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Strychnos alkaloid vesicle and preparation method thereof

A strychnine and alkaloid technology, applied in the directions of capsule delivery, microcapsules, and drug combination, can solve the problems of difficulty in purifying phospholipids, high cost, and limited clinical application, and achieve easy industrial production, low cost, and great promotion value. Effect

Inactive Publication Date: 2009-11-11
BEIJING INCREASEPHARM CORP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are disadvantages in the performance of liposomes: ①Due to its chemical instability, it is difficult to prepare and store, and the drug encapsulation rate is not high and it is prone to leakage and loss of targeting
② The phospholipids used as raw materials are difficult to purify, and are easily oxidized and deteriorated to reduce membrane fluidity and cause leakage of encapsulated drugs
Pharmacological studies have proved that the alkaloids in Nyx nuxica are active ingredients, but the therapeutic window is extremely narrow, the therapeutic dose is close to the poisoning dose, and the clinical application is greatly limited
[0004] There have been patent reports of strychnine liposomes and nano strychnine liposomes, but traditional liposomes are expensive and unstable due to their inherent shortcomings

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve 20600mg of Span, 100mg of cholesterol, and 10mg of strychnine in 200ml of ether, ultrasonically dissolve, and prepare the solution for later use; another 500ml of phosphate buffer (pH7.0) is added dropwise at a constant temperature of 40°C with stirring. After the solution is added, continue to stir until the ether is evaporated, add phosphate buffer to 800ml, pass through a high-pressure homogenizer for 1-3 times, and filter through a 0.22μm microporous membrane to obtain the solution.

Embodiment 2

[0029] Take 1500mg of Span 60, 1000mg of cholesterol and 400mg of strychnine and dissolve them in 1500ml of chloroform, heat to dissolve, and prepare the solution for later use; take another phosphate buffer (pH7.0), and add the above chloroform solution dropwise at a constant temperature at 60°C while stirring After the addition, continue to stir until the chloroform is evaporated, add phosphate buffer to 3000ml, sonicate, and filter at 0.22μm to obtain.

Embodiment 3

[0031] Dissolve 4050 mg of Span, 50 mg of cholesterol, 1000 mg of polyethylene glycol-polylactic acid, and 11 mg of total alkaloids of Nuxychnium chinensis in 1000 ml of ethanol. On a rotary evaporator, vacuum evaporate to a dry film at 30° C., and then add phosphate buffer ( pH7.0) 1200ml, ultrasonically treated for 15min, and filtered through a 0.22μm microporous membrane.

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PUM

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Abstract

The invention relates to a strychnos alkaloid vesicle and a preparation method thereof. The preparation method comprises the following steps: taking non-ionic surfactant span, Tween, single (double) alkyl polyglycerol ether, polyoxyethylene alkyl ether and the like as vesicle materials, and adding cholesterol, dicetyl phosphate and the like as stabilizers to prepare a novel targeting preparation with excellent preparation stability and easiness for industrialization.

Description

technical field [0001] The invention relates to a strychnium alkaloid vesicle and a preparation method thereof. Background technique [0002] Liposomes are unicellular or multicellular vesicles composed of phospholipid bilayers. They are the most studied targeted drug carriers and are mostly used in antineoplastic agents and anti-leishmaniasis antimony preparations, which can significantly reduce drug toxicity and Stay active for longer. However, there are disadvantages in the performance of liposomes: 1. Due to its chemical instability, it is difficult to prepare and store, and the drug encapsulation rate is not high and it is prone to leakage and loses targeting. ② The phospholipids used as raw materials are difficult to purify, and are easily oxidized and deteriorated to reduce membrane fluidity and cause leakage of encapsulated drugs. ③Purified phospholipids are expensive. Therefore, people have extensively studied the carrier with definite chemical composition, relat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/56A61K9/50A61K47/28A61K47/34A61K47/36A61K31/475A61P29/00A61P25/00A61P19/02A61P17/02A61K131/00A61K47/10A61K47/14A61K47/24A61K47/26
Inventor 张卫华张永丽
Owner BEIJING INCREASEPHARM CORP LTD
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