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Anti-cancer medicine composition containing antimetabolite

A technology of anti-cancer drugs and compositions, which is applied in the direction of drug combinations, anti-tumor drugs, active ingredients of heterocyclic compounds, etc., and can solve problems such as difficulty in forming effective drug concentrations

Inactive Publication Date: 2005-07-06
DASEN BIOLOGICAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that the excessive expansive hyperplasia of solid tumors has higher interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity than the surrounding normal tissue. Drug concentration (see KongQingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine to treat brain tumors in rats" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (KongQ et al., J Surg Oncol.1998 Oct;69(2):76-82), simply increasing the dosage is limited by systemic reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Put 90 mg of PLGA (copolymer of glycolic acid and glycolic acid) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix, add 10 mg of gemcitabine, 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 anticancer drug composition containing 10% by weight of gemcitabine. The drug release time of the anticancer drug composition in the physiological saline in vitro is 15-20 days, and the drug release time in the mouse subcutaneous is about 30-40 days.

Embodiment 2

[0050] Embodiment 2. As described in embodiment 1, the difference is that anti-metabolite drugs are:

[0051] (a) 1-50% deoxyfluorouridine, 5-deoxyfluorouridine, fluorouracil, propylthiouracil, butylfluorouracil, bisfluoropyrimidine, 5-fluoropyrimidinol, sodium sulfcaptopurine, thiocarbamide Purine, 6-mercaptopurine, 6-aminopurine hydrochloride, glycine thiopurine, thioguanine, carcinol, hydrazine sulfate, viconol, seroquinone, fencolonine, isopyrone, inhibitor clodronate, clodronate disodium, cycloleucine, dizacitrin, mesinate dichacitrin, berquiqual, oxypurinol, amallide, brombamic acid (sodium ), Bailididine, bromouridine, hexylfluramide, 10-ethyldeazhotrexate, flumethotrexate, dioxetrexate, 5,10-dideazatetrahydrofolate, Methotrexate, butylmercaptopurine, diketamide, cystazine guanidine, carmofur, uracil tegafur, pentene indole, thiorasin, Youfudine, metoxyberine, formyl Sarcoma, amino(yl)pterin, aminopterin sodium, 8-azaguanine, dimethylamine adenosine, (nitro)azathiopri...

Embodiment 3

[0057] Put 80 mg of pharmaceutical excipient ethylene vinyl acetate copolymer (EVAc) into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of raltitrexed, 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 anticancer drug composition containing 20% ​​by weight of raltitrexed. The drug release time of the anticancer drug composition in the physiological saline in vitro is 14-24 days, and the drug release time in the mouse subcutaneous is about 20-35 days.

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Abstract

An anticancer pharmaceutical composition composed of pharmaceutic adjuvant and anti-metabolism medicine is disclosed. Wherein, the anti-metabolism medicine can effectively destroy DNA and / or protein synthesis and repairing function inside the tumor cell so as to inhibit the tumor cell growth, while the pharmaceutic adjuvant can mainly be biological compatible, degradable and absorbable macromolecule polymer, which can make the anti-metabolism drug to release slowly in the local tumor region in the degradation and absorption process, therefore it can both decrease considerably the whole body toxic reaction and sustain the local tumor effective drug level.

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] The treatment of solid tumors mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, anti-metabolite drugs have obvious effects and have been widely used in various malignant tumors. However, further studies have found that the excessive expansive hyperplasia of solid tumors has higher interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity than the surrounding normal tissue. Drug concentration (see KongQingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine to treat brain tumors in rats" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (KongQ et al., J Surg Oncol.1998 Oct; 69 (2): 76-82), simply increasing the dosage is limited by the systemic reaction. Therefore, a specific subject of the present inve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/522A61K31/7064A61K45/00A61P35/00
Inventor 孔庆忠
Owner DASEN BIOLOGICAL PHARMA CO LTD
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