Unlock instant, AI-driven research and patent intelligence for your innovation.

Ginkgolide lipidosome injection

A technology of ginkgolide and liposome, applied in the field of medicine, can solve the problems of low solubility of ginkgolide, poor stability, low toxicity and irritation, etc., so as to improve the quality of preparation products, improve bioavailability, The effect of good formulation stability

Inactive Publication Date: 2014-04-16
海南路易丹尼生物科技有限公司
View PDF10 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN1594319A discloses a ginkgolide extraction process and ginkgolide injection and its preparation method, the injection is a sterilized aqueous solution prepared by compatibilizing hydroxypropyl-β-cyclodextrin, and then adding A certain amount of isotonic regulator and chelating agent, although the inclusion technology is used to increase the dissolution, however, due to the relatively small amount of inclusion and chelating agent, the inclusion rate is not high, and the stability is not good enough
CN1813825A and CN1830981A disclose a kind of ginkgolide emulsion for injection and preparation method thereof, it is prepared by conventional emulsifier preparation method, comprises ginkgolide, injection oil, emulsifier and isotonic regulator composition, However, the stability of the emulsion is not good enough, the amount of vegetable oil is too much, and the bioavailability is low
The freeze-dried powder injection is prepared from mannitol disodium edetate (calcium), sodium metabisulfite, sodium hydroxide, and citric acid. Since ginkgolides are insoluble, the reconstitution of the freeze-dried powder injection is not good enough , the bioavailability of the drug is not high
CN1686111A discloses a ginkgolide injection for injection and its preparation method. The injection is also a freeze-dried powder injection prepared by adding certain cosolvents and excipients. low
The technical problems and standards to be solved by oral liposomes and ginkgolide liposome injections are incomparable. The present invention aims to overcome the problems that the ginkgolides of the above-mentioned injections have little solubility in water and the problems of peroxidation in the body and lactone To solve the problem that the structure is easily hydrolyzed and ring-opened, a ginkgolide liposome injection is provided, the ginkgolide does not open the ring, the toxicity and irritation are small, and the drug effect time is long

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Ginkgolide lipidosome injection
  • Ginkgolide lipidosome injection
  • Ginkgolide lipidosome injection

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0064] On the other hand, the present invention also provides a preparation method of ginkgolide liposome injection, specifically comprising the following preparation steps:

[0065] (1) Under nitrogen protection, dissolve cholesteryl succinate, distearoylphosphatidylethanolamine, soybean phosphatidylinositol, poloxamer 188, and ginkgolide in an organic solvent, stir to dissolve; The above solution is placed in an eggplant-shaped bottle, and the organic solvent is removed under reduced pressure in a water bath at 45°C to form a uniform transparent film on the wall of the bottle;

[0066] (2) Under the protection of nitrogen, add buffered saline solution into the bottle and stir to elute the phospholipid membrane and fully swell and hydrate. After the hydration is complete, do gradient homogenization at 600bar to 800bar for 4 to 6 times, preferably 5 times, 0.22μm Microporous membrane filtration to obtain ginkgolide liposomes;

[0067] (3) Under sterile conditions, add trehalo...

Embodiment 1

[0077] The preparation of embodiment 1 ginkgolide liposome injection

[0078] The ingredients used and their weights are as follows (1000 count):

[0079]

[0080] Ginkgolide liposome injection is prepared by preparation process:

[0081] (1) Under nitrogen protection, dissolve 30g cholesterol succinate, 200g distearoylphosphatidylethanolamine, 20g soybean phosphatidylinositol, 30g poloxamer 188, and 10g ginkgolide in 1000ml volume ratio of 1 : 1 in the mixed organic solvent of ethanol and tert-butanol, stir to make it dissolve; Place the above solution in an eggplant-shaped bottle, remove the organic solvent under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the bottle wall;

[0082] (2) Under the protection of nitrogen, add 5000ml of phosphate buffer solution with a pH of 6.8 to the bottle, stir to elute the phospholipid film and fully swell and hydrate it. μm microporous membrane filtration to obtain ginkgolide liposomes;

[0083]...

Embodiment 2

[0084] The preparation of embodiment 2 ginkgolide liposome injection

[0085] The ingredients used and their weights are as follows (1000 count):

[0086]

[0087]

[0088] Ginkgolide liposome injection is prepared by preparation process:

[0089] (1) Under nitrogen protection, dissolve 55g cholesterol succinate, 360g distearoylphosphatidylethanolamine, 35g soybean phosphatidylinositol, 50g poloxamer 188, and 10g ginkgolide in 1500ml volume ratio of 1 : 1 in the mixed organic solvent of ethanol and tert-butanol, stir to make it dissolve; Place the above solution in an eggplant-shaped bottle, remove the organic solvent under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the bottle wall;

[0090] (2) Under the protection of nitrogen, add 8000ml of phosphate buffer solution with a pH of 6.8 to the bottle, stir to elute the phospholipid film and fully swell and hydrate it. μm microporous membrane filtration to obtain ginkgolide liposome...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses ginkgolide lipidosome injection and a preparation method thereof. The lipidosome injection is prepared by ginkgolide, cholesteryl hydrogen succinate, soyabean phosphatidylinositol, DSPE (distearoyl phosphatidyl ethanolamine), trehalose and poloxamer 188. The provided lipidosome injection has small and even particle sizes; ring opening of the ginkgolide of the injection is avoided; the toxic reaction is reduced; the irritation is small; and the efficacy time is prolonged.

Description

technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a ginkgolide liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the most serious diseases threatening human beings in the world today. Its morbidity and mortality have surpassed tumor diseases and ranked first in the world. With the improvement of people's living standards, the acceleration of population aging, the acceleration of the pace of life, and the development of eating habits towards high fever and hyperlipidemia, many factors have caused diseases such as coronary heart disease, high blood pressure, and hyperlipidemia to become the most serious diseases that threaten human health. , and its morbidity and mortality are increasing year by year. [0003] Ginkgo biloba extract and its preparations have been widely used i...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K36/16A61K31/365A61K47/36A61K47/28A61K47/24A61P9/00
Inventor 王平
Owner 海南路易丹尼生物科技有限公司