Elsevier

Steroids

Volume 55, Issue 4, April 1990, Pages 170-176
Steroids

Stable isotope methodology in the pharmacokinetic studies of androgenic steroids in humans

https://doi.org/10.1016/0039-128X(90)90106-LGet rights and content

Abstract

The use of stable isotopically labeled steroids combined with gas chromatography/mass spectrometry (GC/MS) has found a broad application in pharmacologie studies. Initially, stable isotopically labeled steroids served as the ideal analytic internal standard for GC/MS analysis; however, their in vivo use has expanded and has proven to be a powerful pharmacokinetic tool. We have successfully used stable isotope methodology to study the pharmacokinetic/bioavailability of androgens. The primary advantage of the technique is that endogenous and exogenous steroids with the same basic structure can be differentiated by using stable isotopically labeled analogs. The method was used to examine the pharmacokinetic s of testosterone and testosterone propionate, and to clarify the influence of endogenous testosterone. Another advantage of the isotope methods is that steroidal drugs can be administered concomitantly in two formulations (e.g., solution and solid dosage). A single set of blood samples serves to describe the time course of the formulations being compared. This stable isotope coadministration technique was used to estimate the relative bioavailability of 17α-methyltestosterone. (Steroids 55:170–176, 1990)

References (35)

  • G Foss et al.

    Clinical administration of androgens

    Lancet

    (1939)
  • RZ Sokol et al.

    Comparison of the kinetics of injectable testosterone in eugonadal and hypogonadal men

    Fertil Steril

    (1982)
  • M Fujioka et al.

    Acute suppression of endogenous testosterone levels by exogenous testosterone in normal men

    Life Sci

    (1987)
  • D Alkalay et al.

    Spectrophoto-fluorometric determination of methyltestosterone in plasma or serum

    J Pharm Sci

    (1972)
  • Y Shinohara et al.

    Stable-isotope methodology in the bioavailability study of 17α-methyltestosterone using gas chromatography-mass spectrometry

    J Pharm Sci

    (1986)
  • Y Shinohara et al.

    Quantitative détermination of methyltestosterone and methyltestosterone-dj in serum by gas chromatography-mass spectrometry

    J Chromatogr

    (1985)
  • KM Pirke

    A comparison of three methods of measuring testosterone in plasma: competitive protein bincling, radioimmunoassay without chromatography and radioimmunoassay inclucling thin layer chromatography

    Acta Endocrinol (Copenh)

    (1973)
  • Cited by (0)

    View full text