Slow released anticancer medicine preparation with both amrubicin and its synergist

A technology of amrubicin and anticancer drugs, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems such as increased tolerance and treatment failure

Inactive Publication Date: 2006-11-08
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098]Put 90, 90, and 80 mg of polyphenylene propane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20: 80) copolymers into 3 containers respectively, and add 100 ml of dichloromethane to each , after dissolving and mixing, add medicine (10mg pemetrexed, 10mg amrubicin, 10mg pemetrexed and 10mg amrubicin), shake up again and use spray-drying method to prepare containing 10% pemetrexed, 10% amrubicin, 10% pemetrexed and 10% amrubicin microspheres for injection, and then suspend the microspheres in normal saline containing 15% mannitol to prepare the corresponding suspension Extended-release injections. The drug release time of the obtained slow-release injection in the physiological saline in vitro is 10-15 days, and the drug release time in the mouse subcutaneous is about 20-30 days.

Embodiment 2

[0100] 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:

[0101] (a) 1-40% amrubicin, arubicin, idarubicin, doxorubicin, epirubicin, valrubicin or pirarubicin;

[0102] (b) 1-50% of 6-mercaptopurine, pemetrexed, disodium pemetrexed, lumitrexed, deoxyfluridine, floxuridine, flutamide, mercaptopurine, thioguanine, Carmofur, Tegafur, Zalcitabine, Emtricitabine, Galitabine, Ibacitabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine , mitoquinone, mitotane, cytarabine, hydroxyurea, 5-fluorouridine, capecitabine, gemcitabine, fludarabine, raltitrezhan, raltitrexed, dexrazoxane, cla Drabine, norarexed, or pentoside; or

[0103] (c) 1-40% amrubicin, arubicin, idarubicin, doxorubicin, epirubicin, valrubicin or pirarubicin and 1-50% 6-mercapto Purine, 5-Fluorouracil, Pemetrexed, Pemetrexed Disodium, Lumitrexed, Deoxyfl...

Embodiment 3

[0105] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the sustained-release auxiliary material used is polylactic acid (PLA), and its molecular weight peak value is 30000-50000; the contained anticancer active ingredient and its weight percentage are :

[0106] (a) 1-40% amrubicin, arubicin, idarubicin, doxorubicin, epirubicin, valrubicin or pirarubicin;

[0107] (b) 1-50% of 6-mercaptopurine, pemetrexed, disodium pemetrexed, lumitrexed, deoxyfluridine, floxuridine, flutamide, mercaptopurine, thioguanine, Carmofur, Tegafur, Zalcitabine, Emtricitabine, Galitabine, Ibacitabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine , mitoquinone, mitotane, cytarabine, hydroxyurea, 5-fluorouridine, capecitabine, gemcitabine, fludarabine, raltitrezhan, raltitrexed, dexrazoxane, cla Drabine, norarexed, or pentoside; or

[0108] (c) 1-40% amrubicin, arubicin, idarubicin, doxorubicin, epirubicin, va...

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PUM

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Abstract

The slow released anticancer medicine injection containing both amrubicin and its synergist 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 carboxymethyl cellulose, etc. and with viscosity of 100-3000 cp at 25 deg.c. The effective anticancer component is amrubicin, idarubicin, etc and/or antimetabolite composition selected from carmofur, tegafur, zalcitabine, etc. The slow releasing supplementary material is selected from EVAc, sebacic acid copolymer, lactic acid polymer, etc. The slow released microsphere may be also prepared into slow released implanting agent set around or inside the tumor to strengthen the chemotherapy or radiotherapy effect.

Description

(1) Technical field [0001] The invention relates to an anticancer drug sustained-release agent loaded with amrubicin and its synergist, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release compound anticancer drug containing amrubicin and / or its synergist, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As a new anticancer drug, amrubicin ((+)-(7S, 9S)-9-acetyl-9-amino-7-[(2-deoxy-β-D-erythro-pyranpental (sugar)oxyl]-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-tetracenedione) showed obvious therapeutic effect on solid cancer. However, in the rabbit chronic toxicity experimental model, the cardiotoxicity (Invest.New Drug, 15,219-225 (1997)) shown by anthracycline compounds such as amrubicin and doxorubicin has greatly limit its clinical application. In addition, many anthracyclines exert their antitumor effects through their metabolites. For example, amrubicin is easily reduced ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/10A61K31/704A61K45/06A61K47/24A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42
Inventor 孙娟
Owner JINAN KANGQUAN PHARMA TECH
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