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ADVAIR DISKUS ADVAIR - GlaxoSmithKline

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Partition Coefficient:<br />

The partition coefficient between n-octanol and water is pH dependent and has been<br />

determined by an HPLC procedure.<br />

log D = 3.2 (pH 9.2)<br />

log D = 2.0 (pH 7.4)<br />

log D = 0.6 (pH 4.0)<br />

Drug Substance<br />

Proper name: fluticasone propionate<br />

Chemical name: s-fluoromethyl 6α ,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo17αpropionyloxyandrosta-1,4-diene-17β-carbothioate<br />

Molecular formula and molecular mass: C 25 H 31 F 3 O 5 S 500.6<br />

Structural formula:<br />

HO<br />

COSCH 2 F<br />

CH 3 OCOC 2 H 5<br />

CH 3<br />

CH 3<br />

H<br />

O<br />

F<br />

F<br />

H<br />

Physicochemical properties:<br />

Description: Fluticasone propionate is a white to off-white powder. It is freely soluble<br />

in dimethyl sulfoxide and dimethylformamide, sparingly soluble in acetone,<br />

dichloromethane, ethyl acetate and chloroform, slightly soluble in methanol and 95%<br />

ethanol, and practically insoluble in water. Fluticasone propionate decomposes without<br />

melting. Onset of decomposition occurs at about 225°C.<br />

CLINICAL TRIALS<br />

Clinical Studies in Asthma<br />

There have been very rare reports of anxiety, sleep disorders and behavioural changes<br />

including hyperactivity and irritability (predominantly in children and adolescents).<br />

July 29, 2014<br />

Page 35 of 67

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