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Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers

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)...

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Autores principales: Navarro, Juan A., Díaz, Caridad, Decara, Juan, Medina-Vera, Dina, Lopez-Gambero, Antonio J., Suarez, Juan, Pavón, Francisco Javier, Serrano, Antonia, Vargas, Antonio, Gavito, Ana Luisa, Porras-Perales, Oscar, Aranda, Jesús, Vicente, Francisca, Sanjuan, Carlos, Baixeras, Elena, de Fonseca, Fernando Rodríguez
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9572189/
https://www.ncbi.nlm.nih.gov/pubmed/36235746
http://dx.doi.org/10.3390/nu14194094
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author Navarro, Juan A.
Díaz, Caridad
Decara, Juan
Medina-Vera, Dina
Lopez-Gambero, Antonio J.
Suarez, Juan
Pavón, Francisco Javier
Serrano, Antonia
Vargas, Antonio
Gavito, Ana Luisa
Porras-Perales, Oscar
Aranda, Jesús
Vicente, Francisca
Sanjuan, Carlos
Baixeras, Elena
de Fonseca, Fernando Rodríguez
author_facet Navarro, Juan A.
Díaz, Caridad
Decara, Juan
Medina-Vera, Dina
Lopez-Gambero, Antonio J.
Suarez, Juan
Pavón, Francisco Javier
Serrano, Antonia
Vargas, Antonio
Gavito, Ana Luisa
Porras-Perales, Oscar
Aranda, Jesús
Vicente, Francisca
Sanjuan, Carlos
Baixeras, Elena
de Fonseca, Fernando Rodríguez
author_sort Navarro, Juan A.
collection PubMed
description 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.
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spelling pubmed-95721892022-10-17 Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers Navarro, Juan A. Díaz, Caridad Decara, Juan Medina-Vera, Dina Lopez-Gambero, Antonio J. Suarez, Juan Pavón, Francisco Javier Serrano, Antonia Vargas, Antonio Gavito, Ana Luisa Porras-Perales, Oscar Aranda, Jesús Vicente, Francisca Sanjuan, Carlos Baixeras, Elena de Fonseca, Fernando Rodríguez Nutrients Article 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. MDPI 2022-10-01 /pmc/articles/PMC9572189/ /pubmed/36235746 http://dx.doi.org/10.3390/nu14194094 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Navarro, Juan A.
Díaz, Caridad
Decara, Juan
Medina-Vera, Dina
Lopez-Gambero, Antonio J.
Suarez, Juan
Pavón, Francisco Javier
Serrano, Antonia
Vargas, Antonio
Gavito, Ana Luisa
Porras-Perales, Oscar
Aranda, Jesús
Vicente, Francisca
Sanjuan, Carlos
Baixeras, Elena
de Fonseca, Fernando Rodríguez
Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers
title Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers
title_full Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers
title_fullStr Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers
title_full_unstemmed Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers
title_short Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers
title_sort pharmacokinetics and endocrine effects of an oral dose of d-pinitol in human fasting healthy volunteers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9572189/
https://www.ncbi.nlm.nih.gov/pubmed/36235746
http://dx.doi.org/10.3390/nu14194094
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