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Anti-cancer drug slow release injection containing gemcitabine

A sustained-release injection, zalcitabine technology, applied in the direction of antineoplastic drugs, drug combinations, drug delivery, etc., can solve the problems of chemotherapy drug sensitivity difference, tolerance treatment failure, etc.

Inactive Publication Date: 2012-08-15
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the sensitivity of tumor cells to chemotherapeutic drugs varies greatly
Many tumor cells are not sensitive to drugs, and some tumor cells are sensitive in the early stage of chemotherapy, but quickly tolerate it
Especially when anticancer drugs, such as antimetabolites, are used alone, increased tolerance often leads to treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0137] 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 Pemetrexed and 7-hydroxyl-staurosporine were re-shaken and spray-dried to prepare microspheres for injection containing 10% pemetrexed and 10% 7-hydroxyl-staurosporine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. 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. The viscosity of the injection is 400cp-600cp (at 20°C-30°C).

Embodiment 2

[0139] 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:

[0140] (1) 1-40% Pemetrexed, Pemetrexed Disodium, Lumitrexed, Raltitrexed, Raltitrexed, Noratrexed, Carmofur, Dexrazoxane, Tega Fluorine, temozolomide, zalcitabine, emtricitabine, gallocitabine, ibacitabine, ancitabine, decitabine, flucitabine, enoxitabine, midazitabine, capecitabine Bine, gemcitabine, fludarabine, or cladribine;

[0141] (2) 1-40% of 7-hydroxyl-base staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkyl phosphorylcholine, 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-propanetriyl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-propanetriyl-3 - Phosphocholine, inositol polyphosphate, cyclosporine A, tetradecylphosphorylch...

Embodiment 3

[0144] 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, then add 15 mg of raltitrexed and 15 mg of 7-ethyl-10-hydroxycamptotheca Alkali, shake again and dry in vacuo to remove organic solvents. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% raltitrexed and 15% 7-ethyl-10-hydroxycamptothecin, and then suspended in 1.5% sodium carboxymethylcellulose In physiological saline, the corresponding suspension-type sustained-release injection was prepared. The drug release time of the slow-release injection in physiological saline in vitro is 20-35 days, and the drug release time in mice subcutaneous is about 35-50 days. The viscosity of the injection is 480cp-620cp (at 20°C-30°C)

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PUM

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Abstract

The invention relates to an anti-cancer drug slow release injection containing gemcitabine, which comprises slow release microspheres and a menstruum, wherein the microsphere comprises anti-cancer active ingredients and slow release auxiliary materials, and the menstruum is a special menstruum containing a suspending agent; the anti-cancer active ingredients are gemcitabine, or antimetabolites selected from zalcitabine, emtricitabine, galocitabine, ibacitabine, ancitabine, decitabine, flurocitabine, enocitabine, imidazole gemcitabine, capecitabine, gemcitabine, fludarabine or cladribine, and / or antimetabolite potentiating agents selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogue and / or DNA repair enzyme inhibitor; the slow release auxiliary materials are polifeprosan, dienoic fatty acid, decanedioic acid copolymer, polylactic acid copolymer, EVAc and the like; the suspending agent has a viscosity of 100cp-3000cp (20-30 DEG C), and is selected from sodium carboxymethylcellulose and the like. The slow release microspheres can be prepared into slow release implants. When injected or placed into tumors or at peripheries of tumors, the slow release microspheres can enhance the treatment effect of non-operative treatment methods, such as radiotherapy, chemotherapy, etc.

Description

(1) Technical field [0001] The invention relates to a slow-release preparation of compound anticancer drugs, which belongs to the technical field of medicines. Specifically, the present invention provides a slow-release compound anticancer drug containing anti-metabolite drugs and / or their synergists, mainly slow-release injections and slow-release implants. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, 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 in the local tumor, resulting in poor efficacy and high toxicity. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "Intratumoral placement of cisplatin pl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/08A61K9/10A61K31/519A61K31/7068A61K47/34A61P35/00
Inventor 孔庆忠孙娟刘玉燕宋邦强
Owner SHANDONG LANJIN PHARMA
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