Tasa Pellets

Total Alkaloid of Sophora Alopecuroides which is extracted from the traditional Chinese herb—Sophora Alopecuroides has been mainly used in clinical therapeutics for dysenteric diarrhea caused by bacteria phlegmasia and dump, etc. In this paper Total Alkaloid of Sophora Alopecuroides pellets were prepared and the quality was appraised. The techniques of pellets preparation and film coating were evaluated from different aspects, and the stability of pellets was studied.The pharmacokinetics of the pellets was investigated in rabbits after a single oral administration of commercial tablets or self-made pellets.To assure the quality of pellets, the titration method was developed to determine the contents of Total Alkaloid, while the HPLC method to determine the content of the three main Alkaloids (Sophoridine, Matrine and Sophocarpine). The HPLC method was also established to determine the concentration of sophoridine and matrine in rabbit serum with a simple pretreatment process.Total Alkaloid of Sophora Alopecuroides 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 85% and the average Total Alkaloid content was about 15%. The results suggested the preparation process and formulation of pellets could reach the expected goals.Polyoxylate IV and Opadry OY-B were used respectively as coating materials and coating process was performed on a mini-fluidized bed spray coater. The effects of process variables and formulation variables on coating pellets preparation were investigated. The results showed that the coated pellets had a markedly moistureproof property. With a view to mask the bitterness of the pellets, polyoxylate IV was selected and used in preparing coated pellets. The stability of the preparation was investigated under the condition of strong light, high temperature and high humidity. The results showed that the preparation was stable.The serum concentration in rabbits was determined after a single oral administration of commercial tablets and self-made pellets. The pharmacokinetics parameters and the relative bioavailability were measured. The result indicated that these two preparations were bioequivalent, and the pellets showed an obvious strongpoint that T_max was shorter, whereas C_max was higher than the commercial tablets, owing to that the pellets had large surface area and could be dissolved and absorbed quickly after oral administration.