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Anticancer slow release agent of anticancer antibiotics and its progression agent

A technology of antibiotics and synergists, applied in the field of medicine, can solve the problems of enhanced tolerance of anticancer drugs and treatment failure

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

Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0120] Put 90, 90 and 80 mg of polystyrene (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into (A), (B) and (C) three Then add 100 ml of dichloromethane to each container. After dissolving and mixing, add 10m doxorubicin, 10mg colchicine, 10mg doxorubicin and 10mg colchicine, shake well and spray The microspheres for injection containing 10% doxorubicin, 10% colchicine, 10% doxorubicin and 10% colchicine are prepared by drying method. Then the microspheres are suspended in physiological saline containing 15% mannitol to prepare the corresponding suspension type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20℃-30℃). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

Embodiment 2

[0122] The method steps for processing into a sustained-release injection are the same as in Example 1, but the difference is that the anti-cancer active ingredients and their weight percentages are:

[0123] (a) 2-40% bleomycin, daunorubicin, doxorubicin, triiron adriamycin, epirubicin, 7-O-methyl Noga-4'-epirubicin, Diethoxyacetoxydoxorubicin, Mitomycin C, Actinomycin D, Nocardin, Nocardin, Nocardomycin, Nogamycin, Mitorubin, Polyviscosity Bacteriocin E, Pyrizomycin, Dirithromycin, Antoxomycin, Pelomycin, Puromycin, Spaamycin, Anthramycin, Caminomycin, Puromycin, Axorubicin Bicin, Aclarithromycin-B, Idarubicin, Serpentine, Clarithromycin, Adazol Hydrochloride, Adazol, Doxorubicin, Epirubicin, Valrubicin, Pirubicin, losanantrone, losoxantrone, mitoxantrone, piroxantrone, tiloxantrone or lorzocin;

[0124] (b) 2-40% of colchicine, cell relaxin, α-naphthol, β-naphthol, acodazole, procodazole, arsenic, giradazole or nocodazole; or

[0125] (c) 2-40% bleomycin, daunorubicin, adriamyc...

Embodiment 3

[0127] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into three containers (A), (B) and (C), and then add 100 ml of dichloromethane to each, dissolve and mix well , Respectively add 30mg carboplatin, 30mg cyclophosphamide, 15mg epirubicin and 15mg cyclophosphamide into three containers, shake up again and use spray drying method to prepare 30% epirubicin and 30% cyclophosphamide , 15% epirubicin and 15% cyclophosphamide injection microspheres. The dried microspheres were suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare the corresponding suspension type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20℃-30℃). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

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Abstract

Disclosed is a compound anticancer slow release 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 specific dissolvent containing suspension adjuvant, The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the anticancer active constituents include anticancer antibiotics and / or anticancer antibiotic synergistic agent, the slow release auxiliary material is selected from ethylene-vinylacetate copolymer, polifeprosan, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid) copolymer, poly(fumaric acid-sebacylic acid) copolymer, 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, medicament and radiation.

Description

(1) Technical field [0001] The invention relates to a compound anticancer drug slow-release agent containing anticancer antibiotics, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release anti-cancer drug containing an anti-cancer antibiotic and / or its synergist, which is mainly a sustained-release injection and a sustained-release implant. (2) Background technology [0002] At present, cancer treatment still mainly includes surgery, radiotherapy and chemotherapy. Surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug concentration or therapeutic dose locally on the tumor. The effect is poor and the toxicity is high. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et ...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/704A61K9/10A61P35/00
Inventor 刘玉燕
Owner JINAN KANGQUAN PHARMA TECH