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Anticancer composition containing nimustine

A composition, the technology of sunitinib, is applied in the directions of drug combinations, non-active ingredients of polymer compounds, medical preparations containing active ingredients, etc., and can solve problems such as enhanced tolerance and treatment failure.

Inactive Publication Date: 2007-12-12
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 nimustine, 10mg dasatinib and 10mg nimustine respectively, and prepare 20% dasatinib, 20 % nimustine, and 10% dasatinib and 10% nimustine 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 used auxiliary material is the p(BHET-EOP / TC) of 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0121] (1) 10% tipifarnib;

[0122] (2) 10% nimustine; or

[0123] (3) A combination of 10% tipifarnib and 10% nimustine.

Embodiment 3

[0125] 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 sunitinib, 30mg nimustine, 20mg sunitinib and 10mg nimustine, shake up again and use spray drying method to prepare 30% sunitinib, 30% nimustine, 20 % sunitinib and 10% nimustine 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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Abstract

An anti-cancer composition comprises anti-cancer effective ingredient selected from tyrosine kinase inhibitor and / or nimustine and sustained release adjuvant, and can be made into sustained release injection and sustained release implant agent. Sustained release injection also comprises special dissolvent containing suspending agent. The Suspending agent has a viscocity of 100cp-3000cp (at 20deg.C-30deg.C) and is selected from sodium carboxymethylcellulose, and so on. the sustained release adjuvant 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) or p(CHDM-EOP).Slow releasing injection and implantable agent can keep high medicinal concentration in tumour part through slow releasing for over 60 days after being injected or implanted in or around tumour. The anticancer composition may also be prepared into sustained-release implant. It can reduce systemic toxic reaction of anticancer drugs, and also selectively improve the therapeutic effect of non-operative therapy such as chemotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a tyrosine kinase inhibitor and / or nimustine, 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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IPC IPC(8): A61K45/06A61K31/505A61K9/10A61K47/34A61K47/38A61K47/42A61P35/00
Inventor 张红军邹会凤俞建江张婕
Owner JINAN KANGQUAN PHARMA TECH
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