| Title |
Characterization of Supersaturated Danazol Solutions – Impact of Polymers on Solution Properties and Phase Transitions
|
|---|---|
| Published in |
Pharmaceutical Research, February 2016
|
| DOI | 10.1007/s11095-016-1871-y |
| Pubmed ID | |
| Authors |
Matthew J. Jackson, Umesh S. Kestur, Munir A. Hussain, Lynne S. Taylor |
| Abstract |
Excipients are essential for solubility enhancing formulations. Hence it is important to understand how additives impact key solution properties, particularly when supersaturated solutions are generated by dissolution of the solubility enhancing formulation. Herein, the impact of different concentrations of dissolved polymers on the thermodynamic and kinetic properties of supersaturated solutions of danazol were investigated. A variety of experimental techniques was used, including nanoparticle tracking analysis, fluorescence and ultraviolet spectroscopy and flux measurements to characterize the solution phase behavior. Neither the crystalline nor amorphous solubility of danazol was impacted by common amorphous solid dispersion polymers, polyvinylpyrrolidone, hydroxypropylmethyl cellulose (HPMC) or HPMC-acetate succinate. Consequently, the maximum membrane transport rate was limited only by the amorphous solubility, and not by the presence of the polymers. The polymers were able to inhibit crystallization to some extent at concentrations as low as 1 μg/mL, with the maximum effectiveness being reached at 10 μg/mL. Aqueous danazol solutions formed a drug-rich phase with a mean size of 250 nm when the concentration exceeded the amorphous solubility, and the polymers modified the surface properties of this drug-rich phase. The phase behavior of supersaturated solutions is complex and the kinetics of phase transformations can be substantially modified by polymeric additives present at low concentrations. However, fortunately, these additives do not appear to impact the bulk thermodynamic properties of the solution, thus enabling supersaturated solutions, which provide enhanced membrane transport relative to saturated solutions to be generated. |
Mendeley readers
The data shown below were compiled from readership statistics for 67 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 1 | 1% |
| Unknown | 66 | 99% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 14 | 21% |
| Student > Ph. D. Student | 11 | 16% |
| Student > Master | 7 | 10% |
| Student > Doctoral Student | 5 | 7% |
| Other | 5 | 7% |
| Other | 9 | 13% |
| Unknown | 16 | 24% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 29 | 43% |
| Chemistry | 13 | 19% |
| Materials Science | 2 | 3% |
| Engineering | 2 | 3% |
| Biochemistry, Genetics and Molecular Biology | 1 | 1% |
| Other | 5 | 7% |
| Unknown | 15 | 22% |
Attention Score in Context
This research output has an Altmetric Attention Score of 7. 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 01 May 2016.
All research outputs
#4,188,124
of 22,867,327 outputs
Outputs from Pharmaceutical Research
#407
of 2,859 outputs
Outputs of similar age
#64,331
of 298,021 outputs
Outputs of similar age from Pharmaceutical Research
#9
of 37 outputs
Altmetric has tracked 22,867,327 research outputs across all sources so far. Compared to these this one has done well and is in the 80th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 2,859 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.0. This one has done well, scoring higher than 83% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 298,021 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 77% of its contemporaries.
We're also able to compare this research output to 37 others from the same source and published within six weeks on either side of this one. This one is in the 43rd percentile – i.e., 43% of its contemporaries scored the same or lower than it.