Abstract

“DESIGN AND OPTIMIZATION OF PH-RESPONSIVE PREDNISOLONE DELAYED RELEASE TABLETS FOR COLONIC DRUG DELIVERY”

Ansari Afaque Raza Mehboob* and Waghmode Chetan Satish, Naik Suresh Ramnath

ABSTRACT

Prednisolone (PDS) is a typical glucocorticoid which has been used for the treatment of inflammatory bowel diseases. However, when PDS is orally administered, a large amount of the drug is absorbed from upper gastrointestinal tract which deteriorates its therapeutic efficacy and causes systemic side effects. This pH variation of PDS in different segments of gastrointestinal tract has been exploited for colon specific drug delivery. The present study was aimed to design and optimize pH-responsive delayed release tablets of PDS for colonic drug delivery. A full 32 factorial design was successfully utilized to study and optimize the two independent formulation variables namely; amount of guar gum and pectin to obtain the optimized formulation F9. Optimization of coating was done by using two independent variables; namely ratio of Eudragit L-100: Eudragit S-100 and percent coat weight gain (CWG) and formulation EC8 was found to be the most suitable formulation having minimal drug loss in the upper part of GIT. Enteric coating was performed by two different polymers, Eudragit L-100 and Eudragit S-100 which dissolves at a pH of 6 and more. It was concluded after study that 1:3 ratio of Eudragit L-100: Eudragit S-100 was more effective as enteric coating polymer along with 10% weight gain. As the percent weight gain was increased the percent cumulative drug release (CDR) was decreased. From the study it can be concluded that percent weight gain is inversely proportional to percent CDR. Overall result indicates that batch F9 with guar gum and pectin ratio of 3:2 and coating material with Eudragit L-100: Eudragit S-100 ratio of 1:3 was found to be the optimized formulation of Prednisolone having 10% CWG.

Keywords: Natural polysaccharides, factorial design, inflammatory bowel diseases, colon targeted delivery, pectinase.