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Slow released anticancer combination of medication embedded the interior of the body

A technology of anti-cancer drugs and compositions, which is applied in drug combination, drug delivery, anti-tumor drugs, etc., and can solve the problem of difficult local formation of effective drug concentration in tumors

Inactive Publication Date: 2005-08-31
DASEN BIOLOGICAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor (see Kong Qingzhong "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.1998Oct; 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

[0042] Put 90 mg of polylactic acid (PLA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of ifosfamide, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer drug composition containing 10% by weight of ifosfamide. 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 30-40 days.

Embodiment 2

[0044] The method step of being processed into anticancer drug composition is identical with embodiment 1, and difference is that contained active ingredient is:

[0045] 5-30% by weight of three mustard cyclophosphamide, sulfophosphamide, desphosphamide, mafosfamide, pefosfamide, trofosfamide, carbazolamide, azamethanone, almentan quinone, thymopentin, chlorine Clomid, Letrozole, Sodium Cantharidinate, Cantharidin, Cantharidin Sodium, Methylcantharidinamine, Hydroxycantharidin, Norcantharidin, Sulfur Colchicum, Racemylalanine Mustard, Beauty Scone, Diantrazole, Manlusufan, Quaosufan, Ritrasufan, Improsulfan, Mesulfonate, Spirobromopropionamide, Mannitol Disulfonate, Triazine Imidazolamide, Enprobamate, Epipiridine, Butenolimine, Ebimorph, Ethanol, Ethimine, Etoglu, Phenate, Dipropoxyimine Quinone, Piperbromane, Piposulfan, Pilitrikexin, Bisantelone, Bisantelone, Ruizuosufang, Succinate, Rofecoxib, Cydone, Trimethylolamine Triazine, Urethane, N-Diphenyl Hydrochloride Hydrazi...

Embodiment 3

[0047] Put 80 mg of polyglycolic acid and glycolic acid copolymer (PLGA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 20 mg of letrozole, re-shake, and 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 letrozole. 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 30-40 days.

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PUM

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Abstract

A slowly-releasing anticanser composite medicine implanted in human body is composed of the anticancer medicine prepared from implantation agent, slowly releasing agent and dichloroethane-kind medicine for suppressing the growth of tumor cells and the medicinal additive chosen from biocompatible and biodegradable polymer for slowly releasing said anticancer medicine toward tumor.

Description

(1) Technical field [0001] The invention relates to an anti-cancer drug composition implanted in the body and slowly released, belonging 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, dichloroethylamine drugs have obvious effects and have been widely used in various malignant tumors. However, blood vessels, connective tissue, matrix proteins, fibrinoproteins, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the effect of chemotherapy drugs on the surrounding tumor and tumor tissue. Penetration and diffusion within (see Netti et al. "The influence of the status of the extracellular matrix on the movement of drugs in solid tumors" "Cancer Research" 60 pp. 2497-503 (2000) (Netti PA, Cancer Res.2000, 60 (9): 2497-503). Due to the excessive expan...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/08A61P35/00
Inventor 孔庆忠
Owner DASEN BIOLOGICAL PHARMA CO LTD
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