Nefazodone dosage form
AssigneeBristol-Myers Squibb Company
InventorsAndrew B. Dennis, Peter Timmins, Alison C. Hodsdon
Life of this patent
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Abstract
Extended-release nefazodone compositions containing nefazodone hydrochloride, ionic and non-ionic gelling polymers, an insoluble hydrophilic agent, and optional pharmaceutically acceptable excipients demonstrate pH-modulated release of nefazodone. These compositions are formulated into unit dosage forms for improved oral administration. The improvements comprise an extended drug release profile providing comparative levels of nefazodone with respect to immediate release dosage forms and, additionally, demonstrating the lack of a food effect.
Claims25
A pH-modulated extended release pharmaceutical formulation for the oral administration of nefazodone or a pharmaceutically acceptable salt thereof, wherein the improvements comprise:
- (a) requiring from about 4 to 16 hours for essentially complete drug release from the formulation as measured using standard USP in vitro dissolution protocols employing test media in the pH 1.2 to 7.0 range;
- (b) providing, after oral administration, extended blood levels of nefazodone relative to blood levels seen with immediate release formulations and these extended levels are maintained at or above therapeutic levels for up to 24 hours;
- (c) providing, after oral administration, reduced amounts of nefazodone metabolites, particularly mCPP, while maintaining the blood levels of nefazodone at concentrations comparable to those seen following oral administration with immediate-release formulations;
- and
- (d) lacking a significant food effect on oral administration.
A pharmaceutical formulation useful for making an oral extended-release nefazodone pH-modulated dosage form comprising:
- (a) from about 33 to 45.5 wt % nefazodone hydrochloride;
- (b) from about 16 to 33 wt % of a non-ionic gelling polymer;
- (c) from about 10 to 21 wt % of an ionic gelling polymer;
- and
- (d) from about 16 to 22 wt % of an insoluble hydrophilic agent.
Dependencies are inferred from the claim text.