Clinical Autonomic Research

, Volume 3, Issue 6, pp 369–372 | Cite as

Dose linearity of clonidine after transdermal application

  • G. Wallenstein
  • V. Gladigau
Research Paper


APrerequisite for optimal antihypertensive treatment is the possibility of individualized dosing. Therefore, three different dosages of the clonidine containing transdermal systems have been developed.

The aim of this analysis was to clarify whether a linear enlargement of system size and consequently, a linear increase of the dose coming into contact with the skin will result in a linear increase of bioavailable drug.

Data sets were obtained from a study performed in healthy volunteers, who wore these different TTS systems for 7 days each. Every patch was analysed after removal for residual content of clonidine. Plasma levels were measured. The areas under these plasma level curves were calculated by the trapezoidal rule. Apart from the dose of clonidine in the patch, the actual released amount of drug from the patch as well as the area under the plasma level curve were the parameters selected for the data analyses.

Plasma levels of clonidine are known to vary within individuals. However, we have shown that within the range 2.5–7.5 mg of clonidine, the area under the plasma level curve as well as the released amounts of drug increase linearly with the dose administered. The regression analysis of released amounts versus the area under the plasma level curve further supports linearity of dosage.

Key words

Transdermal application Antihypertensive treatment Catapres TTS Multiple comparisons Regression analysis Dose linearity 


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Copyright information

© Rapid Communications of Oxford Ltd. 1993

Authors and Affiliations

  • G. Wallenstein
    • 1
  • V. Gladigau
    • 1
  1. 1.Department of Research and Development, Boehringer Ingelheim KG, and Corporate Medical DepartmentBoehringer Ingelheim GmbHIngelheimGermany

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