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Determination of the pKa and pH-solubility behavior of an ionizable cyclic carbamate, (S)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4- (trifluoromethyl)-2H-3,1-benzoxazin-2-one (DMP 266).
The ionization behavior of DMP 266 represents a unique case in which the pKa for a carbamate functional group is quite low, and the anomalous pKa value may be attributed to stabilization of the negatively charged species through inductive effects, which originate from the surrounding substituents and delocalization of the negative charge via resonance effects.
Solubilization of nicardipine hydrochloride via complexation and salt formation.
The solubility behavior of nicardipine (1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic+ ++ acid methyl 2-[methyl(phenyl-methyl)amino]ethyl diester), a calcium channel blocker,…
Crystallinity, hygroscopicity and dissolution of moricizine hydrochloride hemihydrate.
Investigation of moricizine hydrochloride polymorphs.
- L. Wu, G. Torosian, K. Sigvardson, C. Gerard, M. Hussain
- Materials ScienceJournal of pharmaceutical sciences
- 1 October 1994
The antiarrhythmic agent moricizine hydrochloride exhibits a single melting-decomposition endotherm peak at temperatures ranging from 209 to 214.5 degrees C (Form I) when recrystallized from polar…
A spectroscopic investigation of DuP 747 polymorphs.
Degradation pathways of a corticotropin-releasing factor antagonist in solution and solid states.
- S. Badawy, M. Hussain, F. Zhao, Q. Ye, Y. Huang, V. Palaniswamy
- Biology, ChemistryJournal of pharmaceutical sciences
- 1 August 2009
Stability of the 1,3,5-triazine derivative (1), a corticotropin-releasing factor inhibitor, was studied in acidic solutions and in solid formulations and degradation appeared to proceed more rapidly in amorphous regions created during processing.
Stabilization of an anthrapyrazole antitumour agent, DuP 937, on complexation with heptakis(2,6-di-O-methyl)-beta-cyclodextrin in aqueous solution.
The impact of crystallinity on Brequinar sodium hygroscopicity.
The results suggest that the less perfect crystals of Brequinar sodium exhibited a faster water uptake and converted to a stable hemihydrate when stored at 75% relative humidity.
Investigations on the cyanogen bromide activation of xanthan gum
The CNBr activation procedure has been investigated as a means of synthesising derivatives of xanthan gum and exhibited a reduced viscosity in solution compared to that of the native polysaccharide, indicating that the mechanism of activation and hence, coupling with amino-ligands, of CNBr-activatedxanthan was similar to that postulated for Sephadex.