Gastroretentive Accordion Pill: Enhancement of riboflavin bioavailability in humans

Leonid Kagan; Noa Lapidot; Michel Afargan; David Kirmayer; Eytan Moor; Yael Mardor; Michael Friedman; Amnon Hoffman

doi:10.1016/j.jconrel.2006.03.022

Gastroretentive Accordion Pill: Enhancement of riboflavin bioavailability in humans

Leonid Kagan, Noa Lapidot, Michel Afargan, David Kirmayer, Eytan Moor, Yael Mardor, Michael Friedman, Amnon Hoffman^*

^*Corresponding author for this work

School of Pharmacy

Research output: Contribution to journal › Article › peer-review

70 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	208-215
Number of pages	8
Journal	Journal of Controlled Release
Volume	113
Issue number	3
DOIs	https://doi.org/10.1016/j.jconrel.2006.03.022
State	Published - 20 Jul 2006

Bibliographical note

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.

Keywords

Controlled release
Gastric residence time
Narrow absorption window
Pharmacokinetics
Saturable absorption

Access to Document

10.1016/j.jconrel.2006.03.022

Cite this

@article{20bfc860974949c48b9b21cd013bc168,

title = "Gastroretentive Accordion Pill: Enhancement of riboflavin bioavailability in humans",

abstract = "The purpose of this study was to evaluate the ability of the Accordion Pill{\texttrademark} (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.",

keywords = "Controlled release, Gastric residence time, Narrow absorption window, Pharmacokinetics, Saturable absorption",

author = "Leonid Kagan and Noa Lapidot and Michel Afargan and David Kirmayer and Eytan Moor and Yael Mardor and Michael Friedman and Amnon Hoffman",

note = "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.",

year = "2006",

month = jul,

day = "20",

doi = "10.1016/j.jconrel.2006.03.022",

language = "אנגלית",

volume = "113",

pages = "208--215",

journal = "Journal of Controlled Release",

issn = "0168-3659",

publisher = "Elsevier B.V.",

number = "3",

}

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

M3 - ???researchoutput.researchoutputtypes.contributiontojournal.article???

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 -

Gastroretentive Accordion Pill: Enhancement of riboflavin bioavailability in humans

Abstract

Bibliographical note

Keywords

Access to Document

Other files and links

Fingerprint

Cite this