Enhanced oral delivery of artemether: An application of Prosochit®

Abstract

This study was aimed at assessing the suitability of the three grades of Prosochit ® for enhanced oral delivery of artemether. The three grades of this novel excipient (PC201, PC101, and PC102) were used as binders (wet granulation) at concentrations equivalent to 2% w/w prosopis gum (PRG) for the formulation of artemether granules, and the flow properties of the granules were determined. The granules were, thereafter, tableted at compaction pressure of 30 KN, and the tablets evaluated for mechanical strength, disintegration and dissolution. The granules had fair-to-good flow before the addition of flow activators. Four tablet formulations were prepared. Tablet crushing strength (CS) was not significantly different, but the friability (FR) of tablet containing PRG was significantly higher than those containing Prosochit ® . Disintegration times (DTs) were 67.44, 62.99, 52.16, and 37.89 minutes for tablets containing PRG, PC201, PC101, and PC102, respectively, and the percent drug release at 1 hour was in the inverse order PRG < PC201 < PC101 < PC102. Prosochit ® is comparable to PRG in terms of the flowability properties of artemether granules and the tablet strength. It is a better agent compared to PRG for delivering artemether, and the grade PC102 offers the best delivery of the drug evidencing that the enhancement of dissolution rate depends on the proportion of chitosan in the new excipient.