title: Evaluation of sustained/controlled-release dosage forms of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors in dogs and humans.
abstract: Seven sustained/controlled-release dosage forms were designed for gastrointestinal delivery of lovastatin or simvastatin, two potent HMG-CoA reductase inhibitors for the treatment of hypercholesterolemia. The in vivo performance of these formulations was evaluated in dogs and healthy volunteers in terms of the cholesterol lowering efficacy and/or systemic concentrations of HMG-CoA reductase inhibitors. Results from the present and previous studies suggest that, through the controlled release of HMG-CoA reductase inhibitors, sustained lower plasma concentrations of HMG-CoA reductase inhibitors may result in an equal or better therapeutic efficacy.
authors.affiliation: Merck Research Laboratories, West Point, Pennsylvania 19468.
authors.forename: H
authors.initials: H
authors.lastname: Cheng
authors.forename: S C
authors.initials: SC
authors.lastname: Sutton
authors.forename: J D
authors.initials: JD
authors.lastname: Pipkin
authors.forename: G M
authors.initials: GM
authors.lastname: Zentner
authors.forename: J D
authors.initials: JD
authors.lastname: Rogers
authors.forename: J I
authors.initials: JI
authors.lastname: Schwartz
authors.forename: Y B
authors.initials: YB
authors.lastname: Mitchel
authors.forename: K
authors.initials: K
authors.lastname: Grasing
authors.forename: M S
authors.initials: MS
authors.lastname: Schwartz
authors.forename: R D
authors.initials: RD
authors.lastname: Amin
mesh_terms: D000328:Adult; D000818:Animals; D003692:Delayed-Action Preparations; D004285:Dogs; D004311:Double-Blind Method; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008148:Lovastatin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008297:Male; D019821:Simvastatin
chemical_list: D003692:Delayed-Action Preparations; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008148:Lovastatin; D019821:Simvastatin