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Development and Human in vivo Evaluation of a Colonic Drug Delivery System

Walid A. Habib a and Adel Sakr b CIMA Labs.a , Brooklyn Park, Minnesota (USA), and Industrial Pharmacy Graduate Program, College of Pharmacy, University of Cincinnati Medical Center b , Cincinnati, Ohio (USA)

The objective of this study was to develop and evaluate a colonic drug delivery system for the polypeptide antimicrobial agent nisin (CAS 1414-45-5). Being a polypeptide, nisin is susceptible to degradation in the small intestine. Nisin was formulated into 100 mg tablets which were coated in the Wurster Fluid Bed Apparatus using methacrylic acid copolymer USP/NF type C, commercially known as Eudragitâ L30D-55, at various coating thicknesses. The effects of Eudragit on the in vitro and in vivo release of nisin were studied. It was found that the coated tablets resisted disintegration in 0.1 N HCl for 2 h and a linear relationship was established between coating thickness and/or percent weight gain, and the time to beginning of disintegration. Tablets containing samarium oxide ( ¹⁵²Sm) were neutron activated ( ¹⁵³Sm) and their disintegration was tested in human volunteers using gamma scintigraphy. An in vivo/in vitro correlation between coating thickness/weight and the disintegration of the coating in humans was found. A coating thickness of 0.381 mm was found to be optimal for targeting nisin to the colon.

Key words Drug targeting · Enteric coating · Methacrylic acid copolymer · Nisin · Polypeptides