• Home
  • Search Results
  • Pharmacokinetic evaluation of formulated levodopa methyl ester nasal delivery systems.

Pharmacokinetic evaluation of formulated levodopa methyl ester nasal delivery systems.

European journal of drug metabolism and pharmacokinetics (2013-12-24)
Yeon Hong Lee, Kyung Hee Kim, In Kyung Yoon, Kyung Eun Lee, In Koo Chun, Jeong Yeon Rhie, Hye Sun Gwak
ABSTRACT

The objective of this study was to investigate the pharmacokinetic characteristics of levodopa (L-dopa) from nasal powder formulations using highly water-soluble levodopa methyl ester hydrochloride (LDME). In vivo pharmacokinetic studies were carried out with formulated LDME nasal powders. After oral and intravenous administration of L-dopa and carbidopa and intranasal administration LDME to the rat, L-dopa concentrations were determined in plasma and the brain using high-performance liquid chromatography. The absolute bioavailabilities of nasal preparations with and without Carbopol were 82.4 and 66.7 %, respectively, which were much higher than that of oral delivery (16.2 %). The drug-targeting efficiencies [area under the curve (AUC) in brain/AUC in plasma] of L-dopa in the nasal formulations (0.98-1.08) were much higher than that of oral preparation (0.69). These results suggest that LDME nasal powder formulations would be useful delivery systems of L-dopa to the brain.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Methanol, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Methanol, anhydrous, 99.8%
Sigma-Aldrich
Methanol, HPLC Plus, ≥99.9%
Sigma-Aldrich
Methanol, HPLC Plus, ≥99.9%, poly-coated bottles
Sigma-Aldrich
Methanol, suitable for HPLC, gradient grade, ≥99.9%
Sigma-Aldrich
Methanol, suitable for HPLC, gradient grade, suitable as ACS-grade LC reagent, ≥99.9%
Supelco
Methanol, analytical standard
Sigma-Aldrich
Methanol, ACS reagent, ≥99.8%
Sigma-Aldrich
Methanol, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.8% (GC)
Sigma-Aldrich
3,4-Dihydroxy-L-phenylalanine, ≥98% (TLC)
USP
Methyl alcohol, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
L-Lysine monohydrochloride, reagent grade, ≥98% (HPLC)
Sigma-Aldrich
Methanol, Laboratory Reagent, ≥99.6%
Supelco
Methanol, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
L-Lysine monohydrochloride, from non-animal source, meets EP, JP, USP testing specifications, suitable for cell culture, 98.5-101.0%
Sigma-Aldrich
Methanol, BioReagent, ≥99.93%
Sigma-Aldrich
Methanol, ACS spectrophotometric grade, ≥99.9%
Supelco
Levodopa, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Methanol, ACS reagent, ≥99.8%
Sigma-Aldrich
Methanol, puriss., meets analytical specification of Ph Eur, ≥99.7% (GC)
Supelco
L-Lysine monohydrochloride, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Xylazine, ≥99%
Sigma-Aldrich
L-Lysine monohydrochloride, BioUltra, ≥99.5% (AT)
Sigma-Aldrich
L-3,4-Dihydroxyphenylalanine methyl ester hydrochloride, solid
Lysine hydrochloride, European Pharmacopoeia (EP) Reference Standard
Supelco
L-Lysine hydrochloride solution, 100 mM amino acid in 0.1 M HCl, analytical standard
USP
Levodopa, United States Pharmacopeia (USP) Reference Standard
Supelco
L-Lysine monohydrochloride, certified reference material, TraceCERT®
Supelco
Methanol solution, contains 0.10 % (v/v) formic acid, UHPLC, suitable for mass spectrometry (MS), ≥99.5%
Sigma-Aldrich
Methanol, ACS reagent, ≥99.8%