SELECTION AND OPTIMIZATION OF MOST EFFICIENT SUPERDISINTEGRANT FOR THE FORMULATION OF DISPERSIBLE TABLETS OF TRAMADOL HYDROCHLORIDE
Keywords:Tramadol Hydrochloride, Superdisintegrants, Dispersible tablets, disintegration time, Dissolution Profile, Patient compliance
Objective: The intent and objective of this research work were to find out the most effective superdisintegrants on the basis of disintegration time dissolution rate and other secondary tablet properties among the three mostly used superdisintegrants (Crospovidone, sodium starch glycolate and croscarmellose). This endeavour was initiated to mitigate dysphagia and for better bioavailability of drugs.
Methods: Nine formulations of Tramadol HCl (50 mg) dispersible tablets were fabricated by direct compression process using different concentrations (3%, 5% and 8%) of mentioned superdisintegrants. Dispersible tablets were formulated and evaluated for various parameters such as thickness, hardness, friability, weight variation, disintegration time, drug content and dissolution rate. Then the stability study was carried out on the selected formulation batch to get a conclusion.
Results: Results were interpreted in mean±SD where the value of n is equal to 3. The formulated dispersible tablets were evaluated for their post-compression parameters after achieving the desired pre-compression attributes. In pre-compression evaluation, the flow property and compressibility of powder were checked and the results found to be acceptable of all the nine formulations having an angle of repose less than 19 °, compressibility index in the range of 14.45 to 15.27 and Hausner’s ratio (≤ 1.29). The thickness of the tablets was found to be 4.19 to 4.28 mm. The tablets have optimum hardness just above 4 kg/sq. cm for better sustainability against mechanical stress and the percentage loss on friability found to be less than 1%. The drug content in the tablets of all nine formulations was found to be in the range of 97.48±0.9% to 99.46±0.4%. The wetting time and disintegration time were found to be within 20 sec and 40 sec, respectively, for all nine batches. The dissolution profile showed that more than 97% of the drug were released within 14 min, which is a great achievement in comparison to marketed dispersible tablets. The formulation batch (B2) with crospovidone as superdisintegrant has shown supremacy in tableting properties with better disintegration and dissolution profile. The bioavailability of the drug would be enhanced due to the increment in these parameters. The results of the stability studies of formulation batch (B2) were satisfactory. This batch with crospovidone as a super disintegrant was selected as the best formulation and recommended for scale-up.
Conclusion: The outcome of the research work suggests that the disintegration efficiency of crospovidone is the most among the three super disintegrants and is recommended for the formulation of most effective dispersible tablets of Tramadol Hydrochloride.
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