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 (<i>n</i> = 10), or (b) 5 mg/kg pur...
| Main Authors: | , , , , , , , , , , , , , , , |
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MDPI AG
2022-10-01
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| Series: | Nutrients |
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| Online Access: | https://www.mdpi.com/2072-6643/14/19/4094 |
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| author | Juan A. Navarro Caridad Díaz Juan Decara Dina Medina-Vera Antonio J. Lopez-Gambero Juan Suarez Francisco Javier Pavón Antonia Serrano Antonio Vargas Ana Luisa Gavito Oscar Porras-Perales Jesús Aranda Francisca Vicente Carlos Sanjuan Elena Baixeras Fernando Rodríguez de Fonseca |
| author_facet | Juan A. Navarro Caridad Díaz Juan Decara Dina Medina-Vera Antonio J. Lopez-Gambero Juan Suarez Francisco Javier Pavón Antonia Serrano Antonio Vargas Ana Luisa Gavito Oscar Porras-Perales Jesús Aranda Francisca Vicente Carlos Sanjuan Elena Baixeras Fernando Rodríguez de Fonseca |
| author_sort | Juan A. Navarro |
| collection | DOAJ |
| 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 (<i>n</i> = 10), or (b) 5 mg/kg pure D-Pinitol (<i>n</i> = 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, <i>n</i> = 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. |
| first_indexed | 2024-03-09T21:19:09Z |
| format | Article |
| id | doaj.art-b27f23215a1d4a3cb9bb2f738848a99f |
| institution | Directory Open Access Journal |
| issn | 2072-6643 |
| language | English |
| last_indexed | 2024-03-09T21:19:09Z |
| publishDate | 2022-10-01 |
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| series | Nutrients |
| spelling | doaj.art-b27f23215a1d4a3cb9bb2f738848a99f2023-11-23T21:25:31ZengMDPI AGNutrients2072-66432022-10-011419409410.3390/nu14194094Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy VolunteersJuan A. Navarro0Caridad Díaz1Juan Decara2Dina Medina-Vera3Antonio J. Lopez-Gambero4Juan Suarez5Francisco Javier Pavón6Antonia Serrano7Antonio Vargas8Ana Luisa Gavito9Oscar Porras-Perales10Jesús Aranda11Francisca Vicente12Carlos Sanjuan13Elena Baixeras14Fernando Rodríguez de Fonseca15Laboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainDepartment of Screening & Target Validation, Fundación MEDINA, 18016 Granada, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainDepartment of Screening & Target Validation, Fundación MEDINA, 18016 Granada, SpainEuronutra S.L. Calle Johannes Kepler, 3, 29590 Málaga, SpainDepartamento de Bioquímica y Biología Molecular, Facultad de Medicina, Universidad de Málaga, 29010 Málaga, SpainLaboratorio de Medicina Regenerativa, Unidad de Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospital Regional Universitario de Málaga, 29010 Málaga, SpainThe 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 (<i>n</i> = 10), or (b) 5 mg/kg pure D-Pinitol (<i>n</i> = 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, <i>n</i> = 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.https://www.mdpi.com/2072-6643/14/19/4094D-Pinitolinositoldiabetescarob fruitghrelininsulin |
| spellingShingle | Juan A. Navarro Caridad Díaz Juan Decara Dina Medina-Vera Antonio J. Lopez-Gambero Juan Suarez Francisco Javier Pavón Antonia Serrano Antonio Vargas Ana Luisa Gavito Oscar Porras-Perales Jesús Aranda Francisca Vicente Carlos Sanjuan Elena Baixeras Fernando Rodríguez de Fonseca Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers Nutrients D-Pinitol inositol diabetes carob fruit ghrelin insulin |
| 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 | D-Pinitol inositol diabetes carob fruit ghrelin insulin |
| url | https://www.mdpi.com/2072-6643/14/19/4094 |
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