FORMULATION AND IN VITRO/ INVIVO EVALUATION OF CHRONOMODULATED DRUG DELIVERY OF BARICITINIB

Rheumatoid arthritis (RA) is a systemic autoimmune disease characterized by chronic joint inflammation which ultimately leads to severe disability and premature mortality. It has a global prevalence of around 1% with the incidence among women being 2–3 times more than in men. The pathogenesis of the disease involves preclinical RA, genetic factors, and environmental factors. The RA has no known cure and the primary aim of treatment remains to attain lowest possible disease activity and recovery if possible. The aim of the present investigation was to formulate and evaluate chronomodulated drug delivery system of Baricitinib such that it releases the drug early in the morning, during which the symptoms of rheumatoid arthritis worsen. To develop chronomodulated drug delivery system of Baricitinib, initially core tablets of Baricitinib were prepared using three different supradisintegrants followed by coating with pH dependent polymer of Eudragit S100. The prepared core tablets are evaluated for physical parameters and an optimal system was identified. Further, coating composition of Eudragit L-100 was optimized and coating tablets of Baricitinib was prepared. The prepared coated tablets were evaluated for the in vitro release studies in 0.1N HCl, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer. Formulation with 12.5% of coating solution had shown a significant drug release after a lag time of 3 h (in pH 6.8 medium), 6 h (in pH 6.8 medium) and 8 h (in pH 7.4 medium), respectively. Thus, chronomodulated drug delivery system of Baricitinib was formulated and that if a tablet is administered around 9 pm to 10 pm, the drug release starts after a lag time of 6 h i. e., around 3am to 4 am.

Keywords: Baricitinib, chronomodulated, supradisintegrants