Lexapro (TN)/Lu-26-054-0/(1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofurane-5-carbonitrile oxalate/Ethandisaure--(1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorphenyl)-1,3-dihydro-2-benzofuran-5-carbonitril(1:1)/ESCIFALOPRAMOXALATE/(S)-Citalopram Oxalate/(1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile ethanedioate/(1S)-1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile ethanedioate (1:1)/Escitalopram oxalate (USAN)/Lexapro/escitalopram oxalic acid/Escitalopram Oxalate/Cipralex/(1S)-1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile oxalate/5-Isobenzofurancarbonitrile, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-, (1S)-, ethanedioate (1:1)/(S)-Escitalopram Oxalate/Citalopram Impurity 2/Escitalopram (oxalate)
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The aim of the present study was to compare the bioavailability of escitalopram (CAS 128196-01-0) from two escitalopram oxalate (CAS 219861-08-2) tablets (escitalopram 10 mg tablet as test preparation and 10 mg tablet commercially available original tablet of the drug as reference preparation) in 20 Chinese healthy male volunteers, aged between 19 and 27. The study was conducted according to an open, randomized, single blind, 2-way crossover study design with a wash-out phase of 14 d. Blood samples for pharmacokinetic profiling were taken up to 156 h post-dose, and escitalopram plasma concentrations were determined with a validated liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) method. Maximum plasma concentrations (C(max)) of 9.85 +/- 1.79 ng/ml (test) and 9.92 +/- 2.14 ng/ml (reference) were achieved. Areas under the plasma concentration-time curve (AUC(0-infinity)) of 428.40 +/- 140.25 ng x h/ml (test) and 413.73 +/- 144.81 ng x h/ml (reference), AUC(0-t) of 401.33 +/- 120.61 ng x h/ml (test), 385.42 +/- 117.73 ng x h/ml (reference) were calculated. The median T(max) was 4.3 +/- 1.8h, 4.1 +/- 1.5 h for test and reference formulation, respectively. Plasma elimination half-lives (t 1/2) of 36.30 +/- 8.93 h (test), 36.70 +/- 9.99 h (reference) were determined. Both primary target parameters, AUC(0-infinity) and AUC(0-t) were tested parametrically by analysis of variance (ANOVA) and relative bioavailabilities were 105.1 +/- 10.8% for AUC(0-infinity), 104.9 +/- 11.1% for AUC(0-t). Bioequivalence between test and reference preparation was demonstrated for both parameters, AUC(0-infinity) and AUC(0-t). The 90% confidence intervals of the T/R-ratios of logarithmically transformed data were in the generally accepted range of 80%-125%. That means that the test formulation is bioequivalent to the reference formulation for escitalopram.
Pharmacokinetics and Bioequivalence Study of Escitalopram Oxalate Formulations After Single-Dose Administration in Healthy Chinese Male Volunteers
Jing Li 1, Yuan Tian, Zun-Jian Zhang, Na Wang, Xiaolei Ren, Yun Chen
Objective: A randomized, two-way crossover study was conducted in 24 fasting healthy male volunteers of Indian origin to compare the bioavailability of two brands of a fixed dose combination of escitalopram oxalate (CAS 219861-08-2) 10 mg and clonazepam (CAS 1622-61-3) 0.5 mg tablets, using Estomine-zee as test and a commercially available formulation as the reference product. The pharmacokinetics of escitalopram oxalate and clonazepam individually after oral administration of tablet formulation has been extensively evaluated in adult volunteers. However, no published data are available regarding the pharmacokinetics and bioavailability of this particular fixed dose combination.
Method: The trial was designed as a randomized, balanced, open-label, 2-period cross-over study. The drug was administered with 240 ml of water after a 10-h overnight fasting on two treatment days separated by a 21-day washout period. After dosing, serial blood samples were collected for a period of 96 h. Plasma harvested from blood was analyzed by simple rapid, selective and validated liquid chromatography-electrospray mass spectrometry (LC-ESI-MS/ MS) using diazepam (CAS 439-14-5) as an internal standard.
Results: The calibration curves were found to be linear in the range of 1-25 ng/ml and 1-10 ng/ml for escitalopram oxalate and clonazepam, respectively, with a mean correlation coefficient of more than 0.99. No statistically significant differences were obtained between the two products with respect to the mean concentration-time profiles or in the pharmacokinetic parameters, including the area under the serum concentration-time curve from the present study.
Conclusion: Based on the statistical inferences, it was concluded that the test product is bioequivalent to the reference product. Both preparations were well tolerated with no adverse reactions throughout the study.
Bioequivalence of Two Commercial Preparations of Escitalopram Oxalate/Clonazepam Using a Liquid Chromatography-Electrospray Mass Spectrometry Method
Sangita Agarwal 1, Kadajji Veeran Gowda, Perumal Senthamil Selvan, Tapas Kumar Chattaraj, Tapan Kumar Pal
Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is beneficial in animal models of Machado-Joseph disease. We identified citalopram, a selective serotonin reuptake inhibitor, in a small molecule screen of FDA-approved drugs that rescued neuronal dysfunction and reduced aggregation using a Caenorhabditis elegans model of mutant ataxin 3-induced neurotoxicity. MOD-5, the C. elegans orthologue of the serotonin transporter and cellular target of citalopram, and the serotonin receptors SER-1 and SER-4 were strong genetic modifiers of ataxin 3 neurotoxicity and necessary for therapeutic efficacy. Moreover, chronic treatment of CMVMJD135 mice with citalopram significantly reduced ataxin 3 neuronal inclusions and astrogliosis, rescued diminished body weight and strikingly ameliorated motor symptoms. These results suggest that small molecule modulation of serotonergic signalling represents a promising therapeutic target for Machado-Joseph disease.
spinocerebellar ataxia type 3, ataxin 3 aggregation, therapy, selective serotonin reuptake inhibitor, citalopram
Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease
Andreia Teixeira-Castro,1,2,3,4,* Ana Jalles,corresponding author1,2,* Sofia Esteves,corresponding author1,2,* Soosung Kang,3,5,6 Liliana da Silva Santos,1,2 Anabela Silva-Fernandes,1,2 Mario F. Neto,3,4 Renee M. Brielmann,3,4 Carlos Bessa,1,2 Sara Duarte-Silva,1,2 Adriana Miranda,1,2 Stephanie Oliveira,1,2 Andreia Neves-Carvalho,1,2 João Bessa,1,2 Teresa Summavielle,7 Richard B. Silverman,3,5,6 Pedro Oliveira,8 Richard I. Morimoto,3,4 and Patricia Macielcorresponding author1,2