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Pharmacokinetics and bioavailability of a new testosterone gel formulation in comparison to Testogel® in healthy men

Olsson, Håkan ; Sandström, Rikard ; Neijber, Anders ; Carrara, Dario and Grundemar, Lars LU (2014) In Clinical Pharmacology in Drug Development 3(5). p.358-364
Abstract

This randomized, open-label, multiple-dose three-way cross-over study compared the pharmacokinetics of a new testosterone gel formulation in two strengths, testosterone gel 1% and testosterone gel 2% (FE 999303), with Testogel® in 11 testosterone-suppressed healthy men. Subjects received one of six treatment sequences; 50 mg of testosterone was administered once daily for 7 consecutive days, with different treatments separated by washout-periods of 6-9 days. Testosterone gel 1% and testosterone gel 2% displayed greater relative bioavailability (2.6- and 1.6-fold, respectively) than Testogel on Day 1, which persisted, to a smaller extent, on Day 7. Initial absorption was highest and most rapid for testosterone gel 1% and 2%, showing... (More)

This randomized, open-label, multiple-dose three-way cross-over study compared the pharmacokinetics of a new testosterone gel formulation in two strengths, testosterone gel 1% and testosterone gel 2% (FE 999303), with Testogel® in 11 testosterone-suppressed healthy men. Subjects received one of six treatment sequences; 50 mg of testosterone was administered once daily for 7 consecutive days, with different treatments separated by washout-periods of 6-9 days. Testosterone gel 1% and testosterone gel 2% displayed greater relative bioavailability (2.6- and 1.6-fold, respectively) than Testogel on Day 1, which persisted, to a smaller extent, on Day 7. Initial absorption was highest and most rapid for testosterone gel 1% and 2%, showing apparent first-order absorption kinetics. Maximum serum concentrations (Cmax ) were 6.25 and 2.97 ng/mL, respectively, occurring ∼5-6 hours post-application on Day 1 versus Cmax of 1.71 ng/mL after ∼24 hours with Testogel, showing apparent zero-order absorption kinetics. Similar differences were observed on Day 7. All treatments appeared to reach approximately the same steady-state level within the first 24 hours. No application-site skin reactions occurred with any preparation. In conclusion, the new testosterone formulation showed higher bioavailability, and the ability to deliver more testosterone in a smaller volume.

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author
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organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Administration, Cutaneous, Adolescent, Adult, Area Under Curve, Biological Availability, Cross-Over Studies, Drug Administration Schedule, Drug Compounding, Gels, Germany, Half-Life, Healthy Volunteers, Hormone Replacement Therapy, Humans, Male, Metabolic Clearance Rate, Middle Aged, Skin Absorption, Testosterone/administration & dosage, Therapeutic Equivalency, Young Adult
in
Clinical Pharmacology in Drug Development
volume
3
issue
5
pages
358 - 364
publisher
Wiley-Blackwell
external identifiers
  • scopus:84908504368
  • pmid:27129008
ISSN
2160-763X
DOI
10.1002/cpdd.110
language
English
LU publication?
no
additional info
© 2014, The American College of Clinical Pharmacology.
id
513219c3-eb2f-4f07-88f5-d0cc3b123177
date added to LUP
2019-09-03 12:59:26
date last changed
2024-01-01 18:32:28
@article{513219c3-eb2f-4f07-88f5-d0cc3b123177,
  abstract     = {{<p>This randomized, open-label, multiple-dose three-way cross-over study compared the pharmacokinetics of a new testosterone gel formulation in two strengths, testosterone gel 1% and testosterone gel 2% (FE 999303), with Testogel® in 11 testosterone-suppressed healthy men. Subjects received one of six treatment sequences; 50 mg of testosterone was administered once daily for 7 consecutive days, with different treatments separated by washout-periods of 6-9 days. Testosterone gel 1% and testosterone gel 2% displayed greater relative bioavailability (2.6- and 1.6-fold, respectively) than Testogel on Day 1, which persisted, to a smaller extent, on Day 7. Initial absorption was highest and most rapid for testosterone gel 1% and 2%, showing apparent first-order absorption kinetics. Maximum serum concentrations (Cmax ) were 6.25 and 2.97 ng/mL, respectively, occurring ∼5-6 hours post-application on Day 1 versus Cmax of 1.71 ng/mL after ∼24 hours with Testogel, showing apparent zero-order absorption kinetics. Similar differences were observed on Day 7. All treatments appeared to reach approximately the same steady-state level within the first 24 hours. No application-site skin reactions occurred with any preparation. In conclusion, the new testosterone formulation showed higher bioavailability, and the ability to deliver more testosterone in a smaller volume.</p>}},
  author       = {{Olsson, Håkan and Sandström, Rikard and Neijber, Anders and Carrara, Dario and Grundemar, Lars}},
  issn         = {{2160-763X}},
  keywords     = {{Administration, Cutaneous; Adolescent; Adult; Area Under Curve; Biological Availability; Cross-Over Studies; Drug Administration Schedule; Drug Compounding; Gels; Germany; Half-Life; Healthy Volunteers; Hormone Replacement Therapy; Humans; Male; Metabolic Clearance Rate; Middle Aged; Skin Absorption; Testosterone/administration & dosage; Therapeutic Equivalency; Young Adult}},
  language     = {{eng}},
  number       = {{5}},
  pages        = {{358--364}},
  publisher    = {{Wiley-Blackwell}},
  series       = {{Clinical Pharmacology in Drug Development}},
  title        = {{Pharmacokinetics and bioavailability of a new testosterone gel formulation in comparison to Testogel® in healthy men}},
  url          = {{http://dx.doi.org/10.1002/cpdd.110}},
  doi          = {{10.1002/cpdd.110}},
  volume       = {{3}},
  year         = {{2014}},
}