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Anti cancer controlled release agent of carried interstitial hydrolytic agent and medication of cell toxin

A technology of hydrolyzing agent 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. Mass-liquid conductivity, the effect of promoting penetration and diffusion

Inactive Publication Date: 2007-05-09
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

[0144] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into the container, add 100ml dichloromethane, dissolve and mix well, then add 10mg Docetaxel and 10 mg collagenase were re-shaken to prepare microspheres for injection containing 10% docetaxel and 10% collagenase 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 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0146] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the p-carboxyphenyl propane of the sustained-release auxiliary material polyphenylpropane: sebacic acid is 50:50; the contained anticancer active ingredient is 5% Hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, ifosfamide, lomustine, estramustine, formustine, samustine, etoposide, Niposide, vinblastine, oxaliplatin, epothilone B, epothilone D, anastrozole, tamoxifen, fluorouracil, or mitomycin C in combination with 15% gefitinib ; The viscosity of the sustained-release injection is 360cp-600cp (at 20°C-30°C).

Embodiment 3

[0148] Put 80 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 40,000-65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 5 mg of hyaluronidase and 15 mg of mitozolomide, 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 5% hyaluronidase and 15% mitozolomide, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (at 20°C-30°C). 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.

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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 cellulotoxic medicine, iterstitial hydrolyte and slowly-releasing auxiliary. Said cellulotoxic medicine is chosen from gemcitabine, 9-nitrocamptothecine, etc. Said interstitial hydrolyte is chosen from Epothilone B, Epothilone D, etc. Said slowly-releasing auxiliary is chosen from p(BHET-EOP / TC), p(LAEG-EOP), 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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IPC IPC(8): A61K9/00A61K45/06A61K38/46A61K47/34A61P35/00
Inventor 孔庆新刘恩祥贺润平
Owner JINAN SHUAIHUA PHARMA TECH