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Albumin-binding anthracycline antitumor antibiotic preparation and preparation method thereof

An anti-tumor and antibiotic technology, which is applied in the direction of anti-tumor drugs, drug combinations, and pharmaceutical formulations, can solve the problems of cumbersome preparation methods, and achieve the effects of simple preparation methods, reduced toxic and side effects, and good drug loading capacity

Active Publication Date: 2018-11-06
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method needs to add a large number of excipients except albumin, and the preparation method is relatively cumbersome

Method used

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  • Albumin-binding anthracycline antitumor antibiotic preparation and preparation method thereof
  • Albumin-binding anthracycline antitumor antibiotic preparation and preparation method thereof
  • Albumin-binding anthracycline antitumor antibiotic preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Take 300 mg of human serum albumin, add 10 mL of water for injection and dissolve to obtain a human serum albumin solution. Take 20 mg of pirarubicin and 40 mg of F6840 mg and dissolve them in an appropriate amount of dichloromethane, and remove the dichloromethane by rotary evaporation. Add human serum albumin solution, ultrasonicate in a water bath for 10 minutes to form a clear and transparent solution, and filter to sterilize. The pirarubicin albumin-bound preparation was obtained by freeze-drying under aseptic conditions.

Embodiment 2

[0063] Take 300 mg of human serum albumin, add 10 mL of water for injection and dissolve to obtain a human serum albumin solution. Take 20 mg of pirarubicin and 40 mg of F68 and dissolve them in an appropriate amount of dichloromethane, add 66.7 mg of glucose, and remove the dichloromethane by rotary evaporation. Add human serum albumin solution, ultrasonicate in a water bath for 10 minutes to form a clear and transparent solution, and filter to sterilize. The pirarubicin albumin-bound preparation was obtained by freeze-drying under aseptic conditions.

Embodiment 3

[0065] Take human serum albumin 300mg, F6840mg, add 6mL water for injection and dissolve to obtain human serum albumin solution. Take 20 mg of pirarubicin and dissolve it in 5 mL of water with pH=6. Mix the two, incubate for 10 minutes, filter and sterilize with a microporous membrane, and let stand for a while to remove the air bubbles in the preparation to obtain the pirarubicin-albumin conjugate preparation.

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PUM

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Abstract

The present invention discloses an anthracycline antitumor antibiotic albumin conjugate comprising an anthracycline antitumor antibiotic or a pharmaceutically acceptable salt thereof and albumin in aweight ratio of 1:1 to 1000. The invention also discloses lyophilized powder for injection, a preparation, application and a preparation method of the anthracycline antitumor antibiotic albumin conjugate. The anthracycline antitumor antibiotic albumin conjugate has high efficiency, low toxicity, good drug stability, simple preparation method and convenient clinical use.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and relates to an albumin-binding anthracycline antitumor antibiotic preparation and a preparation method thereof. Background technique [0002] Anthracycline anti-tumor antibiotics are a class of broad-spectrum anti-tumor drugs commonly used in clinical practice, and are widely used in the treatment of various cancers, such as breast cancer, liver cancer, lung cancer, leukemia, lymphoma and many other solid tumors. This type of antineoplastic drug can produce a wide range of biochemical effects on the body and has strong cytotoxicity. , ADM), daunorubicin (DNR), epirubicin (Epirubicin, EPI), pirarubicin (Pirarubicin, THP-ADM), aclacinomycin (Aclacinomycin, ACM), Mitoxantrone (Mitoxantrone), Idarubicin (Idarubicin) and the like. However, like other cytotoxic anti-tumor drugs, anthracycline anti-tumor antibiotics lack selectivity to tumor tissue and have severe side effects. In addition to cau...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K45/00A61P35/00
CPCA61K45/00A61K47/42A61P35/00
Inventor 龚涛宋旭周楚楚张志荣孙逊朱义丁洋李杰
Owner SICHUAN BAILI PHARM CO LTD
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