Composition of anti cancer medication prepared from carried platinum category compound and consubstantial hydrolytic agent

An anti-cancer drug and hydrolyzing agent technology, which can be used in drug combinations, active ingredients of heavy metal compounds, anti-tumor drugs, etc., can solve the problems of enhanced tolerance of anti-cancer drugs, limited effective diffusion of drugs, obstacles to tumor chemotherapy, etc. Effect of drug injection, improving interstitial fluid conductivity, reducing complications

Inactive Publication Date: 2007-05-09
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] 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

[0124] 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 Cisplatin and 10 mg gefitinib were re-shaken to prepare microspheres for injection containing 10% cisplatin and 10% gefitinib by spray drying. 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

[0126] 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:

[0127] (1) 2-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, sematinib, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teostar, Panito Horse, dispase, bromelain, chymotrypsin, clostripain, plasmin, pancreatin, cathepsin-G, plasminogen activator, collagenase, streptokinase, glycosidase, hyaluronidase, lysozyme , relaxin, interferon, or fibrinase; or

[0128] (2) 2-40% of gefitinib, erlotinib, plasminogen activator, collagenase, streptokinase, glycosidase, hyaluronidase, lysozyme, relaxin, interferon or fibrinase With 1-30% cisplatin, carboplatin, cycloplatin, heptaplatin, denaplatin, cyclopentylaminoplatinum, platinum blue, cyproamideplatinum, eth...

Embodiment 3

[0131] Put 70 mg of polylactic acid (PLA) with a peak molecular weight of 35,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of Sisiplatin and 15 mg of Erlotinib, re-shake, and then vacuum-dry to remove the organic solvent . The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% cisciplatin and 15% erlotinib, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding Suspension-type sustained-release injection. 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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PUM

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Abstract

A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting Pt compound, iterstitial hydrolyte and slowly-releasing auxiliary. Said Pt compound is chosen from cisplatin, carboplatin, etc. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from polylactic acid, polyethanediol, etc.

Description

(1) Technical field [0001] The invention relates to an anticancer slow-release agent containing interstitial hydrolyzing agent, which belongs to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing an interstitial hydrolyzing agent. The anti-cancer slow-release agent can effectively inhibit or destroy the solid tumor stroma and tumor blood vessels, and can inhibit tumor angiogenesis, effectively reduce the tension in the tumor, interstitial pressure, and interstitial viscosity, thereby improving its interstitial fluid conduction. The rate is conducive to the effective diffusion of drugs into solid tumors and tumors. (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; ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/06A61K38/46A61K31/282A61K31/555A61K47/34A61P35/00
Inventor 孔庆忠俞建江
Owner SHANDONG LANJIN PHARMA
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