Colon specific delivery of indomethacin: effect of incorporating pH sensitive polymers in xanthan gum matrix bases.
In the present study, an attempt has been made to design controlled release colon-specific formulations of indomethacin by employing pH responsive polymers Eudragit (L100 or S100) in matrix bases comprised of xanthan gum. The prepared tablets were found to be of acceptable quality with low-weight variation and uniform drug content. In vitro release studies indicated rapid swelling and release of significant percentage of drug in the initial period from matrix tablets composed of xanthan gum alone. Addition of pH responsive polymers Eudragit (L100 or S100) to xanthan gum matrix resulted in negligible to very low drug release in the initial period in acidic to weakly acidic medium. Furthermore, with increase in pH of the dissolution medium due to dissolution of Eudragit L100/Eudragit S100 that resulted in the formation of a porous matrix, faster but controlled drug release pattern was observed. Thus, a sigmoidal release pattern was observed from the designed formulations suitable for colonic delivery. Drug release mechanism in all cases was found to be of super case II type, indicating erosion to be the primary cause of drug release. Since the drug release from almost all the matrix bases in the initial phase was negligibly low and followed with controlled release for about 14-16 h, it was concluded that a matrix design of this composition could have potential applications as a colon-specific drug delivery device with additional advantage of easy scale-up and avoidance of all-or-none phenomenon associated with coated colon-specific systems.
Asghar
Laila F A
LF
Formulation Development & Pharmacokinetics Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani, 333 031, Rajasthan, India.
Chure
Chetan B
CB
Chandran
Sajeev
S
D000818:Animals; D002626:Chemistry, Pharmaceutical; D003106:Colon / Q000378:metabolism*; D003692:Delayed-Action Preparations; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D007213:Indomethacin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D011109:Polymethacrylic Acids / Q000008:administration & dosage*; D011135:Polysaccharides, Bacterial / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D015203:Reproducibility of Results; D012995:Solubility; D013607:Tablets
D003692:Delayed-Action Preparations; D011109:Polymethacrylic Acids; D011135:Polysaccharides, Bacterial; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; C002563:xanthan gum; D007213:Indomethacin