XIANG Lin, ZENG Jia, ZHOU You, et al. Pharmacokinetics of Vincamine Sustained-release Pellets in Beagle Dogs[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(3): 85-88.
XIANG Lin, ZENG Jia, ZHOU You, et al. Pharmacokinetics of Vincamine Sustained-release Pellets in Beagle Dogs[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(3): 85-88. DOI: 10.13422/j.cnki.syfjx.2015030085.
Objective: To prepare vincamine sustained-release pellets and analyze its pharmacokinetics in Beagle dogs for providing an reference for non-pH-dependent release of sustained-release formulations of vincamine. Method: Vincamine sustained-released pellets were prepared by fluidized bed with self-made tartaric acid pills core.Beagle dogs were randomly assigned to receive sustained-release pellets and common tablets with dosage of 150 mg
then a crossover trial was conducted one week later.HPLC was employed to determine plasma drug concentrations to compare pharmacokinetic parameters of each formulation
mobile phase was 0.02 mol·L-1 potassium dihydrogen phosphate-acetonitrile(70: 30) by adjusting pH 2.3 with phosphoric acid
detection wavelength was 268 nm. Result: Pharmacokinetic parameters of sustained-release pellets and common tablets were as follows:Cmax of (1 147.40±554.50)
(1 506.10±327.44) μg·L-1;Tmax of (2.38±0.25)
(1.63±0.25) h;MRT of (6.75±2.44)
(3.19±0.73) h;AUC0-t of (4 766.76±1740.26)
(3 906.81±686.53) μg·h·L-1
respectively.Relative bioavailability of sustained-release pellets to common tablets was 122%.Dissolution test indicated that sustained-release pellets had good in in vivo and in vitro correlation. Conclusion: Compared with common tablets
vincamine sustained-release pellets show slower absorption in Beagle dogs
the average residence time is two times more than the former
relative bioavailability has also been significantly improved
indicating that this formulation can achieve non-pH-dependent release in the gastrointestinal tract.