Sustained-release agent containing taxone and its synergistic agent

A taxane and sustained-release technology, applied in the field of anti-cancer drug sustained-release, can solve problems such as enhanced tolerance and treatment failure

Inactive Publication Date: 2008-08-20
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...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0129] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Paclitaxel and 7-hydroxyl-staurosporine were re-shaken and spray-dried to prepare microspheres for injection containing 10% paclitaxel and 10% 7-hydroxyl-staurosporine. 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 slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0131] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0132] (1) 2-40% taxane or docetaxel;

[0133] (2) 2-40% of 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkylphosphocholine, 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, cyclosporine A, tetradecylphosphorylcholine, hexacylphospho(N-N-N-trimethyl)hexanolamine, octadecylphosphorylcholine or decadecylphosphorylcholine Octyl-[2-(N-methylpiperidinium)ethyl]-phosphate;

[0134] (3) 2-40% taxane or docetaxel and 2-40% 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystar Sporin, alkylphosphocholine, h...

Embodiment 3

[0136] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of paclitaxel and 15 mg of 7-ethyl-10-hydroxycamptothecin, and re- Shake well and dry under vacuum to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 10% paclitaxel and 10% 7-ethyl-10-hydroxycamptothecin, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose , to prepare the corresponding suspension-type sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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Abstract

The invention discloses a slow-release formulation comprising taxoid and the potentiating agent, which comprises sustained release microsphere and solvent; wherein, the sustained release microsphere comprises effective anticancer component and sustained release accessories; the solvent is common solvent or special solvent comprising suspending agent; the effective anticancer component is divided into the taxoid or the potentiating agent of the the taxoid; the potentiating agent of the the taxoid is selected from phosphoinositide 3-kinase inhibitor and pyrimidine analogue and/ or DNA repair enzyme inhibitor; the sustained release accessories are selected from polylactic acid and the copolymer, ethylene-vinyl acetate copolymer, polifeprosan, di-fatty acid and sebacic acid copolymer, poly (erucic acid dimer - sebacic acid), poly (fumaric acid - sebacic acid) and other copolymers; the suspending agent is selected from sodium carboxymethyl cellulose and other substance; the sustained release microspheres also can be produced into sustained-release implant. The slow-release formulation has the advantages of lowering toxic reaction of whole body through injecting or arranging slow-release formulation into or around tumor, but also selectively improving partial drugs concentration for tumor and strengthening therapeutic effect of non-surgical therapy such as chemotherapy and radiotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer drug sustained-release agent containing taxane and its synergist, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing taxane and / or a taxane synergist, mainly slow-release injections and slow-release implants. (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 concentr...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/06A61K31/337A61K31/407A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00A61K47/10A61K47/32
Inventor 刘玉燕
Owner JINAN KANGQUAN PHARMA TECH
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