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.