TABLE 3.

Pharmacokinetic parameters in plasma and saliva

Sample and parameter (unit)Mean value (95% CI) for:
Low doseMedium doseHigh dose
3 mg/kg (n = 14)200 mg (n = 14)4 mg/kg (n = 7)300 mg (n = 7)5 mg/kg (n = 14)400 mg (n = 14)
Plasma
    Cmax (ng/ml)3,006 (2,656-3,400)1,885 (1,515-2,347)5,402 (3,968-7,361)4,839 (3,499-6,698)7,184 (6,199-8,331)5,272 (4,321-6,431)
    AUCτ (ng · h/ml)13,919 (10,471-18,501)9,765 (6,990-13,655)29,467 (15,595-55,677)30,940 (17,816-53,753)43,374 (33,638-55,971)37,549 (28,822-48,879)
    Tmax (h)1.07 (1.00-1.14)1.50 (1.25-1.75)1.04 (0.88-1.22)1.43 (1.25-1.61)1.02 (0.98-1.06)1.81 (1.50-2.12)
    Vss/F (ml)1,478 (1,284-1,671)NAa1,176 (969-1,384)NA817 (750-884)NA
    V/F (ml)1,874 (1,395-2,354)160,241 (124,230-196,252)1,391 (1,032-1,750)106,917 (86,065-127,768)904 (816-992)123,868 (110,919-136,816)
    CL/F (ml/h)200 (138-263)19,985 (14,130-25,840)120 (45-196)8,358 (3,881-12,835)86 (57-116)8,100 (5,699-10,501)
    kel (h−1)0.131 (0.151-0.111)0.147 (0.122-0.171)0.088 (0.054-0.123)0.105 (0.143-0.067)0.085 (0.104-0.066)0.096 (0.116-0.076)
Saliva
    Cmax (ng/ml)2,081 (1,877-2,308)1,309 (1,050-1,632)3,353 (2,556-4,402)2,796 (2,055-3,805)4,308 (3,970-4,672)3,287 (2,810-3,847)
    AUCτ (ng · h/ml)8,591 (6,715-10,981)5,970 (4,530-7,876)19,249 (11,497-32,214)18,634 (11,043-31,460)24,981 (20,378-30,631)22,047 (17,588-27,640)
    Tmax (h)1.001.21 (0.92-1.5)1.04 (0.96-1.12)1.29 (1.04-1.54)1.09 (0.92-1.26)1.54 (1.16-1.92)
  • a NA, not applicable.