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Dihydroergotoxine mesylate for the treatment of sialorrhea in Parkinson's disease.
Parkinsonism Relat Disord
January 2019
Department of Neurology, Nanjing First Hospital, Nanjing Medical University, Nanjing, Jiangsu 210006, China. Electronic address:
Background: Many patients with Parkinson's disease (PD) suffer from sialorrhea. Sialorrhea is often treated with anticholinergics and botulinum toxin, but some adverse effects have limited the use of these treatments. Dihydroergotoxine mesylate is an α-adrenergic blocking agents as well as some affinities to the dopaminergic and serotonin (5-HT) receptors.
View Article and Find Full Text PDFPreparation of ergoloid mesylate submicron emulsions for enhancing nasal absorption and reducing nasal ciliotoxicity.
Int J Pharm
June 2009
Department of Pharmaceutics, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
The aim of this investigation was to prepare ergoloid mesylate submicron emulsions (EMSEs) for enhancing nasal absorption of drug and reducing nasal ciliotoxicity. Following intranasal administrations of EMSE and ergoloid mesylate solution (EMS) and intravenous administration of EMS to rats separately at the dose of 2 mg kg(-1), the levels of EM in blood and the cerebrospinal fluid (CSF) were evaluated by microdialysis method. The nasal ciliotoxicity was evaluated by using in situ toad palate model.
View Article and Find Full Text PDFEvaluation of brain-targeting for the nasal delivery of ergoloid mesylate by the microdialysis method in rats.
Eur J Pharm Biopharm
March 2008
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, China.
The aim of this study was to quantify the nasal delivery of ergoloid mesylate (EM) to the brain by comparing cerebrospinal fluid (CSF) and plasma EM levels after nasal administration at a dose of 4 mg/kg with those after intravenous administration. Following nasal delivery, EM reached a Cmax value (mean+/-SD) in plasma of 348.41+/-19.
View Article and Find Full Text PDFIdentification and human pharmacokinetics of dihydroergotoxine metabolites in man: preliminary results.
Biopharm Drug Dispos
January 2008
Department of Pharmacology, Faculty of Medical Sciences, UNICAMP, PO BOX 6111, 13084-971, Campinas - SP, Brazil.
Dihydroergotoxine is a mixture of semi-synthetic ergot alkaloids mainly used for age-related cognitive impairment. In this study, dihydroergotoxine (30 microM) was added to incubates of rat and bovine liver microsomes, and the resulting major metabolites were identified as hydroxy-dihydroergocornine, hydroxy-dihydroergocryptine and hydroxy-dihydroergocristine on the basis of molecular mass measurements, determined with a time-of-flight mass spectrometer. The relevance of these to humans was then investigated by simultaneously monitoring dihydroergotoxine and its hydroxy-metabolites in human plasma by LC-MS/MS after oral dosing of dihydroergotoxine mesylate (27 mg) to a healthy volunteer (male, age 45, height 1.
View Article and Find Full Text PDFThe effects of ergoloid mesylates and ginkgo biloba on the pharmacokinetics of ticlopidine.
J Clin Pharmacol
June 2006
Department of Neurology, College of Medicine, National Cheng Kung University, Tainan 70101, Taiwan.
Ticlopidine is sometimes coadministered with ergoloid mesylates or ginkgo biloba in clinical situations. Our objective was to examine the effect of ergoloid mesylates and ginkgo biloba on ticlopidine pharmacokinetics. Ticlopidine, ergoloid mesylates, and ginkgo biloba significantly inhibited the organic anion transporting polypeptide (OATP-B)-mediated uptake of [(3)H]-estrone-3-sulfate in a concentration-dependent manner.
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