Slow-release injection contg. platinum compounds and cellulotoxic medicines

A technique for sustained-release injections and compounds, applied in the fields of sustained-release injections and sustained-release implants, sustained-release injections and their preparation, which can solve problems such as difficult operation, poor curative effect, and many complications

Inactive Publication Date: 2006-11-29
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, solid sustained-release implants (Chinese Patent No. ZL96115937.5; ZL97107076.8) and existing sustained-release microspheres for the treatment of brain tumors (ZL00809160.9) or U.S. Patent (US5,651,986) all have inadequacies. Easy operation, poor curative effect, many complications, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] 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 Actinomycin D and 10 mg eplatin were re-shaken and spray-dried to prepare microspheres for injection containing 10% actinomycin D and 10% eplatin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (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

[0114] 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:

[0115] 2-40% sulfoplatin, dicycloplatin, eriplatin, meciplatin, cisciplatin or picoplatin with 2-40% melphalan, 4H-peroxocyclophosphamide, vinorelbine, tamoxifen , methotrexate, doxorubicin, epirubicin, actinomycin D, tamustine, amustine, semustine or a combination of ramustine; the extended release excipient used is racemic polymer Lactic acid, racemic polylactic acid / glycolic acid copolymer, monomethylpolyethylene glycol / polylactic acid, monomethylpolyethylene glycol / polylactic acid copolymer, polyethylene glycol / polylactic acid, polyethylene glycol / Polylactic acid copolymer, carboxy-terminated polylactic acid or carboxy-terminated polylactic acid / glycolic acid copolymer.

Embodiment 3

[0117] 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 sciplatin and 15 mg of tamustine, re-shake and dry in vacuum Remove organic solvents. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% salivaplatin and 15% tamustine, and then suspended in physiological saline containing 1.5% carboxymethylcellulose sodium to prepare the corresponding mixed Suspension-type sustained-release injection with a viscosity of 300cp-400cp (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

A slow-release anticancer injection is composed of the slow-release microballs containing active component and slow-releasing auxiliary and the special solvent containing the suspending aid. Said active component is the combination of Pt compound chosen from dicycloplatinum, etc and the cellulotoxic medicine chosen from doxorubicin, vinorelbine, etc. Said slow-releasing auxiliary is chosen from polylactic acid or its copolymer, monoethyl polyethanediol or its copolymer, EVAc, etc.

Description

(1) Technical field [0001] The invention relates to a slow-release injection simultaneously carrying platinum compounds and cytotoxic drugs and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing platinum compounds and cytotoxic drugs, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As one of the conventional treatment methods for cancer, chemotherapy drugs have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its obvious systemic toxicity greatly limits the application of this drug. [0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conven...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/282A61K31/555A61K47/34A61P35/00A61K47/32
Inventor 孔庆忠张红军俞建江
Owner SHANDONG LANJIN PHARMA
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