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Restrainer containing tyrosine kinase and anticancer hormone medicines composition

A technology of tyrosine kinase and inhibitor, which can be used in drug combination, drug delivery, medical preparations containing active ingredients, etc., can solve problems such as enhanced tolerance and treatment failure

Inactive Publication Date: 2008-03-12
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 gefitinib, 20mg triptorelin, 10mg gefitinib and 10mg triptorelin respectively, re-shake and prepare 20% gefitinib, 20% toporelin by spray drying Relin, and microspheres for injection of 10% gefitinib and 10% trobrelin. 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 4050 days, and the drug release time in mouse subcutaneous liver cancer is more than 50 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) 1-40% gefitinib or rapamycin;

[0122] (2) 1-30% of troprelin, tamoxifen, toremifene, letrozole, angiostatin, exemestane, or bicalutamide; or

[0123] (3) 1-40% gefitinib or rapamycin and 1-30% triptorelin, tamoxifen, toremifene, letrozole, exemestane or bicalutamide The combination.

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 rapamycin, 30mg triptorelin, 20mg rapamycin and 10mg triptorelin, re-shake and use spray drying method to prepare 30% rapamycin, 30% triptorelin, 20% Microspheres for Injection of Amycin and 10% Tresptorelin. 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

An anti-cancer compound containing the PTK enzyme inhibitor (TKi) or the hormones medicine is a slow releasing injection, which consists of a slow-releasing micro sphere and a dissolvent. The slow-releasing micro sphere is selected from the effective component and the slow-releasing adjuvant of the TKi or the hormones medicine. The dissolvent comprises a common dissolvent and a special dissolvent containing the suspending agent. The viscosity of the dissolvent is 100cp-3000cp when the temperature is 20 DEG C to 30 DEG C. The dissolvent is selected from the sodium carboxymethycellulose. The 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), which belong to the polyphosphoric acid ester copolymer or the copolymer of the polylactic acid, the Policeperson, the double fatty acid and the decanedioic acid, or the copolymer and the mixture of the poly-(druidic acid dimer-decanedioic acid) and the poly-(fumaric acid-decanedioic acid). The anti-cancer compound is also produced as a slow-releasing implantation preparation. The effective drug concentration can be maintained for over 40 days when the medicine is injected or arranged in the tumor or around the tumor. The medicine can greatly reduce the systemic reaction of the drug and selectively enhance the therapy effect of the non-surgical treatment such as the chemical therapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a tyrosine kinase inhibitor and / or a hormone drug, 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 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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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 孙娟张红军俞建江邹会风
Owner JINAN KANGQUAN PHARMA TECH
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