TY - JOUR
T1 - Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity
AU - Seville, P.C.
AU - Simons, C.
AU - Taylor, G.
AU - Dickinson, P.A.
PY - 2000/2/15
Y1 - 2000/2/15
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?eid=2-s2.0-0033977107&partnerID=8YFLogxK
U2 - 10.1016/S0378-5173(99)00352-X
DO - 10.1016/S0378-5173(99)00352-X
M3 - Article
AN - SCOPUS:0033977107
SN - 0378-5173
VL - 195
SP - 13
EP - 16
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -