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Anticancer compound carrying phosphatidylinostitol 3-kinase inhibitor and the synergistic agent thereof

A kinase inhibitor and phosphoinositide technology, which can be used in drug combinations, antineoplastic drugs, non-active ingredients of polymer compounds, etc., can solve the problems of ineffective killing of tumor cells, slow release of drugs, and toxic reactions

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

[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

[0110] Put 90, 90 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 10mg UCN-01, 10mg doxorubicin, 10mgUCN-01 and 10mg doxorubicin respectively, shake up again and use spray drying method to prepare 10% UCN-01, 10% doxorubicin, and 10 Microspheres for injection of % UCN-01 and 10% doxorubicin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 100cp-200cp (at 20°C-30°C). 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

[0112] 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:

[0113] (1) 5-30% UCN-01 or UCN-02;

[0114] (2) 1-40% of arubicin, doxorubicin, epirubicin, idarubicin, pirarubicin, valrubicin, mitomycin C, actinomycin D or epirubicin Doxorubicin; or

[0115] (3) 5-30% UCN-02 or UCN-01 and 5-30% 1-40% arubicin, doxorubicin, epirubicin, edarubicin, pirarubicin, Combinations of valrubicin, mitomycin C, actinomycin D, or epirubicin.

Embodiment 3

[0117] 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 polyene UCN-02, 30mg epirubicin, 15mg polyene UCN-02 and 15mg epirubicin, re-shake and use spray drying method to prepare 30% polyene UCN-02, 30% epirubicin Injectable microspheres with 15% polyene UCN-02 and 15% epirubicin. 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 phosphoinositide 3-kinase restrainer and relative booster, 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 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), 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 a phosphoinositide 3-kinase inhibitor and / or a phosphoinositide 3-kinase inhibitor synergist, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release preparation capable of stably releasing a phosphoinositide 3-kinase inhibitor and / or a phosphoinositide 3-kinase inhibitor synergist locally in a solid tumor, mainly for slow-release implantation Drugs and sustained-release injections can prolong the drug release time and 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...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/34A61K47/36A61K47/38A61K47/42A61K45/06A61K31/553A61K31/704A61K38/12A61P35/00
Inventor 孙娟俞建江张红军刘恩祥
Owner JINAN KANGQUAN PHARMA TECH
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