| Title |
The BioGIT System: a Valuable In Vitro Tool to Assess the Impact of Dose and Formulation on Early Exposure to Low Solubility Drugs After Oral Administration
|
|---|---|
| Published in |
The AAPS Journal, May 2018
|
| DOI | 10.1208/s12248-018-0231-8 |
| Pubmed ID | |
| Authors |
Alexandros Kourentas, Maria Vertzoni, Vicky Barmpatsalou, Patrick Augustijns, Stefania Beato, James Butler, Rene Holm, Neils Ouwerkerk, Joerg Rosenberg, Tomokazu Tajiri, Christer Tannergren, Mira Symillides, Christos Reppas |
| Abstract |
The purpose of this study was to evaluate the usefulness of the in vitro biorelevant gastrointestinal transfer (BioGIT) system in assessing the impact of dose and formulation on early exposure by comparing in vitro data with previously collected human plasma data of low solubility active pharmaceutical ingredients. Eight model active pharmaceutical ingredients were tested; Lu 35-138C (salt of weak base in a HP-beta-CD solution, three doses), fenofibrate (solid dispersion, tablet, two doses), AZD2207 EQ (salt of weak base, capsule, three doses), posaconazole (Noxafil® suspension, two doses), SB705498 (weak base, tablets vs. capsules), cyclosporine A (Sandimmun® vs. Sandimmun® Neoral), nifedipine (Adalat® capsule vs. Macorel® tablet), and itraconazole (Sporanox® capsule vs. Sporanox® solution). AUC0-0.75h values were calculated from the apparent concentration versus time data in the duodenal compartment of the BioGIT system. Differences in AUC0-0.75h values were evaluated versus differences in AUC0-1h and in AUC0-2h values calculated from previously collected plasma data in healthy adults. Ratios of mean AUC0-0.75h, mean AUC0-1h, and mean AUC0-2h values were estimated using the lowest dose or the formulation with the lower AUC0-0.75h value as denominator. The BioGIT system qualitatively identified the impact of dose and of formulation on early exposure in all cases. Log-transformed mean BioGIT AUC0-0.75h ratios correlated significantly with log-transformed mean plasma AUC0-1h ratios. Based on this correlation, BioGIT AUC0-0.75h ratios between 0.3 and 10 directly reflect corresponding plasma AUC0-1h ratios. BioGIT system is a valuable tool for the assessment of the impact of dose and formulation on early exposure to low solubility drugs. |
X Demographics
The data shown below were collected from the profiles of 4 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 2 | 50% |
| Greece | 1 | 25% |
| Unknown | 1 | 25% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 4 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 52 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 52 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 12 | 23% |
| Student > Master | 8 | 15% |
| Researcher | 5 | 10% |
| Other | 4 | 8% |
| Professor | 1 | 2% |
| Other | 2 | 4% |
| Unknown | 20 | 38% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 23 | 44% |
| Medicine and Dentistry | 2 | 4% |
| Environmental Science | 1 | 2% |
| Mathematics | 1 | 2% |
| Biochemistry, Genetics and Molecular Biology | 1 | 2% |
| Other | 2 | 4% |
| Unknown | 22 | 42% |
Attention Score in Context
This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 18 October 2018.
All research outputs
#12,806,738
of 23,090,520 outputs
Outputs from The AAPS Journal
#624
of 1,297 outputs
Outputs of similar age
#153,330
of 330,395 outputs
Outputs of similar age from The AAPS Journal
#5
of 16 outputs
Altmetric has tracked 23,090,520 research outputs across all sources so far. This one is in the 44th percentile – i.e., 44% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,297 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.0. This one has gotten more attention than average, scoring higher than 51% of its peers.
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We're also able to compare this research output to 16 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 68% of its contemporaries.