Effect of food on the bioavailability of lisinopril, a nonsulfhydryl angiotensin-converting enzyme inhibitor

• Published in: Journal of pharmaceutical sciences Vol. 75; no. 4; p. 395
• Main Authors: Mojaverian, P, Rocci, Jr, M L, Vlasses, P H, Hoholick, C, Clementi, R A, Ferguson, R K
• Format: Journal Article
• Language: English
• Published: United States 01.04.1986
• Subjects: Adult; Angiotensin-Converting Enzyme Inhibitors; Biological Availability; Enalapril - analogs & derivatives; Enalapril - blood; Enalapril - metabolism; Enalapril - urine; Food; Humans; Intestinal Absorption; Lisinopril; Time Factors
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600750416

A randomized, two-way, crossover study was performed on 18 normal volunteers to assess the influence of food on the bioavailability of lisinopril, (1-[N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline), a long-acting nonsulfhydryl angiotensin converting enzyme inhibitor. A single, 20-mg oral dose of lisinopril was administered to volunteers in the fasting state or following a standardized breakfast. Treatment periods were separated by 2-week intervals. No significant differences existed between fasting and fed regimens in the mean +/- SD area under the serum concentration-time curve (AUC0-120h; 1231 +/- 620 versus 1029 +/- 254 ng X h X ml-1), peak lisinopril serum concentration (86 +/- 48 versus 69 +/- 19 ng/mL), or time to peak lisinopril serum concentration (6.2 +/- 1.1 versus 6.8 +/- 1.0 h). Five-day urinary excretion of lisinopril was not altered by food (5.3 +/- 3.0 versus 5.1 +/- 2.0 mg). Based on the urinary data, the mean +/- SD bioavailability of lisinopril was not different following fasting or fed regimens (27 +/- 15 versus 26 +/- 10%). Unlike with captopril, food did not affect the bioavailability of lisinopril.