DESIGN AND EVALUATION OF BUCCOADHESIVE CONTROLLED RELEASE FORMULATIONS OF PROCHLORPERAZINE MALEATE
Objective: The Purpose of this work was to design mucoadhesive tablets of prochlorperazine maleate to release the drug in buccal cavity for an extended period of time in order to avoid the first-pass metabolism.
Methods: Six formulations were prepared using different polymer like Xanthan gum, Locust bean gum, Carbopol 974P NF, HPMC K100MCR, Polyox-WSR301 and Gantrez AN139 as a mucoadhesive and controlled release agents. The formulations were tested for content uniformity, thickness, weight variation, friability, in vitro drug release, in-vitro bio-adhesion, swelling index and residence time.
Results: Drug excipient compatibility studies performed using DSC. The DSC studies revealed endothermic peak at 200oâ€“205oC for Prochlorperazine maleate. Similarly endothermic peaks were obtained for separate excipient when heated in the range of 50-300 Â°C indicating their melting points. There was no separate peak observed when the drug was mixed with the different polymers like Xanthan gum, locust bean gum, Carbopol 974 P, HPMC K100 MCR, Gantrez AN139 and Polyox-WSR301 in ratio (1:1) indicating that no interaction took place between drug and polymers used in the study. Dissolution studies of the tablets of the optimized batch (BDS-6) containing Carbopol 974P (CP) and HPMC K100 MCR showed extended release 90.65% up to 24 hr. The bioadhesive force of optimized formulation is 12.18Â±.011 gm and the maximum swelling index was observed in 3.87Â±.0057 h.
Conclusion: From the study it can be concluded that formulation BDS-6 containing Carbopol and HPMC K100 MCR give a promising result for sustained release action of PrM.
2. Wong FC, Yuen KH, Peh KK. Formulation and evaluation of controlled release eudragit buccal patches. Int J Pharm 1999;178:11-22.
3. Tiwari D, Sause R, Madan PL. Evaluation of polyoxymethylene homopolymers for buccal bioadhesive drug delivery device formulations. AAPS Pharm Sci 1999;1:50-7.
4. SC Sweetaman. Martindale the complete drug reference. 33rd. edition; 2012.
5. Nagasamy D, Venkatesh SS, Meyyanathan SN, Elango K, Suresh B, Santhi K. Design and evaluation of prochlorperazine maleatae sustained-release tablets: influence of hydrophilic polymers on the release rate and in-vitro evaluation. Int J Pharm Sci Nanotechnol 2010;3:965-77.
6. Shah R, Patel S, Patel H, Pandey S, Shah S, Shah D. Formulation development of Carvedilol compression coated tablet. Pharm Dev Technol 2013;18:906-15.
7. Dey P, Maiti S, Biswanth SA. locust bean gum and its application in pharmacy and biotechnology: an overview. Int J Curr Pharm Res 2012;4:7-11.
8. Sharmin N, Elias-Al-Mamun, Saiful Islam MD, Reza-ul Jalil. Preparation and characterization of lidocaine double layer buccal tablet using mucoadhesive carbopolÂ® polymers. Dhaka Univ J Pharm Sci 2011;10:29-34.
9. Ryan F Donnelly, MaelÄ±osa TC Mc C, Ahlam Zaid A, Eneko L, Emma Mc, Aaron JC. Hydrogel-forming microneedles prepared from â€˜â€˜Super swellingâ€™â€™ polymers combined with lyophilised wafers for transdermal drug delivery. PLOS One 2014;9:1-12.
10. Manivannan R, Balasubramaniam A, Prem Anand DC, Sandeep G, Rajkumar N. Development and in vitro evaluation of novel buccoadhesive tablet formulation of prednisolone. Acta Pharm 2002;52:121â€“7.
11. Desai KG, Kumar TM. Preparation and evaluation of a novel buccal adhesive system. AAPS PharmSciTech 2004;5:1-9.
12. Noha Adel N, Ismail FA, Boraie NA. Mortada LM. Mucoadhesive drug delivery systems. Evaluation of mucoadhesive polymers for buccal tablet formulation. Drug Dev Ind Pharm 2004;30:985-99.
13. Akbari J, Nokhodchi A, Farid D, Adrangui M, Siahi Shadbad RM, Saeedi M. Development and evaluation of buccoadhesive propranolol hydrochloride tablet formulation: effect of fillers. II Farmaco 2004;59:155-61.
14. Noha Adel N, Ismail FA, Boraie NA, Mortada LM. Mucoadhesive drug delivery systems. II. Formulation and in-vitro/in-vivo evaluation of mucoadhesive buccal tablets containing water soluble drugs. Drug Dev Ind Pharm 2004;30:995-1004.
15. Fabregas JL, Garcia N. In-vitro studies on buccoadhesive tablet formulation of hydrocortisone hemisuccinate. Drug Dev Ind Pharm 1995;21:1689-96.
16. Perioli L, Ambrogi V, Rubini D, Giovagnoli S, Ricci M, Balsi P, et al. Novel mucoadhesive buccal formulation containing metronidazole for the treatment of periodontal disease. J Controlled Release 2005;95:521-33.
17. Fergany A, Khedr MH. Preparation and in-vitro/in-vivo evaluation of the buccal bioadhesive properties of slow release tablets containing miconazole nitrate. Drug Dev Ind Pharm 2003;29:321-37.
18. Higiro J, Herald TJ, Alavi S, Bean S. Rheological study of xanthan and locust bean gum interaction in dilute solution: effect of salt. Food Res Int 2007;40:435â€“47.
19. Pandey S, Gupta A, Yadav JS, Shah DR. Formulation and in-vitro evaluation of bilayered buccal tablets of carvedilol. Indian J Pharm Edu Res 2010;44:259-66.