Formulation and Evaluation of Ciprofloxacin Hydrochloride Vaginal Pessaries

Abstract

Ciprofloxacin hydrochloride pessaries were formulated and evaluated for weight uniformity, bioadhesion on pig rectum, drainage through pig rectum and dissolution profile through an artificial membrane as well as determination of their melting points range. The ciprofloxacin pessaries were torpedo shaped with no visible cracks or depressions. The coefficient of weight variations ranged from 0.006 to 0.183%. Pessaries that contained 0.2% Primogel®, 0.01% Ac-Di-Sol® and 0.1% Sterotex® had percentage erosion of 29.73% ± 15.3, 36.46 ± 8.1 and 35.75 ± 1.8% respectively, while those that contained no additive, 0.1% Primogel® 0.2% Sterotex®, 0.01% Carbopol 971 and the pessary containing a mixture of PEG4000 and PEG8000 (ratio 1:1) had percentage erosions of 22.15 ± 3.60, 22.92 ± 7.30, 22.15 ± 3.60, 21.00 ± 3.90 and 18.51 ± 3.40% respectively. Results of bioadhesion of the pessaries to pig rectum showed 100% bioadhesion except the control batch which had bioadhesion of 66.7%. Pessaries containing no additive exhibited the highest drainage (66.9%) and the least percentage of pessary retained on the pig rectum, while the pessaries containing 0.01% Ac-Di-Sol® exhibited the least drainage (11.5%) and the highest percentage of the pessary (88.5%) retained on the pig rectum. All the pessaries melted within the temperature range of 38 to 420C. Fastest release through an artificial membrane occurred from pessaries containing 0.2%. Primogel® and slowest from pessaries that contained no additive. The mechanisms and kinetics of drug release were also evaluated. Results indicated that formulations containing 80% PEG 4000, 1% Primogel® as well as 0.1% Sterotex followed zero order kinetics via non-Fickian mechanism. Formulations containing 0.01% Ac-Di-Sol® followed Higuchi and zero order kinetics (r2 = 0.978, 0.9961) with diffusion controlled mechanism (n = 0.50). The formulation containing 0.1% Carbopol 971® exhibited, Higuchi kinetics with Fickian diffusion mechanism (n = 0.52). (r2 = 0.9032) .