RT Journal Article
T1 Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers.
A1 Navarro, Juan A
A1 Díaz, Caridad
A1 Decara, Juan
A1 Medina-Vera, Dina
A1 Lopez-Gambero, Antonio J
A1 Suarez, Juan
A1 Pavón, Francisco Javier
A1 Serrano, Antonia
A1 Vargas, Antonio
A1 Gavito, Ana Luisa
A1 Porras-Perales, Oscar
A1 Aranda, Jesús
A1 Vicente, Francisca
A1 Sanjuan, Carlos
A1 Baixeras, Elena
A1 Fonseca, Fernando Rodríguez de
K1 D-Pinitol
K1 carob fruit
K1 diabetes
K1 ghrelin
K1 inositol
K1 insulin
K1 insulin resistance
K1 pituitary hormones
AB The present study characterizes the oral pharmacokinetics of D-Pinitol, a natural insulin mimetic inositol, in human healthy volunteers (14 males and 11 females). D-Pinitol absorption was studied in (a) subjects receiving a single oral dose of 15 mg/kg (n = 10), or (b) 5 mg/kg pure D-Pinitol (n = 6), and (c) subjects receiving D-Pinitol as part of carbohydrate-containing carob pods-derived syrup with a 3.2% D-Pinitol (Dose of 1600 mg/subject, n = 9). The volunteers received a randomly assigned single dose of either D-Pinitol or carob pod-derived syrup. Blood samples were collected at 0, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min after intake. Plasma concentration of D-Pinitol was measured and pharmacokinetic parameters obtained. The data indicate that when given alone, the oral absorption of D-Pinitol is dose-dependent and of extended duration, with a Tmax reached after almost 4 h, and a half-life greater than 5 h. When the source of D-Pinitol was a carob pods-derived syrup, Cmax was reduced to 40% of the expected based on the data of D-Pinitol alone, suggesting a reduced absorption probably because of competition with monosaccharide transport. In this group, Tmax was reached before that of D-Pinitol alone, but the estimated half-life remained the same. In the D-Pinitol groups, plasma concentrations of glucose, insulin, glucagon, ghrelin, free fatty acids, and pituitary hormones were additionally measured. A dose of 15 mg/kg of D-Pinitol did not affect glucose levels in healthy volunteers, but reduced insulin and increased glucagon and ghrelin concentrations. D-Pinitol did not increase other hormones known to enhance plasma glucose, such as cortisol or GH, which were surprisingly reduced after the ingestion of this inositol. Other pituitary hormones (gonadotropins, prolactin, and thyroid-stimulating hormone) were not affected after D-Pinitol ingestion. In a conclusion, D-Pinitol is absorbed through the oral route, having an extended half-life and displaying the pharmacological profile of an endocrine pancreas protector, a pharmacological activity of potential interest for the treatment or prevention of insulin resistance-associated conditions.
YR 2022
FD 2022-10-01
LK http://hdl.handle.net/10668/21505
UL http://hdl.handle.net/10668/21505
LA en
DS RISalud
RD Apr 12, 2025