Steady State pharmacokinetic parameters (arithmetic mean) for bupropion and metabolites

 

Test (Bupropion XL)

(% CV)

n=30

Reference (Wellbutrin)

(% CV)

n=30

Bupropion

Tmax (h)a

Cmax (ng/mL)

AUC0-24 (ng*h/mL)

Cmin (ng/ml)

Cav (ng/ml)

Degree of Fluctuation (%)

Swing (%)

 

5.00 (3.00-7.00)

[blacked out] (28)

1612.0 (30)

27.6 (39)

67.2 (30)

212.6 (19)

554.6 (35)

 

1.50 (1.00-3.00)

[blacked out] (32)

1792.0 (27)

34.1 (37)

74.7 (27)

190.0 (21)

439.6 (32)

Bupropion Erythroamino Alcohol

Tmax (h)a

Cmax (ng/mL)

AUC0-24 (ng*h/mL)

Cmin (ng/ml)

Cav (ng/ml)

Degree of Fluctuation (%)

Swing (%)b

 

8.00 (5.00-14.00)

[blacked out] (27)

2145.7 (29)

76.5 (34)

89.4 (29)

38.1 (40)

46.0 (35)

 

2.5 (1.07-3.5)

[blacked out] (22)

2353.7 (27)

85.6 (31)

98.1 (27)

38.9 (87)

46.2 (94.7)

Bupropion Threoamino Alcohol

Tmax (h)a

Cmax (ng/mL)

AUC0-24 (ng*h/mL)

Cmin (ng/ml)

Cav (ng/ml)

Degree of Fluctuation (%)

Swing (%)b

 

8.00 (5.00-14.00)

[blacked out] (27)

10987.9 (29)

364.6 (34)

457.8 (29)

50.5 (34)

65.7 (40)

 

2.50 (1.07-5.00)

[blacked out] (22)

12051.4 (26)

415.7 (29)

502.1 (26)

45.2 (48)

56.3 (52)

Hydroxybupropion

Tmax (h)a

Cmax (ng/mL)

AUC0-24 (ng*h/mL)

Cmin (ng/ml)

Cav (ng/ml)

Degree of Fluctuation (%)

Swing (%)b

 

7.00 (4.00-14.00)

[blacked out] (35)

20824.8 (36)

722.2 (39)

867.7 (36)

44.3 (37)

54.6 (41)

 

2.50 (1.00-4.00)

[blacked out] (29)

22456.1 (31)

800.9 (33)

935.7 (31)

40.8 (77)

49.2 (83)

PAWC

Tmax (h)a

Cmax (µM)

AUC0-24 (µM*h)

Cmin (µM)

Cav (µM)

Degree of Fluctuation (%)

Swing (%)b

 

6.00 (4.00-14.00)

[blacked out] (25)

66.5 (27)

2.2 (32)

2.8 (27)

57.7 (21)

75.2 (35)

 

2.00 (1.00-3.00)

[blacked out] (22)

72.1 (23)

2.4 (26)

3.0 (23)

50.1 (36)

62.9 (39)

amedian (range)

bcalculated by reviewer

 

No evidence of dose-dumping was observed after administration of WELLBUTRIN XL.

 

The 90% confidence intervals on the geometric means of the Cmax, Cmin, and AUC0-24 ratios are within the bioequivalence interval of 0.8 to 1.25 for bupropion and its metabolites, and the PAWC, with the exception of bupropion Cmin.  Cmin was approximately 19% lower for WELLBUTRIN XL than the Reference formulation and the ratio of geometric means was 0.8

 

 

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