Salt form of nefazodone for use in extended release formulations

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544366, A61K 31495, C07D40306

Patent

active

060340851

ABSTRACT:
The crystalline, stable methanesulfonate salt of nefazodone showed significantly higher intrinsic dissolution in water and THAM buffer (pH 7.5) compared to other salts of nefazodone. The faster dissolution rate of this salt at neutral pH suggests better dissolution and absorption in the intestine, allowing controlled release of nefazodone for oral formulations.

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patent: 4910196 (1990-03-01), Terni et al.
patent: 5188836 (1993-02-01), Muhammad et al.
Agharkar, et al., "Enhancement of Solubility of Drug Salts by Hydrophilic Counterions: Properties of Organic Salts of an Antimalarial Drug," Journal of Pharmaceutical Sciences, vol. 65, No. 5, May 1976, pp. 747-749.

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