Pharmacokinetics and Oral Bioavailability of Hydrocortisone
Abstract
The pharmacokinetics of 20 mg hydrocortisone were studied after IV and oral administration. Endogenous hydrocortisone was suppressed by dexamethasone administration. Hydrocortisone concentrations were measured in plasma and saliva. After IV administration, hydrocortisone was eliminated with a total body clearance of 18 L/hr and a half-life of 1.7 hr. The volume of distribution was 34 L. Oral bioavailability averaged 96%. Absorption was rapid, achieving maximum hydrocortisone levels of 300 ng/mL after 1 hour. Saliva levels were not proportional to plasma levels, but could be shown to reflect free, non-protein bound hydrocortisone concentrations in plasma.
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The only previous study of hydrocortisone bioavailability reported absolute bioavailability to be 0.96 (CI 0.82 to 1.09).
“The only previous study of hydrocortisone bioavailability reported absolute bioavailability to be 0.96 (CI 0.82 to 1.09) [3]”
From Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone (2018) · cites this paper as [3]
The previous study of hydrocortisone bioavailability used a radioimmunoassay to measure cortisol.
“The only previous study of hydrocortisone bioavailability reported absolute bioavailability to be 0.96 (CI 0.82 to 1.09) [3], but used a radioimmunoassay to measure cortisol.”
From Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone (2018) · cites this paper as [3]
The mean total plasma AUC, Cmax and median Tmax from this study were similar to those reported by Derendorf et al. following a 20 mg oral dose.
“The mean total plasma AUC of 1009 ± 383 ng/ml*h, Cmax of 319 ± 109 ng/ml and median Tmax of 1.125 h (0.5-1.5 h) from this study was similar to that reported by Derendorf et al of 1163 ng/ml*h, 305 ± 57 ng/ml, and 1.2 h (0.4-2 h) respectively, following a 20 mg oral dose.”
From Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone (2018) · cites this paper as [3]
An increase in the free fraction results in an increase in clearance with dose and therefore less than dose proportional increases in Cmax and bioavailability as measured by area under the curve (AUC).
“An increase in the free fraction results in an increase in clearance with dose and therefore less than dose proportional increases in Cmax and bioavailability as measured by area under the curve (AUC) [3].”
From Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone (2018) · cites this paper as [3]
The results using LC-MS/MS in this study confirm those previously published by Derendorf et al.
“The results using LC-MS/MS in our study confirm those previously published by Derendorf et al., who determined a bioavailability of 96 ± 20% using a radioimmunoassay [3].”
From Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone (2018) · cites this paper as [3]
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- Authors
- Derendorf, H., Möllmann, H., Barth, J., Möllmann, C., Tunn, S., & Krieg, M.
- Affiliations
- University of Florida (US)
- Corresponding author
- Derendorf, Hartmut
- Venue
- The Journal of Clinical Pharmacology
- Publisher
- Wiley
- Published
- 1991-05
- Volume
- 31
- Issue
- 5
- Pages
- 473-476
- ISSN
- 0021-9754 (ISSN-L)
- 0091-2700
- 1552-4604
- OpenAlex
- W2154889019
- Cited by
- 168
- References
- 1
- Citations by year
- 2026: 3 · 2025: 7 · 2024: 6 · 2023: 5 · 2022: 7 · 2021: 6 · 2020: 14 · 2019: 7 · 2018: 5 · 2017: 6 · 2016: 6 · 2015: 9 · 2014: 6 · 2013: 5 · 2012: 2
- FWCI
- 0.89
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Journal of Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Adrenal Hormones and Disorders
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal Regulation and Hypertension
- Keywords
- cortisol, pharmacokinetics, oral bioavailability, intravenous administration, dexamethasone suppression, body clearance, half-life, volume of distribution, absorption, saliva, free cortisol, glucocorticoids
- MeSH terms
- Administration, Oral, Adult, Biological Availability, Dexamethasone, Half-Life, Humans, Hydrocortisone, Injections, Intravenous, Male, Metabolic Clearance Rate, Saliva
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