[Rate of dissolution and polymorphism of carbamazepine: different prescriptions].
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Biomedical subjects
Publications and source records attributed to M Draguet-Brughmans.
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In a study of variations in the physicochemical properties of digoxin powder from several commercial sources, recrystallizations of digoxin were performed under several conditions. Polymorphs were not obtained whereas a pure amorphous form was formed under certain conditions. The amorphous form was more soluble and more stable under compression than was the crystalline form; nevertheless in contact with water it crystallized quickly. Traces of the crystalline form reduced the dissolution rate and stability of the amorphous form. Variations in the thermal behaviour of commercial samples can be explained by the presence of variable proportions of the amorphous form and also by thermal decomposition that varies from one sample to another and generally occurs at 160 degrees C and above.
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A comparison of X-ray powder diffraction patterns, IR spectra, and crystal structures of structurally related compounds belonging to the butyrophenone family has been undertaken to obtain information about the elements of chemical structure which predispose a substance to exhibit polymorphism. Five butyrophenones, differing by the nature of only one substituent, were selected. After crystallization from 15 solvents, it appears that two compounds of the group exhibit more than one crystalline form. An explanation of the absence of polymorphism in the other compounds of the group is proposed and discussed.
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A second polymorph of spiperone, 8-[3-(p-fluorobenzoyl)-propyl]-1-phenyl-1,3,8-triazaspiro[4,5] decan-4-one, has been isolated and characterized by thermal analysis and IR spectrometry. Its structure was solved by X-ray diffraction analysis. The results are compared with those previously obtained on spiperone, the main difference being in the conformation of the side chain and in the nature of the hydrogen bonding.
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Chemical or biochemical oxidation of cyclobarbital yielded 5-(3-oxo-1-cyclohexen-1-yl)-5-ethyl -2,4,6,- (1H,3H,5H)-pyrimidinetrione, and photochemical oxidation gave 5-(6-oxo-1-cyclohexen-1-yl)-5-ethyl-2,4,6-(1H,3H,3H)-pyrimidinetrione. These compounds were isolated and purified by TLC, and their structures were determined by UV, IR, NMR, and mass spectral data; the crystalline structure was determined by X-ray diffraction.
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