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Compound recipe anti-cancer drugs slow release agent comprising anticancer antibiotics and synergist thereof

A technology of antibiotics and sustained release agents, applied in the field of compound anticancer antibiotic sustained release agents, which can solve problems such as treatment failure and increased resistance to anticancer drugs

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

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

[0145] Put 80mg of polyphenylpropanine (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, add 10mg Mitomycin C and 7-hydroxyoxy-staurosporin, shake well and spray-dry to prepare injection containing 10% mitomycin C and 10% 7-hydroxyoxy-staurosporin Microspheres. Then the microspheres are suspended in physiological saline containing 15% mannitol to prepare the corresponding suspension type sustained-release injection. 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

[0147] 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:

[0148] (1) 2 30 arubicin, idarubicin, adazo, doxorubicin, epirubicin, valrubicin, pirarubicin, losanantrone, losoxantrone , Mitoxantrone, Piroxantrone, Tiloxantrone or Lorzocin;

[0149] (2) 2-40% of 7-hydroxyoxy-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkyl phosphocholine, hexadecyl phosphate Choline, octadecyl-(1,1-dimethyl-4-piperidine) phosphate, 1-O-hexadecyl-2-O-methyl-rac-glyceryl-3-phosphocholine , 1-O-octadecyl-2-O-methyl-rac-glyceryl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-glyceryl-3 -Choline Phosphate, Inositol Polyphosphate, Cyclosporin A, Tetradecyl Phosphate, Hexadecyl Phosphate (NNN-Trimethyl) Hexanolamine, Octadecyl Phosphate or Ten Octyl-[2-(N-methylpiperidine)ethyl]-phosphate; or

[0150] (3) 2-30% of arubicin, idarubicin, adazol, dox...

Embodiment 3

[0152] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into the container, add 100ml of dichloromethane, dissolve and mix well, add 15mg of valrubicin and 15mg of 7-ethyl-10-hydroxycamptotheca Alkali, shake well and vacuum dry to remove organic solvents. The dried drug-containing solid composition was freeze-pulverized into a micropowder containing 10% valrubicin and 10% 7-ethyl-10-hydroxycamptothecin, and then suspended in a 1.5% sodium carboxymethylcellulose In physiological saline, the corresponding suspension type sustained-release injection was prepared. The release time of the sustained-release injection in vitro in physiological saline is 20-35 days, and the release time under the skin of mice is about 35-50 days.

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PUM

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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 slowrelease auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer effective ingredients include Aclarubicin, Idarubicin, Doxorubicin, Epirubicin, Valtaxin, Pirarubicin, Losaxantrone, Losoxantrone and / or anticancer antibiotic synergistic agents selected from phosphoinositide-3-kinase inhibitor, pyrimidine analogues and / or DNA restoration enzymeinhibitor, the slow release auxiliary materials are selected from polylactic acid copolymer EVAc, or sebacic acid copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C). The slow release microspheres can also be prepared into slow release implanting agent for lowering down the whole body toxicity reaction of the medicament when locally dispensing on the tumor, and for selectively increasing the tumor local medicinal concentration.

Description

(1) Technical field [0001] The invention relates to a compound anticancer antibiotic sustained-release agent, which belongs to the technical field of medicines. Specifically, the present invention provides a slow-release compound anti-cancer drug containing anti-cancer antibiotics and their synergists, mainly slow-release injections and slow-release implants. (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 al. "Intratumor placement of cisplatin p...

Claims

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Application Information

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