Asian Journal of Research in Pharmaceutical Sciences

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Development and Characterization of Novel Trans Buccoadhesive Bilayer Tablets of Tapentadol Hydrochloride


Affiliations
1 Jawaharlal Nehru Technological University Kakinada, Kakinada, A. P, India
2 Department of Pharmaceutics, Sri Padmavati Mahila Visvavidyalayam, Tirupati, A. P, India
3 Department of Pharmaceutics, Andhra University, Vishakhapatnam, A. P, India
     

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Buccoadhesive bilayer tablets of Tapentadol Hydrochloride were prepared and evaluated in this investigation. Tapentadol is a centrally-acting opioid analgesic, having potency between morphine and tramadol. The direct compression method was used for preparing tablets. The polymers were employed in the formulations are Carbopol 934 P, Eudragit RL 100, sodium alginate, Chitosan, and polyvinylpyrrolidone-K30 (PVP) and ethyl cellulose (EC) as a backing layer. The prepared formulations were evaluated for their physicochemical characteristics, swelling index, surface pH, ex vivo buccoadhesive strength, in vitro, in vivo drug release and ex vivo permeation studies. The significant differences in the results were observed, which dependent on characteristics and composition of bioadhesive materials used. Stability studies were conducted in natural human saliva and accelerated conditions, results reveals no significant change in physical appearance. Drug content, buccoadhesive strength and the P-value shown statistically significant at <0.05. Ex vivo mucous irritation by histological examination reveals, the administration site of buccal tablet over the buccal mucosa did not cause any irritation, ulceration, inflammation and redness, and it resembles to controlled buccal mucosa. Good correlations were observed between in vitro and in vivo drug release, with a correlation coefficient of 0.997. Drug diffusion from buccal tablets showed apparently zero order kinetics and release mechanism was diffusion controlled after considerable swelling.

Keywords

Tapentadol Hydrochloride, Opioid Analgesic, Buccoadhesive, Bilayer Tablets, Zero Order Kinetics.
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  • Andrews G.P., Laverty T.P., Jones D.S., Mucoadhesive polymeric platforms for controlled drug delivery, Eur. J. Pharm. Biopharm. 2009;71: 505-518.

  • Gilles P., Ghazali F.A., Rathbone J. Systemic oral mucosal drug delivery systems and delivery systems, in: M.J. Rathbone (Ed.), Oral Mucosal Drug Delivery, Vol. 74, Marcel Dekker Inc, New York, 1996; 241-285.

  • Titration of tapentadol. www.fresh patents .com/20090108pt an20090012180.php retrieved on 20 Jul 15:04:30 GMT

  • Terlinden R, Ossig J, Fliegert F, et al., Absorption, metabolism, and excretion of 14 C-labeled tapentadol HCl in healthy male subjects. Eur J Drug Me tab Pharmacokinetic. 2007 JulSep;32(3):163-9.

  • M Alagusundaram, C M Chetty, D Dmoorthi., Development and evaluation of novel transbuccoadhesive bilayertablets of Famotidine, Asian Journal of Pharmaceutics; 10.4103/0973- 8398.91990, July -Sep 2012.

  • Sevda Senel and A. Atilla Hincal. Drug permeation enhancement via buccal route: possibilities and limitations. Journal of Controlled Release 2001; 72:133-144.

  • Parvez N, Ahuja A, Khar RK. Development and evaluation of mucoadhesive buccal tablets of Lignocaine Hydrochlorid, Ind J Pharm Sci. 2002; 64(6): 563-567.

  • Rafiee M and Jazayeri C, Development and in-vitro evaluation of Novel Bucoadhesive tablet formulation of prednisolone, Acta Pharm. 2002; 52: 121-127.

  • Sahini J, Raj S, Ahmad F, et l., Design and in vitro characterization of buccoadhesive drug delivery system of insulin. Indian J Pharm Sci 2008;70:61-5.

  • Singh B, Ahuja N. Development of controlled release buccoadhesive hydrophilic matrices of diltiazem hydrochloride: Optimization of bioadhesion, dissolution and diffusion parameters. Drug Dev Ind Pharm 2002;28:431-42.

  • Miyazaki S, Kawasaki N, Nakamura T, et al. Oral mucosal bioadhesive tablets of pectin and HPMC: in vitro and in vivo evaluation. Int J Pharm 2000;204: 127-32.

  • Ribeiro L, Ferreira DC, Veiga FJ. In vitro controlled release of vinpocetine–cyclodextrin–tartaric acid multicomponent complexes from HPMC swellable tablets. J Control Release 2005;103:325-39.

  • Bouckaert S, Lefebvre RA, Colardyn F et al., Influence of the application site on bioadhesion and slow-release characteristics of a bioadhesive buccal slow-release tablet of miconazole. Eur J Clin Pharmacol 1993; 44: 331-335.

  • Jafar A, Ali N, D Javad F, et al., Development and evaluation of buccoadhesive propranolol hydrochloride tablet formulation: effect of fillers. Farmaco 2004; 59:155-161.

  • Gupta A, Garg S, Khar LK. Measurement of bioadhesive strength of mucoadhesive buccal tablets: design of an in vitro assembly. Indian drugs 1993; 30 (4): 152-5.

  • Nakhat PD, Kondawar AA, Babla IB, et al., Studies on buccoadhesive tablets of terbutaline sulphate. Indian J Pharm Sci 2007;69:505-10.

  • Vyas SP, Khar KR, editors. Controlled drug delivery concepts and advances, 1 ed. New Delhi: Vallabh Prakashan; 2002. p. 292.


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  • Development and Characterization of Novel Trans Buccoadhesive Bilayer Tablets of Tapentadol Hydrochloride

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Authors

J. Ravi Kumar Reddy
Jawaharlal Nehru Technological University Kakinada, Kakinada, A. P, India
Y. Indira Muzib
Department of Pharmaceutics, Sri Padmavati Mahila Visvavidyalayam, Tirupati, A. P, India
K. P. R. Chowdary
Department of Pharmaceutics, Andhra University, Vishakhapatnam, A. P, India

Abstract


Buccoadhesive bilayer tablets of Tapentadol Hydrochloride were prepared and evaluated in this investigation. Tapentadol is a centrally-acting opioid analgesic, having potency between morphine and tramadol. The direct compression method was used for preparing tablets. The polymers were employed in the formulations are Carbopol 934 P, Eudragit RL 100, sodium alginate, Chitosan, and polyvinylpyrrolidone-K30 (PVP) and ethyl cellulose (EC) as a backing layer. The prepared formulations were evaluated for their physicochemical characteristics, swelling index, surface pH, ex vivo buccoadhesive strength, in vitro, in vivo drug release and ex vivo permeation studies. The significant differences in the results were observed, which dependent on characteristics and composition of bioadhesive materials used. Stability studies were conducted in natural human saliva and accelerated conditions, results reveals no significant change in physical appearance. Drug content, buccoadhesive strength and the P-value shown statistically significant at <0.05. Ex vivo mucous irritation by histological examination reveals, the administration site of buccal tablet over the buccal mucosa did not cause any irritation, ulceration, inflammation and redness, and it resembles to controlled buccal mucosa. Good correlations were observed between in vitro and in vivo drug release, with a correlation coefficient of 0.997. Drug diffusion from buccal tablets showed apparently zero order kinetics and release mechanism was diffusion controlled after considerable swelling.

Keywords


Tapentadol Hydrochloride, Opioid Analgesic, Buccoadhesive, Bilayer Tablets, Zero Order Kinetics.

References