Development and in vitro Evaluation of Enteric Coated Multiparticulate System for Resistant Tuberculosis

Abstract

The multiparticulate formulation of sodium para aminosalicylate for oral administration was developed by extrusion spheronization technique. Microcrystalline cellulose was used as filler in concentration of 14.4% w/w. Pellets were coated with Eudragit L 30 D-55 using fluidized bed processor. Different weight gains of acrylic polymer were applied onto the pellets and evaluated for in vitro dissolution behavior in 0.1 N HCl for two hours and then media was changed to phosphate buffer pH 6.8. A 60% w/w coating level of Eudragit L30 D 55 has produced the most acceptable results against the gastric attack. 3% Seal coat of HPMC E5 was also applied in order to protect the drug from migration into the Eudragit coat and film coat was applied in order to prevent aggregation of pellets in the dissolution media. Morphological characteristics of developed pellets were also investigated by scanning electron microscopy and found to be smooth and spherical. Developed system was found to be suitable for the delivery of Sod PAS in to intestinal region.

Keywords: Eudragit L 30 D55; Pellets; enteric-coated; extrusion/spheronization; fluidized bed coater.

Fig. 1

Size distribution of coated pellets Size distribution of coated pellets with 40% (), 50% () and 60% () coating

Fig. 2

In vitro release of sod PAS from coated pellets with different weight gain. Release of sodium para aminosalicylate (sod PAS) in vitro in simulated gastric (SGF) and intestinal fluids (SIF) from coated pellets containing 40% (–♦–), 50% (–■–) and 60% (–▲–) coats

Fig. 3

Scanning electron micrograph of developed pellets