ABSTRACT
OBJECTIVE: To prepare the ganoderic acid T (GA-T) tablets and evaluate the pharmacokinetics and bioavailability in rabbits. METHODS: GA-T tablets were prepared by direct powder compression. After investigating the type and amount of excipients by single-factor method, the formulation of GA-T tablets was optimized and prepared by direct powder compression. An HPLC method was used for the determination of plasma concentration in rabbits after administration of GA-T. The main pharmacokinetic parameters were analyzed by pharmacokinetic software kinetica 5.0. The pharmacokinetic characteristics of GA-T tablets were studied. RESULTS: In optimization of formulation, microcrystalline cellulose and spray-dried lactose (1:1) were selected as bulking agent. In addition, 1% of the silica powder and 0.5% magnesium stearate were used as glidant and lubricant, respectively. The prepared tablets were consistent with the requirements of the 2010 edition of Chinese Pharmacopoeia standards, including appearance, hardness, disaggregation and dissolution of the tablets. The absolute bioavailability of oral GA-T tablets was 33.03%. CONCLUSION: The direct powder compression is simple and reliable, and the bioavailability of oral GA-T tablets in rabbits is well. This article provided experimental data for preclinical study of GA-T.