Formulation and Evaluation of Mouth Dissolving Tablets of Metoprolol Tartrate by Sublimation Method

Abstract

Metoprolol tartrate is effective β-blocker which is having antianginal properties and used in the treatment of myocardial infarction. Oral bioavailability of metoprolol tartrate is around 40%. In present work an attempt has been made to prepare fast dissolving tablets of metoprolol tartrate to enhance the dissolution rate. Sublimation method was used to prepare the fast dissolving tablets by using different concentrations of superdisintegrants like indion-414, crospovidone, sodium starch glycolate, croscarmellose sodium. The blend was examined for the pre-compressional parameters and post-compressional parameters. Drug compatibility with excipients was checked by FTIR and DSC studies. The values of pre-compression parameters evaluated were within prescribed limits and indicated good free flowing property. In all the formulations, friability is less than 1%, indicated that tablets had a good mechanical resistance. Drug content was found to be in the range of 99 to 101%, which is within acceptable limits. Hardness of the tablets was found to be in the range of 2.00-2.90 kg/cm². The formulations F1, F8, F9 shows less in vitro dispersion time 18, 25, 19 sec respectively with rapid in vitro dissolution within 5 min. In vitro dispersion time decreases with increase in concentration of indion 414 upto 3% then dispersion time increases. Where as in vitro dispersion time decreases with increase in the concentration of croscarmellose sodium. No chemical interaction between drug and excipients was confirmed by DSC and FTIR studies. The stability study conducted as per the ICH guidelines and the formulations were found to be stable. 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.