METHOD FOR PRODUCTION OF HYDROCHLORIDE 1(10) BETA-EPOXY-13-DIMETHYLAMINO-5,7α,6,11β(H)-GUAIA-3(4)-EN-6,12-OLIDE, LYOPHILIZED ANTITUMOR PREPARATION 'ARGLABIN'

摘要

The invention relates to a method for production of new medicinal preparations from the natural raw material, namely antitumor preparation "Arglabin" and can be used for chemotherapy of malignant tumors and dilating of range of immunomodulating preparations. The aim of the invention is the development of a method for production of an antitumor preparation on the basis of natural sesquiterpene lactone, excluding the use of toxic reagents and providing significant reduction of production process time. Said technical result is achieved by producing hydrohloride 1(10)β-epoxy-13-dimethylamino-5,7α,6,11β(H)-guaia-3(4)-en-6,12-olide hydrochloride, the lyophilized, antitumor preparation having radio-sensitizing and immunomodulating activities. The method includes extraction of the natural raw material - endemic plant Artemisia glabella Kar. et Kir., separation of obtained resin on individual components and extraction of technical arglabin, dimethylaminoarglabin hydrochloride is synthesized therefrom, with the subsequent purification, drying and lyophilization thereof. The extraction is carried out with the use of fluid carbon dioxide as extragent at pressure 150±2-10⁵ Pa and at temperature 60°C±0.5, the separation of resin on individual components is carried out by the method of preparative fluid chromatography, applying reversed phase C18. Technical arglabin is dissolved in acetonitrile at the weight ratio 1:10 with dimethylammonium dimethylcarbamat in the molar ratio 1:1.62 at the synthesis of dimethylaminoarglabin hydrochloride.