Résumé
OBJECTIVE:To investigate the preparation technique and optimal formulation of ketoconazole calcium alginate gel beads.METHODS:Ketoconazole calcium alginate gel beads were prepared by droplet method.The orthogonal experiment was carried out with encapsulation efficiency(EE)and drug loading(LD)as indexes to optimize the optimal formulation of the calcium alginate gel beads.The encapsulation efficiency and drug loading amount for the optimized formulation were determined,and the optimized formulation was compared with crude drug in respect of the in vitro drug release behavior.RESULTS:The result showed that the optimal formulation was as follows:2.0% Na-alginate and 0.3mol? L-1 CaCl2 with the ratio of Na-alginate:ketoconazole at 2∶ 1.The average EE and LD were(90.53? 2.32)% and(31.51? 2.08)%,respectively,and the slow-release was better as compared with that of the crude drug.CONCLUSION:The preparation procedure is simple,feasible,stable and reproducible.
Résumé
OBJECTIVE:To prepare aspirin chitosan-sodium alginate microcapsules(ACSPM)and to investigate its optimal formula and releasing mechanism.METHODS:The formula of ACSPM was optimized by the orthogonal design with entrapment ratio as index,and then ACSPM was prepared,with its release rate determined as well.The releasing mechanism of aspirin from the microcapsules was established by equation fitting of releasing kinetic model.RESULTS:The prepared microcapsules were uniform in size and contents.The optimized formula was as follows:the concentration of sodium polymannuronate and chitosan were 3.0% and 1.0%,respectively,and the proportion of polymannuronate to aspirin was 1∶ 4.The in vitro drug release was in line with both Higuchi equation and Peppas equation.CONCLUSION:This preparation technology was simple and the drug releasing mechanism of the preparation was chiefly characterized by drug diffusion including bulk erosion non-Fickian process.