Anticancer composition containing Sirolimus

A technology of rapamycin and composition, which is applied in the field of anticancer composition containing rapamycin, can solve problems such as enhanced rapamycin tolerance, limitation of effective drug diffusion, obstacles to tumor chemotherapy, etc., and achieve effective Facilitate penetration and diffusion, increase interstitial fluid conductivity, promote penetration and diffusion effects

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

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0006] Not only that, the blood v

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0113] Put 95mg 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 2mg Rapamycin and 3 mg of gefitinib were re-shaken to prepare microspheres for injection containing 2% rapamycin and 3% gefitinib by spray drying. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 280cp-420cp (at 20°C-30°C), and the drug release time in in vitro physiological saline is 25-35 days, and the drug release time in mice subcutaneous is about 30-35 days.

Embodiment 2

[0115] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that polyphenylene is 50:50, and the contained anticancer active ingredients and weight percentage thereof are:

[0116] (1) 0.01%-5% rapamycin; or

[0117] (2) 0.01%-5% rapamycin with 2-40% elastase, trypsin, pepsin, pronase, dispase, bromelain, chymotrypsin, clostripain, plasmin or smoke Combinations of Aspergillus.

Embodiment 3

[0119] Put 90 mg of polylactic acid (PLA) with a peak molecular weight of 10,000-35,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 5 mg of rapamycin and 5 mg of erlotinib, re-shake and dry in vacuum Remove organic solvents. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 5% rapamycin and 5% erlotinib, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding 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.

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PUM

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Abstract

The anticancer composition containing sirolimus is one kind of slow releasing injection comprising slow released microsphere and special solvent containing suspending agent or slow releasing implant. The effective anticancer component is sirolimus, proteolytic enzyme selected from collagenase, hyaluornidase, etc and blood vessel inhibitor selected from gefitinib, thalidomide, etc. The slow releasing supplementary material is selected from polylactic acid, polyethylene glycol, polifeprosan, etc; the suspending agent is selected from sodium carboxymethyl cellulose, etc and has viscosity of 100cp-3000cp. The slow releasing injection and the slow releasing implant are used in treating tumor alone or in conjunction with chemotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing rapamycin, which belongs to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing 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] As a new anticancer drug, rapamycin has shown potential therapeutic effect on many kinds of cancer cells. However, traditional chemotherapy is not selective, and it is difficult to form an effective drug concentration or therapeutic dose locally in the tumor. The effect is poor and the to...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/436A61K38/46A61K45/06A61K47/34A61P35/00A61K47/36A61K47/38A61K47/42
Inventor 孔庆忠苏红清
Owner SHANDONG LANJIN PHARMA
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