In vitro evaluation of dissolution behavior for a colon-specific drug delivery system (CODES) in multi-pH media using United States Pharmacopeia apparatus II and III |
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Authors: | Li Jinhe Yang Libo Ferguson Sheila M Hudson Tom J Watanabe Shunsuke Katsuma Masataka Fix Joseph A |
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Institution: | (1) Yamanouchi Pharma Technologies, Inc, 1050 Arastradero Road, 94304 Palo Alto, CA;(2) Novel Pharma Laboratory, Yamanouchi Pharmaceutical Co. Ltd, Yaizu, 425-0072 Shizuokaken, Japan |
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Abstract: | United States Pharmacopeia dissolution apparatus II (paddle) and III (reciprocating cylinder) coupled with automatic sampling
devices and software were used to develop a testing procedure for acquiring release profiles of colon-specific drug delivery
system (CODES™) drug formulations in multi-pH media using acetaminophen (APAP) as a model drug. System suitability was examined. Several
important instrument parameters and formulation variables were evaluated. Release profiles in artificial gastric fluid (pH
1.2), intestinal fluid (pH 6.8), and pH 5.0 buffer were determined. As expected, the percent release of APAP from coated core
tablets was highly pH dependent. A release profile exhibiting a negligible release in pH 1.2 and 6.8 buffers followed by a
rapid release in pH 5.0 buffer was established. The drug release in pH 5.0 buffer increased significantly with the increase
in the dip or paddle speed but was inversely related to the screen mesh observed at lower dip speeds. It was interesting to
note that there was a close similarity (f
2=80.6) between the release profiles at dip speed 5 dpm and paddle speed 100 rpm. In addition, the release rate was reduced
significantly with the increase in acid-soluble Eudragit E coating levels, but lactulose loading showed only a negligible
effect. In conclusion, the established reciprocating cylinder method at lower agitation rates can give release profiles equivalent
to those for the paddle procedure for CODES™ drug pH-gradient release testing. Apparatus III was demonstrated to be more convenient and efficient than apparatus II by
providing various programmable options in sampling times, agitation rates, and medium changes, which suggested that the apparatus
II approach has better potential for in vitro evaluation of colon-specific drug delivery systems. |
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Keywords: | colon-specific drug delivery acetaminophen (APAP) USP apparatus II (paddle) USP apparatus III (reciprocating cylinder) dissolution automation |
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