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“Background: Eplerenone (CAS 107724-20-9) prevents the binding of aldosterone, a key hormone in the renin-angiotensin-aldosterone-system (RAAS), which is involved in the regulation of blood pressure and the pathophysiology of cardiovascular disease and is indicated, in addition to standard therapy including beta-blockers, to reduce the risk of cardiovascular mortality and morbidity in stable patients with left ventricular dysfunction (LVEF <= 40%) and clinical evidence of heart failure after recent myocardial infarction.
Objective: The aim of this study was to assess the bioequivalence
of a new eplerenone 50 mg formulation (test formulation) vs. the reference product, as required by European regulatory authorities Bafilomycin A1 chemical structure for the marketing of a generic product.
Methods: This was a single-center, randomized, single-dose, open-label, 2-way crossover study in healthy volunteers under fasting conditions.
Plasma samples were collected up to 24 h post-dosing and plasma eplerenone levels were determined by reversed phase high performance liquid chromatography and by tandem mass spectrometry detection (ie, the LC-MS/MS
method). Pharmacokinetic parameters were calculated using non-compartmental analysis.
Area under the concentration-time PARP cancer curve from time zero to time of last non-zero concentration (AUC(last)) and maximum observed concentration (C(max)) were the main evaluation criteria. All of the above-mentioned pharmacokinetic parameters were analyzed using 90% geometric confidence interval of the ratio (T/R) of least-squares means from the ANOVA of the In-transformed parameter. Tolerability
was monitored using physical examination, including vital sign measurements and laboratory analysis.
Results: According to the classical approach, the 90% geometric confidence intervals obtained by analysis of variance for AUC(last) and C(max) were within the pre-defined ranges (80.00-125.00%).
Conclusion: Bioequivalence between test and reference formulations, both in terms of rate and extension of absorption, under fasting conditions was concluded according to European guidelines. Both formulations were well tolerated.”
“OBJECTIVE: To selleck inhibitor assess the prevalence of established cardiovascular disease risk factors and to estimate 10-year absolute risk of cardiovascular disease after early-onset preeclampsia.
METHODS: We assessed major cardiovascular disease risk factors in 243 primiparous women with a history of early-onset preeclampsia (delivery at less than 34 weeks of gestation) at least 6 months after delivery; 374 healthy nonpregnant women of similar age served as a reference group.
RESULTS: After adjustment for age, we observed significantly higher means for body mass index, blood pressure, total and low-density lipoprotein cholesterol, triglycerides, glucose, and lower mean high-density lipoprotein cholesterol (all P<.01) in women with previous early-onset preeclampsia compared with the reference group.