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Anti-cancer slow release injection comprising anticancer antibiotics

A slow-release injection and antibiotic technology, applied in the field of medicine, can solve the problems of poor curative effect, difficult operation, and many complications.

Inactive Publication Date: 2007-03-07
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

[0121] 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 Paclitaxel and 10 mg doxorubicin were re-shaken to prepare microspheres for injection containing 10% paclitaxel and 10% doxorubicin by spray-drying method. 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

[0123] 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:

[0124] (1) 2-40% paclitaxel, docetaxel, 2'-hydroxypaclitaxel, 10-deacetylpaclitaxel, or 7-epi-paclitaxel; or

[0125] (2) 2-40% of bleomycin, daunomycin, arubicin, adriamycin, epirubicin, edarubicin, pirarubicin, valrubicin, mitomyces or

[0126] (3) 2-40% paclitaxel, docetaxel and 2-40% bleomycin, daunorubicin, alarubicin, adriamycin, epirubicin, edarubicin, pirarubicin Combinations of bicin, valrubicin, mitomycin C, actinomycin D, loxoxantrone, mitoxantrone, pyroxantrone, tiloxantrone, or clozocin.

Embodiment 3

[0128] 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 doxorubicin and 15 mg of nimustine, re-shake and vacuum Dry to remove organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 10% doxorubicin and 10% nimustine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain 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 antibiotic agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The anticancer active constituents include anticancer antibiotics and / or anticancer antibiotic synergistic agent, the anticancer antibiotic synergistic agent is selected from anti-taxone, alkyl agent and / or plant alkaloids, the slow release auxiliary materials are selected from Polifeprosan, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), ethylene-vinylacetate copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release microspheres can also be prepared into slow release implanting agent for lowering down the whole body toxicity reaction of the anti-cancer medicament, selectively increasing the tumor local medicinal concentration, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release injection and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides an anticancer drug slow-release preparation containing anticancer antibiotics and / or anticancer antibiotic synergists, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, anticancer antibiotics have been widely used in the treatment of various malignant tumors, and the effect is more obvious. However, its obvious systemic toxicity greatly limits the application of this drug. Not only that, blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the effect of chemotherapy drugs on the surrounding tumor and tumor tissue. Penetration an...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61K31/337A61K31/704A61P35/00
Inventor 高化兰
Owner JINAN KANGQUAN PHARMA TECH
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