ABSTRACT:
The purpose of the present investigation is to develop a new simple method to target a colon specific site, methylprednisolone type low dose drugs can be protect from it disintegration and drug release than reached the colon site by using matrix enteric coated technique, microsomal degradation pectin, and pH sensitive Eudragit S100 polymers have capability to retard the drug release and show sustain release in the upper gastro intestinal system than progressively fast release in the colon. The prepared matrix enteric coated methylprednisolone tablets were optimized using invitro studies, and evaluated for colonic delivery by in vivo x-ray imaging study in human volunteers showed that the tablets reached the colon without disintegrating in the upper GI system and pharmacokinetic studies in healthy humans. The optimized formulation methylprednisolone showed 6.1±0.2 (negligible release) in the initial lag period of 5 h followed by progressive release up to 99.1±0.4 % for 24 h respectively. The Cmax of colon targeted matrix enteric coated tablets was 9871.42 ng/ml at Tmax10hr for metylprednisolone, Differential scanning calorimetry and Fourier Transform Infrared Spectroscopy studies revealed that there was no interaction between drug and polymer and the accelerated stability studies showed the stability of formulation, Thus development of matrix enteric coated tablets was suitable to target the methylprednisolone to colon and treat ulcerative colitis with the conformation of phase 1 trials.