simple and rapid approach to evaluate the in vitro in vivo role of release controlling agent ethyl cellulose ether derivative polymer

ABSTRACT

Diclofenac sodium [DCL-Na] conventional oral tablets exhibit serious side effects when given for a longer period leading to noncompliance. Controlled release matrix tablets of diclofenac sodium were formulated using simple blending [F-1], solvent evaporation [F-2] and co-precipitation techniques [F-3]. Ethocel[R] Standard 7 FP Premium Polymer [15%] was used as a release controlling agent. Drug release study was conducted in 7.4 pH phosphate buffer solutions as dissolution medium in vitro. Pharmacokinetic parameters were evaluated using albino rabbits. Solvent evaporation technique was found to be the best release controlling technique thereby prolonging the release rate up to 24 hours. Accelerated stability studies of the optimized test formulation [F-2] did not show any significant change [p<0.05] in the physicochemical characteristics and release rate when stored for six months. A simple and rapid method was developed for DCL-Na active moiety using HPLC-UV at 276nm. The optimized test tablets [F-2] significantly [p<0.05] exhibited peaks plasma concentration [C[max]=237.66 +/- 1.98] and extended the peak time [t[max]=4.63 +/- 0.24]. Good in-vitro in vivo correlation was found [R[2] =0.9883] against drug absorption and drug release. The study showed that once-daily controlled release matrix tablets of DCL-Na were successfully developed using Ethocel[R] Standard 7 FP Premium