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Slow-released prepn containing taxane and its synergist

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

Inactive Publication Date: 2006-10-18
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

[0119]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

[0121] 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:

[0122] (1) 2-40% taxane or docetaxel;

[0123] (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;

[0124] (3) 2-40% taxane or docetaxel and 2-40% 7-hydroxyl-staurosporine, 7O-alkyl-staurosporine, β-methoxystaurosporine , Alkyl phosphorylchol...

Embodiment 3

[0126] 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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PUM

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Abstract

The slow released injection containing taxane and its synergist consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is taxane and / or taxane synergist of phosphorinositide 3-kinase inhibitor, pyrimidine analogue and / or DNA repair enzyme inhibitor; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, etc. The slow released microballoon may be also prepared into implantation preparation. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.

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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/337A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 刘玉燕
Owner JINAN KANGQUAN PHARMA TECH
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