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Anticancer composition containing lomustine

A technology of composition and copolymer, which can be applied in the directions of drug combination, non-active ingredients of polymer compounds, and medical preparations containing active ingredients, etc., which can solve the problems of treatment failure and enhanced tolerance.

Inactive Publication Date: 2007-12-19
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter 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

[0118] Put 80, 80 and 80 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 80: 20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 20mg dasatinib, 20mg lomustine, 10mg dasatinib and 10mg lomustine respectively, shake up again and prepare 20% dasatinib, 20 % lomustine, and 10% dasatinib and 10% lomustine microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 60-70 days, and the drug release time in mouse subcutaneous is more than 60 days.

Embodiment 2

[0120] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that the p(BHET-EOP / TC) that used adjuvant is 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0121] (1) 10% lomustine; or

[0122] (2) A combination of 10% tipifarnib and 10% lomustine.

Embodiment 3

[0124] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg of sunitinib, 30mg of lomustine, 20mg of sunitinib and 10mg of lomustine, shake up again and use spray drying method to prepare 30% sunitinib, 30% lomustine, 20 % sunitinib and 10% lomustine microspheres for injection. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 60-65 days, and the drug release time in mice subcutaneous is about 60 days.

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PUM

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Abstract

The anticancer composition includes effective anticancer component selected from tyrosine kinase inhibitor and / or lomustine and slow releasing supplementary material, and may be prepared into slow released injection and slow released implant. The slow released injection includes also suspending agent and special solvent. The suspending agent has viscosity at 20-30 deg.c of 100-3000 cp and is selected from sodium carboxymethyl cellulose, etc. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP / TC), p(BHET-EOP / TC), p(BHDPT-EOP / TC), p(BHDPT-EOP / TC), p(CHDM-HOP), p(CHDM-EOP), etc. The released injection and slow released implant may be injected or set in tumor for slow releasing to maintain high medicine concentration for over 60 days to raise the treating effect and lower the systemic reaction on the medicine.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a tyrosine kinase inhibitor and / or lomustine, which is an anticancer sustained-release injection and a sustained-release implant, and belongs to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, tyrosine kinase inhibitors have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs. [0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. In addition, blood vessels, connective tissue, matrix proteins, fib...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/17A61K9/10A61K47/34A61K47/38A61K47/42A61P35/00
Inventor 孙娟张婕邹会凤
Owner JINAN KANGQUAN PHARMA TECH
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