Regional In Vivo Dissolution of Immediate Release Ibuprofen in Human Gastrointestinal Tract and Its Relationship to Luminal pH, GI Motility, and Systemic Absorption

2016 ◽  
Author(s):  
Mark Koenigsknecht
Keyword(s):  
Gastrointestinal Tract ◽  
Immediate Release ◽  
Systemic Absorption ◽  
Human Gastrointestinal Tract ◽  
Luminal Ph ◽  
Gi Motility ◽  
In Vivo Dissolution

scholarly journals In VivoDissolution and Systemic Absorption of Immediate Release Ibuprofen in Human Gastrointestinal Tract under Fed and Fasted Conditions

2017 ◽  
Vol 14 (12) ◽  
pp. 4295-4304 ◽  
Author(s):  
Mark J. Koenigsknecht ◽  
Jason R. Baker ◽  
Bo Wen ◽  
Ann Frances ◽  
Huixia Zhang ◽  
...  
Keyword(s):  
Gastrointestinal Tract ◽  
Immediate Release ◽  
Systemic Absorption ◽  
Human Gastrointestinal Tract

scholarly journals Procyanidins are not bioavailable in rats fed a single meal containing a grapeseed extract or the procyanidin dimer B3

2002 ◽  
Vol 87 (4) ◽  
pp. 299-306 ◽  
Author(s):  
Jennifer L. Donovan ◽  
Adam Lee ◽  
Claudine Manach ◽  
Laurent Rios ◽  
Christine Morand ◽  
...  
Keyword(s):  
Gastrointestinal Tract ◽  
Urinary Excretion ◽  
Ring Structure ◽  
Future Research ◽  
Human Gastrointestinal Tract ◽  
Human Diet ◽  
Single Meal ◽  
Nutritional Effects ◽  
Grapeseed Extract

Flavanols are the most abundant flavonoids in the human diet where they exist as monomers, oligomers and polymers. In the present study, catechin, the procyanidin dimer B3 and a grapeseed extract containing catechin, epicatechin and a mixture of procyanidins were fed to rats in a single meal. After the meals, catechin and epicatechin were present in conjugated forms in both plasma and urine. In contrast, no procyanidins or conjugates were detected in the plasma or urine of any rats. Procyanidins were not cleaved into bioavailable monomers and had no significant effects on the plasma levels or urinary excretion of the monomers when supplied together in the grapeseed extract. We conclude that the nutritional effects of dietary procyanidins are unlikely to be due to procyanidins themselves or monomeric metabolites with the intact flavonoid-ring structure, as they do not exist at detectable concentrations in vivo. Future research should focus on other procyanidin metabolites such as phenolic acids and on the effects of the unabsorbed oligomers and polymers on the human gastrointestinal tract.

scholarly journals Physiologically Relevant In Vitro-In Vivo Correlation (IVIVC) Approach for Sildenafil with Site-Dependent Dissolution

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 251 ◽  
Author(s):  
Tae Hwan Kim ◽  
Soyoung Shin ◽  
Seok Won Jeong ◽  
Jong Bong Lee ◽  
Beom Soo Shin
Keyword(s):  
Dissolution Kinetics ◽  
Immediate Release ◽  
Relative Bioavailability ◽  
Wet Granulation ◽  
Population Pharmacokinetic ◽  
Beagle Dogs ◽  
Concentration Time ◽  
In Vivo Dissolution

This study aimed to establish a physiologically relevant in vitro-in vivo correlation (IVIVC) model reflecting site-dependent dissolution kinetics for sildenafil based on population-pharmacokinetic (POP-PK) modeling. An immediate release (IR, 20 mg) and three sustained release (SR, 60 mg) sildenafil tablets were prepared by wet granulation method. In vitro dissolutions were determined by the paddle method at pH 1.2, 4.5, and 6.8 media. The in vivo pharmacokinetics were assessed after oral administration of the prepared IR and SR formulations to Beagle dogs (n = 12). The dissolution of sildenafil from SR formulations was incomplete at pH 6.8, which was not observed at pH 1.2 and pH 4.5. The relative bioavailability was reduced with the decrease of the dissolution rate. Moreover, secondary peaks were observed in the plasma concentration-time curves, which may result from site-dependent dissolution. Thus, a POP-PK model was developed to reflect the site-dependent dissolution by separately describing the dissolution and absorption processes, which allowed for estimation of the in vivo dissolution of sildenafil. Finally, an IVIVC was established and validated by correlating the in vitro and in vivo dissolution rates. The present approach may be applied to establish IVIVC for various drugs with complex dissolution kinetics for the development of new formulations.

scholarly journals Motor responses of human gastrointestinal tract to 5-hydroxytryptamine in vivo and in vitro

Gut ◽  
1966 ◽  
Vol 7 (3) ◽  
pp. 208-216 ◽  
Author(s):  
J. J. Misiewicz ◽  
S. L. Waller ◽  
M. Eisner
Keyword(s):  
Gastrointestinal Tract ◽  
Human Gastrointestinal Tract ◽  
Motor Responses

In Vivo Endoscopic Optical Coherence Tomography of the Human Gastrointestinal Tract - Toward Optical Biopsy

Endoscopy ◽  
2000 ◽  
Vol 32 (10) ◽  
pp. 743-749 ◽  
Author(s):  
S. Jäckle ◽  
N. Gladkova ◽  
F. Feldchtein ◽  
A. Terentieva ◽  
B. Brand ◽  
...  
Keyword(s):  
Optical Coherence Tomography ◽  
Gastrointestinal Tract ◽  
Optical Biopsy ◽  
Optical Coherence ◽  
Human Gastrointestinal Tract ◽  
Endoscopic Optical Coherence Tomography

scholarly journals Development ofIn Vitro-In VivoCorrelation/Relationship Modeling Approaches for Immediate Release Formulations Using Compartmental Dynamic Dissolution Data from “Golem”: A Novel Apparatus

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Martin Čulen ◽  
Paweł K. Tuszyński ◽  
Sebastian Polak ◽  
Renata Jachowicz ◽  
Aleksander Mendyk ◽  
...  
Keyword(s):  
Small Intestine ◽  
Gastrointestinal Tract ◽  
Direct Observation ◽  
Immediate Release ◽  
Dissolution Behavior ◽  
Human Gastrointestinal Tract ◽  
Release Formulation ◽  
Dissolution Method ◽  
Dissolution Apparatus ◽  
Ph Dependent

Different batches of atorvastatin, represented by two immediate release formulation designs, were studied using a novel dynamic dissolution apparatus, simulating stomach and small intestine. A universal dissolution method was employed which simulated the physiology of human gastrointestinal tract, including the precise chyme transit behavior and biorelevant conditions. The multicompartmental dissolution data allowed direct observation and qualitative discrimination of the differences resulting from highly pH dependent dissolution behavior of the tested batches. Further evaluation of results was performed using IVIVC/IVIVR development. While satisfactory correlation could not be achieved using a conventional deconvolution based-model, promising results were obtained through the use of a nonconventional approach exploiting the complex compartmental dissolution data.

scholarly journals Comparison of five in vitro digestion models to in vivo experimental results: Lead bioaccessibility in the human gastrointestinal tract

2007 ◽  
Vol 42 (9) ◽  
pp. 1203-1211 ◽  
Author(s):  
Tom R. Van de Wiele ◽  
Agnes G. Oomen ◽  
Joanna Wragg ◽  
Mark Cave ◽  
Mans Minekus ◽  
...  
Keyword(s):  
Gastrointestinal Tract ◽  
In Vitro Digestion ◽  
Experimental Results ◽  
Human Gastrointestinal Tract

Distribution of Serotonin (5-Hydroxytryptamine) in the Human Gastrointestinal Tract

1961 ◽  
Vol 41 (2) ◽  
pp. 119-121 ◽  
Author(s):  
Robert H. Resnick ◽  
Seymour J. Gray
Keyword(s):  
Gastrointestinal Tract ◽  
Human Gastrointestinal Tract

The Design of a Hydraulic Suction Tube for Peroral Biopsy of the Human Gastrointestinal Tract

1962 ◽  
Vol 42 (3) ◽  
pp. 281-284 ◽  
Author(s):  
Wayne E. Quinton ◽  
Arnold L. Flick ◽  
Cyrus E. Rubin
Keyword(s):  
Gastrointestinal Tract ◽  
Human Gastrointestinal Tract ◽  
Suction Tube
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