Studies On Arbidol Hydrochloride Sustained-Release Pellets

Arbidol Hydrochloride was selected as a new antiviral drug for the treatment and prophylaxis of influenza and other acute respiratory viral infections (ARVI). At the same time, Arbidol had the immunomodulating activity, capacity of inducing interferon and antioxidant property. Nowadays Arbidol is taken 4 times daily and shows bigger fluctuation in the drug concentration. The aim of this work was desigened to develop a kind of Arbidol sustained-release pellets, which would reduce the dosing frequency, narrow the blood concentration fluctuation and be more convenient for patients to use.UV method was developed for assaying the drug content and drug release of Arbidol sustained release pellets. The method was monitored by methodology and it was simple, accurate to be used in vitro. The preformulation results showed that the apparent solubility of Arbidol in water, 0.1NHC1 and pH 6.8PBS were low, and in 0.5%SDS was high. The apparent partition coefficient in oil and water of Arbidol was dependent on pH, and the maximum value appeared at pH6.8.To investigate the absorption characters of Arbidol in the intestine, the absorption kinetics and the absorption sites were studied by utilizing the rat intestinal absorption single pass perfusion model in situ. The results of perfused rat intestinal model showed that Arbidol could be well absorbed at all segments of intestine in rats. The apparent absorption rate constants at duodenum, jejunum, ileum and colon were 13.6,11.9,9.8 and 6.1 μL·min^-1·cm^-1, respectively. The concentration of drug and Tween-80 had no evident influence on the absorption rate constants. The pH of drug solutions had an effect on the absorption constants, and the absorption was better at low pH. It was showed that the absorption of Arbidol was the passive diffusion mechanism.Extrusion-spheronization technology was used to prepare Arbidol pellets. Technology factors of preparing pellets and formulation factors were investigated and optimized by the influence factors test and orthogonal design test. It was discovered that the yield of the objective...