Quantification of Galantamine in Human Plasma by Validated Liquid Chromatography-Tandem Mass Spectrometry using Glimepride as an Internal Standard: Application to Bioavailability Studies in 32 Healthy Korean Subjects

Park, Yoo-Sin; Kim, Shin-Hee; Kim, Sang-Yeon; Kim, Younhee; Yang, Seung Won; Shaw, Leslie M.; Kang, Ju‐Seop

doi:10.1093/chromsci/bms074

Cited by 6 publications

(6 citation statements)

References 31 publications

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“…The dose range used for GAL in the current work was selected based on several previous studies carried out by investigators on different organ systems (2930). We know that oral bioavailability of GAL is about 90-100% suggesting its remarkable systemic absorption after oral administration (31) indicating that beneficial effects of GAL are due to its systemic activity rather than its local effect within the colon lumen.…”

Section: Discussionmentioning

confidence: 99%

Ameliorative effect of galantamine on acetic acid-induced colitis in rats

2019

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Galantamine (GAL) is a drug for treating Alzheimer’s disease which has reasonable and no significant side effects. Studies have shown that GAL possesses antioxidant, anti-inflammatory, and cholinomimetic effects that might be beneficial for inflammatory bowel disease. Therefore, this study was aimed to investigate the anti-inflammatory effect of GAL on acetic acid-induced colitis in rats. GAL at 0.25, 1.25, 2.5 mg/kg/day was administrated orally (p.o.) to different groups of male Wistar rats 2 h before induction of ulcer with acetic acid 3% and continued for 5 consecutive days. Dicyclomine (DIC) was similarly used alone (5 mg/kg/day, p.o.) or together with GAL at doses already mentioned to delineate the impact of muscarinic pathway in probable beneficial effects of GAL on colitis. Control and reference groups received distilled water (5 mL/kg, p.o.), prednisolone (4 mg/kg/day, p.o.), or mesalazine (100 mg/kg/day, p.o.) respectively. At day 6, tissue injuries were assessed for macroscopic, histopathologic, and biochemical indices of myeloperoxidase and MPO activity. Results showed that GAL at 3 applied doses, alone or in combination with DIC diminished ulcer index, total colitis index, and MPO activity as important biomarkers of colitis. DIC alone was not effective on most parameters and its concurrent administration with GAL couldn’t reverse its antiulcerative effects. Prednisolone and mesalazine were both effective in this relation. The current research indicated that GAL had anti-inflammatory and antiulcerative activities independent of its muscarinic effects. Thus the antioxidant and anti-inflammatory effects may account for its anti-inflammatory and anti-ulcerative properties. Nevertheless, further detailed studies are warranted for exact elucidation of GAL mechanism on inflammation and colitis.

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Section: Discussionmentioning

confidence: 99%

Ameliorative effect of galantamine on acetic acid-induced colitis in rats

2019

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“…Additionally, this method had an analysis time of 15 min, which was still relatively long for high-throughput requirements. It is widely recognized that current HPLC-MS/MS (Nirogi, Kandikere, Mudigonda, & Maurya, 2007;Park et al, 2012;Steiner, 2012;Suresh, Mullangi, & Sukumaran, 2014;Verhaeghe, Diels, de Vries, De Meulder, & de Jong, 2003;Zhou, Liu, Huang, & Liu, 2014) and UPLC-MS/MS (Noetzli, Ansermot, Dobrinas, & Eap, 2012) methods allow for shorter run times and small sample size, but the significantly higher instrument cost limits their application. In this study, we first develop and fully validate an UPLC-MS method which provides efficient chromatographic resolution, acceptable method selectivity and high-throughput capability with lower instrument cost.…”

Section: Cummingsmentioning

confidence: 99%

“…The bioavailability and pharmacokinetic profiles of these two galantamine formulations were evaluated with a hairless guinea pig model and a sensitive and high-throughput method is required to complete the study. It is widely recognized that current HPLC-MS/MS (Nirogi, Kandikere, Mudigonda, & Maurya, 2007;Park et al, 2012;Steiner, 2012;Suresh, Mullangi, & Sukumaran, 2014;Verhaeghe, Diels, de Vries, De Meulder, & de Jong, 2003;Zhou, Liu, Huang, & Liu, 2014) and UPLC-MS/MS (Noetzli, Ansermot, Dobrinas, & Eap, 2012) methods allow for shorter run times and small sample size, but the significantly higher instrument cost limits their application. For more complex biological matrices, two HPLC-UV methods (Claessens, van Thiel, Westra, & Soeterboek, 1983;Tencheva, Yamboliev, & Zhivkova, 1987) were first reported in the 1980s as well as two HPLC-fluorescence methods (Malakova et al, 2007;Zhang et al, 2007).…”

mentioning

confidence: 99%

Development and validation of a UPLC–MS method for the determination of galantamine in guinea pig plasma and its application to a pre‐clinical bioavailability study of novel galantamine formulations

Wang

Pavurala

et al. 2018

Biomedical Chromatography

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To evaluate the bioavailability and pharmacokinetic profiles of two novel galantamine formulations as medical countermeasure products, an ultra-performance liquid chromatography-single quadrupole mass spectrometry (UPLC-MS) method was developed and validated for quantifying galantamine in guinea pig plasma using solid-phase extraction with a mixed mode strong cation exchange reversed-phase cartridge. Chromatographic separation was achieved on a Waters Acquity UPLC BEH C column maintained at 40°C. The mobile phases were solution A, acetonitrile-water, 5:95 (v/v) and solution B, acetonitrile-water 90:10 (v/v), both containing 2 mM ammonium formate and 0.2% formic acid. The mobile phase was delivered utilizing a 3 min gradient program start with 95%A-5%B at a flow rate of 0.6 mL/min. The analyte and internal standard, galantamine-d3, were detected by selected ion monitoring mode on a Waters 3100 single quadrupole mass spectrometer with positive electrospray ionization. The method was validated according to the US Food and Drug Administration bioanalytical guidance. The method was selective and was linear over the analytical range of 2-2000 ng/mL. Accuracy and precision were acceptable with intra- and inter-day accuracies between 96.8 and 101% and precisions (RSD) <4.88%. The method was successfully implemented to measure galantamine plasma levels in a series of pre-clinical bioavailability studies for the evaluation of novel galantamine formulations.

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“…Blood Samples (9 mL) were collected through a catheter with heparin-containing tubes from a suitable antecubital vein before and at 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, and 8 h after dose. The samples were centrifuged at 3000 rpm for 10 min at room temperature and the plasma was stored at −70˚C until analyzed [34] [35] [36] [37] [38]. The C max and T max were determined from each subject's plasma level of cephradine versus time plots.…”

Section: Bioequivalence and Pharmacokinetic Test In Normal Subjectsmentioning

confidence: 99%

Clinical Pharmacokinetic and Bioequivalence Studies of Two Brands of Cephradine in Healthy Korean Using HPLC Method

Kim¹,

Kim²,

Kim³

et al. 2018

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The goal of our research was to compare the pharmacokinetics and evaluate the bioequivalence of two brands of cephradine 500 mg capsules in 24 normal Korean volunteers. The plasma samples were acquired at 13 time points for 8 h after administration. The concentrations of cephradine in human plasma were measured by a high-performance liquid chromatography (HPLC). Isocratic mobile phase which consisted of acetonitrile, methanol, and 20 mM potassium phosphate (15/5/80, v/v/v, pH 3.48) was used to separate the analytical column cosmosil cholester (250 × 4.6 mm, 3 µm). Analytes were detected in ultraviolet (260 nm). The novel analytical method was described as simple sample preparation, a short retention time (less than 6 min) and making it suitable for use in clinical trials. Pharmacokinetic parameters, such as ) were determined for the reference and test drugs in plasma. Pharmacokinetic parameters with a 90% confidence interval were 87% -95% for AUC 0-t and 91% -115% for C max . They were satisfied within the bioequivalence range 80% -125% of the KFDA guidelines. Therefore, our HPLC method was well applied in a bioequivalence and pharmacokinetic study of two formulations in normal subjects.

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Quantification of Galantamine in Human Plasma by Validated Liquid Chromatography-Tandem Mass Spectrometry using Glimepride as an Internal Standard: Application to Bioavailability Studies in 32 Healthy Korean Subjects

Cited by 6 publications

References 31 publications

Ameliorative effect of galantamine on acetic acid-induced colitis in rats

Ameliorative effect of galantamine on acetic acid-induced colitis in rats

Development and validation of a UPLC–MS method for the determination of galantamine in guinea pig plasma and its application to a pre‐clinical bioavailability study of novel galantamine formulations

Clinical Pharmacokinetic and Bioequivalence Studies of Two Brands of Cephradine in Healthy Korean Using HPLC Method

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