In Situ Study of the Effect of Naringin, Talinolol and Protein–Energy Undernutrition on Intestinal Absorption of Saquinavir in Rats

• Published in: Basic & clinical pharmacology & toxicology 2011-10, Vol.109 (4), p.245-252
• Main Authors: Catalán‐Latorre, Ana, Nácher, Amparo, Merino, Virginia, Jiménez‐Torres, Nicolás Víctor, Merino‐Sanjuán, Matilde
• Format: Article
• Language: English
• Subjects: Administration, Oral; Animals; Antiviral agents; Biological and medical sciences; Diffusion; Drug Antagonism; Drugs; Flavanones - pharmacokinetics; HIV Protease Inhibitors - pharmacokinetics; Intestinal absorption; Intestinal Absorption - drug effects; Intestinal Absorption - physiology; Male; Malnutrition; Medical sciences; Metabolic diseases; Other nutritional diseases (malnutrition, nutritional and vitamin deficiencies...); Perfusion; Pharmacokinetics; Pharmacology. Drug treatments; Propanolamines - pharmacokinetics; Protein-Energy Malnutrition - metabolism; Rats; Rats, Wistar; Saquinavir; Saquinavir - pharmacokinetics; Small intestine; Undernutrition
• ISSN: 1742-7835; 1742-7843
• DOI: 10.1111/j.1742-7843.2011.00714.x

:  To study the potential interactions of naringin (NAR), talinolol (TAL) and protein–energy undernutrition (PEU) in the absorption process of saquinavir (SQV), perfusion experiments were performed in the small intestine of rats at different SQV concentrations. The results obtained demonstrated that SQV intestinal absorption was described by simultaneous passive diffusion (kdif = 3.44 hr) and saturable absorption (Vma = 127.31 μM/hr; Kma = 10.50 μM) together with a capacity‐limited efflux (Vms = 270.53 μM/hr; Kms = 23.44 μM). The competitive inhibition constants of NAR on the SQV input and efflux processes were [IC50]a = 3.98 μM and [IC50]s = 5.00 μM, respectively. NAR significantly decreased (23–29%; p