Formulation and In vitro/In vivo evaluation of controlled release Entacapone trilayer matrix tablets by geomatrix

Pavan Kumar Potturi, Y. Sudhakar


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 (1.00±0.01h) indicates rapid absorption while the higher Tmax of the optimized (4.01±0.04h) 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.


Entacapone, Trilayer matrix tablet, HPMC, Xanthan gum, Geomatrix, In-vivo bioavailability studies

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