Formulation and testing of a non-steroidal aromatase inhibitor intravaginal device for the control of ovarian function in XXXX .

@entity18172 @entity4672 @entity1420 @entity53 @entity13558 @entity291
UNASSIGNED: The study was designed to formulate intravaginal devices that provide biologically active circulating concentrations of an aromatase inhibitor for a minimum of 4 days, and to determine their physiologic effects in @entity291 . Three compounds with @entity53 inhibitory capability ( @entity4672 , @entity13558 and @entity18172 ) were tested in vitro using @entity291 granulosa cell culture. @entity4672 was found to be the most efficient and potent inhibitor. A wax-based vehicle was selected for further development of a @entity4672 intravaginal device based on its steady release rate. Cycling heifers were assigned randomly to be given an intravaginal device containing wax plus gel coat (n=4), wax formulation (n=4), no formulation (blank device, control, n=4). Intravaginal devices were inserted on Day 3 (Day 0=ovulation) and kept in place for 8 days. The addition of a @entity4672 -containing gel coating hastened the initial increase on plasma concentrations, while the @entity4672 -containing wax-based vehicle maintained prolonged delivery from the intravaginal device. The dominant follicle diameter profile was larger in heifers treated with the wax plus gel coat device (P<0.04), and the interwave interval was prolonged in heifers in the @entity4672 -treated groups compared to controls (P<0.001). Plasma @entity53 concentrations were reduced significantly in the @entity4672 -treated groups. Plasma @entity1420 concentrations were lower in the wax @entity4672 -treated group (P<0.02). We concluded that wax base plus gel coat intravaginal devices are suitable for the development of a @entity4672 -based protocol for the synchronization of ovulation in @entity291 . It effectively reduced @entity53 production resulting in prolonged dominant follicle growth and lifespan, without adversely affecting @entity1420 production.
