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Slow released compound anticancer injection containing blood vessel inhibitor

A technology of vascular inhibitors and sustained-release injections, which is applied in the field of compound anti-cancer sustained-release injections, and can solve problems such as treatment failure and increased resistance to anticancer drugs

Pending Publication Date: 2006-11-08
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Put 80 mg of polylactic acid (PLGA) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of imatinib and 10 mg of gemcitabine, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain the slow-release anticancer drug containing 10% imatinib and 10% gemcitabine. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 14-21 days, and the drug release time in mouse subcutaneous is 25-45 days.

Embodiment 2

[0109] As described in Example 1, the difference is that the anticancer active ingredient and weight percentage are one of the following:

[0110] (1) 1-50% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito horse;

[0111] (2) 1-50% pemetrexed, pemetrexed disodium, lumitrexed, carmofur, tegafur, temozolomide, zalcitabine, emtricitabine, galocitabine, Ibacitabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine, Capecitabine, Gemcitabine, Fludarabine, Raltitrexed, Raltitrexed, Dexrazoxane, cladribine, or noratrexed; or

[0112] (3) 1-50% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or ...

Embodiment 3

[0114] Put 80mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg of Lotinib and 10 mg doxorubicin were re-shaken and spray-dried to prepare microspheres for injection containing 10% erlotinib and 10% doxorubicin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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PUM

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Abstract

The slow released compound anticancer injection containing blood vessel inhibitor and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is blood vessel inhibitor and / or blood vessel inhibitor synergist selected from antitumor antibiotic and antimetabolite. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, poly(erucic acid dipolymer-sebacic acid), poly(fumaric acid-sebacic acid), etc or their composition. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for use alone or together with chemotherapeutic and / or radiotherapeutic medicine..

Description

(1) Technical field [0001] The invention relates to a compound anticancer sustained-release injection, which belongs to the technical field of medicines. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug concentration or therapeutic dose in the local tumor, resulting in poor efficacy and high toxicity. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (Kong Q et al., J Surg Oncol.1998 Oct; 69(2):76-82). [0003] Local placement of antitumor d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/505A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 高化兰
Owner JINAN SHUAIHUA PHARMA TECH
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