OBJECTIVE: This study was undertaken to determine the placental transfer of the human immunodeficiency virus protease inhibitor saquinavir. STUDY DESIGN: An ex vivo perfused human placental cotyledon model was used. Ten placental perfusion studies were performed, with concentrations of saquinavir in the maternal compartment ranging from 322 to 2197 ng/mL (within reference therapeutic ranges). Drug concentrations were determined by high-performance liquid chromatography. RESULTS: The mean (+/- SD) fetal transfer rate of saquinavir was 1.8% +/- 1.6%, and the mean (+/- SD) clearance index was 0.05 +/- 0.05. A mean (+/- SD) of 1.6% +/- 3.1% of the perfused saquinavir was retained by the cotyledon. The small amount of saquinavir that crossed the placenta corresponded to the fraction not bound to human serum albumin. CONCLUSION: The low rate of placental transfer of saquinavir suggests that use of this antiretroviral drug by pregnant women may not lead to significant exposure of the fetus.
OBJECTIVE: This study was undertaken to determine the placental transfer of the human immunodeficiency virus protease inhibitor saquinavir. STUDY DESIGN: An ex vivo perfused human placental cotyledon model was used. Ten placental perfusion studies were performed, with concentrations of saquinavir in the maternal compartment ranging from 322 to 2197 ng/mL (within reference therapeutic ranges). Drug concentrations were determined by high-performance liquid chromatography. RESULTS: The mean (+/- SD) fetal transfer rate of saquinavir was 1.8% +/- 1.6%, and the mean (+/- SD) clearance index was 0.05 +/- 0.05. A mean (+/- SD) of 1.6% +/- 3.1% of the perfused saquinavir was retained by the cotyledon. The small amount of saquinavir that crossed the placenta corresponded to the fraction not bound to humanserum albumin. CONCLUSION: The low rate of placental transfer of saquinavir suggests that use of this antiretroviral drug by pregnant women may not lead to significant exposure of the fetus.
Authors: Sreeja Sudhakaran; Hany Ghabrial; Roger L Nation; David C M Kong; Neil M Gude; Peter W Angus; Craig R Rayner Journal: Antimicrob Agents Chemother Date: 2005-03 Impact factor: 5.191
Authors: C Vinot; L Gavard; J M Tréluyer; S Manceau; E Courbon; J M Scherrmann; X Declèves; D Duro; G Peytavin; L Mandelbrot; C Giraud Journal: Antimicrob Agents Chemother Date: 2013-01-07 Impact factor: 5.191
Authors: Sreeja Sudhakaran; Craig R Rayner; Jian Li; David C M Kong; Neil M Gude; Roger L Nation Journal: Br J Clin Pharmacol Date: 2007-12-17 Impact factor: 4.335
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