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Medicine composition containing tyrosine kinase restraining agent

A technology of tyrosine kinases and inhibitors, which is applied in drug combinations, drug delivery, and medical preparations containing active ingredients, etc. It can solve the problem of inability to effectively kill tumor cells, the limitation of anticancer drugs used alone, and easy systemic toxicity Response and other issues

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

Release is too slow to obtain effective drug concentration, thereby can not effectively kill tumor cells; If release is too fast, it will cause burst release, which will easily cause systemic toxic reactions, such as polystyrene (A.J.Domb etc., Biomaterials (1995), 16 (14): 1069-1072; Wenbin Dang et al., Journal of Controlled Release (1996), 42: 83-92; Eric P. Sipos et al., Cancer Chemother Pharmacol (1997), 39: 383-389; Lawrence K. Fung et al., Cancer Research (1998), 58: 672-684)
[0005] In addition, the use of anticancer drugs alone has been limited by drug resistance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Put 90, 90 and 80mg p(BHET-EOP / TC), BHET-EOP: TC is 80:20) copolymer into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 10mg sunitinib, 10mg paclitaxel, 10mg sunitinib and 10mg paclitaxel respectively, shake up again and prepare 10% sunitinib, 10% paclitaxel and 10% paclitaxel by spray drying method. Microspheres for Injection of Nitinib and 10% 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 65-80 days, and the release time in mouse subcutaneous is more than 65 days.

Embodiment 2

[0109] Put 80, 80 and 60 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 50: 50) copolymers into three containers of A, B and C respectively, and then add 100 ml of ethanol to each to dissolve After mixing, add 20mg Erbitux, 20mg Docetaxel, 20mg Erbitux and 20mg Docetaxel respectively, re-shake and spray dry to prepare 20% Erbitux, 20% Docetaxel And 20% Erbitux and 20% docetaxel microspheres for injection. 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 50-70 days, and the release time in mouse subcutaneous is more than 65 days.

Embodiment 3

[0111] 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 Iressa, 30mg of deacetyl-paclitaxel, 15mg of Iressa and 15mg of deacetyl-paclitaxel, re-shake and use the spray drying method to prepare 30% of Iressa, 30% of deacetyl-paclitaxel, 15% of Iressa and 15 % deacetylpaclitaxel 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 mice subcutaneously is about 60 days.

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PUM

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Abstract

The anticancer medicine composition containing tyrosine kinase inhibitor is slow released injection and slow released implant. The effective anticancer components include tyrosine kinase inhibitor selected from Erbitux, Iressa, Tarceva, Sunitinib, Trastuzumab, etc, and / or composition selected from Docetaxel, deacetyl taxol, taxol, etc. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), etc. The released injection and slow released implant may be injected or set in tumor for slow releasing to maintain effective medicine concentration for over 50 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 a pharmaceutical composition containing tyrosine kinase inhibitors and / or taxanes, belonging to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing tyrosine kinase inhibitors and / or taxanes locally in solid tumors, mainly sustained-release implants and sustained-release injections, which can release steadily and slowly drugs, and can increase drug sensitivity (2) Background technology [0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. 参见(中国专利申请号200510042234.3,03148624.X,200510042236.2,96116041.1,97107078.4,200510042260.6,200510042261.0,200510042262.5,200510042263.X;美国专利US5651986,RE37410)。 [0003] However, the sustained-release excipients used in the above-mentioned and other existing pharmaceutical preparations more or less ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00A61K47/26
Inventor 孙娟张婕邹会凤
Owner JINAN KANGQUAN PHARMA TECH
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