title: Investigation of pH and Temperature Profiles in the GI Tract of Fasted Human Subjects Using the Intellicap(®) System.
abstract: Gastrointestinal (GI) pH and temperature profiles under fasted-state conditions were investigated in two studies with each 10 healthy human subjects using the IntelliCap(®) system. This telemetric drug delivery device enabled the determination of gastric emptying time, small bowel transit time, and colon arrival time by significant pH and temperature changes. The study results revealed high variability of GI pH and transit times. The gastric transit of IntelliCap(®) was characterized by high fluctuations of the pH with mean values ranging from pH 1.7 to pH 4.7. Gastric emptying was observed after 7-202 min (median: 30 min). During small bowel transit, which had a duration of 67-532 min (median: 247 min), pH values increased slightly from pH 5.9-6.3 in proximal parts to pH 7.4-7.8 in distal parts. Colonic pH conditions were characterized by values fluctuating mainly between pH 5 and pH 8. The pH profiles and transit times described in this work are highly relevant for the comprehension of drug delivery of solid oral dosage forms comprising ionizable drugs and excipients with pH-dependent solubility.
authors.affiliation: Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport (C_DAT), Ernst Moritz Arndt University of Greifswald, Greifswald, D-17487, Germany.
authors.forename: Mirko
authors.initials: M
authors.lastname: Koziolek
authors.affiliation: Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport (C_DAT), Ernst Moritz Arndt University of Greifswald, Greifswald, D-17487, Germany.
authors.forename: Michael
authors.initials: M
authors.lastname: Grimm
authors.affiliation: Vivo Drug Delivery GmbH, Wollerau, CH-8832, Switzerland.
authors.forename: Dieter
authors.initials: D
authors.lastname: Becker
authors.affiliation: Medimetrics Personalized Drug Delivery B.V, NL, 5656, AE Eindhoven, The Netherlands.
authors.forename: Ventzeslav
authors.initials: V
authors.lastname: Iordanov
authors.affiliation: Medimetrics Personalized Drug Delivery Inc., Briarcliff Manor, New York, 10510-2059.
authors.forename: Hans
authors.initials: H
authors.lastname: Zou
authors.affiliation: Medimetrics Personalized Drug Delivery Inc., Briarcliff Manor, New York, 10510-2059.
authors.forename: Jeff
authors.initials: J
authors.lastname: Shimizu
authors.affiliation: Medimetrics Personalized Drug Delivery B.V, NL, 5656, AE Eindhoven, The Netherlands.
authors.forename: Christoph
authors.initials: C
authors.lastname: Wanke
authors.affiliation: Physiolution GmbH, Greifswald, D-17489, Germany.
authors.forename: Grzegorz
authors.initials: G
authors.lastname: Garbacz
authors.affiliation: Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport (C_DAT), Ernst Moritz Arndt University of Greifswald, Greifswald, D-17487, Germany.
authors.forename: Werner
authors.initials: W
authors.lastname: Weitschies
mesh_terms: D000328:Adult; D001831:Body Temperature / Q000502:physiology*; D053705:Capsule Endoscopes; D002626:Chemistry, Pharmaceutical; D003106:Colon / Q000378:metabolism / Q000502:physiology; D016503:Drug Delivery Systems; D005215:Fasting / Q000378:metabolism; D005260:Female; D005746:Gastric Emptying; D041981:Gastrointestinal Tract / Q000502:physiology*; D005772:Gastrointestinal Transit / Q000502:physiology; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007421:Intestine, Small / Q000378:metabolism / Q000502:physiology; D008297:Male; D013686:Telemetry; D062125:Thermometry / Q000295:instrumentation; D055815:Young Adult
keywords: clinical trials; controlled release; drug delivery systems; gastrointestinal transit; intestinal secretion/transport; oral drug delivery; pH; site-specific delivery; solid dosage form; transit time