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Anticancer composition containing tyrosine kinase restraining agent and taxane

A tyrosine kinase and inhibitor technology, applied in the field of anti-cancer compositions, can solve problems such as treatment failure and increased tolerance

Inactive Publication Date: 2007-12-05
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

[0106] 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 tipifarnib, 20mg deacetyl-paclitaxel, 10mg tipifarnib and 10mg deacetyl-paclitaxel respectively, re-shake and prepare 20% tipifarnib, 20% deacetyl-paclitaxel by spray drying method Acetyl-paclitaxel, and microspheres for injection of 10% tipifarnib and 10% deacetyl-paclitaxel. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 40-50 days, and the release time in mouse subcutaneous liver cancer is more than 50 days.

Embodiment 2

[0108] 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:

[0109] (1) 1-40% rapamycin or tipifarnib;

[0110] (2) Combination of 1-40% rapamycin or tipifarnib with 1-40% paclitaxel, docetaxel, hydroxypaclitaxel, epipaclitaxel or deacetylpaclitaxel.

Embodiment 3

[0112] 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 gefitinib, 30mg paclitaxel, 20mg gefitinib and 10mg paclitaxel, shake up again and use spray drying method to prepare 30% gefitinib, 30% paclitaxel, 20% gefitinib and 10% paclitaxel 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 release time of the slow-release injection in physiological saline in vitro is 55-65 days, and the release time in mouse lung cancer is about 60 days.

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PUM

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Abstract

The slow released anticancer injection containing tyrosine kinase inhibitor and / or taxane consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer components of tyrosine kinase inhibitor and / or taxane and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP / TC), etc. The anticancer composition may be also prepared into slow released implant, and the released injection and slow released implant may be injected or set in tumor for slow releasing to maintain effective medicine concentration for over 40 days, and has obviously lowered systemic reaction on the medicine and capacity of enhancing the chemotherapeutic and radiotherapeutic effect.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a tyrosine kinase inhibitor and / or a taxane, which is an anticancer slow-release injection and a slow-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 (TKi) 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, fibrin, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/06A61K31/337A61K47/34A61P35/00
Inventor 孙娟张婕邹会凤
Owner JINAN KANGQUAN PHARMA TECH
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