Anticancer compound including taxanes and phosphatidylinostitol 3-kinase inhibitor

A kinase inhibitor, phosphoinositide technology, applied in the field of anticancer compositions, 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

[0101] 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 paclitaxel, 20mg 7-hydroxyl-staurosporine, 10mg paclitaxel and 10mg 7-hydroxyl-staurosporine respectively, and prepare 20% paclitaxel, Microspheres for injection of 20% 7-hydroxy-staurosporine, and 10% paclitaxel and 10% 7-hydroxy-staurosporine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 60-70 days, and the release time in mouse subcutaneous liver cancer is more than 60 days.

Embodiment 2

[0103] 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:

[0104] (1) 5-40% paclitaxel or docetaxel;

[0105] (2) 1-40% of 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkyl phosphorylcholine, hexadecyl phosphate Choline, octadecyl-(1,1-dimethyl-4-piperidine) phosphate, 1-O-hexadecyl-2-O-methyl-rac-glyceryl-3-phosphocholine , 1-O-octadecyl-2-O-methyl-rac-propanetriyl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-propanetriyl-3 - Phosphocholine, inositol polyphosphate, cyclosporin A, tetradecylphosphorylcholine, hexadecylphosphoryl (N-N-N-trimethyl)hexanolamine, octadecylphosphorylcholine or decadecylphosphorylcholine Octyl-[2-(N-methylpiperidinium)ethyl]-phosphate; or

[0106] (3) 5-40% paclitaxel and 1-40% 7-hydroxyl-staurosporine, 7-O-alkyl-staurosp...

Embodiment 3

[0108] 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 docetaxel, 30mg UCN-02, 20mg docetaxel and 10mg UCN-02, reshake and use spray drying method to prepare 30% docetaxel, 30% UCN-02, 20% docetaxel and 10% UCN -02 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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Abstract

The invention relates to an anti-cancer compound as a slow release injection which contains taxone and / or phosphoinositide 3-kinase restrainer, 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 taxone and / or phosphoinositide 3-kinase restrainer, 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 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 taxane and / or a phosphoinositide 3-kinase inhibitor, which is an anticancer sustained-release injection and a sustained-release implant, and belongs to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, taxanes 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 placement of UCN-02 plus systemic UCN-02 to tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/337A61K31/553A61K45/06A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00A61K47/26
Inventor 孙娟邹会凤刘恩祥苏红清
Owner JINAN KANGQUAN PHARMA TECH
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