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.
ABSTRACT
This article was aimed to study the multicomponent in vivo releasing rules of Zuojin Gastric Floating Sus-tained-release Tablet. Stomach contents of rabbits were collected at different times and then prepared into solutions for the study. The HPLC was used to establish fingerprints of each time and fingerprints of completely dissolved samples. The in vivo releasing rates were calculated. The evaluation was made on releasing behaviors among index components as well as between index components and preparations. The results showed that within 10 h, the f2 of berberine and limonin, rutaecarpine, preparation were 52, 61.5, 66.4, respectively. The f2 of limonin and rutae-carpine, preparation were 70, 46.5, 53.7, respectively. It was concluded that within 10 h, the releasing behavior of berberine and limonin, rutaecarpine, preparation was similar. The releasing behavior of rutaecarpine and limonin, preparation was similar. However, the releasing behavior of limonin and preparation was different.
ABSTRACT
Objective To study the releasing properties and mechanism in vitro of the active ingredients of the gastric floating sustained-release tablet containning Zuojin Pellet extraction(ZJ-GFST).Methods The release rates of berberine,palmatine,evodiamine,and rutaecarpine from ZJ-GFST in vitro within 8 h were measured by using rotating basket method in Chinese Pharmacopeia.The cumulative curve of drug release data was fitted to zero order,first-order and Higuchi equation to ascertain the kinetic modeling of drug release.Release mechanism was ascertained using Peppas equation.Results The similar factors of the cumulative release curve of all the four ingredients mutually compared were more than 80%,indicating that the release of the four ingredients were similar.The cumulative release rate of all the four ingredients fitted Higuchi equation.The value of slopes of Peppas models of all the four ingredients were more than 0.45,indicating that drug released by concurrent action of diffusion and matrix erode(non-fickian diffusion).Conclusion The releasing properties in vitro of the active ingredients of ZJ-GFST is consistent.
ABSTRACT
AIM: To elucidate the effect of HPMC on the floating and releasing performances of Zuojin Gastric Floating Sustained-Release Tablets(ZJ-GFST) and to select the optimum matrix adjuvant for ZJ-GFST. METHODS: Seven kinds of ZJ-GFST from pharmaceutical factories as main adjuvant respectively.The floating lag time and the sustained floating time were used to evaluate the floating performance of ZJ-GFST.The accumulative releasing rates of berberine and palmatine in vitro were used to evaluate the releasing efficiency of ZJ-GFST. RESULTS: The tablets prepared with HPMC MK-100000 and MK-15000 disintegrated quickly when contacting with water, and the tablets prepared with HPMC MK-100M and MK-4000 had too long floating lag time and low release speed.The tablets prepared with HPMC 60RT-50、K-4M and MK-1500 all possessed short floating lag time and long sustained floating time and suitable drug releasing rate. CONCLUSION: The selected HPMC is 60RT-50.