Formulation and Evaluation of Ciprofloxacin Hydrochloride Vaginal Pessaries

Main Article Content

E. I. Akpabio
S. I. Ofoefule

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) .

Downloads

Download data is not yet available.

Article Details

How to Cite
Akpabio, E. I., & Ofoefule, S. I. (2020). Formulation and Evaluation of Ciprofloxacin Hydrochloride Vaginal Pessaries. Nigerian Journal of Pharmaceutical and Applied Science Research, 3(2), 43–50. Retrieved from http://mail.nijophasr.net/index.php/nijophasr/article/view/65
Section
Articles
Author Biographies

E. I. Akpabio

Department of Pharmaceutics and Pharmaceutical Technology, University of Uyo, Uyo. Akwa Ibom State,
Nigeria

S. I. Ofoefule

Department of Pharmaceutical Technology and Industrial Pharmacy University of Nigeria, Nsukka, Nigeria

References

Cater, S. J. (2008) In: Cooper and Gunn’s Dispensing for Pharmaceutical Students. 12th ed., CBS India. p 326 – 328.

Chein, Y. W. (2007) Novel drug delivery systems. 2nd ed., Marcel Dekker, Inc. New York, pp. 529 – 583.

Gissinger and Stam (1980) A comparative evaluation of the properties of some tablet disintegrants. Drug Dev and Ind. Pharmacy, 6: 511– 538.

Hilier, S. Melissa, C. S. and William C. S. (2008) Bacterical Vaginosis In: K. K. Holmes et al. Sexually Transmitted Disease, 4th ed., MC Graw Hill, New York, pp 737 – 768.

Kalam, M. A., Humayunn, M., Par Vez, N., Yadav, S., Garg, A., Amin, K. S. and Sultand, Ali, A. (2007) Release kinetics of modified Pharmaceutical dosage forms: a review Continental J. Pharm. Sciences 1: 30– 35.

Ofoefule, S. I. and Ike-Unor, U. O. (2001) In vitro evaluation of bioadhesive polymers and tablet delivery systems for the dministration of dequialinium chloride to the vaginal epithelium. J. Phyto medicine and Therapeutics, 6: 98 – 105.

Ofoefule, S. I. (2002) Tablets In: A Textbook of Pharmaceutical Technology and Industrial Pharmacy. Samakin (Nig.) Ltd., Lagos pp 9 – 10.

Onyechi, J. O. and Martin, G. M. (2009) A method to determine adhesion of suppository mass on excised Intestinal tissue. Animal Research International, 6: 966 – 971.

Sitruk-Ware, R. (2005) vaginal delivery of contraceptives. Expert opinion drug delivery 2: 729 – 736.

Woolfson, A., Malcom, R., K. and Gallagher, R. (2000) Drug delivery by the Intra-vaginal route, Crit. Rev. Ther. Drug Carrier system, 17: 509 – 555.