In-vitro and in-vivo evaluation of a matrix-controlled bromocriptine mesilate-releasing vaginal ring.

Abstract

The aim of this study was to evaluate the in-vitro release rates and in-vivo effectiveness of a controlled release, intravaginal dosage form of bromocriptine mesilate. The dimeticone (poly(dimethylsiloxane)) elastomer vaginal ring contained 3 mg bromocriptine mesilate and low molecular weight gelatin in a ratio of 1:3, and 10% propylene glycol. The daily release rate of the drug was designed to be 10% of the total administered dose and was confirmed with release experiments under sink conditions. The effect of the vaginal ring preparation on plasma prolactin level in the rabbit was investigated over a 10-day period. The results showed that the vaginal ring of bromocriptine mesilate significantly decreased the plasma prolactin level of the test group (P < 0.001-0.05) compared with the control and placebo groups. It was concluded that bromocriptine mesilate was effectively absorbed from rabbit vagina and that this controlled release intravaginal ring preparation of bromocriptine mesilate was effective in decreasing the plasma prolactin level in rabbits for ten days.