A sustained release anticancer agent carrying angiogenesis inhibitor and clorfarabine

A new blood vessel and inhibitor technology, applied in the field of sustained-release injections and sustained-release implants, and the preparation of sustained-release preparations, can solve the problems of systemic toxicity and drug resistance that limit the application

Inactive Publication Date: 2006-12-13
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its obvious systemic toxicity and development of drug resistance greatly limit the application of this drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Clorabine and 10 mg marimastat were shaken again to prepare microspheres for injection containing 10% clorabine and 10% marimastat 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 220cp-460cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0108] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0109] (a) 2-40% marimastat, SU5416, SU6668, fumagillin or TNP-470 in combination with 2-40% clorabine;

[0110] (b) 2-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito Combinations of horses with 2-40% clorabine.

Embodiment 3

[0112] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of fumagillin and 15 mg of clolarabine, re-shake and vacuum Dry to remove organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% fumagillin and 15% clorabine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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PUM

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Abstract

Disclosed is an anticancer slow release injection carrying both anti-angiogenesis agent and clofarabine, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents, slow release auxiliary materials, and specific dissolvent containing suspension adjuvant. The anti-angiogenesis agent is selected from Marimastat, Fumagillin, gefinitib, erlotinib, lapatinib, lapatinib, endothelium chalone, imatinib, Imatinib, Gasanib, Avastin, Cananib, sorafenib, sunitinib, oersteda or panitoma, the slow release auxiliary materials are selected from Polifeprosan, sebacylic acid copolymer, EVAc, polylactic acid and copolymer, The viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose.

Description

(1) Technical field [0001] The invention relates to a preparation method of a sustained-release agent loaded with angiogenesis inhibitor and clorabine, and belongs to the technical field of medicines. Specifically, the present invention provides a slow-release anticancer drug containing angiogenesis inhibitor and / or clorabine, mainly slow-release injections and slow-release implants. (2) Background technology [0002] Angiogenesis is necessary for the growth and metastasis of solid tumors. When the diameter of solid tumor is larger than 0.5cm, tumor cells depend on their own vascular system. Tumor cells can obtain nutrients and oxygen from the host through tumor blood vessels, and can continuously transport metastatic cells to the host through tumor blood vessels, and continue to grow and induce blood vessel formation in other parts of the body, leading to tumor metastasis. The emergence of new metastases is the main reason for treatment failure. Therefore, the effective ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/7076A61K47/34A61P35/00A61K47/26A61K47/32A61K47/36A61K47/42
Inventor 王明华
Owner JINAN KANGQUAN PHARMA TECH
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