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Anticancer composition containing phosphoinositide 3-kinase inhibitor and topology enzyme inhibitor

A technology of topozyme inhibitor and kinase inhibitor, applied in the field of anti-cancer compositions, can solve the problems of treatment failure, enhanced tolerance and the like

Inactive Publication Date: 2008-12-31
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

[0106] 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-1, 20mg irinotecan, 10mg UCN-1 and 10mg irinotecan respectively, reshake and use spray drying method to prepare 20% UCN-1, 20% irinotecan , and microspheres for injection with 10% UCN-1 and 10% irinotecan. 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

[0108] 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:

[0109] (1) 1-40% UCN-1 or UCN-2;

[0110] (2) 1-40% camptothecin, hydroxycamptothecin, letotecan, topotecan, irinotecan, etoposide, teniposide, amrubicin, arubicin, Detorubicin, Adriamycin, Epirubicin, Esorubicin, Carrubicin, Rhodobicin, Liurubicin, Medorubicin, Naimorubicin, Zorubicin, doxorubicin, pirarubicin, valrubicin, or idarubicin; or

[0111] (3) 1-40% UCN-1 or UCN-2 and 1-30% camptothecin, hydroxycamptothecin, letotecan, topotecan, irinotecan, etoposide, tinib Poside, Amrubicin, Erubicin, Detorubicin, Adriamycin, Epirubicin, Esorubicin, Carrubicin, Rhodorubicin, Rurubicin, Medobe Star, nemorubicin, zorubicin, doxorubicin, pirarubicin, valrubicin or idarubicin.

Embodiment 3

[0113] 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-2, 30mg irinotecan, 20mgUCN-2 and 10mg irinotecan, re-shake and use spray drying method to prepare 30% UCN-2, 30% irinotecan, 20% UCN-2 and 10% irinotecan microspheres 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 mouse lung cancer is about 60 days.

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PUM

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Abstract

An anti-cancer combination containing a phosphoinositide3-kinase inhibitor (PI3Ki) and / or a topoisomerase inhibitor is a sustained-release injection, which contains a sustained-release microsphere and a menstruum. The sustained-release microsphere contains PI3Ki and / or topoisomerase inhibitor and sustained-release auxiliary materials; the menstruum is an ordinary menstruum or a special menstruum containing a suspending agent. The viscosity of the suspending agent is 100cp to 3000cp (at the temperature of 20 DEG to 30 DEG) and the suspending agent is selected from carboxymethylcellulose sodium, etc. The sustained-release auxiliary materials are selected from a polyphosphonate copolymer of 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), and the like, or a copolymer of polyphosphate ester and polylactic acid, polifeprosan, dienoic fatty acid or decanedioic acid, a copolymer or a mixture of p(erucic acid dimer-decanedioic acid) or a copolymer or a mixture of p(boletic acid-decanedioic acid). The anti-cancer combination is also made into a sustained-release implanting agent, which can be injected or placed in or around tumor to maintain the effective medicine density for more than 40 days. The anti-cancer combination can also obviously reduce the general reaction of the medicine and selectively enhance the curing effect of non-operational therapies such as radiotherapy and chemotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a phosphoinositide 3-kinase inhibitor and / or a topoenzyme inhibitor, 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, 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. In addition, blood vessels, connective tissu...

Claims

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Application Information

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IPC IPC(8): A61K31/553A61K31/4745A61K9/08A61K9/00A61K47/30A61P35/00
Inventor 孙娟刘玉燕孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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