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Anticancer sustained-released formulation loaded with blood vessel inhibitor and synergist thereof

A technology of sustained-release injection and vascular inhibitor, which is applied in the field of compound anti-cancer drug sustained-release injection, compound anti-cancer drug sustained-release preparation, sustained-release injection and sustained-release implant, and can solve the problems of treatment failure, anti-cancer drug resistance. Receptivity enhancement and other issues to achieve the effect of reducing costs, facilitating drug injection, and reducing drug concentration

Inactive Publication Date: 2009-03-11
SHANDONG LANJIN PHARMA +1
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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

[0156] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml methylene chloride, dissolve and mix well, then add 10mg Gefitinib and 7-hydroxyl-staurosporine, re-shaken and spray-dried to prepare microspheres for injection containing 10% gefitinib and 10% 7-hydroxyl-staurosporine . 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 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0158] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0159] (1) 1-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito horse;

[0160] (2) 1-40% of 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkyl phosphorylcholine, hexadecyl phosphate Choline, octadecyl-(1,1-dimethyl-4-piperidine) phosphate, 1-O-hexadecyl-2-O-methyl-rac-glyceryl-3-phosphocholine , 1-O-octadecyl-2-O-methyl-rac-propanetriyl-3-phosphocholine, 1-Ooctadecyl-2-O-methyl-sn-propanetriyl-3- Phosphocholine, inositol polyphosphate, cyclosporin A, tetradecylphosphorylcholine, hexacylphospho(N-N-N-trimethyl)hexanolamine, octadecylphosphorylc...

Embodiment 3

[0164] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, then add 15 mg of erlotinib and 15 mg of 7 ethyl-10-hydroxyl The resin was shaken again and dried under vacuum to remove the organic solvent. The dried drug-containing solid composition is frozen and pulverized to make micropowder containing 15% erlotinib and 15% 7-ethyl-10-hydroxycamptothecin, and then suspended in 1.5% sodium carboxymethylcellulose In physiological saline, the corresponding suspension-type sustained-release injection was prepared. The drug release time of the slow-release injection in physiological saline in vitro is 20-35 days, and the drug release time in mice subcutaneous is about 35-50 days.

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Abstract

An anticarcinogenic slow release injection carrying an angiogenesis inhibitor and a synergist thereof is made from slow release microspheres and a dissolvant. The slow release microspheres comprise anticancer active components and a slow release adjuvant, and the dissolvant is a special dissolvant containing a suspending agent. The anticancer active components are angiogenesis inhibitors such as gefitinib, erlotinib, lapatinib, vatalanib, pelitinib, thalidomide, ranolamine, angiostatin, endostatin, imatinib, thalidomide, ranolamine, simatinib, dasatinib, avastin, kanatini, sorafenib, sunitinib, telstar or panitoma, and the like, and / or cytotoxic drugs selected from a phosphoinositide-3-kinase inhibitor, pyrimidine analogue and / or a DNA repair enzyme inhibitor; the slow release adjuvant is biocompatible macromolecule; the viscosity of the suspending agent is 100cp-3,000cp (at the temperature of 20-30 DEG C), and the suspending agent is selected from sodium carboxymethyl cellulose, and the like. The slow release microspheres can be also made into a slow release implant, and the curative effects of non-operative therapies such as radiotherapy, chemotherapy, and the like, can be improved when the slow release injection is injected or placed in tumors or around the tumors.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection of a compound anticancer drug, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release compound anticancer drug containing angiostatin and / or its synergist, mainly slow-release injections and slow-release implants. (2) Background technology [0002] Currently, 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/00A61K31/4706A61K31/519A61K47/30A61P35/00
Inventor 孔庆忠张红军邹会凤
Owner SHANDONG LANJIN PHARMA
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