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Liposome of 10-hydroxycamptothecine, and its prepn. method

A technology of hydroxycamptothecin and hydroxycamptothecin, which is applied in the field of 10-hydroxycamptothecin liposome and its preparation, can solve the problems of limiting the clinical application of 10-hydroxycamptothecin, low anti-topoisomerase I activity, Eliminate leukopenia and other problems, achieve good water solubility, improve drug efficacy, and improve stability

Inactive Publication Date: 2004-10-20
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 1.0g of 10-hydroxycamptothecin, 20g of refined lecithin and 2.0g of cholesterol in a round bottom flask, add chloroform to completely dissolve the above mixture into a clear solution, put it in a constant temperature water bath and dry it under reduced pressure to form a film, add 2.0g of gluten Aqueous solution of amino acid and 25g mannitol dissolves the film, and ultrasonically pulverizes with an ultrasonic instrument to obtain a 10-hydroxycamptothecin liposome solution.

Embodiment 3

[0027] Take 1.0g of 10-hydroxycamptothecin, 80g of refined lecithin and 5.0g of cholesterol and put them in a round bottom flask, add chloroform to completely dissolve the above mixture into a clear solution, put it in a constant temperature water bath to dry under reduced pressure to form a film, add 50g of mannitol The aqueous solution dissolves the film, and ultrasonically pulverizes 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 invention relates to 10-hydroxycamptothecin liposome and a preparation method thereof. Background of the invention: [0002] Topoisomerase inhibitors are an important class of chemotherapeutic drugs for cancer treatment. These compounds can inhibit the enzymatic activity of topoisomerase, and inhibit topoisomerase from participating in DNA replication, repair, genetic recombination and transcription. 10-Hydroxycamptothecin is a representative of topoisomerase inhibitors. 10-Hydroxycamptothecin is an alkaloid that is proposed from the seeds or root bark of the deciduous plant Camptothecin in the Davidiaceae family. Camptothecin is widely distributed in South my country is rich in resources. At present, my country has successfully produced 10-hydroxycamptothecin through chemical synthesis and biological fermentation. According to statistics, plant-based antineoplastic drugs have always been the leading class of anti-tumor clinical drugs. 10-Hydroxy...

Claims

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Application Information

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