Heimer G M, Englund D E
Maturitas. 1986 Oct;8(3):239-43. doi: 10.1016/0378-5122(86)90031-9.
The aim of this trial was to study the vaginal absorption of oestriol and to investigate whether morning rather than evening oestriol administration would produce different plasma oestriol patterns. The influence of food intake on plasma oestriol levels was also investigated. Nine post-menopausal women were given 0.5 mg oestriol (ovula supplied by Leo AB, Sweden) intravaginally every evening for 16 days. Thereafter, 1 mg oestriol was given every evening for another 5 days, except on treatment days 18 and 19 when 1 mg oestriol was given in the morning instead. Venous blood samples were collected at frequent intervals on day 19 (morning administration) and a meal was allowed 4 h later. On the day 21 (evening administration), venous blood samples were taken at frequent intervals during the night and no meal was given until the next morning. Plasma concentrations of unconjugated oestriol were measured by means of a specific radioimmunoassay (RIA). A difference was seen in the plasma oestriol patterns when the results following morning and evening administration were compared. However, no significant difference as regards the total 24-h systemic availability of oestriol was observed. A minimal increase in plasma oestriol levels was seen after a meal in the case of both morning and evening intravaginal oestriol administration, possibly as a result of enterohepatic recirculation.
本试验的目的是研究雌三醇的阴道吸收情况,并调查早晨而非晚上给予雌三醇是否会产生不同的血浆雌三醇模式。还研究了食物摄入对血浆雌三醇水平的影响。9名绝经后妇女每晚阴道内给予0.5毫克雌三醇(由瑞典Leo AB公司提供的栓剂),持续16天。此后,除了在治疗的第18天和第19天早晨给予1毫克雌三醇外,每晚再给予1毫克雌三醇,持续5天。在第19天(早晨给药)频繁采集静脉血样,4小时后允许进食。在第21天(晚上给药),夜间频繁采集静脉血样,直到第二天早晨才给予食物。通过特定的放射免疫测定法(RIA)测量未结合雌三醇的血浆浓度。比较早晨和晚上给药后的结果时,血浆雌三醇模式存在差异。然而,未观察到雌三醇24小时全身总可用性有显著差异。无论是早晨还是晚上阴道内给予雌三醇,进食后血浆雌三醇水平均有轻微升高,这可能是肠肝循环的结果。