(aclidinium bromide and formoterol fumarate) Inhalation Powder, for Oral Inhalation
DUAKLIR PRESSAIR consists of a dry powder formulation of aclidinium bromide and formoterol fumarate for oral inhalation only.
Aclidinium bromide, is an anticholinergic with specificity for muscarinic receptors. Aclidinium bromide is a synthetic, quaternary ammonium compound, chemically described as 1- azoniabicyclo[2.2.2]octane, 3-[(hydroxydi-2-thienylacetyl)oxy]-1-(3-phenoxypropyl)-, bromide, (3R)-. The structural formula is:
Aclidinium bromide is a white powder with a molecular formula of C26H30 NO4S2Br and a molecular mass of 564.56. It is very slightly soluble in water and ethanol and sparingly soluble in methanol.
Formoterol fumarate, a racemate, is a selective beta2-adrenergic agonist. Its chemical name is (±)-2- hydroxy-5-[(1RS)-1-hydroxy-2-[[(1RS)-2-(4-methoxyphenyl)-1methylethyl]- amino]ethyl]formanilide fumarate dihydrate. The structural formula is:
Formoterol fumarate (as a dihydrate) has a molecular weight of 840.91, and its molecular formula is (C19H24N2O4)2• C4H4O4•2H2O. Formoterol fumarate is a white to yellowish crystalline powder, which is freely soluble in glacial acetic acid, soluble in methanol, sparingly soluble in ethanol and isopropanol, slightly soluble in water, and practically insoluble in acetone, ethyl acetate, and diethyl ether.
DUAKLIR PRESSAIR is a breath-actuated multi-dose dry powder inhaler. Each actuation of DUAKLIR PRESSAIR provides a metered dose of 12 mg of the formulation which contains lactose monohydrate (which may contain milk proteins) as the carrier, 400 mcg of aclidinium bromide (equivalent to 343 mcg of aclidinium), and 12.0 mcg of formoterol fumarate (as a dihydrate, equivalent to 11.5 mcg of formoterol fumarate anhydrous and 9.8 mcg of formoterol). This results in delivery of 396 mcg of aclidinium bromide (equivalent to 340 mcg of aclidinium) and 11.8 mcg of formoterol fumarate (as a dihydrate, equivalent to 11.3 mcg of formoterol fumarate anhydrous and 9.7 mcg of formoterol) from the mouthpiece, based on in vitro testing at an average flow rate of approximately 63 L/min with constant volume of 2 L. The amount of drug delivered to the lungs will vary depending on patient factors such as inspiratory flow rate and inspiratory time.