Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity

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

doi:10.1016/S0378-5173(99)00352-X

Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity

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

Pharmacy

Research output: Contribution to journal › Article › peer-review

2 Citations (Scopus)

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. (C) 2000 Elsevier Science B.V.

Original language	English
Pages (from-to)	13-16
Number of pages	4
Journal	International Journal of Pharmaceutics
Volume	195
Issue number	1-2
DOIs	https://doi.org/10.1016/S0378-5173(99)00352-X
Publication status	Published - 15 Feb 2000

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title = "Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity",

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. (C) 2000 Elsevier Science B.V.",

author = "P.C. Seville and C. Simons and G. Taylor and P.A. Dickinson",

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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 - https://www.scopus.com/pages/publications/0033977107

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 -

Prodrug to probe solution HFA pMDI formulation and pulmonary esterase activity

Abstract

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