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Anticancer medicine composition of platinum compound and clorfarabine

A technology of anti-cancer drugs and compositions, applied in the field of anti-cancer drug sustained-release agents, sustained-release injections and sustained-release implants, which can solve problems such as treatment failure and enhanced tolerance of anti-cancer drugs

Inactive Publication Date: 2009-12-16
SHANDONG LANJIN PHARMA
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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

[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 Cisplatin and 10 mg clorabine were re-shaken and spray-dried to prepare microspheres for injection containing 10% cisplatin and 10% clorabine. 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% clorabine; or

[0123] (2) 2-40% Clorabine and 1-30% Cisplatin, Carboplatin, Cycloplatin, Heptaplatin, Denaplatin, Cyclopentyl Aminoplatinum, Platinum Blue, Cypromine Platinum, Ethylenediamine Propine Acid platinum, niniplatin, enloplatin, epithioplatin, cispiroplatin, dextromethopretin, isoproplatin, lobaplatin, rice platinum, picoplatin, nedaplatin, omaplatin, oxaliplatin, siplatin, Combinations of spiroplatin, sciplatin, dicycloplatin, eriplatin, meciplatin, cisliplatin, picoplatin, or zeniplatin.

[0124] The excipients used are: racemic polylactic acid, racemic polylactic acid / glycolic acid copolymer, monomethyl polyethylene glycol / polylactic acid, monomethyl polyethylene glycol / polylactic acid copolymer, polyethylene glycol / polylactic acid, pol...

Embodiment 3

[0126] 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, add 15 mg of Sisiplatin and 15 mg of clolarabine, re-shake and dry in vacuo Remove organic solvents. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% cisciplatin and 15% clorabine, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding mixed Suspension-type sustained-release injections. 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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Abstract

The anticancer medicine composition of platinum compound and clorfarabine is slow released injection or slow released implanting agent, and the slow released injection consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is clorfarabine or its composition with platinum compound, cisplatin, carboplatin, etc. The slow releasing supplementary material is polylactic acid or its copolymer, polyethylene glycol, EVAc or other biocompatible polymer. The suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The present invention can inhibit the growth of tumor and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.

Description

(1) Technical field [0001] The invention relates to an anticancer pharmaceutical composition loaded with a platinum compound and its synergist, belonging to the technical field of pharmaceuticals. 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, chemotherapy is still the main treatment for cancer. Among them, platinum compounds are more commonly used. However, traditional chemotherapy is not selective, and it is difficult to form an effective drug concentration or therapeutic dose locally in the tumor. The effect is poor and the toxicity is high. Simply increasing the drug or radiation dose is limited by systemic toxicity. See Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/08A61K31/7076A61K31/282A61K47/38A61K47/08A61K9/08A61P35/00
Inventor 孙娟
Owner SHANDONG LANJIN PHARMA