The Study On The Compound Sustained-Released Pellets Of Pseudoephedrine Hydrochloride And Ibuprofen

In this paper, Pseudoephedrine Hydrochloride and Ibuprofen were selected as the model drugs to prepare compound sustained-release pellets by fluidized bed. The HPLC method of assay, dissolution. Micromeritics parameters, yield were employed to optimize the formulation and technolgy parameters by single factor and the total score of dissolution was used in the orthogonal test to determine the best formulation. The data of testing result was dealed with by SPSS statistical software, and the optimized formulation and technique parameters were obtained. Eudragit^? RS and Surelease^? aqueous dispersions were used to prepare membrane-matrix hybrid sustained-release pellet of Pseudoephedrine Hydrochloride and matrix sustained-release pellet of Ibuprofen as coating material ,matrix material and adhesives respectively. According to the ratio of Pseudoephedrine Hydrochloride and Ibuprofen in designed formulation, the Pseudoephedrine Hydrochloride sustained-release pellets and Ibuprofen sustained-release pellets were mixed evenly and filled into capsule.The drug release character and mechanism from different sustained-release pellets were studied.Finally, the pharmacokinetic study of compound Pseudoephedrine Hydrochloride and Ibuprofen sustained-release pellets was performed. With the commercial compound Pseudoephedrine Hydrochloride and Ibuprofen tablet as the reference preparation, the pharmacokinetic study was performed in six Beagle dogs. HPLMC method was employed to detect the drug concentration in plasma of dogs administered with single dose by crossover design. The pharmacokinetic parameters of the test and reference tablets were as follows: AUC_{0～∞} of Pseudoephedrine Hydrochloride were 14496.35±1556.49 and 15726.28±2014.32 (ng·h·mL^-1), C_max were 1015.27±141.44 and 1981.70±121.12 (ng.ml^-1), T_max were 5.67±1.51 and 2.6±0.38 (h), AUC_{0～∞} of Ibuprofen were 888.00±43.99 and 768.99±46.91 (μg·h·mL^-1), C_max were 84.44±16.43 and 117.02±1:15.9 (μg·mL^-1),T_max were 5.17±1.29 and 2.58±0.38 (h).The relative bioavailability of Pseudoephedrine Hydrochloride and Ibuprofen were 92.18% and 115.47%. The two one-sided test results showed that bioavailability of two dosage forms were equivalent. The results of statistical judgment indicated that the in vitro release of compound Pseudoephedrine Hydrochloride and Ibuprofen sustained-release pellets was correlative well with absorption fraction in vivo.