Use of the BioDis to generate a physiologically relevant IVIVC

In the last decades there has been continual interest in site-specific delivery to the colon. Recently, new types of site-specific delivery formulations have been developed for the treatment of ulcerative colitis and other colon related diseases. The aim of the present study was to establish a physi...

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Bibliographic Details
Published in:Journal of controlled release 2008-09, Vol.130 (3), p.216-219
Main Authors: Klein, Sandra, Rudolph, Markus W., Skalsky, Brigitte, Petereit, Hans-Ulrich, Dressman, Jennifer B.
Format: Article
Language:English
Subjects:
Adjuvants, Pharmaceutic - chemistry
BioDis
Biological and medical sciences
Biological Availability
Caffeine - administration & dosage
Caffeine - blood
Caffeine - pharmacokinetics
Central Nervous System Stimulants - administration & dosage
Central Nervous System Stimulants - blood
Central Nervous System Stimulants - pharmacokinetics
Colon - metabolism
Colon targeting
Drug Delivery Systems - methods
EUDRACOL™ IVIVC
Fasting - metabolism
General pharmacology
Humans
Hydrogen-Ion Concentration
Intestinal Absorption
Male
Medical sciences
pH-gradient
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polymethacrylic Acids - chemistry
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Summary:In the last decades there has been continual interest in site-specific delivery to the colon. Recently, new types of site-specific delivery formulations have been developed for the treatment of ulcerative colitis and other colon related diseases. The aim of the present study was to establish a physiologically relevant IVIVC for two prototypes using a prospective in vitro study. Caffeine, a drug being absorbed along the entire gastrointestinal tract, was selected as a model drug. USP apparatus 3, the BioDis, was used for all experiments and the passage through the gastrointestinal tract was simulated with a physiologically based pH-gradient. Subsequently, the fraction of drug released in vitro was compared with the fraction of drug released in vivo, which was determined in humans in a separate study. Results indicated that the BioDis method is very useful in terms of predicting the site/timing and extent of drug release from the prototypes, since an a priori IVIVC could be established. Moreover, from the results generated in the present study, it is obvious that novel pH- and time-based multi-unit formulations would improve selectivity of drug delivery to the distal ileum and the colon and therefore might be very helpful in the treatment of colonic diseases.
ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2008.06.014