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Toad venom alcohol plastid and preparation method thereof

A technology of bufalinol and plastid, applied in the field of bufalin plastid and preparation thereof, can solve the problems of phospholipid being difficult to purify, easily oxidized and deteriorated, not stable enough, etc., and achieves the effects of easy industrialized production, great promotion value, and product stability.

Active Publication Date: 2009-11-11
BEIJING INCREASEPHARM SAFETY & EFFICACY CO 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
[0004] There have been reports of liposomes made from the fat-soluble components of Bufoni, but they are not stable enough

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Dissolve 20 mg of hydrogenated soybean lecithin and 1 mg of toad venom extract in 20 ml of ethanol and dissolve the solution for later use; take another 20 ml of phosphate buffer (pH 7.0) and add the above ethanol solution dropwise at a constant speed at 40°C while stirring. Then continue to stir for 30 minutes and filter with 0.22μm microporous membrane to obtain.

Embodiment 2

[0020] Take 120mg of hydrogenated soy lecithin, 60mg of cholesterol, 60mg of dicetyl phosphate, 60mg of phosphatidylamide, and 10mg of toad venom extract dissolved in 50ml of ethanol. The solution is ready for use; another 80ml of phosphate buffer (pH7.0) is taken at 30°C Under constant temperature and stirring, add the above ethanol solution dropwise at a constant speed, continue to stir after the addition, and filter with a 0.22 μm microporous membrane to obtain.

Embodiment 3

[0022] Take 60 mg of soy lecithin and 4 mg of toad venom extract dissolved in 20 ml of ether, evaporate on a rotary evaporator at 35 ℃ to a dry film, then add 30 ml of phosphate buffer (pH 7.0), and add ethanol to make the ethanol concentration at 35% , 40 ℃ constant temperature hydration for 30 minutes, ultrasonic treatment for 10 minutes, 0.22μm microporous membrane filtration, it is ready.

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PUM

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Abstract

The invention relates to toad venom alcohol plastid and a preparation method thereof. The preparation method adopts a novel preparation technique to prepare a phospholipids vesicle vector containing ethanol with high concentration capable of reaching 20 to 50 percent. The plastid having the advantage of good stability is a novel preparation easy to industrialize.

Description

Technical field [0001] The invention relates to toad venom alcohol plastids and a preparation method thereof. Background technique [0002] Liposomes are unilamellar or multilamellar vesicles composed of phospholipid bilayers. They are the most studied targeted drug carriers. They are mostly used in anti-tumor drugs and anti-leishmaniasis antimony preparations, which can significantly reduce drug toxicity and Stay active for longer. However, the performance of liposomes has shortcomings: ①Due to its chemical instability, preparation and storage are difficult, the drug encapsulation rate is not high, leakage is easy to occur, and the targeting property is lost. ②The phospholipids used as raw materials are difficult to purify, and are easy to oxidize and deteriorate, which reduces the fluidity of the membrane and leads to the leakage of the wrapped drug. ③The purified phospholipid has a high price. Therefore, people have extensively studied the carrier with a certain chemical compo...

Claims

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Application Information

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IPC IPC(8): A61K35/56A61K9/127A61K47/24A61K35/65
Inventor 张卫华胡克菲
Owner BEIJING INCREASEPHARM SAFETY & EFFICACY CO LTD
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