Preparation and pharmacokinetics of imperatorin sustained-release tablets / 西安交通大学学报(医学版)

ABSTRACT

Objective To prepare imperatorin sustained-release tablets and study their pharmacokinetics and bioavailability in rabbits.Methods Hydroxy-propyl methyl cellulose(HPMC) and carbomer were used to constitute the binary polymer matrix.Orthogonal design was used to optimize the formulation of imperatorin sustained-release tablets.The preliminary pharmacokinetic study in the rabbits was carried out by single-dose crossover design using imperatorin plain tablets as control.An appropriate GC-MS method was developed for measuring the concentration of imperatorin in the blood.Results Optimized formulation contained 1∶20 HPMC K100M and 2∶25 carbomer.Single dose test with 300mg showed that the relative bioavailability of imperatorin sustained-release tablets was(115.37?45.46)%;AUC of the studied tablets and control tablets was(391.08?47.22) and(368.25?136.15)?g/(h?L),tmax(2.26?0.25) and(0.33?0.05)h,Cmax(59.66?6.28) and(295.91?127.00)?g/L,T1/2ke(2.27?0.09) and(0.60?0.10)h,respectively.Conclusion The release behavior of the imperatorin sustained-release tablets prepared with binary polymer system shows evident sustained-release characteristics.