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Anticancer compound including alkylate agent and epothilones

A technology of epothilone and hydrogenepothilone is applied in the directions of non-active ingredients of polymer compounds, drug combinations, medical preparations containing active ingredients, etc., and can solve problems such as enhanced tolerance and treatment failure.

Inactive Publication Date: 2007-09-26
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Put 80, 80 and 80 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 80: 20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 20mg carmustine, 20mg epothilone D, 10mg carmustine and 10mg epothilone D respectively, reshake and prepare 20% carmustine by spray drying method , 20% epothilone D, and 10% carmustine and 10% epothilone D microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 40-50 days, and the release time in mouse subcutaneous liver cancer is more than 50 days.

Embodiment 2

[0116] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that used auxiliary material is the p(BHET-EOP / TC) of 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0117] (1) 1-40% carmustine or nimustine;

[0118] (2) 1-30% epothilone D, epothilone A, epothilone B, epothilone F, epothilone E or epothilone C; or

[0119] (3) 1-40% carmustine or nimustine and 1-30% epothilone D, epothilone A, epothilone B, epothilone F, epothilone A combination of prime C or isopothilone D.

Embodiment 3

[0121] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg of nimustine, 30mg of epothilone D, 20mg of nimustine and 10mg of epothilone D, shake up again and use the spray drying method to prepare 30% nimustine, 30% epothilone D. Microspheres for injection of 20% nimustine and 10% epothilone D. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 55-65 days, and the release time in mouse lung cancer is about 60 days.

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PUM

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Abstract

The invention relates to an anti-cancer compound as a slow release injection which contains alkyl agent and / or aepmycin, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings, selected from alkyl agent and / or aepmycin, the solvent is a common solvent or a special solvent with suspending agent, while the viscosity of suspending agent is 100cp-3000cp (at 20-30Deg. C), selected from carboxymethyl cellulose, the anti-cancer effective component is phosphoinositide 3-kinase restrainer and / or the phosphoinositide 3-kinase restrainer booster selected from self-anti-cancer antibiotics and / or tetrazine drug, the slow release finding is selected from phosphate polyester as p (LAEG-EOP), p (DAPG-EOP), p (BHET-EOP / TC), p (BHET-EOP / TC), p (BHDPT-EOP / TC), p (BHDPT-EOP / TC), p (CHDM-HOP) or p (CHDM-EOP), or the polyester or mixture of phosphate and polylactic acid, polyphenyl, 2-aliphatic acid, sebacic acid polyester, poly (erucic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid). The anti-cancer compound can be made as slow release plant agent, to inject cancer or around cancer to hold the effective drug density for more than 40 days, while it can significantly reduce the general reaction of drug and selectively strengthen the effect of non-surgery treatments as chemotherapy or the like.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing an alkylating agent and / or epothilone, which is an anticancer slow-release injection and a slow-release implant, and belongs to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, alkylating agents have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs. [0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. In addition, blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/06A61K47/34A61K47/36A61K47/38A61K47/42A61K31/427A61P35/00A61K47/26
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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