Vaginal distribution and retention of tablets comprising starch-based multiparticulates: evaluation by colposcopy

Abstract

We have developed fast-disintegrating tablets comprising starch-based pellets and excipient granules for intravaginal drug delivery. The purpose of this study was to evaluate the intravaginal disintegration, distribution and retention behavior of these tablets in sheep and women using colposcopy as visualization technique. One tablet was administered to each study subject (n = 6) and repeated colposcopy examination was performed over a 48 h and 24 h period in sheep and women, respectively. Colposcopy in sheep indicated that in vivo tablet disintegration was initiated within 30 min of vaginal administration and that due to disintegration of the pellets themselves, the formulation was transformed into a gel-like mass which distributed throughout the entire vaginal cavity within 2–4 h. In vivo tablet disintegration after intravaginal administration to women was complete within 4 h, whereby the formulation gradually spread throughout the vaginal cavity as complete covering was observed after 12 and 24 h. The persistent retention (up to 24 and 48 h in women and sheep, respectively) confirmed the long retention time of this vaginal formulation.