Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle.
J Med Chem
; 60(20): 8580-8590, 2017 10 26.
Article
em En
| MEDLINE
| ID: mdl-28968087
ABSTRACT
Phosphonamidate 3a of methoxymethylphosphonic acid (MMPA) with propofol (1) and l-alanine ethyl ester was found to be an efficient scaffold for the oral delivery of compound 1. The synthesis and evaluation of MMPA based phosphonamidates of compound 1, HSK3486 (2), and other phenolic drugs revealed the general application of MMPA as the effective delivery vehicle for phenolic drugs. On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97.6% and 34.1%, respectively.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Portadores de Fármacos
/
Propofol
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Organofosfonatos
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Hipnóticos e Sedativos
Limite:
Animals
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article