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Effects of Biorelevant Media Components on Dissolution Behaviour of 1,2,4‐Thiadiazole Derivative Designed for Alzheimer ʼs Disease Prevention
Author(s) -
Promzeleva Maria,
Chislov Mikhail,
Volkova Tatyana,
Proshin Alexey,
Kumeev Roman,
Terekhova Irina
Publication year - 2018
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201700459
Subject(s) - chemistry , dissolution , solubility , micelle , derivative (finance) , pulmonary surfactant , sodium dodecyl sulfate , chromatography , organic chemistry , aqueous solution , biochemistry , financial economics , economics
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 (Fa SSGF , pH 1.6) and Fasted State Simulated Intestinal Fluid (Fa SSIF , 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 Fa SSIF . Interactions occurring between 1,2,4‐thiadiazole derivative and the components of biorelevant media were investigated in detail by means of UV / VIS spectroscopy, 1 H‐ NMR and phase solubility methods.