Systemic delivery of sympathomimetic amines by transdermal iontophoresis

Robert William Caldwell, M. Antonia Chryssanthis, Vanessa O. Davis

Research output: Contribution to journalArticle

Abstract

Certain sympathomimetic amines may be useful in the treatment or diagnosis of cardiovascular disease. However, obtaining sufficient blood levels of these drugs when given orally is difficult because of gastrointestinal destruction and their is a danger associated with intravenous administration. These problems have prompted the investigation of iontophoretic delivery of a novel sympathomimetic amine, KM-13, across the skin of anesthetized dogs. Dogs were monitored to determine cardiac rate or cardiac contractility. The KM-13 was dissolved in distilled H2O to a concentration of 50 mM and placed in a 15 cm2 matrix pad beneath the positive electrode of a DC constant current device. Delivered currents of 0.5-4.0 mA caused graded increases in cardiac contraction which reached a plateau within 20-30 min. In other dogs, delivery of 1 mA current for 15 min caused an increase in heart rate which peaked at about 24 min and decayed with a T 1 2 of approx. 95 min. Prior treatment of skin beneath the positive electrode pad with tolazoline (an a-adrenergic blocker) caused a more rapid response (peak with 15 min) and decay (T 1 2 of approx. 51 min) to KM-13. This study demonstrates that iontophoretic delivery of a sympathomimetic amine is feasible. Prolonged latency of onset and decay may cause problems in some uses. Prior use of vasodilators before applications of sympathomimetic amines can accelerate onset and decay.

Original languageEnglish (US)
Pages (from-to)181-185
Number of pages5
JournalInternational Journal of Pharmaceutics
Volume123
Issue number2
DOIs
StatePublished - Sep 12 1995

Fingerprint

Iontophoresis
Sympathomimetics
Dogs
Electrodes
Tolazoline
Skin
Adrenergic Antagonists
Vasodilator Agents
Intravenous Administration
Cardiovascular Diseases
Heart Rate
Equipment and Supplies
Therapeutics
Pharmaceutical Preparations
4-(2-((3-(3-benzenecarboxamide)-1-methylpropyl)amino)ethyl)-1,2-benzenediol

Keywords

  • Cardiotonic action
  • Sympathomimetic amine
  • Transdermal iontophoresis

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Systemic delivery of sympathomimetic amines by transdermal iontophoresis. / Caldwell, Robert William; Chryssanthis, M. Antonia; Davis, Vanessa O.

In: International Journal of Pharmaceutics, Vol. 123, No. 2, 12.09.1995, p. 181-185.

Research output: Contribution to journalArticle

Caldwell, Robert William ; Chryssanthis, M. Antonia ; Davis, Vanessa O. / Systemic delivery of sympathomimetic amines by transdermal iontophoresis. In: International Journal of Pharmaceutics. 1995 ; Vol. 123, No. 2. pp. 181-185.
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