Pharmaceutical design of a novel colon-targeted delivery system using two-layer-coated tablets of three different pharmaceutical formulations, supported by clinical evidence in humans

Drug delivery systems to the colon are being actively investigated in order to develop oral preparations of peptides and treat local colonic diseases. However, it is difficult to ensure that an oral preparation disintegrates specifically in the human colon. To make a colonic delivery system practica...

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Bibliographic Details
Published in:Journal of controlled release 2004-05, Vol.97 (1), p.31-42
Main Authors: Goto, Takeshi, Tanida, Norifumi, Yoshinaga, Takaaki, Sato, Shuji, Ball, D.J, Wilding, I.R, Kobayashi, Eiji, Fujimura, Akio
Format: Article
Language:English
Subjects:
Adult
Biological and medical sciences
Chemistry, Pharmaceutical
Colon - drug effects
Colon - physiology
Colon-targeted delivery
Cross-Over Studies
Disintegration
Drug Delivery Systems - methods
Drug Design
Female
Gamma scintigraphy
General pharmacology
Humans
Intestinal Absorption - drug effects
Intestinal Absorption - physiology
Male
Medical sciences
Middle Aged
Pharmaceutical Preparations - administration & dosage
Pharmaceutical Preparations - metabolism
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Samarium
Solubility - drug effects
Tablets, Enteric-Coated
Two-layer-coated tablets
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Summary:Drug delivery systems to the colon are being actively investigated in order to develop oral preparations of peptides and treat local colonic diseases. However, it is difficult to ensure that an oral preparation disintegrates specifically in the human colon. To make a colonic delivery system practical for medical use, in vitro testing methods need to be established in order to determine the specifications of the preparations. To achieve this objective, three pharmaceutical preparations, designed to have different tablet disintegration times, were used to examine three buffers in seven combinations intended to simulate pH changes in the stomach, small intestine, and colon of humans. To validate the in vitro methodology, furthermore, the fate of all the formulations was examined in the gastrointestinal (GI) tract of healthy volunteers. A three-way crossover trial by scintigraphy revealed that the three formulations—in spite of presenting different in vitro tablet disintegration profiles—have comparable transit profiles and excellent colon-targeting properties in the human gastrointestinal tract regardless of gender and age. These facts strongly suggest that this novel delivery system may be useful for the delivery of drugs to the human colon.
ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2004.02.023