title: [Preparation process of rutacarpine-hydroxypropyl-beta-cyclodextrin inclusion complex].
abstract: Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.
authors.forename: Chun-Lin
authors.initials: CL
authors.lastname: Yan
authors.forename: Ji
authors.initials: J
authors.lastname: Zhang
authors.forename: Yong
authors.initials: Y
authors.lastname: Hou
authors.forename: Gui-Ping
authors.initials: GP
authors.lastname: Xue
authors.forename: Shu
authors.initials: S
authors.lastname: Wang
authors.forename: Qing-Ya
authors.initials: QY
authors.lastname: Zhao
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000470:Alkaloids / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000737:chemistry*; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D027821:Rutaceae / Q000737:chemistry*; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D047392:beta-Cyclodextrins; C560377:rutacarpine; D000073738:2-Hydroxypropyl-beta-cyclodextrin