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Hydroxycamptothecin liposome and its preparation

A technology of hydroxycamptothecin and hydroxycamptothecin, applied in the field of hydroxycamptothecin preparation and preparation thereof, can solve problems such as toxicity, and achieve the effects of reducing toxicity, prolonging time and increasing stability

Active Publication Date: 2005-02-23
HUNAN YINENG BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are literatures reporting the preparation method of hydroxycamptothecin and its physical and chemical performance parameters (Lei Yingjie, Wang Zuoquan, Liu Hong, etc. Preparation and mechanism of 10-hydroxycamptothecin, Shaanxi Chemical Industry, 1999, 28(4): 10) , the substance is a water-insoluble and fat-insoluble drug, and has certain toxicity, so its clinical application has been limited to a certain extent

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Dissolve 1.0 mg of hydroxycamptothecin, 100.0 mg of soybean lecithin, and 1.0 mg of cholesterol in 10 ml of ethanol to obtain solution A.

[0029] Film A was formed into a film by rotary evaporation in a water bath at 40°C to obtain film B.

[0030] Dissolve 200 mg of poloxamer in 5 ml of phosphate buffer at pH=6.8 to obtain solution C.

[0031] Add solution C to membrane B, refrigerate at below 4°C for 30 minutes to fully hydrate the membrane, and then vortex for 15 minutes to prepare the product.

[0032] Apply Sephadex column to separate liposome and unencapsulated free drug, add methanol to dissolve, take methanol solution and apply high performance liquid chromatography to measure peak area, substitute peak area into regression equation to find concentration, calculate encapsulation The sealing rate is 55.5%.

[0033] Take 1.0mg of the raw material, dilute to 50ml with methanol, take 1ml to 5ml, 10ml, 25ml, 50ml volumetric flasks respectively, dilute to the mark,...

Embodiment 2

[0038] Dissolve 1.0 mg of hydroxycamptothecin, 100.0 mg of soybean lecithin, 1.0 mg of cholesterol, and 5.0 mg of polyethylene glycol 4000 in 10 ml of ethanol to obtain solution A. Others are with embodiment 1.

Embodiment 3

[0040] Dissolve 10 mg of hydroxycamptothecin, 90 mg of phosphatidylcholine, and 10 mg of cholesterol in 10 ml of a mixture of ethanol and chloroform (1:1, volume ratio) to obtain solution A.

[0041] Film A was formed into a film by rotary evaporation in a water bath at 40°C to obtain film B.

[0042] Dissolve 200mg of Tween 80 in 5ml of pH=9 phosphate buffer to obtain solution C.

[0043] Add solution C to membrane B, refrigerate below -4°C for 30 minutes to fully hydrate the membrane, and then vortex and mix for 15 minutes to prepare the product.

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Abstract

A hydroxy camptothecin lipid used for preparing freeze-dried powder injection is prepared from hydroxy camptothecin, phosphatide or cholesterine through dissolving them in organic solvent, spinning evaporating at 40-70 deg.C to become film, adding the buffering liquid containing surfactant, cold storing for hydrating, and stirring.

Description

technical field [0001] The invention relates to a hydroxycamptothecin preparation and a preparation method thereof. Background technique [0002] Hydroxycamptothecin is the 10-hydroxyl derivative of camptothecin, which belongs to the same class of cellular anticancer drugs as camptothecin. In recent years, studies have also found that the target of hydroxycamptothecin is topoisomerase, which kills At the same time as cancer cells, it also affects normal cell metabolism. There are literatures reporting the preparation method of hydroxycamptothecin and its physical and chemical performance parameters (Lei Yingjie, Wang Zuoquan, Liu Hong, et al. Preparation and mechanism of 10-hydroxycamptothecin, Shaanxi Chemical Industry, 1999, 28(4): 10) , the substance is a water-insoluble and fat-insoluble drug, and has certain toxicity, so its clinical application has been limited to a certain extent. Therefore, how to improve the performance of hydroxycamptothecin has become one of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/475A61P35/00
Inventor 奉建芳张乐乐祝林芦洁
Owner HUNAN YINENG BIOLOGICAL PHARMA
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