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Anti-cancer combination including phosphatidylinositol 3-kinase inhibitor and antimetabolite medicine

A kinase inhibitor and phosphoinositide technology, which is applied in the field of anticancer compositions, anticancer sustained-release injections and sustained-release implants, and can solve problems such as increased tolerance and treatment failure

Inactive Publication Date: 2007-09-26
JINAN KANGQUAN 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

[0103] 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 UCN-01, 20mg cytarabine, 10mg UCN-01 and 10mg cytarabine respectively, re-shake and use spray drying method to prepare 20% UCN-01, 20% cytarabine , and microspheres for injection with 10% UCN-01 and 10% cytarabine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 60-70 days, and the drug release time in mouse subcutaneous is more than 60 days.

Embodiment 2

[0105] 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:

[0106] (1) 5-40% UCN-01 or UCN-02;

[0107] (2) 1-30% cytarabine, fluorouracil, methotrexate, capecitabine, or gemcitabine; or

[0108] (3) A combination of 5-40% UCN-01 or UCN-02 and 1-30% cytarabine, fluorouracil, methotrexate, capecitabine or gemcitabine.

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 UCN-02, 30mg methotrexate, 20mg UCN-02 and 10mg methotrexate, re-shake up and use spray drying method to prepare injection containing 30% UCN-02, 30% methotrexate, 20% UCN-02 and 10% methotrexate ball. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 60-65 days, and the drug release time in mice subcutaneous 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 phosphoinositide 3-kinase restrainer and / or antimetabolite drug, 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 phosphoinositide 3-kinase restrainer and / or antimetabolite drug, 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 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 60 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 phosphoinositide 3-kinase inhibitors and / or anti-metabolite drugs, which are anticancer sustained-release injections and sustained-release implants, and belong to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, phosphoinositide 3-kinase inhibitors 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. See Kong Qingzhong "Intratumoral placem...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61P35/00
Inventor 张红军邹会凤张婕
Owner JINAN KANGQUAN PHARMA TECH
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