Drug /

Parameters

Cmax

(mg/L)

t1/2

(min)

MRT0-∞

(min)

Vss

(L/kg)

AUC0-∞

(g.min/L)

CL

(L/h/kg)

Lip 175

31.6 ±

127 ±

184 ±

0.21 ±

5.7 ±

1.2 ±

 

6.3

25

35

0.04

1.2

0.3

Lip 400

17.3 ±

26.5 ±

38.3 ±

0.26 ±

0.63 ±

7.0 ±

 

5.4

7.9

11.5

0.07

0.14

1.6

Free

172 ±

15.2 ±

25.5 ±

0.60 ±

4.1 ±

24.4 ±

Drug

37

9.8

9.8

0.16

0.5

2.5

aDogs (n= 4-5) received small size liposomes (Lip 175, 6.5 mg Sb/kg body weight), medium size liposomes (Lip 400, 4.2 mg Sb/kg) or free drug (100 mg Sb/kg). Blood samples were collected at different time intervals for determination of Sb by graphite furnace atomic absorption spectroscopy. Pharmacokinetic parameters were determined using Rstrip 4.03 computer program. Cmax, maximum blood concentration of Sb; t1/2, half- life of blood elimination of Sb; MRT0-∞, mean residence time of Sb projected to infinity; Vss, volume of distribution at steady state; AUC0-∞, area under the blood concentration–time curve projected to infinity; CL, total body clearance of Sb.
Table 1: Blood pharmacokinetics parametersa (mean ± SD) in dogs with VL after intravenous bolus injection of different formulations of meglumine antimoniate.