Abstract
Objective: In the present work, the main objective was to develop bilayer extended release matrix tablets of etoricoxib by providing a loading dose followed by maintenance dose that expected to improve the therapeutic efficacy of the medication with less toxic effect.
 Methods: Bilayer tablets of etoricoxib was developed successfully with the meticulous proportion of release controlling Hydroxy propyl methyl cellulose K100 (HPMC K100) and lactose. The tablets were prepared by wet granulation technique. Granules for immediate layer and extended layer for different formulations were prepared separately. The formulations were developed and evaluations were performed to examine the parameters that affect the in vitro performance of the tablets. The drug-excipient compatibility was ensured by Fourier transform infrared spectroscopy (FTIR) study.
 Results: The values of physical parameters of all formulations were found within appreciable limit. Formulation containing HPMC K 100 and lactose in the proportion of 2:1 in the extended release layer was able to release 26.22% of drug in 15 min and shown a steady release of drug for an extended period of 12 h. The dissolution data was put in Korsemeyer–Peppas model in order to find out n value, which describes the drug release mechanism. The n-value of different formulations were found to be variable. The Fourier transform infrared spectroscopy (FTIR) study revealed absence of any other new peaks and also no differences in the positions of the absorption bands in the bilayer tablet F8 that indicate the lack of significant interactions between etoricoxib and other excipients.
 Conclusion: It had been concluded that once daily immediate-and extended release bilayer tablet of etoricoxib can be formulated with profound physical characteristics and dissolution properties. This resulted in reducing the daily dose and thus minimise the cardiovascular toxicity of etoricoxib.
Highlights
Etoricoxib; (5-chloro-2-[6-methyl pyridin-3-yl]-3-[4-methyl sulfonyl phenyl] pyridine) is a selective second generation cyclooxygenase-2 inhibitor administered orally as an analgesic and anti-inflammatory drug [1, 2]
The fast release of drug from the immediate release layer achieve the quick onset and the extended release of drug capable of maintaining the therapeutic level. This resulted in reducing the daily dose and minimise the cardiovascular toxicity of etoricoxib
From the dissolution profile of all formulation it had been observed that F7 and F8 are suitable for once daily immediate-and extended release bilayer tablet of etoricoxib
Summary
Etoricoxib; (5-chloro-2-[6-methyl pyridin-3-yl]-3-[4-methyl sulfonyl phenyl] pyridine) is a selective second generation cyclooxygenase-2 inhibitor administered orally as an analgesic and anti-inflammatory drug [1, 2]. The drug possesses a saturation solubility of 78.48±1.47 μg/ml. This leads to formulation problems and limit its therapeutic efficacy by delaying the rate of absorption and the onset of action [3]. The recommended dose for etoricoxib is between 60 and 120 mg/day. It has an estimated logP of 3.14 and pKa of 4.6. Pharmacokinetic studies reveal that despite of a potent drug for osteoarthritis, it suffers from severe cardiovascular toxicity issues. The cardiovascular risks of etoricoxib may increase with dose and duration of exposure. The possible lowest effective daily dose should be developed to combat this problem [4]
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