NDA
20-358: WELLBUTRIN® SR tablets
The % CV for bupropion was about 25%, for metabolite 306U73 it was about 40% and was the highest for 494U73 – AUC0-00 was about 80%. Cmax about 45%. For PAWC it was about 30%.
The
effect of food on WELLBUTRIN® SR does not appear to be clinically significant.
Under
fasted conditions, the 150 mg bupropion SR tablet showed comparable
availability to the 2 x 75 mg WELLBUTRIN® IR tablets.
Study
206: Thirty four (34) healthy male
volunteers received 1 x 150 mg bupropion HCL SR tablet b.i.d. (q12h) and 1 x
100 mg WELLBUTRIN® IR tablet t.i.d. (as 6h, 6h, and 12h dosings) for 14 days on
two separate occasions in a multiple dose crossover study.
For
bupropion AUC(0-24) and Cmin were inside the confidence intervals of 80-125%,
while Cmax was slightly outside (78-98%).
For the three metabolites, and PAWC, the pharmacokinetic parameters were
within the 80-125% range.
The
fluctuation index for bupropion was about 15% lower for the SR tablets than for
the IR tablets. The fluctuation
indices for 306U73, 494U74, 17U67 and the pharmacologic activity weighted
composite for the SR tablet ranged from 95-102% of the respective index for IR
tablet.
At
steady state, the 150 mg SR tablet given every 12 hours is equivalent to the
100 mg IR tablet given every 6, 6, and 12 hours.
In
general, the adverse events were less frequent with the SR tablet than with the
IR tablet.
Study 207: Thirty six (36) healthy male volunteers received 6x50 mg bupropion HCL SR tablets, 3x100 mg bupropion HCL SR tablets, and 2x150 mg bupropion HCL SR tablets on three separate occasions in a single dose crossover study. The 150 mg SR tablet was used as the reference as it had participated in the pivotal multiple dose bioequivalency study.
Both 6 x 50 mg and 3 x 100 mg bupropion HCL SR tablets are equivalent to 2 x 150 mg bupropion HCL SR tablets. This was with respect to both AUC0-00 and Cmax of bupropion, its active metabolites (306U73 and 494U73), and PAWC.
FORMULATION: WELLBUTRIN® SR (bupropion HCL SR) is proposed for marketing
as biconvex, round, film-coated tablets in strengths of 50 mg (white, 100 mg
(blue), and 150 mg (purple).
(Detailed composition of formulations are presented in APPENDIX II).
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