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Anticancer composition

A technology of composition and copolymer, applied in drug combination, anti-tumor drug, drug delivery, etc., can solve the problems of treatment failure, increased tolerance of anti-cancer drugs, etc.

Inactive Publication Date: 2007-05-16
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, single-agent chemotherapy often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0149] Put 80 mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 20,000-40,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of epothilone B and 10 mg of camptothecin, and re-shake After homogenization, the organic solvent was removed by vacuum drying. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain the anticancer slow-release product containing 10% epothilone B and 10% camptothecin. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 15-25 days, and the drug release time in mouse subcutaneous is 25-50 days.

Embodiment 2

[0151] As described in Example 1, the difference is that the peak molecular weight of polylactic acid is 40000-60000 (PLGA, 75:25), and the anticancer active ingredient and weight percentage are one of the following: 10% epothilone D, Isopothilone D, BMS-247550, azaepothilone B, furan epothilone D or BMS-310705 with 10% camptothecin, hydroxycamptothecin, 9-nitrocamptothecin, SN-38, CPT-11, HCPT, homocamptothecin, MD-CPT, podophyllotoxin, trihydroxyisoflavones, letotecan, topotecan, irinotecan, etoposide, teniposide Glycosides, 14-Hydroxydaunorubicin, Amrubicin, Erubicin, Detorubicin, Detorubicin, 7-O-Methylnoga-4'-Epirubicin, Esobi Star, Carrubicine, Idarbistar, Liuroubixing, Meiduobixing, Naimorubicing, Doxorubicing, Rhodobixing, Wurubicin, Zorobixing, XK469, Combinations of Zorubicin, AD312, ICRF-187 or ICRF-193.

Embodiment 3

[0153] Put 70mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Pothilone D and 20 mg mitozolomide were re-shaken to prepare microspheres for injection containing 10% epothilone D and 20% mitozolomide by spray drying. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 15-25 days, and the drug release time in mice subcutaneous is about 30-40 days.

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Abstract

Disclosed is an anti-cancer composition slow release injection which comprises slow release microspheres and dissolvent, the slow release microspheres comprise slow release auxiliary materials, Epothilone derivatives, glyoxaline piperazidine, Topo enzyme inhibitor combination selected from SN-38, CPT-11, HCPT, Topotecan, Irinotecan, Etoposide, Teniposide, Amrubicin, Valtaxin, XK469, AD312, ICRF-187 or ICRF-193, the dissolvent being specific dissolvent containing suspension adjuvant, the slow release auxiliary materials are selected from polylactic acid and its copolymer, polyethylene / polylactic acid, glycollic acid copolymer, aliphatic acid and sebacylic acid copolymer, the viscosity of the suspension adjuvant is 80-3000cp (at 20-30 deg C), and is selected from carboxymethylcellulose, The slow release microspheres can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a release period of about 40 days. The slow release injection and slow release implanting agent can be used independently for effectively suppressing tumor accretion, or used in combination with non-operative methods such as chemotherapy and / or radiotheraphy with the function of improving their treatment effects.

Description

(1) Technical field [0001] The invention relates to an anticancer composition and belongs to the technical field of medicines. Specifically, the present invention provides a composition loaded with epothilone and its derivatives and anticancer drugs, mainly sustained-release injections and sustained-release implants. The intratumoral or peritumoral application of the anticancer slow-release agent is beneficial to obtain and maintain effective drug concentration of the drug in solid tumors, and can increase the sensitivity of tumor cells to the drug. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug concentration or therapeutic dose in the local tumor,...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/427A61K45/06A61K47/34A61P35/00
Inventor 孙娟张婕邹会凤
Owner JINAN SHUAIHUA PHARMA TECH
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