Elevation of Plasma Levels of L-Dopa in Transdermal Administration of L-Dopa-Butylester in Rats

Autor:	Jun-ichi Sudo, Fumiji Miyasaka, Kimio Higashiyama, Takashi Meguro, Kozo Takayama, Hiroaki Iwase, Katsuhiko Kakuno
Rok vydání:	2002
Předmět:	Male Stereochemistry Skin Absorption Pharmaceutical Science In Vitro Techniques Administration Cutaneous Hydrogel Polyethylene Glycol Dimethacrylate Permeability Dosage form Levodopa chemistry.chemical_compound Drug Stability Pharmacokinetics Drug Discovery Blood plasma Animals Rats Wistar Transdermal Pharmacology Chromatography Ethanol Organic Chemistry Penetration (firestop) Permeation Rats nervous system diseases chemistry Methanol
Zdroj:	Drug Development and Industrial Pharmacy. 28:59-65
ISSN:	1520-5762 0363-9045
Popis:	To increase delivery of L-dopa in its transdermal absorption, a new lipophilic derivative of L-dopa, L-dopa-butylester, was synthesized. An in-vitro study employing two-chamber diffusion cells, in which the excised rat abdominal skin was mounted, revealed that, in the presence of L-menthol and ethanol, L-dopa-butylester penetrated in its original form more effectively than L-dopa. L-Dopa-butylester sheets were made by immersing wiper sheets in methanol containing the compound, and then evaporating the methanol. An extraction study of the compound from the sheets revealed that its stability was maintained for at least 12 weeks. In an in-vivo cutaneous absorption study, an L-dopa-butylester sheet was attached to the shaved rat abdominal skin. A hydrogel containing L-menthol and ethanol was spread on vinyl tape, and this sheet was placed over it. In plasma, the L-dopa level rose linearly between 30 and 180 min after the cutaneous application; L-dopa-butylester was not detected. The L-dopa level was higher than that in which L-dopa was applied. These findings indicated that the lipophilic nature of L-dopa-butylester further increased its penetration through the skin, and that L-dopa-butylester that was taken up into the general circulation system was rapidly converted to L-dopa by hydrolysis in the body.
Databáze:	OpenAIRE
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