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Anticancer composition containing both platinum compound and Sirolimus

A technology of rapamycin and composition, which is applied in the field of anticancer composition, can solve the problems of anticancer drug resistance enhancement, treatment failure, etc., to improve interstitial fluid conductivity, promote penetration and diffusion, and reduce tension Effect

Inactive Publication Date: 2007-06-06
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, and single-drug chemotherapy is more likely to lead to enhanced resistance of tumor cells to anticancer drugs, resulting in treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Put 80 parts of polylactic acid (PLA) with a peak molecular weight of 10,000-35,000 into a container, add an appropriate amount of dichloromethane to dissolve and mix well, add 19 parts of cisplatin and 1 part of rapamycin, re-shake and remove by vacuum drying Organic solvents. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 19% cisplatin and 1% rapamycin, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding mixed Suspension-type sustained-release injections. The sustained-release injection has a viscosity of 150cp-300cp (at 20°C-30°C), a drug release time of 20-35 days in vitro in physiological saline, and a drug release time of about 35-50 days in mice subcutaneously.

Embodiment 2

[0123] The method steps for processing into sustained-release injections are the same as in Example 1, but the difference is that the excipients used are polylactic acid with a peak molecular weight of 30,000-50,000, containing anticancer active ingredients and their weight percentage: 0.01% rapamycin or 0.01% rapamycin in combination with 10% cisplatin, carboplatin, nedaplatin, omaplatin, or oxaliplatin.

Embodiment 3

[0125]Put 90mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 9.2 mg cisplatin and 0.8 mg rapamycin, re-shake and prepare microspheres for injection containing 9.2% cisplatin and 0.8% rapamycin by spray-drying method. 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 sustained release injection in the physiological saline in vitro is 20-25 days, and the drug release time in the mouse subcutaneous is about 20-30 days.

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Abstract

The anticancer composition containing both platinum compound and sirolimus is one kind of slow releasing injection or slow releasing implant. The slow releasing injection consists of slow released microsphere and special solvent containing suspending agent. The platinum compound is selected from cisplatin, carboplatin, lobaplatin, etc; the slow releasing supplementary material is selected from polylactic acid, lactic acid copolymer, polifeprosan, etc; and the suspending agent is selected from sodium carboxymethyl cellulose, iodine glycerin, etc. The slow releasing injection and the slow releasing implant are injected or set into solid tumor to diffuse and produce synergistic curative effect.

Description

(1) Technical field [0001] The invention relates to an anticancer composition and belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant simultaneously loaded with a platinum compound and rapamycin. 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; radiotherapy and traditional...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/282A61K31/555A61K31/436A61K47/34A61P35/00A61K47/26
Inventor 孔庆忠俞建江
Owner SHANDONG LANJIN PHARMA
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