Journal
PHARMACEUTICAL CHEMISTRY JOURNAL
Volume 48, Issue 3, Pages 201-208Publisher
SPRINGER
DOI: 10.1007/s11094-014-1077-8
Keywords
Amphiphilic drugs; imipramie hydrochloride; cloud point; bile salts; hydrotropes; fatty acids
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The clouding behaviour of an amphiphilic antidepressant drug imipramine hydrochloride (IMP) with several additives (hydrotropes, bile salts, fatty acids and sugars) over the entire composition range at pH = 7.6 was investigated in the present study. The magnitude of clouding (increase or decrease) of IMP in the presence of additives (pharmaceutical excipients) depends on the nature and types of additives. Bile salts and fatty acids showed peak behaviour i.e., cloud point (CP) increases at lower concentrations while decrease in cloud points was observed at higher concentrations. Thermodynamics at the CP were also evaluated (except for sugars, because sugars does not form mixed micelles with IMP), assuming that the clouding indicates the solubility limit when phase separation occurs. Thus, the various thermodynamic parameters e.g., standard Gibbs free energy (Delta G (s) (o) ), the enthalpy (Delta H (s) (o) ) and entropy (T Delta S (s) (o) ) were calculated at this point. The results showed that the Delta G (s) (o) , was found to be negative for all the additives, however Delta H (s) (o) and T Delta G (s) (o) of the clouding phenomenon were found to be positive or negative depending upon the types and nature of additives.
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