Nelfinavir suspension obtained from nelfinavir tablets has equivalent pharmacokinetic profile

J Chemother. 2001 Oct;13(5):569-74. doi: 10.1179/joc.2001.13.5.569.

Abstract

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.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Antiretroviral Therapy, Highly Active
  • Area Under Curve
  • Chemistry, Pharmaceutical
  • Chromatography, High Pressure Liquid
  • Excipients
  • Female
  • HIV Infections / drug therapy
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / pharmacokinetics*
  • Humans
  • Kinetics
  • Male
  • Nelfinavir / administration & dosage
  • Nelfinavir / pharmacokinetics*
  • Patient Compliance
  • Tablets
  • Therapeutic Equivalency

Substances

  • Excipients
  • HIV Protease Inhibitors
  • Tablets
  • Nelfinavir