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Evaluate whether the test formulation and reference formulation of bisoprolol amlodipine tablets are bioequivalent after a single oral administration in healthy subjects under fasting and postprandial conditions.
A single-dose, randomized, open-label, two-period, self-crossover trial design was adopted. Fasting and postprandial tests were randomly divided into 2 administration sequence groups according to 1∶1 ratio, the subjects were administered orally one tablet of either the test or reference formulation of the bisoprolol-amlodipine tablet, containing 5 mg bisoprolol fumarate and 5 mg amlodipine besylate (equivalent to 5 mg amlodipine). Liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) was applied to determine the concentration of bisoprolol and amlodipine in plasma of healthy subjects after fasting or fed administration, while Phoenix WinNonlin 8.1 software were used for pharmacokinetics (PK) parameters calculation and bioequivalence analysis.
Healthy subjects took one tablet of test product (T) and the reference product (R), under fasting condition. The main pharmacokinetic parameters of bisoprolol were as follows: Cmax were (26.94±5.93) and (27.85±6.06) ng·mL-1, respectively; AUC0-t were (325.81±59.30) and (345.77±87.04) ng·mL-1·h-1, respectively; AUC0→∞ were (337.94±63.91) and (360.03±95.94) ng·mL-1·h-1, respectively; the main pharmacokinetic parameters of amlodipine were as follows: Cmax were (3.56±0.89) and (3.63±0.93) ng·mL-1, respectively; AUC0-t were (165.78±47.60) and (170.76±48.63) ng·mL-1·h-1, respectively; AUC0→∞ were (188.76±67.62) and (188.40±54.85) ng·mL-1·h-1, respectively; the 90% confidence intervals of Cmax、AUC0-t and AUC0-∞ after logarithmic conversion of bisoprolol and amlodipine of the two products were all within 80.00%-125.00%. Healthy subjects took the test and reference product under fed condition. The main pharmacokinetic parameters of bisoprolol were as follows: Cmax were (22.66±2.91) and (22.68±3.85) ng·mL-1, respectively; AUC0-t were (310.42±59.44) and (303.39±53.21) ng·mL-1·h-1, respectively; AUC0→∞ were (320.68±67.30) and (313.31±60.15) ng·mL-1·h-1, respectively; the main pharmacokinetic parameters of amlodipine were as follows: Cmax were (3.24±0.53) and (3.15±0.55) ng·mL-1, respectively; AUC0-t were (180.74±40.77) and (178.27±33.53) ng·mL-1·h-1, respectively; AUC0→∞ were (199.02±50.12) and (197.77±39.64) ng·mL-1·h-1, respectively. The 90% confidence intervals of Cmax、AUC0-t and AUC0-∞ after logarithmic conversion of bisoprolol and amlodipine of the two products were all within 80.00%-125.00%.
Healthy adult subjects demonstrate bioequivalence between the test formulation and reference formulation of bisoprolol amlodipine tablets following a single oral administration under both fasting and postprandial conditions.
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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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