Study design
BLOOD
This was a randomized, single center, open-label, single-dose, two-period crossover phase I clinical trial designed to enroll healthy volunteers with the aim of comparing PK parameters of Ezetrol® (10 mg, batch no.5 EZPA42002, from MSD Pharma (Singapore) Pte. Ltd.) to those of ezetimibe tablet (10 mg, batch no. 170301, from Chongqing shenghuaxi Pharmaceutical Co., Ltd.). All study drugs were provided by the sponsor at no cost.Randomization was planned to generate two subject groups (fasting conditions and fed conditions) with administration of the products in two stages, separated by a 14-day washout period. Each eligible subject will be given a randomization number from small to large according to the screening number.The qualified volunteers were hospitalized in the phase I clinical research center on the day before dosing and placed on a uniform diet during hospitalization. The fasting group were fasted for overnight (10 h) before administration. The fed group was requested to take a high-fat breakfast (total energy 1000 cal, 65% fat, 15% protein, 20% carbohydrate) within 0.5 h before administration. The management provided standard lunch and dinner for participants at 4 h and 10 h after dosing, separately. They then returned to the facility for regular blood sampling up to a total duration of 14 days. Blood samples (4 ml) were collected in precooled vacuum tubes containing sodium citrate anticoagulant in each stage (pre-administration and at 0.16, 0.3, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72 h after administration).The plasma samples were centrifuged at 4000 g for 10 min at 4 °C and future stored at − 80 °C. Bio-analysis experiment was analyzed by LC–MS/MS methods at Chongqing shengshifuma Technology Co., Ltd, [