| Title |
Crystallization from Supersaturated Solutions: Role of Lecithin and Composite Simulated Intestinal Fluid
|
|---|---|
| Published in |
Pharmaceutical Research, June 2018
|
| DOI | 10.1007/s11095-018-2441-2 |
| Pubmed ID | |
| Authors |
Anura S. Indulkar, Yi Gao, Shweta A. Raina, Geoff G. Z. Zhang, Lynne S. Taylor |
| Abstract |
The overall purpose of this study was to understand the impact of different biorelevant media types on solubility and crystallization from supersaturated solutions of model compounds (atazanavir, ritonavir, tacrolimus and cilnidipine). The first aim was to understand the influence of the lecithin content in FaSSIF. As the human intestinal fluids (HIFs) contain a variety of bile salts in addition to sodium taurocholate (STC), the second aim was to understand the role of these bile salts (in the presence of lecithin) on solubility and crystallization from supersaturated solutions, METHODS: To study the impact of lecithin, media with 3 mM STC concentration but varying lecithin concentration were prepared. To test the impact of different bile salts, a new biorelevant medium (Composite-SIF) with a composition simulating that found in the fasted HIF was prepared. The crystalline and amorphous solubility was determined in these media. Diffusive flux measurements were performed to determine the true supersaturation ratio at the amorphous solubility of the compounds in various media. Nucleation induction times from supersaturated solutions were measured at an initial concentration equal to the amorphous solubility (equivalent supersaturation) of the compound in the given medium. It was observed that, with an increase in lecithin content at constant STC concentration (3 mM), the amorphous solubility of atazanavir increased and crystallization was accelerated. However, the crystalline solubility remained fairly constant. Solubility values were higher in FaSSIF compared to Composite-SIF. Longer nucleation induction times were observed for atazanavir, ritonavir and tacrolimus in Composite-SIF compared to FaSSIF at equivalent supersaturation ratios. This study shows that variations in the composition of SIF can lead to differences in the solubility and crystallization tendency of drug molecules, both of which are critical when evaluating supersaturating systems. |
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 % |
|---|---|---|
| Unknown | 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 54 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 54 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 13 | 24% |
| Student > Ph. D. Student | 12 | 22% |
| Researcher | 4 | 7% |
| Student > Doctoral Student | 3 | 6% |
| Other | 3 | 6% |
| Other | 7 | 13% |
| Unknown | 12 | 22% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 25 | 46% |
| Chemistry | 3 | 6% |
| Medicine and Dentistry | 2 | 4% |
| Biochemistry, Genetics and Molecular Biology | 1 | 2% |
| Agricultural and Biological Sciences | 1 | 2% |
| Other | 5 | 9% |
| Unknown | 17 | 31% |
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 18 June 2018.
All research outputs
#15,536,861
of 23,090,520 outputs
Outputs from Pharmaceutical Research
#2,249
of 2,873 outputs
Outputs of similar age
#208,391
of 328,114 outputs
Outputs of similar age from Pharmaceutical Research
#14
of 27 outputs
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