Pharmacokinetics of lovastatin extended-release dosage form (Lovastatin XL) in healthy volunteers
| Autor: | Gale Phillips, Robert Niecestro, Michael Lamson, Peter Lukacsko, Jason Shen, Lawrence Friedhoff |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Adult
Male Metabolite Biological Availability Pharmaceutical Science Pharmacology Dosage form chemistry.chemical_compound Pharmacokinetics Oral administration polycyclic compounds Humans Medicine Pharmacology (medical) Lovastatin Active metabolite Cross-Over Studies Dose-Response Relationship Drug business.industry organic chemicals nutritional and metabolic diseases General Medicine Crossover study chemistry Area Under Curve Delayed-Action Preparations lipids (amino acids peptides and proteins) Hydroxymethylglutaryl-CoA Reductase Inhibitors Lovastatin Acid business medicine.drug |
| Zdroj: | Biopharmaceutics & Drug Disposition. 23:143-149 |
| ISSN: | 1099-081X 0142-2782 |
| DOI: | 10.1002/bdd.304 |
| Popis: | The purpose of this study was to evaluate pharmacokinetics and dose proportionality of lovastatin extended-release dosage form (ER-lovastatin) in the dosage levels of 10, 20 and 40 mg in 9 healthy male subjects. Each subject was randomized to receive a single oral dose of ER-lovastatin either 10, 20 or 40 mg in a three-way crossover design with a washout period of 7 days between the treatments. Subjects were served dinner at approximately 5:30 PM followed by dosing at approximately 10:00 PM in each study period. Serial plasma samples were collected up to 48 h after dosing and assayed for lovastatin and its active metabolite lovastatin acid using an LC/MS/MS method. The plasma concentration-time profiles of lovastatin and its active metabolite lovastatin acid exhibited delayed- and extended-release characteristics at each dose. Mean (+/-) values for the C(max) of lovastatin were 1.04+/-0.43, 2.03+/-0.65 and 4.03+/-3.02 ng/ml for the 10, 20 and 40 mg dosage, respectively. The corresponding values for the AUC(0-48 h) of lovastatin were 14.6+/-7.8, 34.1 +/-13.7, and 53.9+/-35.6 ng h/ml. The same tendency was also found for C(max) and AUC(0-48 h) values of lovastatin acid. Results from this study demonstrated as the dose of ER-lovastatin increased from 10 to 40 mg, the C(max) and AUC(0-48 h) values of lovastatin as well as lovastatin acid appeared to increase linearly. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text