Anticancer composition containing tyrosine kinase inhibitor

A tyrosine kinase and kinase inhibitor technology, applied in the field of sustained-release implants, sustained-release injections, and anti-cancer compositions, can solve the problem of ineffective killing of tumor cells, insufficient release to obtain effective drug concentration, easy to cause systemic toxicity

Inactive Publication Date: 2007-11-28
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)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] 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, 10mgUCN-01, 10mg sunitinib and 10mgUCN-01 respectively, reshake and use spray drying method to prepare 10% sunitinib, 10% UCN-01 And 10% sunitinib and 10% UCN-01 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 sustained-release injection in physiological saline in vitro is 60-70 days, and the release time in mouse subcutaneous is more than 65 days.

Embodiment 2

[0100] 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 dichloromethane to each , after dissolving and mixing, add 20mg Erbitux, 20mg UCN-02, 20mg Erbitux and 20mg UCN-02 respectively, shake again and use spray drying method to prepare 20% Erbitux, 20% UCN-02 and 20% Microspheres for injection of Erbitux and 20% UCN-02. 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 slow-release injection in physiological saline in vitro is 50-60 days, and the drug release time in mouse subcutaneous is more than 55 days.

Embodiment 3

[0102] 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 Iressa, 30mg alkylphosphocholine, 15mg Iressa and 15mg alkylphosphocholine, re-shake and use spray drying method to prepare 30% Iressa, 30% alkylphosphocholine, 15 % Iressa and 15% Alkyl Phosphocholine for Injection Microspheres. 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 composition containing tyrosine kinase inhibitor is slow released injection and slow released implanted preparation. Its effective anticancer component is the composition of Erbitux, Iressa, Tarceva, Sunitinib, Trastuzumab and other tyrosine kinase inhibitor, and Edelfosine, miltefosine, perifosine, ilmofosine and other phosphoinositide-3-kinase inhibitor. Its slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), other polyphosphate copolymer, poly(erucic acid dipolymer-sebacic acid), etc. The anticancer composition may injected or set into tumor and can maintain the effective medicine concentration for over 50 days with obviously reduced general reaction and capacity of raising the treating effect of chemotherapeutic and / or radiotherapeutic medicine.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a tyrosine kinase inhibitor and / or a phosphoinositide 3-kinase inhibitor, and belongs to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing tyrosine kinase inhibitors and / or phosphoinositide 3-kinase inhibitors locally in solid tumors, mainly sustained-release implants and sustained-release injections , can release the drug steadily and slowly, and can increase the sensitivity of the drug. (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-m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00A61K47/10A61K47/36A61K47/42
Inventor 孙娟俞建江张红军刘恩祥
Owner JINAN KANGQUAN PHARMA TECH
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