Gemcitabine-containing anti-cancer medicine sustained-release injection

A technology for sustained-release injections and drugs, which is applied in the fields of sustained-release injections, sustained-release implants, and compound anticancer drug sustained-release preparations, and can solve problems such as differences in chemotherapeutic drug sensitivity and failure of tolerance therapy.

Inactive Publication Date: 2009-05-13
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 polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml methylene chloride, dissolve and mix well, then add 10mg Pemetrexed and 7-hydroxyl-staurosporine, 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-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, tetradecylphosphorylcholine...

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 subcutaneously is about 3550 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 cancer therapy drug sustained-release injection containing gemcitabine. The injection comprises sustained-release microspheres and dissolvent, wherein, the sustained-release microspheres comprise active ingredients for cancer therapy and sustained-release auxiliary materials, and the dissolvent is special dissolvent containing suspending agent. The active ingredients for cancer therapy comprise antimetabolite of gemcitabine or antimetabolite selected from zalcitabine, emtritabine, galocitabine, ibacitabine, ancitabine, decitabine, flurocitabine, enocitabine, imidazoletabine, capecitabine, gemcitabine, fludarabine or cladribine, and / or antimetabolite synergist selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogs and / or DNA repair enzyme inhibitor; the sustained-release auxiliary materials comprise polifeprosan, bi-fatty acid, decanedioic copolymer, polylactic copolymer and EVAc; the viscocity of the suspending agent is 100cp to 3000cp (at 20 to 30 DEG C) and the suspending agent is selected from sodium carboxymethyl cellulose. The sustained-release microspheres can also be produced into sustained-release implant, and by injecting or positioning the sustained release agent in tumor or tumor margin, the efficacy of non-operative treatment such as radiation treatment and chemical treatment can be enhanced.

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 Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K9/10A61K45/06A61K31/519A61K31/553A61K47/34A61P35/00
Inventor 孔庆忠孙娟刘玉燕宋邦强
Owner SHANDONG LANJIN PHARMA
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