Irinotecan preparation

A technology for irinotecan preparations, which is applied in the field of irinotecan preparations and pharmaceutical compositions containing the preparations, can solve the problems of maintaining SN-38 concentration and difficulty in stabilization, so as to improve the stability of preparations and improve blood retention sexual effect
CN1960729AInactive Publication Date: 2007-05-09TERUMO KK +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TERUMO KK
Publication Date
2007-05-09
Estimated Expiration
Not applicable · inactive patent

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Abstract

An irinotecan preparation having irinotecan and / or a salt thereof highly carried by a closed vesicle carrier, which exhibits a strikingly prolonged retention in blood as compared with that of conventional irinotecan liposome preparations and is capable of being present in blood for a prolonged period of time. There is provided an irinotecan preparation comprising closed vesicles formed of a lipid membrane wherein irinotecan and / or a salt thereof is sealed in a concentration of at least 0.07 mol / mol (medicine mol / total membrane lipid mol). The irinotecan preparation preferably has an ion gradient between an inner water phase and an outer water phase within the closed vesicles. The closed vesicles are preferably liposomes, and the liposomes preferably have only the external surface thereof modified with a surface modifier containing a hydrophilic polymer.
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Description

Technical field

[0001] The present invention relates to an irinotecan preparation which is highly loaded with irinotecan and / or its salt in a closed vesicle carrier and a pharmaceutical composition containing the preparation. Background technique

[0002] Topoisomerase inhibitors are a class of drugs used in cancer treatment, such as camptothecin. Camptothecin is a pentacyclic alkaloid extracted and isolated from a Chinese native plant: Camptotheca acuminata by Wall and others in the United States in 1966. It has high anti-tumor activity and a broad anti-tumor spectrum. Patent Document 1). Existing cancer chemotherapy agents show anti-tumor activity by inhibiting type II topoisomerase, and camptothecin inhibits type I topoisomerase to inhibit topoisomerism that plays a role in DNA replication, repair, gene recombination and transcription The role of enzymes.

[0003] However, camptothecin has some problems in its use as a medicine. Among them, several water-soluble camptothecin a...

Claims

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