Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity

P.C. Seville, C. Simons, G. Taylor, P.A. Dickinson

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)


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. (C) 2000 Elsevier Science B.V.
Original languageEnglish
Pages (from-to)13-16
Number of pages4
JournalInternational Journal of Pharmaceutics
Issue number1-2
Publication statusPublished - 15 Feb 2000


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