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: 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, Fonseca, Fernando Rodríguez de
Tipo de recurso: artículo
Fecha de publicación:2022
País:España
Institución:Instituto de Salud Carlos III (ISCIII)
Repositorio:Repisalud
Idioma:inglés
OAI Identifier:oai:repisalud.isciii.es:20.500.12105/18831
Acceso en línea:http://hdl.handle.net/20.500.12105/18831
Access Level:acceso abierto
Palabra clave:D-Pinitol
carob fruit
diabetes
ghrelin
inositol
insulin
insulin resistance
pituitary hormones
Blood Glucose
Fabaceae
Fasting
Fatty Acids, Nonesterified
Female
Ghrelin
Glucagon
Glucose
Healthy Volunteers
Humans
Hydrocortisone
Inositol
Insulin
Male
Prolactin
Thyrotropin
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oai_identifier_str oai:repisalud.isciii.es:20.500.12105/18831
network_acronym_str ES
network_name_str España
repository_id_str
spelling Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers.Navarro, Juan ADíaz, CaridadDecara, JuanMedina-Vera, DinaLopez-Gambero, Antonio JSuarez, JuanPavón, Francisco JavierSerrano, AntoniaVargas, AntonioGavito, Ana LuisaPorras-Perales, OscarAranda, JesúsVicente, FranciscaSanjuan, CarlosBaixeras, ElenaFonseca, Fernando Rodríguez deD-Pinitolcarob fruitdiabetesghrelininositolinsulininsulin resistancepituitary hormonesBlood GlucoseFabaceaeFastingFatty Acids, NonesterifiedFemaleGhrelinGlucagonGlucoseHealthy VolunteersHumansHydrocortisoneInositolInsulinMaleProlactinThyrotropinThe 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.20242024-02-2720222022-10-0120222022-10-01research articlehttp://purl.org/coar/resource_type/c_2df8fbb1VoRhttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/articlehttp://hdl.handle.net/20.500.12105/18831reponame:Repisaludinstname:Instituto de Salud Carlos III (ISCIII)Inglésengopen accesshttp://purl.org/coar/access_right/c_abf2Attribution 4.0 Internationalhttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccessoai:repisalud.isciii.es:20.500.12105/188312026-06-12T12:43:37Z
dc.title.none.fl_str_mv 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.
spellingShingle Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers.
Navarro, Juan A
D-Pinitol
carob fruit
diabetes
ghrelin
inositol
insulin
insulin resistance
pituitary hormones
Blood Glucose
Fabaceae
Fasting
Fatty Acids, Nonesterified
Female
Ghrelin
Glucagon
Glucose
Healthy Volunteers
Humans
Hydrocortisone
Inositol
Insulin
Male
Prolactin
Thyrotropin
title_short 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_sort Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers.
dc.creator.none.fl_str_mv 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
Fonseca, Fernando Rodríguez de
author Navarro, Juan A
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
Fonseca, Fernando Rodríguez de
author_role author
author2 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
Fonseca, Fernando Rodríguez de
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv
dc.subject.none.fl_str_mv D-Pinitol
carob fruit
diabetes
ghrelin
inositol
insulin
insulin resistance
pituitary hormones
Blood Glucose
Fabaceae
Fasting
Fatty Acids, Nonesterified
Female
Ghrelin
Glucagon
Glucose
Healthy Volunteers
Humans
Hydrocortisone
Inositol
Insulin
Male
Prolactin
Thyrotropin
topic D-Pinitol
carob fruit
diabetes
ghrelin
inositol
insulin
insulin resistance
pituitary hormones
Blood Glucose
Fabaceae
Fasting
Fatty Acids, Nonesterified
Female
Ghrelin
Glucagon
Glucose
Healthy Volunteers
Humans
Hydrocortisone
Inositol
Insulin
Male
Prolactin
Thyrotropin
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.
publishDate 2022
dc.date.none.fl_str_mv 2022
2022-10-01
2022
2022-10-01
2024
2024-02-27
dc.type.none.fl_str_mv research article
http://purl.org/coar/resource_type/c_2df8fbb1
VoR
http://purl.org/coar/version/c_970fb48d4fbd8a85
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv http://hdl.handle.net/20.500.12105/18831
url http://hdl.handle.net/20.500.12105/18831
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
Attribution 4.0 International
http://creativecommons.org/licenses/by/4.0/
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
Attribution 4.0 International
http://creativecommons.org/licenses/by/4.0/
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv reponame:Repisalud
instname:Instituto de Salud Carlos III (ISCIII)
instname_str Instituto de Salud Carlos III (ISCIII)
reponame_str Repisalud
collection Repisalud
repository.name.fl_str_mv
repository.mail.fl_str_mv
_version_ 1869410224842997760
score 15,812429

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