Dj. Kesler et al., THE EFFECT OF ESTERIFICATION ON THE RELEASE OF TESTOSTERONE AND ESTRADIOL FROM SILICONE IMPLANTS, Drug development and industrial pharmacy, 22(3), 1996, pp. 275-279
Four experiments were conducted to determine the effect of esterificat
ion on the release of testosterone and estradiol from capsule-type sil
icone implants. In castrated male rats testosterone propionate and, te
stosterone enanthate implants increased (P < .05) blood testosterone c
oncentrations and seminal vesicle weights move than empty and testoste
rone implants. Testosterone propionate and testosterone enanthate impl
ants released 4 times and 10 times, respectively, more equivalent test
osterone per cm(2) per day than testosterone implants. The increase in
blood testosterone concentrations was proportional to the increase in
implant release rate for testosterone propionate, but not for testost
erone enanthate. Although estradiol-17 beta implants increased (P < .0
5) uterine weights of ovariectomized rats, uterine weights in estradio
l benzoate implanted ovariectomized rats were 1.3 times greater than i
n estradiol-17 beta implanted rats. Estradiol benzoate implants releas
ed less than 0.5 times the amount of equivalent estradiol per cm(2) pe
r day than estradiol-17 beta implants.