Combination of slow released anticancer medication

A technology of anti-cancer drugs and compositions, applied in the field of drugs, can solve problems such as difficulty in forming effective drug concentrations, and achieve the effect of strengthening the anti-cancer effect

Inactive Publication Date: 2005-08-31
SHANDONG LANJIN PHARMA +1
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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

[0044] Put 90 mg of PLGA (copolymer of glycolic acid and glycolic acid, weight ratio 50:50) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of edoxifene, and shake again Then dry in vacuo 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 edoxifene.

Embodiment 2

[0046] The method step of being processed into anticancer drug composition is identical with embodiment 1, and difference is that contained active ingredient is:

[0047] (a) 1-50% Anastrozole, Edoxifene, Miprexifen, Tamoxifen, 4-Monohydroxytamoxifen, Comoxifen, Steroid Estrogen, Anticancer Sterol, 4-hydroxytamoxifen, gamma-linolenic acid, 2-methoxyestradiol, or methoxynorgestrel; or

[0048] (b) 1-50% 4-hydroxytamoxifen, DDT, hexachlorocyclohexane, ramoxifene, diethylstilbestrol, estradiol, zearalenone, estrone, 17α-estradiol, estradiol Diols, 2-hydroxyestrone, 5,7,4-trihydroxyisoflavones, progesterone, meandrostane, or androgens; or

[0049] (c) 1-50% piglutethimide, rubiticol, toremifene, flutamide, quartrosilicon blue, bicalutamide, aminoglutethimide, betamethasone benzoate, carutesosterone , megestrol, datiscoside, thiosterol, ethestrepine bromacetate, hesfin, or testolactone.

[0050] All the above are percentages by weight.

Embodiment 3

[0052] 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 anastrozole, 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 anastrozole. 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 20-35 days.

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PUM

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Abstract

A slowly-releasing anticancer composite medicine is composed of the hormone-kind anticancer medicine chosen from steroid-type hormone and hormone antagon for regulating the cell reproduction of hormone dependent tumor and the medicinal additive chosen from biocompatible and biodegradable high-molecular polymer for slowly releasing said anticanser medicine toward tumor.

Description

(1) Technical field [0001] The invention relates to a hormone-based anticancer pharmaceutical composition, which belongs to the technical field of medicines. (2) Background technology [0002] The treatment of solid tumors mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, hormone anticancer drugs have more 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 systemic reactions. (3) Contents of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/08A61P35/00
Inventor 孔庆忠
Owner SHANDONG LANJIN PHARMA
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