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Transdermal iontophoretic delivery of apomorphine in patients improved by surfactant formulation pretreatment.
J Control Release. 2005 Jan 03; 101(1-3):199-208.JC

Abstract

The objective of the present study is to evaluate the efficacy and the safety of transdermal iontophoretic delivery of R-apomorphine, 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 microA/cm2. 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/cm2 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.

Authors+Show Affiliations

Department of Pharmaceutical Technology, Leiden Amsterdam Centre for Drug Research, University of Leiden, P.O. Box 9502, 2300 RA, Leiden, The Netherlands.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15588905

Citation

Li, G L., et al. "Transdermal Iontophoretic Delivery of Apomorphine in Patients Improved By Surfactant Formulation Pretreatment." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 101, no. 1-3, 2005, pp. 199-208.
Li GL, de Vries JJ, van Steeg TJ, et al. Transdermal iontophoretic delivery of apomorphine in patients improved by surfactant formulation pretreatment. J Control Release. 2005;101(1-3):199-208.
Li, G. L., de Vries, J. J., van Steeg, T. J., van den Bussche, H., Maas, H. J., Reeuwijk, H. J., Danhof, M., Bouwstra, J. A., & van Laar, T. (2005). Transdermal iontophoretic delivery of apomorphine in patients improved by surfactant formulation pretreatment. Journal of Controlled Release : Official Journal of the Controlled Release Society, 101(1-3), 199-208.
Li GL, et al. Transdermal Iontophoretic Delivery of Apomorphine in Patients Improved By Surfactant Formulation Pretreatment. J Control Release. 2005 Jan 3;101(1-3):199-208. PubMed PMID: 15588905.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transdermal iontophoretic delivery of apomorphine in patients improved by surfactant formulation pretreatment. AU - Li,G L, AU - de Vries,J J, AU - van Steeg,T J, AU - van den Bussche,H, AU - Maas,H J, AU - Reeuwijk,H J E M, AU - Danhof,M, AU - Bouwstra,J A, AU - van Laar,T, PY - 2004/04/23/received PY - 2004/09/16/accepted PY - 2004/12/14/pubmed PY - 2005/4/22/medline PY - 2004/12/14/entrez SP - 199 EP - 208 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 101 IS - 1-3 N2 - The objective of the present study is to evaluate the efficacy and the safety of transdermal iontophoretic delivery of R-apomorphine, 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 microA/cm2. 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/cm2 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. SN - 0168-3659 UR - https://www.unboundmedicine.com/medline/citation/15588905/Transdermal_iontophoretic_delivery_of_apomorphine_in_patients_improved_by_surfactant_formulation_pretreatment_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0168-3659(04)00444-4 DB - PRIME DP - Unbound Medicine ER -