Pharmacokinetic/Pharmacodynamic modelling of Saxagliptin and its active metabolite, 5-hydroxy Saxagliptin in rats with Type 2 Diabetes Mellitus

Table 11 Parameters of the PK model of SAX in T2DM rats (n = 3)

Parameter	Mean	SD	CV (%)
C_max (ng/mL)	2197.13	1205.08	54.85
T_max (h)	0.11	0.03	27.63
AUC (ng*h/mL)	3282.06	1085.78	33.08
t_1/2Ka (h)	0.07	0.03	37.50
t_1/2a (h)	0.08	0.02	20.79
t_1/2β (h)	6.13	6.20	101.21
V (mL/kg)	2307.24	1097.52	47.57
V₂ (mL/kg)	18393.30	16552.77	89.99
CL (mL/h/kg)	3245.80	902.06	27.79
CL₂ (mL/h/kg)	17090.42	11724.77	68.60
K₁₂ (1/h)	6.62	3.06	46.22
K₂₁ (1/h)	1.07	0.40	37.47

C_max maximum plasma concentration, T_max time to maximum plasma concentration, AUC area under the curve, t_1/2Kα absorption phase half-life, t_1/2α distribution phase half-life, t_1/2β elimination half-life, V apparent distribution volume of central compartment, V₂ apparent distribution volume of peripheral compartment, CL the clearance rate of central compartment, CL₂ the clearance rate of peripheral compartment, K₁₂ rate constant from compartment 1 to compartment 2, K₂₁ rate constant from compartment 2 to compartment 1

ISSN: 2050-6511