Podophyllotoxin vesicle and preparation method thereof

A technology of podophyllotoxin and vesicles, applied in antiviral agents, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of high cost, easy oxidation and deterioration, difficult purification of phospholipids, etc., and achieve low cost and large scale Promote the value, the effect of easy industrial production

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
In addition, the ineffectiveness of latent infection is an important reason for its high recurrence rate
There have been patent reports such as podophyllotoxin 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

[0017] Dissolve 20 50 mg of Span, 50 mg of cholesterol, and 10 mg of podophyllotoxin in 50 ml of ether for later use; take another 130 ml of phosphate buffer, add the above ether solution dropwise at a constant temperature at 35°C while stirring, and continue stirring after the addition is complete , until the diethyl ether is evaporated, sonicated for 10 minutes, filtered through a 0.22 μm microporous membrane, and obtained.

Embodiment 2

[0019] Dissolve 1200mg of Span 40, 1000mg of dicetyl phosphate, and 100mg of podophyllotoxin in 260ml of chloroform, heat to dissolve, and prepare the solution for later use; another 800ml of ammonium sulfate buffer solution (350mmol / L) is mixed at a constant temperature of 40°C with stirring. Add the above chloroform solution dropwise, continue to stir until the chloroform is completely evaporated, pass through a high-pressure homogenizer twice, and filter through a 0.22 μm microporous membrane to obtain the product.

Embodiment 3

[0021] Dissolve 60 500 mg of Span, 600 mg of cholesterol, and 20 mg of podophyllotoxin in 200 ml of chloroform, evaporate in vacuum at 40°C on a rotary evaporator to a dry film, then add 400 ml of phosphate buffer (pH7.0), and sonicate for 10 min, 0.22 μm microporous membrane filtration, that is.

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PUM

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Abstract

The invention relates to a podophyllotoxin vesicle and a preparation method thereof. The preparation method takes a non-ionic surfactant and modification lipids as vesicle materials, and adds cholesterol, dicetyl phosphate and the like as stabilizers. The vesicle having the advantage of good preparation stability is a novel preparation easy to industrialize.

Description

technical field [0001] The invention relates to podophyllotoxin vesicles 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, relatively...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/365A61P31/12A61P35/00
Inventor 张卫华郑清娉
Owner BEIJING INCREASEPHARM CORP LTD
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