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Transdermal iontophoretic delivery of apomorphine in patients improved by surfactant formulation pretreatment
- Source :
- Journal of Controlled Release, 101(1-3), 199-208. Elsevier Bedrijfsinformatie b.v.
- Publication Year :
- 2005
- Publisher :
- Elsevier Bedrijfsinformatie b.v., 2005.
-
Abstract
- The objective of the present study is to evaluate the efficacy and the safety of transdermal iontophoretic delivery of Rapomorphine, a potent dopamine agonist, in combination with surfactant pretreatment in patients with advanced Parkinson's disease. Iontophoresis patches were applied in 16 patients for 3.5 h, with 0.5 h of passive delivery followed by 3 h Of Current application at a current density of 250 mu A/cm(2). Eight of these patients were treated with a surfactant formulation prior to iontophoresis. The pharmacokinetics, pharmacodynamic effects, systemic and local side effects of R-apomorphine were assessed. The plasma concentration vs. time profiles upon iontophoresis of R-apomorphine were described successfully by a novel pharmacokinetic model. The model suggests that only 1.9% of the dose that has been released from the patch accumulated in the skin. The patients treated with the surfactant formulations showed a statistically significant increase of bioavailability (from 10.6 +/- 0.8% to 13.2 +/- 1.4%) and of the steady state input rate (from 75.3 +/- 6.6 to 98.3 +/- 12.1 nmol/cm(2) h) compared to the control patients (iontophoresis without absorption enhancers). In five out of eight patients in the study group and in three out of eight patients in the control group, clinical improvement was observed. (c) 2004 Elsevier B.V. All rights reserved.
- Subjects :
- Male
PHARMACOKINETICS
Apomorphine
Parkinson's disease
Pharmaceutical Science
Absorption (skin)
Pharmacology
Administration, Cutaneous
Dopamine agonist
Surface-Active Agents
ENHANCEMENT
Pharmacokinetics
Pulmonary surfactant
PARKINSONS-DISEASE
ELECTROTRANSPORT SYSTEM
absorption enhancer
Humans
Medicine
Aged
Transdermal
AGENT
Iontophoresis
business.industry
R-APOMORPHINE
STRATUM-CORNEUM
Parkinson Disease
IN-VITRO
Middle Aged
TRANSPORT
Bioavailability
Anesthesia
Pharmacodynamics
Female
business
transdermal iontophoresis
SKIN
medicine.drug
Subjects
Details
- Language :
- English
- ISSN :
- 18734995 and 01683659
- Volume :
- 101
- Issue :
- 1-3
- Database :
- OpenAIRE
- Journal :
- Journal of Controlled Release
- Accession number :
- edsair.doi.dedup.....02b40f18f4bbdcbf4537346b3b64dfa8