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Anticancer sustained-release implantation agent

A technology of implants and anti-cancer drugs, which is applied in anti-tumor drugs, organic active ingredients, pharmaceutical formulations, etc., and can solve problems such as treatment failure and increased resistance to anti-cancer drugs

Inactive Publication Date: 2008-12-24
JINAN SHUAIHUA 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

[0098]Put 70 mg of polyglycolic acid and glycolic acid copolymer (PLGA, 65:35) with a peak molecular weight of 20000-40000 into a container, add 100 milliliters of dichloromethane, dissolve and mix well, then add 10 mg of colchicine (anti-mitotic drug) and 20mg5-FU (antimetabolite drug), re-shake well and then vacuum dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to prepare an anticancer implant containing 10% colchicine and 20% 5-FU. The drug release time of the anticancer implant in physiological saline in vitro is 15-25 days, and the drug release time of subcutaneous implantation in mice is 30-40 days.

Embodiment 2

[0100] The method steps of being processed into anticancer implants are the same as in Example 1, but the difference is that the anticancer active ingredients contained in the anticancer implants are:

[0101] 5-30% 6-mercaptopurine, 5-fluorouracil (5-FU), pemetrexed, pemetrexed disodium, lumitrexed, deoxyfluridine, fluoxuridine, mercaptopurine, thioguanine Purine, methotrexate, carmofur, tegafur, zalcitabine, emtricitabine, gallocitabine, ibacitabine, ancitabine, decitabine, flucitabine, Nortabine, Mizotabine, Mitoquinone, Mitotane, Cytarabine, Hydroxyurea, 5-Fluorouridine, Capecitabine, Gemcitabine, Fludarabine, Raltitridine, Raltitridine dexrazoxane, cladribine, noratrexed or pentasylate and 5-30% of cytochalasin, mitocloramine, mitorazone, mitoguanidine hydrazone, mitonaphthylamine, mitogen Hydrazine, Mitoquinone, Mitospex, Mitotane, Mitophenamine, Mitozolomide, Mitoransone, Colchicine Salicylate, Colchicine, Colcemid, Cell Relaxation Combinations of naphthol, naphthol, ...

Embodiment 3

[0103] Put 70mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 15000-25000 into a container, add 100ml of dichloromethane, dissolve and mix well, then add 20mg of pemetrexed (antimetabolite drug) and 10mg of Tumor mustard (nitrogen mustard drug), re-shake and vacuum-dry to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer implant containing 20% ​​of pemetrexed and 10% of Zormust. The drug release time of the anticancer implant in the physiological saline in vitro is 15-25 days, and the drug release time when placed subcutaneously in mice is 20-40 days.

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PUM

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Abstract

An anticancer sustained-release implant is characterized in that active anticancer ingredient is wrapped into pharmaceutical excipient to be made into the sustained-released implant or sustained injection. The active anticancer ingredient is the combination of anti-metabolism anticancer medicine and synergistic agent thereof. The synergistic agent is made from mustine drug and / or antimitotic drug and / or plant alkaloids. The pharmaceutical excipient is made from polylactic acid, copolymer of polyglycolic acid and glycolic acid, ethylene-vinyl acetate copolymer, FAD: sebacic acid (SA) copolymer and / or polifeprosan, etc. The sustained-release injection is composed of sustained release microspheres and menstruum, and the menstruum is classified into common menstruum and special menstruum with suspending agent. The suspending agent is made from sodium carboxymethyl cellulose, mannite, etc. and is used for suspending active anticancer ingredients or sustained-release gains or microspheres containing active anticancer ingredients so as to facilitate injection. Partial tumor placement or sustained-release agent injection can reduce medicine systemic toxicity effect as well as can selectively increase medicine concentration at partial tumor to enhance the curative effect of non-operative treatments such as chemotherapeutic drug, radiation therapy, etc.

Description

(1) Technical field [0001] The invention relates to an anticancer implant and belongs to the technical field of medicines. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment not only 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. However, simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82, 1998 (Kong Q et al., J Surg Oncol.1998 Oct; 69 (2): 76-82). [0003] Local placement of antitumor drugs can bet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/519A61K31/475A61K31/4375A61K31/53A61K31/7068A61P35/00
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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