Studies On Sinomenine Hydrochloride Sustained-Release Pellets

Sinomenine Hydrochloride (SM HCl) which extracted from the traditional Chinese medicine —Sinomenium acutum Rehd. et Wils. has been mainly used for rheumatoid arthritis in clinical therapeutics . In this dissertion, the study was aiming at the preparation of SM HCl 24h sustained-released pellets and validation in vivo, consisting of preparation methods for pellets, the sustained-release system of coated pellets, stability, pharmacokinetics. Results show: the sustained-release pellets had good appearance and stability,the drug was released in vivo over 24h.UV spectrophotometry was developed for in vivo assay during the studies of release and HPLC ultraviolet method was utilized to determine the SM HCl content in pellets. The plasma concentration in dogs was also minitored by using the HPLC ultraviolet method.The preformulation research showed that the equilibrium solubility of SM HCl in different pH phosphate buffer was decreased with the value of pH increasing. The compatibility of drug and exipients was assessed as well.SM HCl pellets were prepared by means of power layering with the centrifugal granulation equipment made in China. Through the formulation filtration and process observation, it was discovered that the yield of the objective pellets was over 90% and the average SM HCl content was about...