Anticancer compound including neoangiogenesis inhibitors and alkylate agent

A new blood vessel and inhibitor technology, applied in the field of sustained-release implants, sustained-release injections, anti-cancer compositions, and sustained-release preparations, can solve the problems of slow release, uneven release, and burst release of drugs

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

[0003] However, the sustained-release excipients used in the existing above-mentioned and other pharmaceutical preparations more or less cause sudden release or uneven release of the drug when the drug is released.
Some drugs are released too slowly, which is not enough to obtain effective drug concentration in the local area, so they cannot effectively kill tumor cells; some release drugs too fast, often causing burst release, which is likely to cause systemic toxic reactions like conventional injections

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Put 90, 90 and 80mg p(BHET-EOP / TC), BHET-EOP: TC is 80:20) copolymer into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 10mg erlotinib, 10mg carmustine, 10mg erlotinib and 10mg carmustine respectively, prepare 10% erlotinib, 10 % carmustine, and 10% erlotinib and 10% carmustine 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 mice subcutaneously is more than 50 days.

Embodiment 2

[0105] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that the p(BHET-EOP / TC) that used adjuvant is 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0106] (1) 5-30% erlotinib or gefitinib;

[0107] (2) 5-30% carmustine, nimustine, formustine, bendamustine, bendamustine, lomustine, ramustine or samustine; or

[0108] (3) 5-30% of erlotinib or gefitinib and 5-30% of carmustine, nimustine, formustine, bendamustine, bendamustine, A combination of lomustine, ramustine, or samustine.

Embodiment 3

[0110] 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 gefitinib, 30mg bendamustine, 15mg gefitinib and 15mg bendamustine, re-shake and use spray drying method to prepare 30% gefitinib, 30% bendamustine 15% gefitinib and 15% bendamustine for injection. 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 mice subcutaneously 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 vessel restrainer and / or alkyl agent, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings, 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 the combination of vessel restrainer and / or the alkyl agent selected from nimuxitin, or the like, the slow release finding is selected from phosphate polyester as p (LAEG-EOP), p (DAPG-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 into 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 a new blood vessel inhibitor and / or an alkylating agent, and belongs to the technical field of medicines. Specifically, the invention relates to a slow-release preparation capable of stably releasing angiogenesis inhibitors and / or alkylating agents locally in solid tumors, mainly slow-release implants and slow-release injections, which can prolong drug release time, And can increase drug sensitivity. (2) Background technology [0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. 参见(中国专利申请号200510042234.3、03148624.X、200510042236.2、96116041.1、97107078.4、200510042260.6、200510042261.0、200510042262.5、200510042263.X;美国专利US5651986、RE37410)。 [0003] However, the sustained-release excipients used in the above-mentioned and other existing pharmaceutical preparations more or less ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/10A61K47/38A61K47/10A61K47/30A61K31/505A61K9/00A61P35/00A61K31/436
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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