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1.
Artigo em Inglês | MEDLINE | ID: mdl-38805871

RESUMO

Rivastigmine hydrogen tartrate (RHT), a reversible cholinesterase inhibitor, is considered as the first-line therapy for mild to moderate Alzheimer's disease. Asiaticoside (AS), a pentacyclic triterpenoid saponin, is well known as cognitive enhancer due to its antioxidant effect. Based on the hypothesis of their synergistic therapeutic potential, RHT and AS were co-encapsulated in niosomal formulation. A simple, precise, and accurate high-performance liquid chromatography method was developed for simultaneous quantitative analysis. The chromatographic parameters were optimized by Box-Behnken experimental design. The separation was performed on a reversed-phase Phenomenex C18 (150 mm × 4.6 mm, 5 µm) column at 30 °C under the UV detection of 210 nm. The optimized mobile phase consisted of a mixture of 20 mM potassium dihydrogen phosphate buffer (pH 2.6) and acetonitrile (72:28 % v/v) under the isocratic mode at the flow rate of 0.9 mL/min. The developed method was fully validated under the ICH guidelines and could be successfully applied for simultaneous quantitative analysis of RHT and AS in niosomal formulation.


Assuntos
Limite de Detecção , Lipossomos , Rivastigmina , Triterpenos , Cromatografia Líquida de Alta Pressão/métodos , Triterpenos/análise , Triterpenos/química , Lipossomos/química , Reprodutibilidade dos Testes , Rivastigmina/análise , Rivastigmina/química , Modelos Lineares
2.
Chem Commun (Camb) ; 57(71): 8909-8912, 2021 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-35225993

RESUMO

In this work, a pendant droplet-based sensor is developed for the rapid and label-free detection of acetylcholinesterase (AChE) and its inhibitors. The detection limit of AChE reaches 0.17 mU mL-1. The pIC50 values of AChE inhibitors such as neostigmine, rivastigmine and galantamine are determined to be 0.45 µM, 0.64 µM and 4.93 µM, respectively.


Assuntos
Acetilcolinesterase/análise , Inibidores da Colinesterase/análise , Galantamina/análise , Limite de Detecção , Neostigmina/análise , Rivastigmina/análise
3.
Eur J Mass Spectrom (Chichester) ; 26(6): 388-399, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33153323

RESUMO

This study has been carried out to obtain the thermochemical parameters of drugs used for Alzheimer's disease. The measurement of gas-phase basicity (GB) and proton affinity (PA) values of four important and commercially available drugs for Alzheimer's disease namely, rivastigmine, galantamine, memantine, and tacrine, is attempted for the first time. This study also includes the measurement of GB and PA values for the proposed drug curcumin, a natural product. We calculated the GB and PA values for all these drugs by applying electrospray ionization tandem mass spectrometry (ESI-MS/MS) with the extended kinetic method. Since, all these drugs possessing amino groups (basic nature), the PA values for all these drugs are high i.e., the PA values range from 923.6 to 979.7 kJ/mol and the GB values range from 886.2 to 943.3 kJ/mol. The GB and PA values obtained from the mass spectrometric experiments are well supported with the theoretical calculations. A high-level theoretical B3LYP/6-311 + G(d,p) method is used for the PA and GB calculation and the deviations are in the acceptable range.


Assuntos
Fármacos Neuroprotetores/análise , Fármacos Neuroprotetores/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Doença de Alzheimer , Curcumina/análise , Curcumina/química , Galantamina/análise , Galantamina/química , Humanos , Prótons , Rivastigmina/análise , Rivastigmina/química , Espectrometria de Massas em Tandem
4.
J Sep Sci ; 41(10): 2214-2220, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29427354

RESUMO

In this work, a simple method, namely, tandem dispersive liquid-liquid microextraction, with a high sample clean-up is applied for the rapid determination of the antidementia drugs rivastigmine and donepezil in wastewater and human plasma samples. This method, which is based on two consecutive dispersive microextractions, is performed in 7 min. In the method, using a fast back-extraction step, the applicability of the dispersive microextraction methods in complicated matrixes is conveniently improved. This step can be performed in less than 2 min, and very simple tools are required for this purpose. To achieve the best extraction efficiency, optimization of the variables affecting the method was carried out. Under the optimized experimental conditions, the relative standard deviations for the method were in the range of 6.9-8.7%. The calibration curves were obtained in the range of 2-1100 ng/mL with good correlation coefficients, higher than 0.995, and the limits of detection ranged between 0.5 and 1.0 ng/mL.


Assuntos
Inibidores da Colinesterase/análise , Indanos/análise , Fármacos Neuroprotetores/análise , Piperidinas/análise , Rivastigmina/análise , Águas Residuárias/química , Algoritmos , Calibragem , Inibidores da Colinesterase/sangue , Cromatografia Líquida de Alta Pressão , Donepezila , Humanos , Concentração de Íons de Hidrogênio , Indanos/sangue , Limite de Detecção , Modelos Lineares , Microextração em Fase Líquida , Fármacos Neuroprotetores/sangue , Piperidinas/sangue , Plasma/química , Reprodutibilidade dos Testes , Rivastigmina/sangue , Sais , Solventes
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