Measurement of drug concentration in the stomach after intragastric administration of drug solution to healthy volunteers: analysis of intragastric fluid dynamics and drug absorption.
Pharm Res
; 30(4): 951-8, 2013 Apr.
Article
en En
| MEDLINE
| ID: mdl-23179782
ABSTRACT
PURPOSE:
To evaluate the time-profile of intragastric fluid volume in humans after intragastric administration of drug solution.METHODS:
Eight healthy volunteers were intragastrically administered 150 mL of drug solution containing atenolol (non-absorbable marker) and salicylic acid, then, aliquots of gastric fluid (ca. 2 mL) were sampled for 2 h through the catheter. Rate constants for secretion and emptying of the fluid were obtained by fitting the time-course of atenolol concentration to the simple gastric fluid transit model. Absorption of salicylic acid from the stomach was estimated by comparing its gastric concentration with that of atenolol.RESULTS:
Kinetic analysis of atenolol concentration in the stomach indicated a rapid emptying of the fluid with an average half-life of 4.2 min. Steady-state intragastric fluid volume in 8 volunteers was estimated as 4-133 mL with an average of 42 mL. Intragastric concentration (normalized by dose) of salicylic acid was always lower than that of atenolol, showing approximately 40% of salicylic acid was absorbed from the stomach before emptying to the intestine.CONCLUSIONS:
This study provided valuable information on intragastric fluid dynamics and gastric drug absorption in humans to establish a better in vitro-in vivo correlation in oral drug absorption.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Atenolol
/
Estómago
/
Ácido Salicílico
/
Vaciamiento Gástrico
/
Absorción Intestinal
Límite:
Adult
/
Humans
/
Male
Idioma:
En
Revista:
Pharm Res
Año:
2013
Tipo del documento:
Article
País de afiliación:
Japón