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Compound platinum medicine sustained-release agent

A technology of platinum drugs and sustained-release injections, applied in the fields of sustained-release injections, sustained-release implants, compound anti-cancer drug sustained-release preparations, and can solve problems such as enhanced tolerance of anti-cancer drugs and treatment failures

Inactive Publication Date: 2009-03-11
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0148] Put 80mg of polyphenylpropane (p-CPP: sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Cisplatin and 7-hydroxyl-staurosporine, re-shake and spray-dry to prepare microspheres for injection containing 10% cisplatin 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

[0150] 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:

[0151] (1) 2-30% cisplatin, carboplatin, omaplatin, dexomaplatin, heptaplatin, lobaplatin, nedaplatin or oxaliplatin;

[0152] (2) 2-40% 7-hydroxyl staurosporine, 7-O-alkyl staurosporine, β-methoxy staurosporine, alkyl phosphorylcholine, hexadecyl phosphorylcholine , octadecyl-(1,1-dimethyl-4-piperidine) phosphate, 1-O-hexadecyl-2-O-methyl-rac-propanetriyl-3-phosphocholine, 1 -O-octadecyl-2-O-methyl-rac-glyceryl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-glyceryl-3-phosphate Choline, Inositol Polyphosphate, Cyclosporin A, Tetradecyl Phosphocholine, Hexacyl Phospho(N-N-N-Trimethyl)hexanolamine, Octadecyl Phosphocholine, or Octadecyl Phosphocholine -[2-(N-Methylpiperidinium)ethyl]-phosphate; or

[0153] (3) 2-30% cisplatin, carboplatin, omaplatin, dextro-omaplatin, ...

Embodiment 3

[0155] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, then add 15 mg of carboplatin and 15 mg of 7-ethyl-10-hydroxycamptothecin , shake again and dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 10% carboplatin and 10% 7-ethyl-10-hydroxycamptothecin, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose In the preparation of the corresponding suspension sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 20-35 days, and the drug release time in mice subcutaneous is about 35-50 days.

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PUM

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Abstract

A slow release compound platinum drug is a slow release injection which is composed of slow release microspheres and a dissolvant. The slow release microspheres comprise anticancer active components and a slow release adjuvant, and the dissolvant is a common dissolvant or a special dissolvant containing a suspending agent. The anticancer active components are platinum drugs such as ormaplatin, hetaplatin, lobaplatin, nedaplatin or oxaliplatin, and the like, and / or platinum drug synergists selected from a phosphoinositide-3-kinase inhibitor, pyrimidine analogue and / or a DNA repair enzyme inhibitor; the slow release adjuvant is selected from the copolymer of polylactic acid, EVAc, polifeprosan, sebacic acid copolymer, and the like; the viscosity of the suspending agent is 100cp-3,000cp (at the temperature of 20-30 DEG C), and the suspending agent is selected from sodium carboxymethyl cellulose, and the like. The slow release microspheres can be also made into a slow release implant. By injecting the slow release injection or placing in tumors or around the tumors, the general toxic reaction of the drug can be reduced, the local drug concentration of the tumors can be selectively improved, and the curative effects of non-operative therapies such as radiotherapy, chemotherapy, and the like, can be improved.

Description

(1) Technical field [0001] The invention relates to a sustained release agent of compound platinum drugs, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release compound anticancer drug containing platinum-based drugs and their synergists, mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] Currently, cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment not only cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug concentration or therapeutic dose in the local tumor, resulting in poor efficacy and high toxicity. However, simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "I...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/00A61K45/06A61P35/00
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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