Premium
Comparative Pharmacokinetics of Lovastatin Extended‐Release Tablets and Lovastatin Immediate‐Release Tablets in Humans
Author(s) -
Sun Jim X.,
Niecestro Robert,
Phillips Gale,
Shen Jason,
Lukacsko Peter,
Friedhoff Lawrence
Publication year - 2002
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 - 10.1177/00912700222011111
Subject(s) - lovastatin , pharmacokinetics , pharmacology , bioavailability , chemistry , medicine , chromatography , cholesterol , biochemistry
The pharmacokinetics of lovastatin and its active metabolite lovastatin acid was evaluated in 9 healthy subjects in a three‐period crossover study following a single oral dose of lovastatin extended‐release (ER) tablets and lovastatin immediate‐release (IR) tablets. Participants were dosed with lovastatin IR 40 mg tablets following a standard breakfast, lovastatin ER 40 mg tablets following a standard breakfast, and lovastatin ER 40 mg tablets under fasting conditions. Serial plasma samples were collected for up to 48 hours postdose and assayed for lovastatin and lovastatin acid using a liquid chromatography/mass spectroscopy/mass spectroscopy method. Lovastatin ER tablets, unlike lovastatin IR tablets, exhibited delayed‐ and extended‐release characteristics. The relative bioavailabilitv, in terms of area under the curve values, of lovastatin (156%) and lovastatin acid (124%) was greater from lovastatin ER tablets as compared with lovastatin IR tablets when given with breakfast. An even greater increase in the bioavailability of lovastatin (261%) and lovastatin acid (231%) was observed when the lovastatin ER tablets were administered under fasting conditions. Thus, greater gastrointestinal tract drug absorption of lovastatin from lovastatin ER tablets was demonstrated. Ingestion of a standard breakfast prior to administration of lovastatin ER tablets decreased absorption of lovastatin by approximately 40%, relative to lovastatin ER tablets under fasting conditions.