Delivery of dehydroepiandrosterone to premenopausal women: effects of micronization and nonoral administration.
OBJECTIVE
This single-dose study compares three dehydroepiandrosterone delivery methods (oral crystalline steroid, micronized steroid, and vaginal administration) to ascertain whether physiologic levels of circulating dehydroepiandrosterone and dehydroepiandrosterone sulfate can be obtained while increases in testosterone are minimized.


METHODS
Two randomized, double-blind, placebo-controlled single-dose comparisons were made. For oral micronized versus crystalline dehydroepiandrosterone 300 mg doses of micronized or crystalline dehydroepiandrosterone were administered, followed by 6 hours of blood sampling (n=7). Serum dehydroepiandrosterone, dehydroepiandrosterone sulfate, and testosterone levels were measured; areas under the curve and mean peak values were analyzed by Student-Newman-Keuls tests. For oral versus vaginal micronized dehydroepiandrosterone 150 mg oral or vaginal doses of micronized dehydroepiandrosterone were administered, followed by blood sampling over 12 hours (n=5). Data analysis was as described.


RESULTS
Oral micronized and unmicronized dehydroepiandrosterone resulted in increases in serum dehydroepiandrosterone, dehydroepiandrosterone sulfate, and testosterone. Micronization increased the area-under-the-curve ratios for dehydroepiandrosterone sulfate/dehydroepiandrosterone and dehydroepiandrosterone sulfate/testosterone. Vaginal administration provided equivalent serum dehydroepiandrosterone; however, it failed to increase dehydroepiandrosterone sulfate or testosterone over placebo.


CONCLUSIONS
Micronization of oral dehydroepiandrosterone diminishes bioconversion to testosterone. Vaginal dehydroepiandrosterone delivers equivalent dehydroepiandrosterone but substantially diminishes dehydroepiandrosterone bioconversion.
Casson
P R
PR
Division of Reproductive Endocrinology and Infertility, The University of Tennessee, Memphis, USA.
Straughn
A B
AB
Umstot
E S
ES
Abraham
G E
GE
Carson
S A
SA
Buster
J E
JE
D000282:Administration, Intravaginal; D000284:Administration, Oral; D000328:Adult; D003460:Crystallization; D003687:Dehydroepiandrosterone / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics; D019314:Dehydroepiandrosterone Sulfate; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D010919:Placebos; D011208:Powders; D017697:Premenopause; D013739:Testosterone / Q000097:blood
D010919:Placebos; D011208:Powders; D013739:Testosterone; D003687:Dehydroepiandrosterone; D019314:Dehydroepiandrosterone Sulfate