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Slow-releasing injection contg. platinum compounds and its potentiator type anticarcinogen

A technology for sustained-release injections and anti-cancer drugs, applied in the fields of sustained-release injections and sustained-release implants, compound anti-cancer drug sustained-release preparations, compound anti-cancer drug sustained-release injections, and can solve the problem of enhanced anti-cancer drug tolerance , treatment failure, etc.

Inactive Publication Date: 2006-11-15
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

[0139] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Epplatin and 7-hydroxyl-staurosporine, re-shake and spray-dry to prepare microspheres for injection containing 10% eplatin 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

[0141] 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:

[0142] (1) 1-40% of cisplatin, bicycloplatin, eberplatin, meciplatin, cisplatin or picoplatin;

[0143] (2) 1-40% of sulfoplatin, bicycloplatin, eplatin, meciplatin, cisplatin or picoplatin and 1-40% of 7-hydroxyl-staurosporine, 7-O-alkyl - combinations of staurosporine, beta-methoxystaurosporine, alkylphosphocholine or hexadecylphosphocholine;

[0144] (3) 1-40% of sulfoplatin, bicycloplatin, eplatin, meciplatin, siciplatin or picoplatin and 1-40% of O4-benzyl folic acid, 2,4,5-triamino-6- Benzyloxypyrimidine, 2,4-diamino-6-benzyloxy-5-nitrosopyrimidine, 2,4-diamino-6-benzyloxy-5-bromopyrimidine, 2-amino-4- Benzyloxy-5-nitropyrimidine, 2-amino-4-benzyloxy-6-methyl-5-nitropyrimidine, 2,4-diamino-6-benzyloxy-s-triazine or 2 - a combination of amino-O4-benzylpteridine;...

Embodiment 3

[0148] 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 Siciplatin and 15 mg of 7-ethyl-10-hydroxycamptothecin , shake again and dry in vacuo to remove the organic solvent. The dried drug-containing solid composition is frozen and pulverized to make micropowder containing 15% cisciplatin and 15% 7-ethyl-10-hydroxycamptothecin, and then suspended in a physiological solution containing 1.5% sodium carboxymethylcellulose. In 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

A slow-release anticancer injection contains the slow-release microspheres and solvent. Said slow-release microsphere contains the active anticancer component chosen from 6 Pt compounds including bicycloplatinum, etc and 3 cytotoxins including phosphoinositide 3-kinase inhibitor, pyrimidine analog or DNA repairase inhibitor, and the slow-release auxiliary.

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 sustained-release compound anticancer drug containing platinum compounds and their synergists, mainly sustained-release injections and sustained-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 place...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/282A61K31/555A61K45/00A61K47/34A61P35/00
Inventor 孔庆忠张红军俞建江
Owner SHANDONG LANJIN PHARMA
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