Effects of Biorelevant Media Components on Dissolution Behaviour of 1,2,4‐Thiadiazole Derivative Designed for Alzheimerʼs Disease Prevention

Effects of Biorelevant Media Components on Dissolution Behaviour of 1,2,4‐Thiadiazole... In this study, dissolution behaviour of 1,2,4‐thiadiazole derivative (1‐[5‐(3‐chloro‐phenylamino)‐1,2,4‐thiadiazol‐3‐yl]‐propan‐2‐ol) displaying an anti‐Alzheimer activity was examined in biorelevant media such as Simulated Gastric Fluid (SGF, pH 1.2), Fasted State Simulated Gastric Fluid (FaSSGF, pH 1.6) and Fasted State Simulated Intestinal Fluid (FaSSIF, pH 6.5). It was found that solubility and dissolution rate of 1,2,4‐thiadiazole derivative under consideration are not strongly dependent on pH, whereas these parameters are significantly affected by the buffer composition. Dissolution was found to be more effective in buffers composed of the surfactant micelles. It was demonstrated that considerable increase in solubility and dissolution rate in SGF is achieved through the interaction of 1,2,4‐thiadiazole derivative with the micelles of sodium dodecyl sulfate. On the contrary, CMC of sodium taurochalate was shifted in the presence of 1,2,4‐thiadiazole derivative, therefore, dissolution process is not so efficient in FaSSIF. Interactions occurring between 1,2,4‐thiadiazole derivative and the components of biorelevant media were investigated in detail by means of UV/VIS spectroscopy, 1H‐NMR and phase solubility methods. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Chemistry & Biodiversity Wiley

Effects of Biorelevant Media Components on Dissolution Behaviour of 1,2,4‐Thiadiazole Derivative Designed for Alzheimerʼs Disease Prevention

Loading next page...
 
/lp/wiley/effects-of-biorelevant-media-components-on-dissolution-behaviour-of-1-F1fi2aN9Qy
Publisher
Wiley Subscription Services, Inc., A Wiley Company
Copyright
© 2018 Wiley‐VHCA AG, Zurich, Switzerland
ISSN
1612-1872
eISSN
1612-1880
D.O.I.
10.1002/cbdv.201700459
Publisher site
See Article on Publisher Site

Abstract

In this study, dissolution behaviour of 1,2,4‐thiadiazole derivative (1‐[5‐(3‐chloro‐phenylamino)‐1,2,4‐thiadiazol‐3‐yl]‐propan‐2‐ol) displaying an anti‐Alzheimer activity was examined in biorelevant media such as Simulated Gastric Fluid (SGF, pH 1.2), Fasted State Simulated Gastric Fluid (FaSSGF, pH 1.6) and Fasted State Simulated Intestinal Fluid (FaSSIF, pH 6.5). It was found that solubility and dissolution rate of 1,2,4‐thiadiazole derivative under consideration are not strongly dependent on pH, whereas these parameters are significantly affected by the buffer composition. Dissolution was found to be more effective in buffers composed of the surfactant micelles. It was demonstrated that considerable increase in solubility and dissolution rate in SGF is achieved through the interaction of 1,2,4‐thiadiazole derivative with the micelles of sodium dodecyl sulfate. On the contrary, CMC of sodium taurochalate was shifted in the presence of 1,2,4‐thiadiazole derivative, therefore, dissolution process is not so efficient in FaSSIF. Interactions occurring between 1,2,4‐thiadiazole derivative and the components of biorelevant media were investigated in detail by means of UV/VIS spectroscopy, 1H‐NMR and phase solubility methods.

Journal

Chemistry & BiodiversityWiley

Published: Jan 1, 2018

Keywords: ; ; ; ;

References

You’re reading a free preview. Subscribe to read the entire article.


DeepDyve is your
personal research library

It’s your single place to instantly
discover and read the research
that matters to you.

Enjoy affordable access to
over 12 million articles from more than
10,000 peer-reviewed journals.

All for just $49/month

Explore the DeepDyve Library

Unlimited reading

Read as many articles as you need. Full articles with original layout, charts and figures. Read online, from anywhere.

Stay up to date

Keep up with your field with Personalized Recommendations and Follow Journals to get automatic updates.

Organize your research

It’s easy to organize your research with our built-in tools.

Your journals are on DeepDyve

Read from thousands of the leading scholarly journals from SpringerNature, Elsevier, Wiley-Blackwell, Oxford University Press and more.

All the latest content is available, no embargo periods.

See the journals in your area

DeepDyve Freelancer

DeepDyve Pro

Price
FREE
$49/month

$360/year
Save searches from
Google Scholar,
PubMed
Create lists to
organize your research
Export lists, citations
Read DeepDyve articles
Abstract access only
Unlimited access to over
18 million full-text articles
Print
20 pages/month
PDF Discount
20% off