Anticancer drug composition loading both platinum compound and tetrazole violet

A kind of anticancer drug, violet technology, applied in the field of slow-release injections and slow-release implants, slow-release anticancer drugs, can solve the problems of anticancer drug resistance enhancement, treatment failure, etc.

Inactive Publication Date: 2007-03-14
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

[0115] 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 of violet tetrazolium were re-shaken and spray-dried to prepare microspheres for injection containing 10% cisplatin and 10% violet tetrazolium. 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

[0117] 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:

[0118] 2-40% tetrazolium violet, tetrazolium bromide, thiazole blue, tetrazolium blue, tetrazolium red, p-iodonitro tetrazolium violet or nitro tetrazolium violet with 1-30% cisplatin, carboplatin, Cycloplatin, heptaplatin, denaplatin, cyclopentylaminoplatinum, platinum blue, cyproamideplatinum, ethylenediaminemalonate platinum, niniplatin, enloplatin, cyclothioplatinum, cisspiroplatin, dexomaplatin, isoplatin Propplatin, lobaplatin, miplatin, picoplatin, nedaplatin, omaplatin, oxaliplatin, spiroplatin, spiroplatin, dicycloplatin, erbaplatin, meciplatin, cisplatin, picoplatin or Combinations of zeniplatin.

[0119] The excipients used are: racemic polylactic acid, racemic polylactic acid / glycolic acid copolymer, monomethyl polyethylene glycol / polylactic acid, monomethy...

Embodiment 3

[0121] 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 Siciplatin and 15 mg of tetrazolium violet, re-shake and dry in vacuum Remove organic solvents. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% cisciplatin and 15% violet tetrazolium, 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

Disclosed is an anti-cancer pharmaceutical composition carrying both platinum-group compounds and tetrazole lonone, characterized in that the pharmaceutical composition is in the form of slow release injection or slow release implanting agent, the slow release injection comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include the combination of tetrazole lonone or its analogues with cisplatin, Carboplatin, Eptaplatin, Enloplatin, Lobaplatin, Nedaplatin, Ormaplatin, Oxaliplatin, the slow release auxiliary materials include polylactic acid and its copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, poly(lactic acid), biological compatible EVAc, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release agent can be injected or placed in or around tumor, or used in combination with non-operative treatment methods such as chemotherapy.

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 drug delivery methods are 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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/41A61K31/282A61K31/555A61K47/34A61P35/00
Inventor 孔庆忠孙娟张红军
Owner JINAN SHUAIHUA PHARMA TECH
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