EA Review #1, NDA 20-358

Page 18

ATTACHMENT 3

TIER 0

Attribute

Compound

Test Method

Compliance w/method (Y/N)

Result

Comments

Water Solubility

Bupropion Hydrochloride

As described on page 42

No

Water             11.3 x

10^-1 M

0.1 N HCl       12.1 x

10^-1 M

0.1 NNaOH    3.6 x

10^-3 M

Temperature not specified

Single determinations in each solvent

Hydrolytic Stability

(Kh)

@ - 1ppm

Bupropion hydrochloride

As described on page 58

No

pH 5                2.95 x 10^-10

S^-1

pH 7.4             4.80 x 10^-7

S^-1

pH 9.0             1.23 x 10^-7

S^-1

Dissociation Constant

Bupropion hydrochloride

Spectrometric titration described on page 51

No

pka-8.25

Octanol/Water Log Kow

Bupropion hydrochloride

As described on page 44

No

pH 1.2             Log Kow =

-0.60

pH 6.0             Log Kow =

0.91

pH 7.4             Log Kow =

1.54

Distilled

Water             Log Kow =

-1.32

Single determination at each pH

Vapor Pressure

Bupropion hydrochloride

FDA TAD 3.03

Yes

3.74 x 10^-7 torr