TY - JOUR
T1 - Gastroretentive Accordion Pill
T2 - Enhancement of riboflavin bioavailability in humans
AU - Kagan, Leonid
AU - Lapidot, Noa
AU - Afargan, Michel
AU - Kirmayer, David
AU - Moor, Eytan
AU - Mardor, Yael
AU - Friedman, Michael
AU - Hoffman, Amnon
N1 - Funding Information:
This paper is a part of Leonid Kagan's Ph.D. dissertation. Prof. Amnon Hoffman and Prof. Michael Friedman are affiliated with the David R. Bloom Center for Pharmacy. This research was supported by Intec Pharma Ltd.
PY - 2006/7/20
Y1 - 2006/7/20
N2 - The purpose of this study was to evaluate the ability of the Accordion Pill™ (AP), a novel controlled release gastroretentive unfolding dosage form (DF), to increase the bioavailability of riboflavin (RF) in humans. Three formulations containing 75 mg of RF and differing in release rate (immediate release (IR) capsule, AP#1, and AP#2) were administered with a low-calorie meal. Gastric residence time (GRT) of the AP was assessed by magnetic resonance imaging. Serial blood and urine samples were taken and assayed for RF. The AP demonstrated prolonged (up to 10.5 h) GRT in humans. Significant elevation in RF bioavailability (209 ± 37%, mean ± S.E.) was achieved by the AP#1 in comparison to the IR capsule. A correlation was established between the in-vitro release rates from DF and bioavailability of RF in humans, and it was modeled taking into account the saturable nature of RF absorption transport and its narrow absorption window (NAW) in the upper gastro-intestinal tract. It is anticipated that the AP will provide a valuable pharmaceutical solution to enhance therapy with NAW drugs.
AB - The purpose of this study was to evaluate the ability of the Accordion Pill™ (AP), a novel controlled release gastroretentive unfolding dosage form (DF), to increase the bioavailability of riboflavin (RF) in humans. Three formulations containing 75 mg of RF and differing in release rate (immediate release (IR) capsule, AP#1, and AP#2) were administered with a low-calorie meal. Gastric residence time (GRT) of the AP was assessed by magnetic resonance imaging. Serial blood and urine samples were taken and assayed for RF. The AP demonstrated prolonged (up to 10.5 h) GRT in humans. Significant elevation in RF bioavailability (209 ± 37%, mean ± S.E.) was achieved by the AP#1 in comparison to the IR capsule. A correlation was established between the in-vitro release rates from DF and bioavailability of RF in humans, and it was modeled taking into account the saturable nature of RF absorption transport and its narrow absorption window (NAW) in the upper gastro-intestinal tract. It is anticipated that the AP will provide a valuable pharmaceutical solution to enhance therapy with NAW drugs.
KW - Controlled release
KW - Gastric residence time
KW - Narrow absorption window
KW - Pharmacokinetics
KW - Saturable absorption
UR - http://www.scopus.com/inward/record.url?scp=33745494695&partnerID=8YFLogxK
U2 - 10.1016/j.jconrel.2006.03.022
DO - 10.1016/j.jconrel.2006.03.022
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C2 - 16806558
AN - SCOPUS:33745494695
SN - 0168-3659
VL - 113
SP - 208
EP - 215
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 3
ER -