Search

In this study, a heterologous competitive indirect enzyme-linked immunosorbent assay (ciELISA) for the determination of estriol (E3) in milk was developed. Rabbit polyclonal antibody specific for E3 was raised by introducing a carboxyl spacer arm from bromoacetic acid of E3 as immunizing hapten. A heterologous ciELISA using a coating hapten containing a carboxyl spacer arm from 6-ketoestriol of E3. The assay exhibited the required sensitivity for detection of E3 with limit of detection of 0.07 ng mL−1 and a working range from 0.41 ng mL−1 to 15.78 ng mL−1. Good recoveries were obtained ranging from 83.2% to 125.8% for E3 spiked milk samples. A satisfactory correlation (R2 = 0.994) between the results of ciELISA analysis and that of LC–MS/MS analysis indicated good accuracy and reproducibility of the proposed method, which was ideally suited as a rapid screening tool for routine E3 monitoring. [ABSTRACT FROM AUTHOR]

Objectives: To investigate the pharmacokinetics, safety and preliminary effectiveness of ultra-low-dose estriol vaginal gel formulations (20 μg/g (T1) and 50 μg/g (T2)) compared to Ovestinon® (estriol 500 μg/0.5 g (R)) and placebo in postmenopausal women.Methods: Forty-three volunteers were randomly assigned to received T1, T2, R or placebo once daily for 21 days. Absorption of estriol after single and multiple administration was analyzed. Cytological changes in the vagina, tolerability and safety were also investigated.Results: Thirty-six women were included in the pharmacokinetic analysis. Systemic absorption was lower with test formulations (AUC0-t: 171.65 ± 80.18 (T1) and 406.75 ± 199.53 (T2) pg/ml × h) than with Ovestinon® (1221.97 ± 549.06 pg/ml × h). Estriol exposure of the test formulations after multiple administration (AUCss: 36.33 ± 30.52 (T1) and 73.71 ± 46.86 (T2) pg/ml × h) was significantly lower than after single-dose administration and not significantly different between them. In contrast, the exposure after repeated administration of Ovestinon® was considerable and not statistically different from levels after single administration. All estriol formulations produced similar improvement in the vaginal maturation value, while placebo showed a small and not significant change. Overall safety and acceptability were good.Conclusions: Estriol 20 and 50 μg/g formulations, while showing a comparable capacity for reversing vaginal atrophy, present a highly favorable safety profile, producing a very low systemic absorption of estriol and significantly lower than that of Ovestinon®. [ABSTRACT FROM AUTHOR]