Liposome of 10-hydroxycamptothecine, and its prepn. method

A technology of hydroxycamptothecin and hydroxycamptothecin is applied in the field of 10-hydroxycamptothecin liposome and its preparation, and can solve the problems of limiting the clinical application of 10-hydroxycamptothecin, low anti-topoisomerase I activity, Leukopenia and other problems, to achieve the effects of good water solubility, improved efficacy, and improved stability

Inactive Publication Date: 2006-01-18
江苏省药物研究所有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the side effects of this drug are relatively large, mainly manifested as: bone marrow suppression, causing leukopenia, gastrointestinal reactions, urinary tract irritation, etc. These side effects limit the clinical application of 10-hydroxycamptothecin
And because of the water insolubility of 10-hydroxycamptothecin, the current clinical preparation is to use NaOH solution to adjust the pH to make the α-hydroxylactone ring in the structure open and dissolve, but the lactone ring is a functional group, which is formed after opening Drug carboxylate form exhibits very low anti-topoisomerase I activity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Total lipid (mg / ml)

Embodiment 2

[0025] Take 1.0 g of 10-hydroxycamptothecin, 20 g of refined lecithin and 2.0 g of cholesterol and put them in a round-bottomed flask, add chloroform to completely dissolve the above mixture into a clear solution, set it in a constant temperature water bath and dry under reduced pressure to form a film, add 2.0 g of gluten containing The aqueous solution of amino acid and 25 g of mannitol was used to dissolve the membrane, and ultrasonically pulverized with an ultrasonic instrument to obtain a 10-hydroxycamptothecin liposome solution.

Embodiment 3

[0027] Take 1.0 g of 10-hydroxycamptothecin, 80 g of purified lecithin and 5.0 g of cholesterol, and put them in a round-bottomed flask, add chloroform to completely dissolve the above mixture into a clear solution, set it in a constant temperature water bath and dry under reduced pressure to form a film, add 50 g of mannitol The aqueous solution dissolves the film, and ultrasonically pulverizes it with an ultrasonic instrument to obtain a 10-hydroxycamptothecin liposome solution.

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PUM

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Abstract

A 10-hydroxy camptothecine lipoid is disclosed, which has high anticancer function and curative effect and high water solubility and stability. Its preparing process is also disclosed, in which phosphatide and cholesterin are used as filming material, the chloroform, alcohol or ether is used as solvent, and the mannitol or glucose is used as the protectant for freeze drying.

Description

Technical field: [0001] The present invention relates to 10-hydroxycamptothecin liposome and its preparation method. Background of the Invention: [0002] Topoisomerase inhibitors are an important class of chemotherapeutic drugs for cancer treatment. These compounds have the effect of inhibiting the enzymatic activity of topoisomerase, and inhibiting topoisomerase involved in DNA replication, repair, genetic recombination and transcription. 10-Hydroxycamptothecin is a representative of topoisomerase inhibitors. 10-Hydroxycamptothecin is an alkaloid raised from the seeds or root bark of the deciduous plant Camptotheca, which is widely distributed in South my country is very rich in resources. At present, my country has successfully produced 10-hydroxycamptothecin through chemical synthesis and biological fermentation. According to statistics, botanical anti-tumor drugs have always been the leading category of anti-tumor clinical drugs. 10-Hydroxycamptothecin and its analogs ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/475A61K9/127A61P35/00
Inventor 周卫
Owner 江苏省药物研究所有限公司
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