Preparation technology of Haimeng Zhisuan sustained release tablets / 中草药

ABSTRACT

Objective: To optimize the formulation of Haimeng Zhisuan gastric floating sustained-release tablets and to investigate its in vitro release properties. Methods: Plackett-Burman design was used to screen three most influential factors, i.e. matrices, floating material, and fillers which had significant impact on the preparation of floating sustained-release tablet by evaluating the cumulative release rate of CaCO3 at 2, 4, and 12 h; The levels of non-important factors were also determined. A 3-factor, 3-level Box-Behnken design was led to optimize the formulation, using cumulative release rate as index. The experiment result was optimized and the drug release kinetics equation was fitted by response optimizer. Results: The optimized tablet formulation was as follows cuttlebone 225.0 mg, Montmorillonite 25.0 mg, HPMC K100M 100.0 mg, MCC 48.3 mg, EC 25.0 mg, searyl alcohol 74.7 mg, and 5% PVP-K30 ethanol solution as adhesive. The experimental data of optimized tablet were similar to the predicted values. The floating duration was over 12 h in simulated gastric fluid. Data of the in vitro release were fitted to the first-order equation. Conclusion: Formulation of Haimeng Zhisuan floating sustained-release tablet is found to be reasonable. The preparation technology is feasible. The tablet shows good in vitro release properties within 12 h.