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Anti-cancer drugs slow release agent comprising anticancer antibiotics and synergist thereof

A technology of anticancer drugs and sustained-release preparations, which is applied in the field of sustained-release injections, sustained-release implants, compound anticancer drug sustained-release preparations, and can solve problems such as treatment failure and increased tolerance

Inactive Publication Date: 2010-05-19
SHANDONG LANJIN PHARMA
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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

[0113] 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 doxorubicin, 10mg pemetrexed and 10mg doxorubicin), re-shake and use spray drying method to prepare 10% pemetrexed, 10% Doxorubicin, 10% pemetrexed and 10% doxorubicin injection microspheres, and then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension sustained-release injection. 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

[0115] 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:

[0116] (a) 5-30% of bleomycin, daunomycin, doxorubicin, triiron doxorubicin, epirubicin, 7-O-methylnoga-4'-epirubicin, Diethoxyacetydoxorubicin, Mitomycin C, Actinomycin D, Nocardycin, Nocardioerythrin, Nocardycin, Nogamycin, Mitomycin, Polymycin Mycocin E, pilimycin, dirithromycin, antramycin, pelomycin, puromycin, spamycin, anthramycin, caraminomycin, puromycin, aromycin Bixing, Aclarubicin-B, Idarubicin, Serpentin, Clarithromycin, Adazol Hydrochloride, Adazol, Doxorubicin, Epirubicin, Valrubicin, pirarubicin, loxantrone, loxoxantrone, mitoxantrone, piroxantrone, tiloxantrone, or clozocin;

[0117] (b) 5-40% of 6-mercaptopurine, pemetrexed, disodium pemetrexed, lumitrexed, deoxyfluridine, fluoxuridine, mercaptopurine, thioguanine, carmofur, Tegafur, Zalcitabine, Em...

Embodiment 3

[0120] 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 :

[0121] (a) 5-40% of 6-mercaptopurine, pemetrexed, disodium pemetrexed, lumitrexed, deoxyfluridine, fluoxuridine, mercaptopurine, thioguanine, carmofur, Tegafur, Zalcitabine, Emtricitabine, Gallocitabine, Ibacitabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine, Mitoquinone , mitotane, cytarabine, hydroxyurea, 5-fluorouridine, capecitabine, gemcitabine, fludarabine, raltitrezhan, raltitrexed, dexrazoxane, cladribine, nor latrexed or pentoside; or

[0122](b) 5-30% of bleomycin, daunorubicin, doxorubicin, triiron doxorubicin, epirubicin, 7-O-methylnoga-4'-epirubicin, Diethoxyacetydoxorubicin, Mitomycin C, Actinomycin D, Nocardycin, N...

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Abstract

Disclosed is an anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow releaseauxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer antibiotics are selected from Idarubicin, Valtaxin, Pirarubicin and Mitoxantrone, The anti-metabolite drugs are selected from Pemetrexed, Carmustine, Tegafur, Zalcitabine, Emtritabine, Galocitabine, Ibacitabine, Ancitabine, Decitabine, Flurocitabine, Enocitabine, Imidazoletabine, Capecittabine, Gemcitabine, Fludrarbine, Raltitrexed, Dexrazoxane, Cladribine, Nolatrexed and folic acid, The slow release auxiliary materials are selected from EVAc, Polifeprosan, sebacylic acid copolymer, lactic acid, 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 injection or placement in or around tumor.

Description

(1) Technical field [0001] The invention relates to an anticancer drug sustained-release agent loaded with anticancer antibiotics and synergists, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release compound anticancer drug containing anticancer antibiotics and / or their synergists, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As a commonly used chemotherapeutic drug, anticancer antibiotics have been widely used in the treatment of various malignant tumors, and the effect is more obvious. However, its unexpected systemic toxicity greatly limits the application of this drug. 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 penetration of chemotherapy drugs around the tumor and in the tumor tissue and diffusion (see Netti et al. "The...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61K31/704A61P35/00A61K47/26
Inventor 孔庆新
Owner SHANDONG LANJIN PHARMA
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