Abstract

FORMULATION AND EVALUATION OF FELODIPINE SUBLINGUAL TABLET

Rohit J. Patel, Bhavik N. Patel*, Dasharath M. Patel and Chhagan N. Patel

ABSTRACT

Objective: Felodipine is the drug of choice in hypertension and congestive heart failure.Its bioavailability is very low about 15%. Present investigation was undertaken to formulate sublingual tablet of Felodipine to overcome the first pass metabolism and provide fast onset of action. Experimental Work: The solid dispersion of Felodipine were prepared with β-cyclodextrin, poloxamer 407, PEG 6000 and PVP K-30 in various ratios (1:2, 1:4, 1:6 1:8) and phase solubility study was performed to select the carrier. The selected solid dispersion was then utilized for the preparation of sublingual tablet by direct compression utilizing different superdisintegrant like Cross carmelose sodium, Crosspovidone, Kyron T-314 and Sodium starch glycolate. Prepared tablets were evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time and in-vitro drug release. Stability study of optimized formulation was performed as per ICH guideline. Result: The optimized formulation (batch F3) containing Drug-Poloxamer-407 (1:6) complex and Kyron-T314(5%) showed greater drug dissolution (87% in 15 min) and satisfactory in vitro disintegration time (22 sec). Stability study of optimized formulation showed that optimized formulation was stable at accelerated environment condition. Conclusion: Felodipine sublingual tablet were prepared successfully by the use of solid dispersion of Felodipine-poloxamer 407 (1:6) complex using Kyron-T314 as a superdisintegrant.Thus, sublingual tablet of Felodipine could be an alternative route to avoid gastrointestinal side effect as well as bypass hepatic first pass metabolism. The formulated sublingual tablets may act as a potential alternate for the Felodipine oral tablet.

Keywords: Felodipine, Solid Dispersion, Poloxamer-407, Sublingual Tablet, Hypertension