Full
Outline
To study the pharmacokinetics of rivaroxaban tablets in healthy subjects and to evaluate the bioequivalence of the 2 preparations.
60 healthy subjects were administered oral rivaroxaban test agent and reference reagent (Xarelto®). An open, single-dose, random, completely repeated, four-cycle crossover design was adopted. The subjects were divided 2 groups, such as a single administration ofthe test (30 subjects) under fasting state and a single postprandial oral administration of the test (30 subjects). The liquid chromatography-mass spectrometry was applied to determine the blood drug concentration at 14 different time points within 72 h after administration of the preparations, and the main drug parameters were calculated. Bioequivalence was evaluated using analysis of variance, two-sided one-sided t test, and 90% confidence interval analysis.
After oral administration of test and reference preparation in fasting state, the main pharmacokinetic parameters Cmax, t1/2 and AUC0-72h are (186.38±51.46) ng·mL-1, (8.67±2.56) h, (1 346.80±325.67) ng·h·mL-1 and (183.21±57.06) ng·mL-1, (8.42±2.67) h, (1 308.91±293.86) ng·h·mL-1. The main pharmacokinetic parameters of Cmax, t1/2 and AUC0-72h after oral administration of test and reference preparations after high-fat diet are (257.72±37.10) ng·mL-1, (5.04±0.71) h, (1 929.80±292.45) ng·h·mL-1 and (257.52±40.29) ng·mL-1, (5.45±0.87) h, (1 925.58±333.20) ng·h·mL-1. The geometric mean ratio points of Cmax, AUC0-t, and AUC0-∞ are between 80.00% and 125.00%, and the 90% confidence interval upper limit values of the intra-individual variation ratio are all ≤2.5, indicating that the test rivaroxa tablet and the reference preparation are bioequivalent.
In this study, the LC-MS/MS method was used to determine the content of rivaroxaban in human plasma. The rivaroxaban test preparation and the reference preparation were bioequivalent when administered under fast state and after a high-fat diet.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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