Preparation and pharmacokinetics study on gastro-floating sustained-release tablets of troxipide

Abstract

The purpose of this research aimed at preparing gastro-floating sustained-release tablets of troxipide and a further study on in vitro release and in vivo bioavailability. Under the circumstances of direct powder compression, the floating tablets were successfully prepared with HPMC as main matrix material, Carbopol as assistant matrix material, octadecanol as floating agent and sodium bicarbonate as foaming agent to float by gas-forming. The floating time and accumulative release amount as evaluation indexes were utilized to perform pre-experiment screening and single-factor test, respectively, while central composite design response surface method was applied for formulation optimization, followed by in vivo pharmacokinetic study in beagles after oral administration for floating tablets and commercial tablets used as the control. The results indicated that the floating sustained-release tablets held a better capability for floating and drug release and more satisfactory pharmacokinetic parameters, such as a lower Cmax, a prolonged Tmax, but an equivalent bioavailability calculated by AUC0-24 compared to commercial tablets. So a conclusion was finally drawn that the floating sustained-release tablets possessing a good release property could be suitable for demands of design.

Metabolites profiling and pharmacokinetics of troxipide and its pharmacodynamics in rats with gastric ulcer

“…More importantly, from the Concentration-time (C-t) curve the troxipide concentration in the GUGIG was slightly increased compared with that in the NCGIG, suggesting that troxipide was more easily absorbed into the blood of rats with GU than that of NC rats 41 . The T max of the GUGIG was not significantly different from that of the NCGIG, which suggested that the T max not related to dose and disease; this result is consistent with the findings of Gao's report 23 . The V z (0.069 ± 0.012, 0.061 ± 0.008, 0.064 ± 0.003 L/kg) of the GUGIG was significantly decreased (P < 0.01) compared with the V z (0.102 ± 0.015, 0.117 ± 0.024, 0.123 ± 0.02 L/kg) of the NCGIG, which suggested that the drug was more slowly distributed in GUGIG rats than in NCGIG rats.…”

“…Troxipide (3,4,5-trimethoxy-N-3-piperidinyl, Fig. 1 ), a defensive factor-enhancing therapeutic agent for gastritis and GU that exerts inhibitory, therapeutic and preventive effects to specifically those in the stomach by enhancing gastric mucosal blood flow and gastric mucosal defense factors and promoting tissue repair, blood circulation, metabolism and GU repair 23 – 25 . It is used to alleviate gastric mucosal lesions (erosion, hemorrhage, redness, and edema) in the acute gastritis and acute exacerbation stages of chronic gastritis.…”

Preparation and evaluation of floating tablets of pregabalin

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