Vijaya College of Pharmacy, Hayath Nagar, Hyderabad-501511, Telangana, India.
Keywords:
Entacapone, Trilayer matrix tablet, HPMC, Xanthan gum, Geomatrix, In-vivo bioavailability studiesAbstract
The purpose of the present study was to develop and optimize controlled release (CR) matrix tablets of Entacapone trilayer tablets to achieve zero-order drug release for sustained plasma concentration. Entacapone tablets were prepared by direct compression and consist of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), xanthan gum, ethyl cellulose; upper and lower layers were prepared with Carnauba wax, xanthan gum, sodium CMC and DCP. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo (Rabbit) bioavailability studies were carried out on the optimized formulation (HF14) as marketed conventional release product as a reference standard. Entacapone was available in plasma within an hour after oral administration of reference product. The Tmax of the optimized formulation was significantly different (p < 0.05) from that of the marketed product. Low Tmax value for the reference product (1.00μ0.01h) indicates rapid absorption while the higher Tmax of the optimized (4.01μ0.04h) suggests slower absorption. This delayed absorption of test preparation is most likely due to the sustained release of the drug. A fair correlation between the in vitro dissolution profile and in vivo pharmacokinetic profile of the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a controlled release formulation of the drug. These results also demonstrated the suitability of three-layered tablet formulation of Entacapone to provide controlled release for prolonged period of time and improved linearity for Entacapone in comparison to marketed product with conventional drug release profile.
References
Ho-Wah H, Robinson J, Lee V. Design and fabrication of oral controlled release drug delivery systems. In: Controlled Drug Delivery. New York: Marcell Dekker Inc; 1987. 373.
Conte U, Maggi L. Multi-layer tablets as drug delivery devices. Pharm Techn. 1998; 2: 18–25;
Chidambram N, Porter W, Flood K, Qiu Y. Formulation and characterization of new layered diffusional matrices for zero-order sustained release. J. Control. Release. 1998; 52: 149–158;
Efentakis M, Politis S. Comparative evaluation of various structures in polymer controlled drug delivery systems and the effect of their morphology and characteristics on drug release. Eur. Polym. J. 2006; 42:1183–1195.
Conte U, Maggi L, Colombo P, La Manna A. Multi-layered hydrophilic matrices as constant release devices. J Control Rel. 1993; 26: 39-47.
Yihong Qui, Chidambaram N, Kolette F. Design and evaluation of layered diffusional matrices for zero order sustained-release tablets. J Control Rel. 1998; 51: 123-130.
Conte U, Maggi L. Modulation from Geomatrix multi-layer matrix tablets containing drugs of different solubility. Biomaterials.1996; 17 (9): 889-896.
Yihong Q, Kolette F. Design of sustained release matrix system for a highly water soluble compound ABT-089. Int J Pharm. 1997; 157: 46-52.
Tobyn MJ, Stani forth JN, Baichwal AR, Mc Call TW. Prediction of physical properties of a novel polysaccharide controlled release system. Int J Pharm. 1996; 128: 113-22.
Talukdar MM, Mooter VD, Augustijns P, Maga TT, Verbeke N, Kinget R. In vitro evaluation of xanthan gum as potential excipients for oral controlled release matrix tablet formulation. Int J Pharm. 1998; 169: 105-13.
Talukdar MM, Vercammen JP. Evaluation of xanthan gum as a hydrophillic matrix for controlled release dosage forms. Drug Dev Ind Pharm. 1993; 19:1037-46.
Hong Wen, Kinam Park. Oral controlled release formulation design and drug delivery. Theory to practice, Wiley publication, New Jercy, 2010, 94-95.
Praveen Kumar T, Pallavi Y, Deepthi K, Narayana Raju P. Formulation and evaluation of Entacapone sustained release matrix tablets. The Pharma Innovation. 2014; 3(8): 80-88.
C.V.S Subrahmanyam. Textbook of Physical Pharmaceutics. N.K. Jain Publisher for Vallabh Prakashan, 11th edition, 215-224.
Sinko P.J, Martin’s Physical Pharmacy and Parmaceutical Sciences. Published by Wolters Klwner Health Pvt. Ltd, New Delhi. 2007, 5, 553-559.
Yeole PG, Galgatte UC, Babla IB, Nakhat PD. Design and evaluation of Xanthan gum-based sustained release Matrix tablets of Diclofenac sodium. IJPS. 2006; 68:185-189.
