| Title |
Ranking Itraconazole Formulations Based on the Flux through Artificial Lipophilic Membrane
|
|---|---|
| Published in |
Pharmaceutical Research, June 2018
|
| DOI | 10.1007/s11095-018-2440-3 |
| Pubmed ID | |
| Authors |
Konstantin Tsinman, Oksana Tsinman, Ram Lingamaneni, Saijie Zhu, Bernd Riebesehl, Arnaud Grandeury, Michael Juhnke, Bernard Van Eerdenbrugh |
| Abstract |
The goal of the study was to evaluate a miniaturized dissolution-permeation apparatus (μFLUX™ apparatus) for its ability to benchmark several itraconazole (ITZ) formulations for which in vivo PK data was available in the literature. Untreated and micronized powders of ITZ and various enabling formulations of ITZ (commercial Sporanox® solid dispersion, a Soluplus®-based solid dispersion and a nanosuspension) were introduced to the donor compartment of μFLUX™ apparatus. Donor and acceptor chambers were divided from each other by a lipophilic membrane. In addition to the flux evaluations, changes in solid state as a function of time were investigated to gain further insight into the flux changes observed over time for the solid dispersion formulations. Initial flux values from Sporanox®, the nanosuspension and the micronized ITZ showed ratios of 52/4/1 with a decreasing flux from nanosuspension and both solid dispersions after 2.5-3 h. Although the initial flux from the Soluplus® formulation was 2.2 times lower than the one observed for Sporanox®, the decrease in flux observed was milder and became ~ 2 times higher than Sporanox® after approximately 2.5 h. The total amounts of ITZ in the receiver compartment after 240 min showed the same rank order as the rodent AUCs of these formulations reported in literature. It was demonstrated that in vitro flux measurements using lipophilic artificial membranes could correctly reproduce the rank order of PK results for ITZ formulations. The drop in flux over time for solid dispersions could be backed by experimental indications of crystallization. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 46 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 46 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 8 | 17% |
| Student > Master | 6 | 13% |
| Other | 4 | 9% |
| Researcher | 4 | 9% |
| Lecturer | 3 | 7% |
| Other | 9 | 20% |
| Unknown | 12 | 26% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 14 | 30% |
| Chemistry | 5 | 11% |
| Medicine and Dentistry | 3 | 7% |
| Chemical Engineering | 2 | 4% |
| Unspecified | 1 | 2% |
| Other | 4 | 9% |
| Unknown | 17 | 37% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. 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 27 June 2018.
All research outputs
#18,640,437
of 23,092,602 outputs
Outputs from Pharmaceutical Research
#2,492
of 2,873 outputs
Outputs of similar age
#253,012
of 328,090 outputs
Outputs of similar age from Pharmaceutical Research
#25
of 27 outputs
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