Comparative Pharmacokinetics of Lovastatin Extended‐Release Tablets and Lovastatin Immediate‐Release Tablets in Humans

Journal of Clinical Pharmacology - Tập 42 Số 2 - Trang 198-204 - 2002
Jim X. Sun1, Robert Niecestro1, Gale Phillips1, Jiajian Shen1, Peter Lukacsko1, Lawrence Friedhoff1
1Department of Clinical Research, Andrx Laboratories, Inc., Andrx Corporation, Fort Lauderdale, Florida.

Tóm tắt

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.

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Journal of Clinical Pharmacology

Tập 42 Số 2

198-204

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