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Tuesday 15 February 2000

Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity.

By: Seville PC, Simons C, Taylor G, Dickinson PA.

Int J Pharm 2000 Feb 15;195(1-2):13-6

A novel salbutamol prodrug was synthesised. Solubility in HFA-134a and susceptibility to rat lung homogenate, blood and plasma esterase enzymes were investigated. Whereas salbutamol had a very low solubility in HFA-134a, the prodrug was found to be miscible in all proportions. In lung homogenate, the prodrug hydrolysed with a half-life of 45 min, re-generating approximately 17% of expected salbutamol after 8 h incubation. The use of a solution pMDI for pulmonary delivery of the salbutamol prodrug is predicted to result in liberation of salbutamol in the lungs following in vivo hydrolysis by lung esterases.

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