Compound platinum medicine slow-release preparation

A technology of platinum-based drugs and sustained-release preparations, applied in the field of compound platinum-based drug sustained-release preparations, can solve problems such as increased tolerance of anticancer drugs and treatment failure

Inactive Publication Date: 2006-10-25
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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Put 80mg of polyphenylpropanol (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, add 10mg The cisplatin and 7-hydroxyoxy-staurosporin were shaken again and spray-dried to prepare injection microspheres containing 10% cisplatin and 10% 7-hydroxyoxy-staurosporin. Then the microspheres are suspended 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 10-15 days, and the release time under the skin of mice is about 20-30 days.

Embodiment 2

[0135] The method steps for processing into a sustained-release injection are the same as in Example 1, but the difference is that the anti-cancer active ingredients and their weight percentages are:

[0136] (1) 2-30% cisplatin, carboplatin, omaplatin, dexomaplatin, heptanoplatin, lobaplatin, nedaplatin or oxaliplatin;

[0137] (2) 2-40% of 7-hydroxyoxy-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkyl phosphocholine, 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-glyceryl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-glyceryl-3 -Choline Phosphate, Inositol Polyphosphate, Cyclosporin A, Tetradecyl Phosphate, Hexadecyl Phosphate (NNN-Trimethyl) Hexanolamine, Octadecyl Phosphate or Ten Octyl-[2-(N-methylpiperidine)ethyl]-phosphate; or

[0138] (3) 2-30% of cisplatin, carboplatin, omaplatin, dexomaplatin, heptanoplatin, lobaplatin, nedaplatin or ox...

Embodiment 3

[0140] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into a container, add 100ml of dichloromethane, dissolve and mix well, add 15mg of carboplatin and 15mg of 7-ethyl-10-hydroxycamptothecin, Shake well and vacuum dry to remove organic solvents. The dried drug-containing solid composition was freeze-pulverized into a micropowder containing 10% carboplatin and 10% 7-ethyl-10-hydroxycamptothecin, and then suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose In, the corresponding suspension type sustained-release injection was prepared. The release time of the sustained-release injection in vitro in physiological saline is 20-35 days, and the release time under the skin of mice is about 35-50 days.

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Abstract

The present invention relates to a compound platinum medicine slow-released preparation. It is a slow-released injection formed from slow-released microsphere and solvent, in which the slow-released microsphere includes anticancer effective component and slow-released auxiliary material. The solvent is general solvent or special solvent containing suspension adjuvant. The anticancer effective component includes platinum medicines of omaplatin, heptylplatin, loplatin, neidaplatin or oxaliplatin and/or platinum medicine synergist selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogues and/or DNA repairase inhibitor, the slow-released auxiliary material is selected from polylactic acid copolymer, EVAc and sebacic acid copolymer, etc. The viscosity of suspension adjuvant is 100 cp-3000 cp (20 deg.C-30 deg.C) and the suspension adjuvant is selected from sodium cellulose glycollate. The slow-released microsphere also can be made into slow-released implant preparation.

Description

(1) Technical field [0001] The invention relates to a compound platinum drug sustained-release agent, 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, which are mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] At present, the treatment of cancer still mainly includes surgery, radiotherapy and chemotherapy. Surgical treatment not only fails to remove scattered tumor cells, 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 locally on the tumor. The effect is poor and the toxicity is high. However, simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/282A61K31/555A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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