PMID: 6403693Feb 1, 1983Paper

Vaginal absorption of a potent luteinizing hormone-releasing hormone analogue (leuprolide) in rats III: Effect of estrous cycle on vaginal absorption of hydrophilic model compounds

Journal of Pharmaceutical Sciences
H OkadaH Mima

Abstract

The effect of estrous cycle stages on vaginal absorption was determined by the use of insulin, phenolsulfonphthalein, and salicylic acid as hydrophilic model compounds. Absorption of these compounds was markedly affected by the stage, possibly due to the change of transport rate through the pore-like pathways. The absorption of phenolsulfonphthalein during proestrus and estrus is roughly one-tenth of that during metestrus and diestrus. An increase of the nonionized form of salicylic acid, produced by a lowered pH, resulted in an enhancement of absorption during proestrus and diestrus; higher contribution of the transport through the cell membrane possibly reduced an effect of the estrous cycle. However, consecutive daily administration of leuprolide halted the cycle at diestrus and reduced the cycle effect on the vaginal absorption of phenolsulfonphthalein; when the treatment was started at any of the four stages of the cycle, vaginal absorption was enhanced approximately 20%, with less variance than that observed in normal diestrous rats.

Citations

Jan 1, 1990·Journal of Clinical Pharmacology·V V Ranade
Jun 16, 2005·Animal Reproduction Science·A M Padula
Dec 19, 2009·Expert Opinion on Drug Delivery·Nisreen HassanJaved Ali
Feb 9, 2016·Reproductive Toxicology·Anthony R ScialliKary E Thompson
Feb 15, 2011·Journal of Controlled Release : Official Journal of the Controlled Release Society·Sherry Y WuNigel A J McMillan
Nov 8, 2015·Reproductive Toxicology·Anthony R ScialliKary E Thompson
Sep 1, 1989·Cancer Treatment Reviews·I M JacksonJ M Diver
Jun 25, 2008·International Journal of Pharmaceutics·T KanazawaH Okada

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