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Slow released anticancer medicien containing both platinum compound and its synergist

A technology of compounds and synergists, applied in the field of slow-release anticancer drugs, which can solve problems such as enhanced resistance of anticancer drugs and treatment failure

Inactive Publication Date: 2006-11-08
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

[0104] Put 90, 90 and 80 mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymers into (A), (B) and (C) three In two containers, add 100 milliliters of dichloromethane in each, after dissolving and mixing, add 10m sciplatin, 10mg colchicine, 10mg sibplatin and 10mg colchicine respectively, shake up again and use the spray drying method to prepare the 10% Suplatin, 10% Colchicine and Microspheres for Injection of 10% Suplatin and 10% Colchicine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20°C-30°C). 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

[0106] 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:

[0107] or

[0108] (b) 1-30% of sulfoplatin, bicycloplatin, eberplatin, meciplatin, cisliplatin or picoplatin and 2-40% of colchicine, cytochalasin, α-naphthol, β-naphthalene Combinations of phenol, alcodazole, procodazole, arsenic, giradazole, or nocodazole.

Embodiment 3

[0110] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into three containers (A), (B) and (C) respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well , add 30mg bicycloplatinum, 30mg cyclophosphamide, 15mg bicycloplatin and 15mg cyclophosphamide to three containers respectively, shake up again and prepare 30% bicycloplatinum, 30% cyclophosphamide, 15% bicyclo Injectable Microspheres of Platinum and 15% Cyclophosphamide. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20°C-30°C). 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 slow released injection containing both platinum compound and its synergist consists of slow released microsphere and solvent. The solvent is special solvent containing suspending agent, and the suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The effective anticancer component is platinum compound dicycloplatin, etc or the composition of platinum compound and platinum compound synergist selected from antimitotic medicine and alkylating agent. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, poly (erucic acid dipolymer-sebacic acid), poly (fumaric acid-sebacic acid), etc. The slow released microsphere may be also prepared into slow released implanting agent set or injected to in tumor to lower the systemic toxic reaction, raise the local tumor medicine concentration and to raise chemotherapeutic and radiotherapeutic effect.

Description

(1) Technical field [0001] The invention relates to a compound anticancer drug sustained-release agent containing platinum compounds, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing platinum compounds and their synergists, mainly slow-release injections and slow-release implants. (2) Background technology [0002] Currently, cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment 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. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "Intra...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/282A61K31/555A61K45/00A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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