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A sustained release injection carrying clorfarabine and cytotoxic drug

A technology of slow-release injections and slow-release implants, which is applied in the field of slow-release injections and slow-release implants, slow-release injections and their preparation, and can solve problems such as difficult operation, poor curative effect, and many complications

Pending Publication Date: 2006-12-13
JINAN KANGQUAN PHARMA TECH
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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

[0110] 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 clorabine were re-shaken and spray-dried to prepare microspheres for injection containing 10% actinomycin D and 10% clorabine. 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

[0112] 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:

[0113] 2-40% clorabine with 2-40% melphalan, 4H-cyclophosphamide peroxide, vinorelbine, tamoxifen, methotrexate, doxorubicin, epirubicin, actinomycin D, the combination of tamustine, amustine, semustine or ramustine; the sustained-release excipients used are racemic polylactic acid, racemic polylactic acid / glycolic acid copolymer, monomethyl Polyethylene 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 / ethanol acid copolymer.

Embodiment 3

[0115] 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 clorabine and 15 mg of tamustine, re-shake and vacuum Dry to remove organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% clorabine and 15% tamustine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding 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

Disclosed is an anticancer slow release injection carrying both clofarabine and cytotoxic drugs, which comprises slow release micro-balloons 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 clofarabine and cytotoxic drugs selected from adriamycin, pidorubicin, Melphalan, 4-hydroperoxycyclophosphamide, actinomycin D, Vinorelbine, Tamoxifen, Tallimustine, Atrimustine, Semustine and ranimustine, the slow release auxiliary materials are selected from polylactic acid and copolymer, monomethyl polyethylene glycol, polyethylene glycol and polylactic acid copolymer, EVAc, aliphatic acid and sebacylic acid copolymer, The viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing clorabine 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 clorabine 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 conventional chemotherapy to for...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/7076A61K31/675A61K31/704A61K31/4025A61K31/538A61K47/34A61K47/38A61P35/00
Inventor 孙晋海
Owner JINAN KANGQUAN PHARMA TECH
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