• The Korean Journal of Pharmacology
• /
• v.26 no.2
• /
• pp.219-226
• /
• 1990

Enalapril maleate tablets of two different producers were tested for bioequivalence. Enalapril is rapidly metabolized to an active metabolite, enalaprilat which inhibits angiotensin-converting enzyme (ACE). The pharmacokinetics of enalapril maleate and the time course of inhibition of plasma ACE activity after administration of the drugs were studied. Two single doses of 10mg each of enalapril maleate were administered orally to twelve male volunteers in a balanced, randomized, two-way crossover investigation. Plasma enalaprilat concentrations were determined over a 23-hour after the dose by enzyme inhibition assay and enalapril by the same method following in vitro hydrolysis. Urinary recoveries of enalapril and enalaprilat were determined for the calculation of renal clearance. Plasma ACE activity was determined by an enzyme assay. Peak plasma levels of enalapril were observed about 1 hour after the doses, and practically all enalapril had disappeared from plasma within 6 hour. Peak enalapril concentrations of both formulations were almost identical ($Vasotec^{\circledR}$, 61.38 ng/ml; $Beartec^{\circledR}$, 64.27 ng/ml). The values of the pharmacokinetic parameters of enalaprilat computed for $Vasotec^{\circledR}$ and $Beartec^{\circledR}$ tablets are presented in that order; area under the curve=330.63:320.96 $ng{\cdot}hr/ml$; peak concentration=38.63:39.43 ng/ml; time to peak=3.83:4.08 hour; elimination half-life=3.95:3.92 hours. No statistically significant difference was detected when area under the curve and all other parameters were compared. Using criteria of 95% confidence interval for the comparison of these parameters, only the upper limits of area under the curve and time to peak of enalapril were over 120%. All the parameters of enalaprilat were acceptable. Percent inhibition of plasma ACE to plasma enalaprilat concentration showed the sigmoid concentration-inhibition relationship. Time courses of plasma ACE inhibition after the administration of both formulations were quite similar. The formulations were found to be equivalent when compared on the premise that no significant difference was detected when pharmacokientic parameters and inhibition of ACE activity were compared, based on the confidence limits analysis.

• Korean Journal of Clinical Laboratory Science
• /
• v.47 no.4
• /
• pp.216-224
• /
• 2015

This study aims to identify the prevalence of sleep related disease in those who experienced car accidents caused by drowsy driving. To this end, a survey of usual sleep habits, polysomnography, and multiple sleep latency tests were conducted in 34 persons who experienced an accident after normal sleep (Group 1), 22 persons who experienced an accident after abnormal sleep (Group 2), and 17 persons who was proven to be normal as a result of polysomnography and had no accident (Group 3). In all, 192 persons responded to the preliminary survey and the results were compared and analyzed. Crossover analysis was conducted to test the homogeneity of statistical characteristics, and the physical characteristics by age were analyzed. In the survey of sleeping habits, there was a significance between groups in how often they woke up while asleep (p<0.01), how difficult it was to go back to sleep again after waking up from sleep (p<0.05), how early they woke up in the morning (p<0.05), how difficult it was to get up in the morning (p<0.05), how sleepy they felt in the daytime (p<0.01), and how tired they felt in the daytime (p<0.01). Furthermore, among 56 subjects who had an accident during drowsy driving, 94.6% (53 persons) were found to have sleep related diseases. This suggests that car accidents during drowsy driving is not simply caused by temporary lack of sleep but by sleep related diseases even when sleep is adequate, leading to car accidents. Therefore, this study is significant identifying the association between car accidents during drowsy driving and sleep related disorders. Furthermore, the data would be considered basic to prepare social measures against drowsy driving related to such sleep related disorders.