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Slow released anticarcinogen containing vasoinhibitor

A technology of vascular inhibitor and sustained-release agent, applied in the field of anti-cancer sustained-release agent, can solve the problems of enhanced tolerance of anti-cancer drugs, limited effective diffusion of drugs, obstacles to tumor chemotherapy, etc. The effect of reducing complications

Inactive Publication Date: 2007-07-25
JINAN SHUAIHUA PHARMA TECH
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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

[0137] 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 Paclitaxel and 10 mg of vandetanib were re-shaken to prepare microspheres for injection containing 10% of paclitaxel and 10% of vandetanib by spray-drying method. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 30-35 days, and the drug release time in mice subcutaneous is about 30 days.

Embodiment 2

[0139] 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:

[0140] (a) 5% vandetanib, tipifarnib, sirolimus, lenalidomide or isatecan in combination with 25% paclitaxel or docetaxel;

[0141] (b) 20% vandetanib, tipifarnib, sirolimus, lenalidomide or isatecan with 10% carmustine, nimustine, bendamustine, Garmustine, ramustine, formustine, comustine, lomustine, methyllomustine, uramustine, samustine, semustine, streptozocin or a combination of midazolamide; or

[0142] (c) 20% combination of vandetanib, tipifarnib, sirolimus, lenalidomide, or ixatecan with 20% vincristine, vinblastine, vinorelbine, or vindesine combination.

[0143] The viscosity of the sustained-release injection is 10cp-650cp (at 20°C-30°C).

Embodiment 3

[0145] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 20,000-45,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of tipifarnib and 15 mg of nimustine, and re-shake After homogenization, the organic solvent was removed by vacuum drying. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% tipifarnib and 15% nimustine, and then suspending in physiological saline containing 1.5% carboxymethylcellulose sodium to prepare the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (at 20°C-30°C). 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

A slowly-releasing anticancer medicine containing vascular depressant is composed of the slowly-released microballs consisting of the anticancer medicine chosen from taxane, alkylating agent and / or vegetative alkaloid, the vascular depressant (sirolimus, tacrolimus, etc) and slowly-released assistant, and the special solvent containing suspending aid.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release agent containing angiostatin, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing a blood vessel inhibitor. 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. It is beneficial to the effective diffusion of drugs into solid tumors and in tumors, and enhances the antitumor effect of anticancer drugs. (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 me...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 孙娟俞建江张红军刘恩祥
Owner JINAN SHUAIHUA PHARMA TECH