Prodrug to Probe Solution HFA pMDI Formulation and Pulmonary Esterase Activity

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

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Seville, Peter C. ORCID: https://orcid.org/0000-0001-8546-3474, Simons, C., Taylor, G. and Dickinson, P.A. (2000) Prodrug to Probe Solution HFA pMDI Formulation and Pulmonary Esterase Activity. International Journal of Pharmaceutics, 195 (1-2). pp. 13-16. ISSN Print: 0378-5173 Online: 1873-3476

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Abstract:

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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Uncontrolled Discrete Keywords:

salbutamol, ester, prodrug, solution, inhaler, lung

Legacy Divisions (Admin Only):

College of Health, Life and Environmental Sciences > School of Science and the Environment

Academic Schools:

School of Science and the environment

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