Formulation and In Vivo Evaluation of Mucoadhesive Buccal Tablets of Carvedilol

DOI:

https://doi.org/10.37285/ijpsn.2013.6.3.8

Authors

  • S. B. Shirsand
  • G V Wadageri
  • S A Raju
  • Gopikrishna Kolli

Abstract

In present study we studied the feasibility of preparing mucoadhesive buccal delivery systems containing carvedilol to improve drug residence time on buccal mucosa and drug dissolution rate, to circumvent the first-pass metabolism and quick drug entry into the systemic circulation. Bilayer buccal tablets of carvedilol prepared using controlled release and mucoadhesive polymers (hydroxypropyl methylcellulose 15 cps, 50 cps, K4M and Carbopol 934p) along with impermeable backing layer (ethyl cellulose). 15 formulations were developed with varying concentrations of polymers. The designed tablets were evaluated for tablet size, shape, in vitro drug release, stability studies, bioavailability studies and drug-excipients interaction (FTIR). Among the 15 formulations, F151 containing hydroxypropyl methylcellulose 15 cps (48% w/w of matrix layer), Carbopol 934p (2% w/w of matrix layer) and mannitol (channeling agent, 34.5% w/w of matrix layer) was found to be promising. Dissolution tests revealed that 84.73% of carvedilol was dissolved from the formulation F151 in 8 h along with satisfactory bio adhesion strength (5.71 g). Bioavailability studies of the promising formulation were compared with that of the oral solution.  The percentage relative bioavailability of the buccal tablets was found to be 121.27%. Stability studies, on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics (p<0.05). FTIR studies show no evidence of interaction between drug and excipients. It was concluded that mucoadhesive buccal tablets of carvedilol with controlled unidirectional drug release along with satisfactory bioadhesion strength and with sufficient residence time can be successfully developed by direct compression method.

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Buccal tablets, Carvedilol, Carbopol 934p, Swelling index, Bioadhesive strength

Downloads

Published

2013-11-30

How to Cite

1.
Shirsand SB, Wadageri GV, Raju SA, Kolli G. Formulation and In Vivo Evaluation of Mucoadhesive Buccal Tablets of Carvedilol. Scopus Indexed [Internet]. 2013 Nov. 30 [cited 2024 Oct. 16];6(3):2164-71. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/637

Issue

Section

Research Articles

References

Alur H.H., Pather S.I., Mitra A.K. and Johnston T.P (1999). Transmucosal sustained delivery of chlorpheniramine maleate in rabbits using a novel, natural mucoadhesive gums as an excipient in buccal tablets. Int. J. Pharm. 188: 1-10.

Ambrogiv V., Perioli L., Stefano G., Ricci. M., Blasi P. and Carlo. R (2007). Mucoadhesive bilayered tablets for buccal sustained release of flurbiprofen. AAPS. Pharm. Sci. Tech. 8: E1-E6.

Arya R.K., Garud A., Jain N.K. and Garud N (2010). Development and evaluation of mucoadhesive buccal tablets of salbutamol sulphate. Int. J. Pharma. Pharm. Sci. 2: 40-2.

Beckett A.H., and Hossie R.D (1971). Buccal absorption of drugs. Handbuch der Experimentellen pharmakologie. Gillette. Berline. 28: 1-60.

Carvalho F.C., Bruschi M.L., Evangelista R.C. and Gremião M.P.D (2010). Mucoadhesive drug delivery systems. J Pharm Sci 46: 1-17.

Choi H.G. and Kim C.K (2000). Development of omeprazole buccal adhesive tablets with stability enhancement in human saliva. J.Control Rel 68: 397-404.

Desai K.G.H. and Kumar T.M.P (2004). Preparation and evaluation of a novel buccal adhesive systems. AAPS Pharm.Sci Tech 5: 1-9.

Deshmukh V.N., Jadhav J.K. and Sakarkar D.M (2009). Formulation and in vitro evaluation of theophylline anhydrous bioadhesive tablets. Asian. J. Pharm. 3: 54-58.

Gupta A. Garg S. and Khar R.K (1992). Mucoadheshive buccal drug delivery system- A review. Indian Drugs 29: 586-93.

Hägerström., Edsman K. and Strømme M (2003). Low-Frequency Dielectric Spectroscopy as a Tool for Studying the Compatibility between Pharmaceutical Gels and Mucus Tissue. J Pharm Sci 92: 1869-1881.

Harries D., and Robinson J.R (1992). Drug delivery via the mucous membranes of the oral cavity. J. Pharm. Sci. 81: 1-10.

Huang Y., Leobandung W., Foss A. and Peppas N.A (2000). Molecular aspects of muco- and bioadhesion: Tetheres structures and site-specific surfaces. J. Control. Release. 65: 63-71.

Madgulkar A., Bhalekar M., Wable N., Patel K. and Kolhe V (2008). Egg shell membrane as substrate for bioadhesion measures. Indian Drugs. 45: 219-21.

Manivannan R., Balasubra M.A., Preanand D.C., Sandeep G. and Rajkumar N (2008). Formulation and in-vitro evaluation of mucoadhesive buccal tablets of diltiazem hydrochloride. Res. J. Pharm. Tech. 1: 478-480.

Mohammed F.A. and Khedr H (2003). Preparation and in vitro/in vivo evaluation of buccal bioadhesive properties of slow release tablets containing miconazole nitrate. Drug Dev Ind Pharm. 29: 321-37.

Mutalik S., Naha A., Usha A.N., Ranjith A.K. and Musmade. P (2007). Preparation, in vitro, preclinical and clinical evaluation of once daily sustained release tablets of aceclofenac. Arch. Pharm. Res. 30: 222-34.

Patel V.M., Bhupendra G.P., Patel H.V. and Patel K.M (2007). Mucoadhesive bilayer tablets of propranolol hydrochloride. AAPS. Pharm. Sci. Tech. 8: E1-E6.

Paul W.S., Heng. and Jinsong Hao (2003). Buccal Delivery Systems. Drug. Devel Ind Pharm. 29: 821-32.

Shindhaye S.S., Thakkar P.V., Dand N.M. and Kadak V.J (2010). Buccal drug delivery of pravastatin sodium. AAPS. Pharm.Sci.Tech 11: 416-23.

Swamy P.V., Pawndeep Singh., Hiremath S.N., Shirsand S.B., Neelima and Raju SA (2007). Preparation and evaluation of chitosan buccal films of diltiazem hydrochloride. Indian Drugs. 44: 137-9.

Sweetman SC (2007). The complete drug referene, 35th ed. Pharmaceutical Press, London, pp.1211.

Woodley J (2001). Bioadhesion, new possibilities for drug administration. Clin. Pharmacokinet. 40: 77-84.