Abstract

COLON TARGETING OF BUDESONIDE USING PULSIN CAP TECHNIQUE FOR CROHN’S DISEASE

Ayesha Kubbra*, Abdul Waris Khan and Manjunath K.

ABSTRACT

Objectives: The main aim of the present work is to formulate the pulsin cap targeting to colon containing the budesonide drug which is used in the treatment of crohn‟s disease. Method: Pulsin cap technique, The physicochemical characteristics of Budesonide granules was determined by techniques such as FTIR, in vitro release and Release kinetics were evaluated. From the obtained results the better formulation was selected for further fabrication of pulsatile capsule. The pulsin cap was evaluated for in vitro dissolution studies and release kinetics study. Results: The FTIR Spectra reveled that there was no interaction between polymer and drug. Preformulation study was performed in which granules has shown a good flow property. The in vitro performance of Budesonide(BUD) granules showed faster drug release depends upon the concentration of superdisintegrants used, in which best was F2 formulation with 20% of Cross caramellose sodium where 99.14% of drug release is within 15mins. In the later part granules were filled into cross linked gelatin capsule which is fitted with a hydrogel plug, cap and body were sealed with 5% ethanolic ethyl cellulose to create a pulsin cap. The in vitro dissolution profile of budesonide from pulsin cap has shown increased lag time with increase in the concentration of hydrogel plug. In which F2-P5 used in combination of 50mg of both ethyl cellulose and HPMC E15 has shown 5hrs of desired lag time. Drug release data obtained were fitted to zero order, first order, Higuchi‟s square root of time and Korsemeyer-Peppas equations to understand the mechanism of drug release from the budesonide Pulsin cap (fig.14 to 17). The slopes and the regression co-efficient of determinations (r2) were listed. The co-efficient of determination indicated that the release data of F2-P4, F2-P5 was best fitted with zero order kinetics and F2-P1, F2-P2, F2-P3 were best fitted with first order kinetics. The n value obtained from krosmeyer peppas plot ranges from (0.733 to 3.66) Indicated that mechanism of release of formulation F2-P2 to F2-P5 is Non Fickian super case II. Conclusion: The study demonstrates that budesonide granules could be successfully targeted to colon. In conclusion, 99.60±0.2% of drug release at 9th hour and drug began to release after 5hrs of lag time while being in the colon, can be achieved from cross linked gelatin capsule, in which granules were sealed by means of a hydrogel plug.

Keywords: Budesonide, Pulsin cap, Lag time, Colon targeting, Crohn?s disease.