NDA
20-358: WELLBUTRIN® SR tablets
Study 201: Two bupropion HCL SR 150 mg tablets each with different in vitro release rates (fast release: BUR-01A1 and slow release BUR-01C1) were compared to the WELLBUTRIN® IR formulation (2x75 mg tablets) in twelve (12) healthy male subjects following a single-dose oral administration in a 3-way crossover study. For both SR formulations (faster and slow), mean Cmax for bupropion was reduced by about 60% compared to the IR formulation. The mean AUC0-00 of bupropion was approximately 90% and 76% for the faster SR and slow SR formulations, respectively, of the corresponding value for the IR formulation.
The Slow SR formulation (test) is not equivalent to the IR formulation (reference) with respect to both AUC0-00 and Cmax for bupropion and the three moieties (306U73, 494U73, and the pharmacologic activity-weighted composite).
For the fast SR formulation, both the AUC and Cmax were higher than those seen for the slow SR formulation; however, the fast SR tablet was still bioinequivalent to the IR tablet. The sponsor selected the fast SR formulation for further development work. The final (to-be-marketed) SR formulation (BUR-02A1) differs from the fast release formulation (BUR-01A1) in that the former has carnauba wax added to the film-coated to facilitate imprinting (APPENDIX II).
Study 204: Twenty one (21) healthy male volunteers received 2 x 50 mg bupropion HCL SR tablets. 1 x 100 mg bupropion HCL SR tablet, and 1 X 100 mg WELLBUTRIN® IR tablet on three separate occasions in a single dose crossover study. Plasma samples in this study were analyzed only for bupropion.
The 2 x50 mg SR tablets and the 1 x 100 mg SR tablet were separately shown to be equivalent to the 1 x 100 mg IR tablet based on AUC comparisons. This was not the case for Cmax as Cmax for the SR was about 50% the Cmax for the IR dosage form.
The 2 x 50 mg SR tablets were equivalent to the 1 x 100 mg SR tablet with respect to AUC and Cmax.
Study 202: The effect of a standard high fat breakfast on the performance of the 150 mg bupropion HCL SR tablet (highest strength, to-be-marketed) was evaluated following single-dose oral administration to twenty four (24) healthy male volunteers. The third leg in the study was 2 x 75 mg IR tablet under fasted conditions.
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