technique [0002] Ginkgo is a plant of the Ginkgo family and the genus Ginkgo. It has been used as a Chinese medicinal material for hundreds of years in my country. It has the functions of astringing exhaust gas, relieving asthma and cough, and relieving turbidity. The ingredients and pharmacological effects were revealed in the 1970s: Ginkgo biloba extract mainly contains active ingredients such as ginkgo flavonoid glycosides and terpenoid lactones, among which ginkgo flavonoid glycosides can scavenge oxygen free radicals, protect lipoprotein peroxidation, and reduce microvascular permeability Ginkgo terpene lactones A, B, C, D, J, especially B (code name BN52021) are strong antagonists of platelet activating factor (PAF), and have signifi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K31/365A61K36/16A61P9/10
Inventor 陈建海
Owner 陈建海
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