Gregg Patrick Adams,Ildiko Badea,Maria Jimena Yapura,Roger A. Pierson
申请号：
BR112015026298
公开号：
BR112015026298A8
申请日:
2014.04.17
申请国别(地区):
BR
年份:
2019
代理人:
摘要：
1/2 summary â € œDispensing vehicle, methods for delivering an aromatase inhibitor to the plasma of an individual, to synchronize ovulation, to induce superovulation, to improve fertility, to induce double ovulation and to improve the formation of twins in a mammal, use of a delivery vehicle, a luteolitic dose of a prostaglandin, and an ovulatory dose , and, kit to provide an aromatase inhibitor in the plasma of a fertile mammal described herein an intravaginal device that provides biologically active circulating concentrations of an aromatase inhibitor for at least about 4 days. three compounds with estradiol inhibiting capacity (letrozole, anastrozole and fenbendazole) were tested in vitro using bovine granular cell culture. letrozole was found to be the most efficient and potent inhibitor. liposome-based and wax-based formulations were used to evaluate letrozole diffusion through the bovine vaginal mucosa in a diffusion chamber study. the samples were collected over a 24-hour period. the wax-based vehicle was selected for the further development of an intravaginal letrozole device based on its fixed dispensing rate. in an in vivo study on cattle, 3 different intravaginal devices containing 3 g of letrozole were tested: wax (with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine, dope) + gel coating (n = 2), wax + gel coating (n = 4) and wax (n = 4). blood samples were collected in series from time 0 to 120 hours, and daily thereafter to measure circulating concentrations of letrozole by lc / ms / ms. the addition of a gel coating containing letrozole improved the initial absorption and accelerated the increase in plasma concentrations of the active ingredient, while the 2/2 wax-based vehicle maintained letrozole prolonged release from the intravaginal device.1 / 2 resumo “veã�culo de dispensaã‡ãƒo, mã‰todos para fornecer um inibidor da aromatase ao plasma de um indivã�duo, para sincronizar a ovulaã‡ãƒo, para induzir a superovulaã‡ãƒo, para melhorar a fertilidade, p
