Comparing different salt forms of rotigotine to improve transdermal iontophoretic delivery

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 74, Issue 2, 2010, Pages 304-310

  Ackaert, O W ^a   Eikelenboom, J ^a   Wolff, H M ^b   Bouwstra, J A ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b Schwarz Pharma AG   (Germany)

Author keywords

Iontophoresis; Modeling; Rotigotine; Salt form; Solubility; Transdermal

Indexed keywords

HYDROCHLORIC ACID; PHOSPHORIC ACID; ROTIGOTINE; SODIUM CHLORIDE;

ANALYTIC METHOD; ARTICLE; CELL TRANSPORT; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM COMPARISON; DRUG SOLUBILITY; ELECTROOSMOSIS; HUMAN; HUMAN CELL; HUMAN TISSUE; IONTOPHORESIS; PH; PHYSICAL CHEMISTRY; SIMULATION; STEADY STATE; STRATUM CORNEUM;

ADMINISTRATION, CUTANEOUS; CHEMISTRY, PHARMACEUTICAL; COMPUTER SIMULATION; DOPAMINE AGONISTS; EPIDERMIS; HUMANS; HYDROGEN-ION CONCENTRATION; IONTOPHORESIS; NONLINEAR DYNAMICS; SALTS; SOLUBILITY; TETRAHYDRONAPHTHALENES; THIOPHENES;

EID: 75449117461     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2009.11.016     Document Type: Article

References (22)

1. Honeywell-Nguyen P.L., Arenja S., and Bouwstra J.A. Skin penetration and mechanisms of action in the delivery of the D2-agonist rotigotine from surfactant-based elastic vesicle formulations. Pharmaceutical Research 20 10 (2003) 1619-1625
2. Nugroho A.K., Li G., Grossklaus A., Danhof M., and Bouwstra J.A. Transdermal iontophoresis of rotigotine: influence of concentration, temperature and current density in human skin in vitro. J Control Release 96 1 (2004) 159-167
3. Nugroho A.K., Li G.L., Danhof M., and Bouwstra J.A. Transdermal iontophoresis of rotigotine across human stratum corneum in vitro: influence of pH and NaCl concentration. Pharmaceutical Research 21 5 (2004) 844-850
4. Serajuddin A.T. Salt formation to improve drug solubility. Advanced Drug Delivery Reviews 59 7 (2007) 603-616
5. Fang J., Wang R., Huang Y., Wu P.C., and Tsai Y. Passive and iontophoretic delivery of three diclofenac salts across various skin types. Biological and Pharmaceutical Bulletin 23 11 (2000) 1357-1362
6. Fang J.Y., Wang R.J., Huang Y.B., Wu P.C., and Tsai Y.H. Influence of electrical and chemical factors on transdermal iontophoretic delivery of three diclofenac salts. Biological and Pharmaceutical Bulletin 24 4 (2001) 390-394
7. O. Ackaert, J. De Graan, R. Capancioni, D. Dijkstra, M. Danhof, J.A. Bouwstra, Transdermal iontophoretic delivery of a novel series of dopamine agonists in vitro: physicochemical considerations, submitted for publication.
8. Nugroho A.K., Li L., Dijkstra D., Wikstrom H., Danhof M., and Bouwstra J.A. Transdermal iontophoresis of the dopamine agonist 5-OH-DPAT in human skin in vitro. J Control Release 103 2 (2005) 393-403
9. Nugroho A.K., Romeijn S.G., Zwier R., de Vries J.B., Dijkstra D., Wikstrom H., Della-Pasqua O., Danhof M., and Bouwstra J.A. Pharmacokinetics and pharmacodynamics analysis of transdermal iontophoresis of 5-OH-DPAT in rats: in vitro-in vivo correlation. Journal of Pharmaceutical Sciences 95 7 (2006) 1570-1585
10. N. Holford, The Visual Predictive Check-Superiority to Standard Diagnostic (Rorschach) Plots. PAGE 14, Abstr 738 , (2005).
11. Berge S.M., Bighley L.D., and Monkhouse D.C. Pharmaceutical salts. Journal of Pharmaceutical Sciences 66 1 (1977) 1-19
12. Li S., Wong S., Sethia S., Almoazen H., Joshi Y.M., and Serajuddin A.T. Investigation of solubility and dissolution of a free base and two different salt forms as a function of pH. Pharmaceutical Research 22 4 (2005) 628-635
13. Higuchi T. Physical chemical analysis of percutaneous absorption process from creams and ointments. Journal of the Society of Cosmetic Chemists 11 (1960) 85-97
14. Jeans C.W., and Heard C.M. A therapeutic dose of primaquine can be delivered across excised human skin from simple transdermal patches. International Journal of Pharmaceutics 189 1 (1999) 1-6
15. L. Schwarz pharma, Neupro®, Mequon, WI, 2007.
16. Cawello W., Braun M., Horstmann R., Funaki T., and Tadayasu Y. Pharmacokinetics, safety and tolerability of rotigotine after transdermal patch administration in Japanese and Caucasian healthy subjects. Movement Disorders 21 S15 (2006) S547
17. Cawello W., Braun M., and Boekens H. (A) DME of the dopamine agonist rotigotine in man. Drug Metabolism and Disposition 37 10 (2009) 2055-2060
18. W. Cawello, M. Braun, R. Horstmann, Pharmacokinetics of transdermal rotigotine in subjects with impaired renal function, in: ACCP 34th Annual Meeting, Rockville, MD, 2005.
19. Cawello W., Elshoff J., Boekens H., Braun M., and Horstmann R. Characteristics of rotigotine elimination after patch removal. European Journal of Neurology 13 suppl. 2 (2006) 85
20. Cawello W., Wolff H.M., Meuling W.J., Horstmann R., and Braun M. Transdermal administration of radiolabelled [14C] rotigotine by a patch formulation: a mass balance trial. Clinical Pharmacokinetics 46 10 (2007) 851-857
21. EMEA. European Public Assessment Report (EPAR), Annex I: Summary of Product Characteristics for Neupro. , 2009.
22. W. Cawello, R. Horstmann, Pharmacokinetics of transdermal rotigotine in subjects with impaired renal function, in: ACCP 34th Annual Meeting, Rockville, MD, 2005.