Formulation and evaluation of colon targeted drug delivery system of levetiracetam using pectin as polymeric carrier.

ABSTRACT

The aim of the present work was to develop and evaluate colon specific sustained release tablet using levetiracetam (LEV), microbially degradable polymeric carrier (pectin), coating material and matrix forming polymers. The colon targeted tablet was prepared by wet granulation technique using different percentage of pectin as matrix carrier, starch mucilage as a binding agent, HPMC K-100 as swellable polymer and coated with Eudragit polymers. Pectin, drug and physical mixture were evaluated for incompatibility study by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). All the batches of matrix tablet (F1-F4) were subjected for in-vitro dissolution in various simulated gastric fluids for suitability for colon specific drug delivery system. Tablets were evaluated for micromeritic properties of granules, physical properties, drug content, water uptake and erosion characteristics. F2 was optimized and subjected to coating based on evaluation results. The dissolution study of F2 revealed, in simulated intestinal fluid (SIF) release was 40.48% at the end of 6h and in simulated colonic fluids (rat caecal content) was 102.88% after degradation at the end of 8h. The colon targeted matrix tablet of LEV showed no change either in physical appearance, drug content or dissolution pattern after performing stability study for 3 months. The studies confirmed that, the designed formulation could be used potentially for colon delivery by controlling drug release in stomach and the small intestine.