Formulation and in vitro evaluation of sustained release matrix tablets of Rimopride Citrate Dihydrate

Abstract

Drugs are most frequently administered by oral route. Although a few drugs taken orally are intended to be dissolved in the mouth, nearly all drugs taken orally are swallowed. A few drugs such as antacids are swallowed for their local action in the gastrointestinal tracts. Hence the above study demonstrated that combination of HPMC K4M and HPMC K15M can be used to formulate sustained release matrix tablets of Rimopride Citrate Dihydrate. This can sustain the drug release up to 24 hours as per standard dissolution profile. This can be expected to reduce the frequency of administration and decrease the dose – dependent side effects associated with repeated administration of conventional Rimopride Citrate Dihydrate dihydrate tablets.

The cumulative drug release of innovators brand (MOZA SR, Intas Pharmaceuticals) of sustained release tablet of Rimopride Citrate Dihydrate were compared for in vitro dissolution study. The formulation F9 matrix tablet releases the drug appropriately in comparison of innovators brand. The cumulative drug release at the end of 24th hour from formulation F9 (98.01%) and the cumulative drug release at the end of 24th hour from innovators brand was (97.30%).

The in vitro drug release result indicates that formulation F9 released more drug than innovators brand and hence more drug is available at the absorption site from formulation F9 as compared to innovators brand, hence the formulation F9 has better bioavailability than innovators brand of Rimopride Citrate Dihydrate sustained release matrix tablet and also the sustained release matrix tablet was found to be beneficial in terms of reduction in frequency of administration. The formulation F9 best suited with zero order release kinetics (corr.coefficient =0.943) than the first order release kinetics (corr. Coefficient = 0.910). The formulation F9 follows Higuchi model of drug release kinetics (corr. coefficient=0.41).

The Koresmyer peppas drug release kinetics showed correlation coefficient (0.926) and release exponent (n) 0.724 which indicates that the drug release mechanism is non-fickanian diffusion. Hence it can be concluded that once daily sustain release matrix tablet of Rimopride Citrate Dihydrate having short half life, was found to exert a satisfactory sustained release profile which may provide an improved bioavailability, increased therapeutic efficacy and patient compliance.