Nelfinavir suspension obtained from nelfinavir tablets has equivalent pharmacokinetic profile.
The pharmacokinetics of nelfinavir tablets (A) and an oral simplified nelfinavir suspension (B) were studied. Twelve healthy volunteers randomly received either five 250-mg nelfinavir tablets or a simplified oral suspension obtained from tablets dissolved in water (nelfinavir 1250 mg in 100 mL of water) in a single dose before being crossed over to the second treatment after a one-week washout period. Blood samples were drawn up to 24 h after drug administration. Nelfinavir concentrations in plasma were analyzed by a specific and validated reverse-phase high-performance liquid chromatography assay (HPLC) with UV detection, and pharmacokinetic values were determined. For the AUC(0-infinity) with means+/-SD of 31.71+/-7.85, 30.88+/-10.28 (microg/L) respectively for treatments B and A, the ratio (F(B/A)) was of 1.1 with a C.I. of 0.90-1.24. For Cmax with means+/-SD of 3.1+/-0.6 (treatment B) and 3.2+/-0.8 mg/mL (treatment A), the ratio was 1.0. with C.I. of 0.92-1.08. The two treatments evidenced no significant differences in AUC(0-inifnity) and Cmax values and the two-one sided t-test showed that the two preparations are bioequivalent. There was no significant difference in Tmax between the liquid and tablets. Nelfinavir suspension might be a option for treating HIV-infected patients with swallowing disturbances or compliance problems.
Regazzi
M B
MB
Department of Pharmacology, I.R.C.C.S. Policlinico San Matteo, University of Pavia, Italy.
Seminari
E
E
Villani
P
P
Carriero
P L
PL
Montagna
M
M
Marubbi
F
F
Maserati
R
R
D000284:Administration, Oral; D000328:Adult; D023241:Antiretroviral Therapy, Highly Active; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D005079:Excipients; D005260:Female; D015658:HIV Infections / Q000188:drug therapy; D017320:HIV Protease Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007700:Kinetics; D008297:Male; D019888:Nelfinavir / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010349:Patient Compliance; D013607:Tablets; D013810:Therapeutic Equivalency
D005079:Excipients; D017320:HIV Protease Inhibitors; D013607:Tablets; D019888:Nelfinavir