Studies On The Chemical Constituents Of Total Stemona Alkaloidsand The Preparation Of Sustained-release Tablets

Radix Stemonae is a traditional Chinese medicine(TCM), which was firstly recorded in Tao Jing-hong’s "Mingyi bielu". Nowdays, it is still commonly used as an antitussive TCM. Stemona sessilifolia, S. japonica and S. tuberosa are the three original sources of Stemonae Radix, and have been traditionally used for antitussive and insecticidal remedy. The purpose of this study is to explore the effective parts extracted Baibu antitussive and its sustained release tablets preparation and quality control method, in order to provide foundation for the development of a new long-acting antitussive drug. We use chromatographic techniques to isolate Stemona alkaloids, and identifying their structures. An HPLC method was established for the content determination of Stemona alkaloids, and the method was used for the quality control of the sustained-release tablet preparationFirstly, we studied the chemical components of Radix Stemonae. The ethanol extracts of commercial Radix Stemonae were chemically investigated by various chromatographic methods. Ten compounds were isolated and structurally identified by spectroscopic methods as Stemocochinin(BB-1)、isostemochocochinin(BB-2)、Stemoninine(BB-3)、croomine(BB-4)、Neotuberostemonine(BB-5) 、 tuberostemonine(BB-6) 、 tuberostemonine H(BB-7) 、didehydrotuberostemonin(BB-8)、tuberostemonine K(BB-9)、neostenine(BB-10)。Stemona alkaloids was easier to crystallize in cyclohexane- ethyl acetate solvent system, their structures were confirmed by single-crystal X- ray diffraction method.The preparation process of Stemona alkaloids sustained-release tablets was studied by using single factor test. A SPE-HPLC-ELSD method was established for determination of the content of total alkaloids sustained-release tablets. This method is simple, rapid, accurate and representative. At the same time, the prescription of sustained-release tablets was optimized: the main drugs and the mixture of 15%HPMCK4M and 15%HPMCK15M equivalent, compressible starch and lactose 2:1 added to the enough, with 85% alcohol solution as adhesive made of soft material, wet granulation, and 1% magnesium stearate tablet.The quality control method of total alkaloids sustained-release tablets was studied, which including the chemical marker identification, tablet weight variation, dissolution, heavy metals, arsenic salt and microbial limit), content determination(tentative Stemona alkaloids content should not be less than 7.50 mg in each tablet). Results showed that the sustained-release tablets are stable and quality controllable.