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Steady‐State Relative Bioavailability of Three Oral Ganciclovir Dosage Regimens Delivering 6,000 mg/day in Patients with Human Immunodeficiency Virus
Author(s) -
Jung Donald,
Griffy Kay,
Wong Rodney,
Colburn Wayne,
Hulse Jim
Publication year - 1998
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/009127009803801106
Subject(s) - ganciclovir , bioavailability , regimen , pharmacokinetics , crossover study , medicine , pharmacology , human cytomegalovirus , dosage form , gastroenterology , virus , immunology , placebo , alternative medicine , pathology
This study was designed to determine the steady‐state relative bioavailability of ganciclovir after three dosage regimens designed to deliver 6,000 mg/day. The study design was an open‐label, randomized, three‐treatment crossover design in which 22 human immunodeficiency virus (HIV) and cytomegalovirus (CMV) seropositive patients received in random order multiple oral doses of ganciclovir 1,000 mg six times a day, 1,500 mg four times a day, and 2,000 mg three times a day. Blood samples were obtained on day 3 of each oral regimen over a 24‐hour time interval. Mean steady‐state average serum concentrations of ganciclovir were greater than 1.0 μg/mL, which exceeds the median in vitro inhibitory concentration (IC 50 ) of most CMV isolates (0.5–1.0 μg/mL). All three regimens resulted in values for area under the concentration—time curve from 0 to 24 hours (AUC 0–24 ) that were comparable to those seen after maintenance ganciclovir intravenous infusions of 5 mg/kg/day. The 1,000 mg six times daily regimen resulted in an AUC 0–24 that was significantly higher than that of the 1,500 mg four times daily or the 2,000 mg three times daily regimens, although the differences were less than 12.5% .