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A kind of ginkgo damole liposome pharmaceutical preparation and preparation method thereof

A technology of pharmaceutical preparations and damolipid, applied in the field of medicine, can solve the problems of limited physical and chemical properties and pharmacokinetic characteristics, low bioavailability of preparations, and difficulty in obtaining curative effects, etc., to achieve improved bioavailability, improved therapeutic effect, The effect of prolonging the residence time

Active Publication Date: 2017-12-12
GUIZHOU YIBAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, since the main active ingredients of Ginkgo biloba extract, total ginkgo flavonoids, total ginkgo lactones and dipyridamole are insoluble in water, and are limited by the physical and chemical properties and pharmacokinetic characteristics of the main active ingredients of Ginkgo biloba extract, its The active ingredients and their phase II metabolites are easily effluxed by efflux transfer proteins such as P-gp, MRP-2, BCRP, etc., resulting in low bioavailability, poor stability, and large and complicated side effects of the preparation, so it is difficult to treat diseases achieve satisfactory results

Method used

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  • A kind of ginkgo damole liposome pharmaceutical preparation and preparation method thereof
  • A kind of ginkgo damole liposome pharmaceutical preparation and preparation method thereof
  • A kind of ginkgo damole liposome pharmaceutical preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0039] Embodiment 1 Ginkgo Damole liposome preparation

[0040] Preparation prescription: Ginkgo biloba extract 4.0g, dipyridamole 0.4g, dimyristoyl lecithin 18.0g, distearoylphosphatidylcholine 6.0g, cholesterol 3.0g, sucrose ester 2.0g;

[0041]Preparation method: Using film hydration-high pressure homogenization method, 4.0g of Ginkgo biloba extract, 0.4g of dipyridamole, 18.0g of dimyristoyl lecithin, 6.0g of distearoylphosphatidylcholine, and 3.0g of cholesterol g and sucrose ester 2.0 in an eggplant-shaped bottle, add 300ml of a 1:3 mixture of absolute ethanol-dichloromethane to dissolve it, place it in a rotary evaporation at 40°C until a film is formed, dry it under reduced pressure overnight, and add pH=6.5 PBS phosphate buffer solution was hydrated at room temperature, and the resulting milky white suspension was homogenized by a high-pressure homogenizer with a homogenization pressure of 15,000 psi, circulated 3 times, and dried to obtain Ginkgo Damole liposomes.

Embodiment 2

[0042] Embodiment 2 ginkgo damo liposome preparation

[0043] Preparation prescription: Ginkgo biloba extract 4, dipyridamole 0.4g, soybean lecithin 24.0g, distearoylphosphatidylcholine 8.0g, cholesterol 4.0g, sucrose ester 3.5g;

[0044] Preparation method: Using film hydration-high pressure homogenization method, 4.0g of Ginkgo biloba extract, 0.4g of dipyridamole, 24.0g of dimyristoyl lecithin, 8.0g of distearoylphosphatidylcholine, and 4.0g of cholesterol g and sucrose ester 3.5 are placed in an eggplant-shaped bottle, add 400ml of a 1:3 mixture of absolute ethanol-dichloromethane to dissolve it, place it in a rotary evaporation at 40°C until a film is formed, dry it under reduced pressure overnight, and add pH=6.5 PBS phosphate buffer solution was hydrated at room temperature, and the resulting milky white suspension was homogenized by a high-pressure homogenizer with a homogenization pressure of 15,000 psi, circulated 3 times, and dried to obtain Ginkgo Damole liposomes....

Embodiment 3

[0045] Embodiment 3 ginkgo damo liposome preparation

[0046] Preparation prescription: Ginkgo biloba extract: 4.0, dipyridamole: 0.4g, dimyristoyl lecithin: 30.0g, distearoylphosphatidylcholine: 10.0g, cholesterol: 5.0g, sucrose ester: 5.0g ;

[0047] Preparation method: using film hydration-high pressure homogenization method, 4.0g of ginkgo biloba extract, 0.5g of dipyridamole, 30.0g of soybean lecithin, 10.0g of distearoylphosphatidylcholine, 5.0g of cholesterol and sucrose ester Put 5.0g in an eggplant-shaped bottle, add 400ml of 1:3 absolute ethanol-dichloromethane mixture to dissolve it, put it in a rotary evaporation at 40°C to form a film, dry it under reduced pressure overnight, add PBS phosphoric acid with pH=6.5 The salt buffer solution was hydrated at room temperature, and the obtained milky white suspension was homogenized by a high-pressure homogenizer at a homogenization pressure of 15,000 psi, circulated 3 times, and dried to obtain Ginkgo Damole liposomes. ...

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Abstract

The invention discloses a ginkgo damole liposome pharmaceutical preparation, which comprises 40 parts of ginkgo leaf extract, 4 parts of dipyridamole, 180-300 parts of dimyristoyl lecithin, distearoyl It is made of 60-100 parts of phosphatidylcholine, 30-50 parts of cholesterol, 20-50 parts of sucrose ester and other preparation auxiliary materials. The ginkgo damole liposome pharmaceutical preparation of the present invention can not only improve the storage stability of the pharmaceutical preparation, but also enable the sustained release of the medicine in the liposome, prolong the residence time of the medicine in the blood circulation, improve the bioavailability of the medicine, and achieve Efficient and long-acting therapeutic purposes.

Description

Technical field: [0001] The invention belongs to the field of medicine, and relates to a pharmaceutical preparation and a preparation method thereof, in particular to a ginkgo damole liposome pharmaceutical preparation and a preparation method thereof. Background technique: [0002] Ginkgo biloba has the functions of improving cardiovascular and cerebrovascular circulation, improving memory, scavenging free radicals, and delaying aging. It has dual effects of treatment and health care. The injection prepared from Ginkgo biloba has been used clinically for many years and has achieved good results. Ginkgo biloba extract has complex components, the main active ingredients are total flavonol glycosides and total ginkgo lactones, among which the total flavonol glycosides are mainly composed of ketoglycosides such as quercetin, kaempferol and isorhamnetin and monosaccharides such as glucose The composition of glycosides connected by oxygen glycosidic bonds has the functions of di...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K36/16A61K47/28A61P9/10
Inventor 窦啟玲
Owner GUIZHOU YIBAI PHARMA CO LTD
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