KUMARAVELRAJAN RAJAGOPAL, SRİ HARSHA THATAVARTHY, AJAY BABU CHIRUMELLA, SUBA VENKATESAN
Acta Pharmaceutica Sciencia - 2023;61(4):334-354
DOI : 10.23893/1307-2080.APS6122 Montelukast compressed tablets were prepared by dry blending of excipients and direct compression. The inner layer containing 3 mg of Montelukast to provide a burst release at 6.5 h. A sustained-release layer consisting of 7 mg and different proportions of HPMC K4M was used to optimise the formulation. The different drug: layer ratio, from 3:7 to 5:5 used for F1 to F10 batch, but 20 % of HPMC K4M (F5) with the layer ratio of 3:7, gave the desired release profile within 8 h and achieved burst release from the immediate release layer in 6.5 h. The swelling and erosion properties of optimised formulation were investigated at different pH. In vivo pharmacokinetic studies in rabbits confirmed the sustained release with an average T max value at 10 h and C max value of 478.32 ng/mL compared to the conventional tablet, as C max was 490.10 ng/mL attained by 2 h (T max).
