Formulation and development of extended release dosage form for BCS class IV drug

Abstract

quotBCS class IV drugs need a tailor made drug delivery system in order to overcome poor solubility and permeability issues. Moreover, molecular like furosemide with pH dependent solubility create additional challenge for formulation development as it further restricts absorption window. Current study is aimed at formulating a modified release drug delivery platform of model drug furo to overcome these challenges. In order to overcome solubility problem of durg,solid dispersion technique was utilised. While pH dependent solubility was addressed by adding a pH modulator forming a third generation solid dispersion. Composition of solid dispersion with highest solubility was further development as a plain mucoahesive tablets to improve contact area , keep tablet surface in close proximity of GI track surface for maximize absorption probability and to keep it retained into stomach which is the major absorption site. Drug release from this site specific modified release system was further optimised by applying central composite design.solubility studies of prepared by drug :PvP k -30 ratio of 1:0.5 increased furo solubility in 0.1 N HCl up to 0.3 mg/ml . While in presence of basic pH modulator above solid dispersion showed further 10 times increase in solubility. Optimised formulation derived from the design of experiments showed extended drug release up to 24 hrs. It was having sufficient mucoahesive strength and agreeable in vitro characteristics . In vivo pharmacokinetics data revealed upto 55%increase in bioavailability as compared to plain mucoahesive formulation without solid dispersion and permeation enhancers. These promising results maybe further explored through clinical studies to check the applicability of such strategies in human subjects. newline newlinequot newline