Design and evaluation of matrices of Eudragit with polycarbophil and carbopol for colon-specific delivery

作者：Asghar Laila Fatima Ali; Chandran Sajeev^*

来源：Journal of Drug Targeting, 2008, 16(10): 741-757.

DOI：10.1080/10611860802473345

• Colon-specific delivery
• controlled release
• matrix embedding
• Eudragit
• polycarbophil
• carbopol

The purpose of the present study was to investigate the effect of incorporating pH-responsive polymers Eudragit (L100 or S100) in matrix bases composed of hydrophilic polymers polycarbophil and carbopol to design oral controlled release formulations with sigmoidal release profile for colon-specific delivery. Matrix tablets were prepared by wet granulation technique using indomethacin as model drug and were characterized for physical parameters, in vitro drug release, release kinetics, and stability on storage. The gastrointestinal (GI) transit of selected formulations was also investigated in human subjects using gamma scintigraphy. In vitro release studies indicated that the presence of pH-sensitive polymers in hydrophilic polymer base retarded the initial release significantly (10-15% release in 6h) followed with controlled release for the next 8-10h in simulated GI fluid pH (without enzymes). The presence of Eudragit in hydrophilic matrix base retarded the swelling of the matrix base in acidic to weakly acidic pH, but in alkaline pH, enhancement in drug release rate was observed due to the dissolution of Eudragit from the base resulting in a porous matrix structure, resulting in around 80-90% release in 14h of study. In vivo gamma scintigraphy studies in healthy human subjects proved that the formulations had acceptable matrix strength to withstand gastric and colonic transit. The mean colonic residence time of selected designed formulations varied between 15 and 19h. Such a matrix design could have potential application as colon-specific drug delivery systems with pH- and time-dependent drug release profile.

• 出版日期2008