Design and characterization of mouth dissolving tablets of Metoprolol Tartrate

Abstract

The demand for mouth dissolving tablet (MDT) has been growing during the last decade especially for elderly and children who have swallowing difficulties. Metoprolol tartrate is a selective beta1-­‐adrenoreceptor blocking agent used in Essential hypertension, prevention after a myocardial infarction, tachycardia, coronary heart disease, treatment of heart failure. Oral bioavailability of metoprolol tartrate is around 40% and having half life 3 to 5 hrs. In present work an attempt has been made to prepare mouth dissolving tablets of metoprolol tartrate with increased rate of dissolution may leads to increase bioavailability. Mouth dissolving tablet of metoprolol tartrate prepared using Indion 414, croscarmellose sodium and crospovidone as superdisintegrants by direct compression and sublimation methods. The tablets prepared were evaluated for various parameters like weight variation, hardness, friability, in vitro dispersion time, drug-­polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies and short term stability studies. The tablets prepared by direct compression method possess a weight variation in the range 196 to 205 mg which is below ± 7.5%, hardness of 2.0 to 3.0Kg/cm², percentage friability of 0.54 to 0.81 %, in vitro dispersion time of 21 to 59 sec, drug content uniformity was in between 99.08 to 100.76%, water absorption ratio of 46.77 to 85.64%, wetting time of 37 to 50 sec, and in vitro drug release showed 69.12% - 99.83% within 9 min. IR spectral analysis and DSC study showed that there was no drug interaction with formulation additives of the tablet, short term stability studies on the formulations indicated that there are no significant change in hardness, friability, drug content and in vitro drug release. (p<0.05). Similarly the tablets prepared by sublimation method possess a weight variation in the range 197 to 204 mg which is below ± 7.5%, hardness of 2.1 to 2.9 kg/cm², in vitro dispersion time of 18 to 48 sec. IR spectral analysis the pure drug characteristic absorption bands and formulations absorption bands have shown all most same range. As there is no variation and shift in the position of characteristic absorption bands it can be justified there is no interaction between drug and polymer. The DSC study during the formulation chemical reaction has not taken place to result into a single product. The DSC results shows that there was no drug interaction with the formulation additives of the tablet, drug content uniformity was in between 98.56 to 100.65%, water absorption ratio showed 51.15 to 85.15%, wetting time between 37 to 50 sec and in vitro drug release of 72.88 to 99.75% within 9 min respectively. Short term stability studies on the formulations indicated that there are no significant changes in drug content and in in vitro drug release (p<0.05). The results concluded that fast dissolving tablets of metoprolol tartrate showing enhanced dissolution will lead to improved bioavailability and effective therapy by using sublimation method.