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Ginkgolide B lipid microsphere injection

A technology of ginkgolide and lipid microspheres, applied in the field of medicine, can solve the problems of easy aggregation, fusion, poor release controllability of lipid microsphere injection, leakage of encapsulated drugs, etc. The effect of low leak rates

Inactive Publication Date: 2013-04-17
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The stability of liposphere injections has been an important problem that has limited its application for a long time. Liposphere injections are generally prone to aggregation and fusion, resulting in leakage of encapsulated drugs, and the release of liposphere injections is poorly controlled. Therefore, the pharmaceutical field has general experience The technicians clearly know that there are various technical difficulties in the preparation of liposphere injections, which are by no means expected to be solved by existing theories, and many technical difficulties need to be overcome

Method used

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  • Ginkgolide B lipid microsphere injection
  • Ginkgolide B lipid microsphere injection
  • Ginkgolide B lipid microsphere injection

Examples

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preparation example Construction

[0063] On the other hand, the present invention also provides a preparation method of ginkgolide B lipid microsphere injection, specifically comprising the following preparation steps:

[0064] (1) Dissolve dioleoylphosphatidylethanolamine, distearoylphosphatidylglycerol and ginkgolide B in an appropriate amount of solvent under nitrogen protection, and stir magnetically at about 50°C for 1-2 hours to obtain ginkgo biloba Ester B lipid solution; the above-mentioned phospholipid solution is filtered with a 0.45 μm microporous membrane, and the filtrate is freeze-dried until it is completely dry to obtain a loose ginkgolide B solid;

[0065](2) Dissolve PEG400 and polyoxyethylene 40 hydrogenated castor oil in an appropriate amount of buffered saline solution, stir evenly at 500-800 rpm, and add the above-mentioned ginkgolide B solid under continuous stirring at 60°C to obtain a uniform suspension liquid, and then transferred to a high-speed homogenizer for gradient homogenizatio...

Embodiment 1

[0073] The preparation of embodiment 1 ginkgolide B lipid microsphere injection

[0074] The ingredients used and their weights are as follows (1000 count):

[0075]

[0076] Ginkgolide B lipid microsphere injection was prepared by preparation process:

[0077] (1) Under nitrogen protection, dissolve 100g of dioleoylphosphatidylethanolamine, 20g of distearoylphosphatidylglycerol and 10g of ginkgolide B in 300ml of a mixed solvent of ethanol and tert-butanol with a volume ratio of 2:3 Ginkgolide B lipid solution was obtained under magnetic stirring at 50°C for 1 hour; the above-mentioned phospholipid solution was filtered through a 0.45 μm microporous membrane, and the filtrate was pre-frozen at -60°C for 2 hours, and then - Freezing at 40°C for 6 hours, then sublimating to 20°C for 18 hours, and finally drying at 30°C for 1 hour to obtain loose ginkgolide B solid;

[0078] (2) Dissolve 30g of PEG400 and 25g of polyoxyethylene 40 hydrogenated castor oil in 3000ml of phos...

Embodiment 2

[0080] Preparation of Example 2 Ginkgolide B Lipid Microsphere Injection

[0081] The ingredients used and their weights are as follows (1000 count):

[0082]

[0083] Ginkgolide B lipid microsphere injection was prepared by preparation process:

[0084] (1) Under nitrogen protection, dissolve 250g of dioleoylphosphatidylethanolamine, 50g of distearoylphosphatidylglycerol and 10g of ginkgolide B in 600ml of a mixed solvent of ethanol and tert-butanol with a volume ratio of 2:3 Ginkgolide B lipid solution was obtained by magnetic stirring at 50°C for 1.5 hours; the above-mentioned phospholipid solution was filtered through a 0.45 μm microporous membrane, and the filtrate was pre-frozen at -65°C for 2.5 hours, and then - Freezing at 45°C for 7 hours, then sublimating to 23°C for 20 hours, and finally drying at 32°C for 2 hours to obtain loose ginkgolide B solid;

[0085] (2) Dissolve 45g of PEG400 and 63g of polyoxyethylene 40 hydrogenated castor oil in 5000ml of phosphat...

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Abstract

The invention discloses ginkgolide B lipid microsphere injection and a preparation method thereof. The lipid microsphere injection is prepared by ginkgolide B, DOPE (dioleoyl phosphatidyl ethanolamine), polyoxyl (40) hydrogenated castor oil, distearoyl phosphatidyl glycerol and PEG (polyethylene glycol) 400 in a specific weight ratio. The lipid microsphere injection has the advantages of even microsphere particle sizes, good stability and entrapment efficiency, and very low leakage rate; the problems that the ginkgolide B is easy to overoxidize and is prone to hydrolysis failure in vivo are solved; and the preparation method is good in reproducibility and suitable for industrialized production.

Description

technical field [0001] The invention relates to a lipid microsphere injection and a preparation method thereof, in particular to a ginkgolide B lipid microsphere injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] With the development of Ginkgo biloba research, it has been confirmed that the active ingredients of Ginkgo biloba are mainly flavonoids and lactones. Ginkgolide is a kind of important component with special structure and significant pharmacological activity found only in Ginkgo biloba, and has not been found to exist in any other plants so far. More importantly, they have unique pharmacological effects and therapeutic value. Ginkgolide compounds include: Ginkgolide A, Ginkgolide B, Ginkgolide C, Ginkgolide M, Ginkgolide J and Bilobalide. It has been proved that Ginkgolides are strong platelet activating factor receptor antagonists. agent. With the clarification of the active ingredients in Gink...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/365A61K47/44A61K47/34A61K47/24A61P9/02A61P17/02A61P9/10A61P37/08A61P7/08A61P11/06
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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