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Anti-cancer drug slow release injection containing gemcitabine

A technology for sustained-release injections and drugs, which is applied in antineoplastic drugs, drug combinations, drug delivery, etc., and can solve problems such as treatment failure of tolerance and differences in sensitivity of chemotherapeutic drugs

Inactive Publication Date: 2010-02-03
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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  • Anti-cancer drug slow release injection containing gemcitabine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0137] Put 80 mg of polystyrene (p-carboxyphenyl propane (p-CPP): sebacic acid (SA) as 20: 80) copolymer into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg Pemetrexed and 7-hydroxy-staurosporine, re-shake and spray-dry to prepare microspheres for injection containing 10% pemetrexed and 10% 7-hydroxy-staurosporine . Then the microspheres were 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 of the sustained-release injection under the skin of mice is about 20-30 days. The viscosity of the injection is 400cp-600cp (at 20℃-30℃).

Embodiment 2

[0139] The method steps of being processed into sustained-release injections are the same as those in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0140] (1) 1-40% of pemetrexed, pemetrexed disodium, lumitrexed, raltitrexed, raltitrexed, noradrexed, carmofur, dexrazoxane, tegafur Fluoride, temozolomide, zalcitabine, emtricitabine, galotabine, ibatabine, amcitabine, decitabine, flucitabine, enocitabine, midazocitabine, capecitabine Bing, gemcitabine, fludarabine, or cladribine;

[0141] (2) 1-40% of 7-hydroxy-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkylphosphocholine, 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- Phosphocholine, inositol polyphosphate, cyclosporine A, tetradecylphosphorylcholine, h...

Embodiment 3

[0144] Put 70 mg of polylactic acid (PLGA, 75:25) with a molecular weight peak of 65000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of raltitrexed and 15 mg of 7-ethyl-10-hydroxycamptotheca Alkali, shake again and vacuum dry to remove organic solvent. The dried drug-containing solid composition was frozen and pulverized to prepare a micropowder containing 15% raltitrexed and 15%-7ethyl-10-hydroxycamptothecin, and then suspended in a 1.5% sodium carboxymethyl cellulose solution. In physiological saline, the corresponding suspension-type sustained-release injection was prepared. The release time of the sustained-release injection in physiological saline in vitro is 20-35 days, and the release time of the sustained-release injection under the skin of mice is about 35-50 days. The viscosity of the injection is 480cp-620cp (at 20℃-30℃)

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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 compound anticancer drug sustained-release preparation, which belongs to the technical field of drugs. Specifically, the present invention provides a compound anticancer drug sustained-release preparation containing antimetabolites and / or their synergists, mainly sustained-release injections and sustained-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 locally in the tumor, with poor effect and high toxicity. Simply increasing the drug or radiation dose is limited by systemic toxicity. See Kong Qingzhong et al. "Intratumoral placement of cispla...

Claims

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Application Information

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Patent Type & Authority Applications(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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