Evaluation of Pharmacokinetics and Safety Profile of Estradiol in Postmenopausal Females of India after Oral Administration of Estrogen Tablets

Abstract

Purpose: The study was conducted for assessing the pharmacokinetic evaluation and safety profile of the estrogen, when administered in postmenopausal women of Lidian race. Experimental Design: 10 postmenopausal females received oral estrogen tablet of 2 mg once daily. We measured plasma concentrations of Estradiol by LC-MS/MS method at different time points i.e. -48 hrs, -24 hrs, 0 hrs, 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 7.5, 12, 16, 24, 48, 72 hrs. The incidence and severity of adverse events were assessed by physical examination and patient reporting. Results: Following oral administration of 2 mg of estrogen tablets to 10 post menopausal females, we observed for Estradiol the Cmax 457.05 (±144.53), AUCt of 5460.12 (±1726.64), AUCoo 47247.271 (±16704.43), tmax 8.5 (± 2.68), Kel 0.028 (±0.10) and tVz 230.496 (±81.49). Few adverse events have been reported like hot flushes, vomiting, and diarrhea during the study. All drug-related adverse events were either grades 1 or 2 as per CTCAE guidelines (ver 04); none was unexpected. Conclusions; This study provides evidence that administration of estrogen in hidian post menopausal females was well tolerated and provides both pharmacokinetics and safety profile of the drug. Further clinical investigation is recommended. Key Words: Pharmacokinetic, Estrogen, Estradiol, Postmenopausal.