Anticancer medicine composition containing antimetabolite

An anti-cancer drug and anti-metabolism technology, applied in the direction of non-active ingredients of polymer compounds, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as increased resistance of anti-cancer drugs and treatment failure

Inactive Publication Date: 2006-10-18
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 80 mg of polylactic acid (PLGA) with a peak molecular weight of 15,000-25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of 5-FU and 10 mg of cyclophosphamide, re-shake, and then vacuum-dry to remove the organic solvent . The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anti-solid tumor pharmaceutical composition (sustained-release implant) containing 10% 5-FU and 10% cyclophosphamide. All are percentages by weight. The release time of the sustained-release implant in physiological saline in vitro is 14-21 days, and the release time in mouse subcutaneous is 30-45 days.

Embodiment 2

[0100] As described in Example 1, the difference is that the anticancer active ingredients are 1-50% by weight of 6-mercaptopurine, 5-fluorouracil (5-FU), pemetrexed, pemetrexed disodium, Lumitrexed, deoxyfluridine, fluoxuridine, mercaptopurine, thioguanine, methotrexate, carmofur, tegafur, zalcitabine, emtricitabine, galocitabine, i Batabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine, Mitoquinone, Mitotane, Cytarabine, Hydroxyurea, 5-Fluorouridine, Cardiac Petabine, gemcitabine, fludarabine, raltitrexam, raltitrexed, dexrazoxane, cladribine, noratrexed or pentosine with 1-50% cyclophosphamide, melphalan, Lianke Ning, Ifosfamide, 4H-peroxycyclophosphamide, Dephosphamide, Mafosfamide, Pefosfamide, Hexamethazine, Cantharidin, Norcantharidin, Manlusufan, Quaosufan, Ritrasufan, Improsufan, Etoglu, Pipobromane, Piposufan, Aining, Epoxypiperazine, Benzotepa, Purimantipa, Metutepa, Uritinib Combinations of Piper or Azatepa.

Embodiment 3

[0102] Put 70 mg of polylactic acid (PLGA) with a peak molecular weight of 25,000-35,000 into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of methotrexate and 10 mg of paclitaxel, re-shake, and then vacuum dry to remove the organic solvent . The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 20% ​​methotrexate and 10% paclitaxel. All are percentages by weight. The release time of the sustained-release implant in physiological saline in vitro is 15-20 days, and the release time in mouse subcutaneous is 30-40 days.

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PUM

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Abstract

The anticancer medicine composition connecting antimetabolite includes effective anticancer component and medicinal supplementary material, and features the effective anticancer component, which includes antimetabolite and antimetabolite synergist selected from bichlorethamm medicine, taxol anticarcinogen, and tetrazine. The medicinal supplementary material is mainly biocompatible and degradable absorptive polymer. The anticancer medicine composition is mainly slow released implantation preparation or slow released injection. The slow released injection consists of slow released microballoon and solvent. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.

Description

(1) Technical field [0001] The invention relates to an anticancer drug composition, which belongs to the technical field of drugs. (2) Background technology [0002] Malignant tumors have become the main cause of death from diseases. Although various new treatment methods are constantly emerging, the current treatment of cancer still 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/10A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42
Inventor 孙中先
Owner JINAN SHUAIHUA PHARMA TECH
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