Escitalopram Research Articles

Coffee Biomass-Based Carbon Material for the Electrochemical Determination of Antidepressant in Synthetic Urine

Escitalopram (ESC) is commonly prescribed as an antidepressant to enhance serotonin levels in the brain, effectively addressing conditions such as depression and anxiety. The COVID-19 pandemic, along with ongoing mental health crises, has exacerbated the prevalence of these disorders, largely due to factors such as social isolation, fear of the virus, and financial difficulties. This study presents the enhancement of a glassy carbon electrode (GC) through the incorporation of hydrochar (HDC) derived from spent coffee grounds and copper nanoparticles (CuNPs) for the detection of ESC in synthetic urine. Characterization of the nanocomposite was conducted using scanning electron microscopy (SEM), energy-dispersive spectroscopy (EDS), and cyclic voltammetry (CV). The analytical parameters were systematically optimized, and a sensing platform was utilized for the quantification of ESC via square-wave voltammetry (SWV). The established linear range was found to be between 1.0 µmol L−1 and 50.0 µmol L−1, with a limit of detection (LOD) of 0.23 µmol L−1. Finally, an electrochemical sensor was employed to measure ESC levels in synthetic urine, yielding recovery rates ranging from 91.7% to 94.3%. Consequently, the HDC-CuNPs composite emerged as a promising, sustainable, and cost-effective alternative for electroanalytical applications.

Drug-Drug Interactions of Selective Serotonin Reuptake Inhibitors: A Pharmacovigilance Study on Real-World Evidence from the EudraVigilance Database.

As the most common psychiatric symptom, depression represents a subject of high interest for the medical community. Background/Objectives: International guidelines consider selective serotonin reuptake inhibitors (SSRIs) the first-line treatment of depression. Although having better efficacy and tolerability in comparison to tricyclic antidepressants or monoamine oxidase inhibitors, the diversity and potential severity of adverse effects and interactions manifested by SSRIs, combined with the frequency of prescriptions, lead to the necessity of evaluating real-world data. The aim of this study was to identify and evaluate the drug interactions reported in EudraVigilance (EV) for the six SSRIs representatives that are authorized in Europe: fluoxetine (FXT), fluvoxamine (FVM), citalopram (CIT), escitalopram (ESC), paroxetine (PAR) and sertraline (SER). The entire class of SSRIs was examined as a comparator to identify whether one of the representatives was more prone to reporting. Methods: Descriptive analysis and disproportionality analysis were conducted on data extracted from the EV database. Results: A total of 326,450 adverse reactions (ADRs) were reported for the SSRIs group. Approximately a quarter of these (n = 83,201; 25.46%) were reported for SER and 22.37% (n = 73,131) for PAR. Of the total ADRs reported, 2.12% (n = 6925) represent preferred terms related to drug-drug interactions (DDIs): SER (n = 1474; 22.37%), CIT (n = 1272, 19.86), and FXT (n = 1309, 19.83%). Specific ADRs related to inhibitory activity represent 0.98%, and for potentiating activity, 1.89%. Conclusions: Although representing a small value of the total ADRs, DDIs may be related to severe outcomes. Awareness should be raised for this category of ADRs that can be reduced by the joined efforts of physicians and pharmacists.

Shugan Jieyu capsule effects on peripheral blood micro-124, micro-132, and brain-derived neurotrophic factor in patients with mild to moderate depression

BACKGROUND To assess the effectiveness of Shugan Jieyu capsules on peripheral blood miR-124, miR-132, and brain-derived neurotrophic factor (BDNF) levels in patients with mild to moderate depression following coronary artery intervention [percutaneous coronary intervention (PCI)] for coronary heart disease. AIM To evaluate the therapeutic efficacy of Shugan Jieyu capsules and their effects on the peripheral blood levels of miR-124, miR-132, and BDNF in patients with mild to moderate depression following PCI for coronary heart disease. METHODS Patients with mild-to-moderate depression of the liver-qi stagnation type after PCI for coronary heart disease at the 305th Hospital of the People’s Liberation Army were enrolled from June 2022 to November 2023 and randomly assigned to two groups: Experimental (treated with Shugan Jieyu capsules) and control (treated with escitalopram oxalate tablets). This study compared the antidepressant effects of these treatments using 17-item Hamilton Rating Scale for Depression (HAMD-17) scores, metabolic equivalents, low-density lipoprotein cholesterol, BDNF, high-sensitivity C-reactive protein levels, miR-124 and miR-132 levels, distribution of immune-related lymphocyte subsets, and traditional Chinese medicine syndrome scores before and after 6 weeks of treatment. RESULTS No significant difference was observed in any index between the two groups before treatment (P > 0.05). After treatment, the total efficacy rates were 93.33% and 90.00% in the experimental and control groups, respectively. Experimental group had significantly lower scores for the main and secondary syndromes compared to the control group (P < 0.05). No significant difference was observed in the metabolic equivalents between the two groups before and after treatment (P > 0.05). The levels of low-density lipoprotein cholesterol, high-sensitivity C-reactive protein, and miR-132 were significantly lower, whereas those of miR-124, BDNF, CD3+T lymphocytes, CD3+CD4+T helper lymphocytes, and CD3+CD4+/CD3+CD8+ cells were significantly higher in the experimental group compared to the control group (P < 0.05). The incidence of adverse reactions during experimental group was significantly lower than that in control group (P < 0.05). CONCLUSION Shugan Jieyu capsules have good efficacy in patients with mild-to-moderate depression after PCI, and its mechanism may contribute to the regulation of miR-124, miR-132, BDNF levels, and lymphoid immune cells.

Observation on the Clinical Efficacy of Danzhi Xiaoyao San Combined with Traditional Chinese Medicine Qigong in Treating Depression Caused by Liver Stagnation and Qi Stagnation

This study focuses on evaluating the therapeutic effectiveness of the traditional Chinese medical formula Danzhi Xiaoyao San in conjunction with Qigong practices, specifically for depression linked to liver and qi stagnation. In this approach, a group of 30 individuals suffering from this type of depression were split into two groups: a control group, where 15 patients received 10 mg of Escitalopram Oxalate per dose, and a treatment group, where 15 patients were administered Danzhi Xiaoyao Powder twice daily and engaged in traditional Chinese medicine Qigong exercises. Each treatment cycle lasted 7 days, with participants completing four such cycles in total.

Preparation, characterization, and evaluation of an acetylene black polyurethane composite electrode modified with copper nanoparticles for the determination of escitalopram

Escitalopram (ESC) is a widely prescribed antidepressive drug worldwide and must be monitored in biological fluids and environmental samples. Thus the preparation of an acetylene black-polyurethane composite electrode modified with copper metallic nanoparticles by electrodeposition intended for the determination of ESC in synthetic urine and mineral water samples is presented. The surface was further electrochemically pretreated in 0.50 mol L−1 NaOH in order to obtain a stable mixture of Cu (II) oxides on top of the Cu° nanoparticles. After preconditioning in 0.10 mol L−1 phosphate buffer pH = 7.0, the modified electrode was used in the determination of ESC in the proposed matrixes using CV and DPV, after optimizing experimental parameters. The interaction of the analyte with copper (II) ions promoted a decrease of the Cu(II) reduction peak which was proportional to the ESC concentration in the 0.020–0.10 µmol L−1 (LOD = (5 ± 1) nmol L−1) and 0.040–0.20 µmol L−1 (LOD = (5.1 ± 0.9) nmol L−1) in cyclic voltammetry (CV) and differential pulse voltammetry (DPV) respectively. Interferences from ascorbic acid, uric acid, dopamine and creatinine were evaluated, however the last one present in synthetic urine did not prevented the determination of ESC, as well as the other chemical species naturally present in the mineral water.

Integrative Genetic Variation, DNA Methylation, and Gene Expression Analysis of Escitalopram and Aripiprazole Treatment Outcomes in Depression: A CAN-BIND-1 Study.

Little is known about the interplay between genetics and epigenetics on antidepressant treatment (1) response and remission, (2) side effects, and (3) serum levels. This study explored the relationship among single nucleotide polymorphisms (SNPs), DNA methylation (DNAm), and mRNA levels of four pharmacokinetic genes, CYP2C19, CYP2D6, CYP3A4, and ABCB1, and its effect on these outcomes. The Canadian Biomarker Integration Network for Depression-1 dataset consisted of 177 individuals with major depressive disorder treated for 8 weeks with escitalopram (ESC) followed by 8 weeks with ESC monotherapy or augmentation with aripiprazole. DNAm quantitative trait loci (mQTL), identified by SNP-CpG associations between 20 SNPs and 60 CpG sites in whole blood, were tested for associations with our outcomes, followed by causal inference tests (CITs) to identify methylation-mediated genetic effects. Eleven cis-SNP-CpG pairs (q<0.05) constituting four unique SNPs were identified. Although no significant associations were observed between mQTLs and response/remission, CYP2C19 rs4244285 was associated with treatment-related weight gain (q=0.027) and serum concentrations of ESCadj (q<0.001). Between weeks 2-4, 6.7% and 14.9% of those with *1/*1 (normal metabolizers) and *1/*2 (intermediate metabolizers) genotypes, respectively, reported ≥2 lbs of weight gain. In contrast, the *2/*2 genotype (poor metabolizers) did not report weight gain during this period and demonstrated the highest ESCadj concentrations. CITs did not indicate that these effects were epigenetically mediated. These results elucidate functional mechanisms underlying the established associations between CYP2C19 rs4244285 and ESC pharmacokinetics. This mQTL SNP as a marker for antidepressant-related weight gain needs to be further explored.

IPSC-derived hindbrain organoids to evaluate escitalopram oxalate treatment responses targeting neuropsychiatric symptoms in Alzheimer’s disease

Alzheimer’s disease (AD) is the most common cause of dementia, and the gradual deterioration of brain function eventually leads to death. Almost all AD patients suffer from neuropsychiatric symptoms (NPS), the emergence of which correlates with dysfunctional serotonergic systems. Our aim is to generate hindbrain organoids containing serotonergic neurons using human induced Pluripotent Stem Cells (iPSCs). Work presented here is laying the groundwork for the application of hindbrain organoids to evaluate individual differences in disease progression, NPS development, and pharmacological treatment response. Human peripheral blood mononuclear cells (PBMCs) from healthy volunteers (n = 3), an AD patient without NPS (n = 1), and AD patients with NPS (n = 2) were reprogrammed into iPSCs and subsequently differentiated into hindbrain organoids. The presence of serotonergic neurons was confirmed by quantitative reverse transcription PCR, flow cytometry, immunocytochemistry, and detection of released serotonin (5-HT). We successfully reprogrammed PBMCs into 6 iPSC lines, and subsequently generated hindbrain organoids from 6 individuals to study inter-patient variability using a precision medicine approach. To assess patient-specific treatment effects, organoids were treated with different concentrations of escitalopram oxalate, commonly prescribed for NPS. Changes in 5-HT levels before and after treatment with escitalopram were dose-dependent and variable across patients. Organoids from different people responded differently to the application of escitalopram in vitro. We propose that this 3D platform might be effectively used for drug screening purposes to predict patients with NPS most likely to respond to treatment in vivo and to understand the heterogeneity of treatment responses.

Investigation of the immunological effects of escitalopram oxalate in the breast cancer co-culture model.

During breast cancer treatment, approximately half of the patients are prescribed psychotropic medication, such as selective serotonin reuptake inhibitors (SSRIs). Escitalopram oxalate is an SSRI used as an antidepressant. In this study, by creating a breast cancer microenvironment with THP-1, MCF-7 and MDA-MB-231 breast cancer co-culture models were created. MCF-7, MDA-MB-231, and THP-1 cell lines to determine the concentration range of the cytotoxic effect of escitalopram oxalate MTS and MTT test were used. IC50 values were determined by the xCELLigence real-time cell analysis (RTCA) system. Apoptotic activities and cytokine levels were determined by flow cytometry. In the xCELLigence real-time analysis made according to the results, the IC50 value of escitalopram oxalate was measured as 13.7 μM for MCF-7 and 10.9 μM for MDA-MB-231. The IC50 value was measured as 54.6 μM for MCF-7 and 58.4 μM for MDA-MB-231 in xCELLigence analysis with tamoxifen. According to the MTS test results, the IC50 value of tamoxifen for THP-1 was 92.03 μM and the IC50 value for escitalopram oxalate was 95.32 μM. In the co-culture model, the immunological effects of escitalopram oxalate on MCF-7 cells were 2.8%, 11.1%, 15.6%, 10.6%, and 12.1% for interleukin (IL)-1β, IL-6, IL-8, IL-10, and TNF-α, respectively, while MDA effects on MB-231 cells, respectively, were 2.1%, 15.9%, 16.2%, 8.8%, and 11.8%. According to the results obtained, it was concluded that the immunological effects of escitalopram oxalate are more effective than tamoxifen and that it can be used as an adjunctive agent in breast cancer treatment.

Eco-friendly based stability-indicating HPTLC technique for the determination of Escitalopram and Etizolam by employing quality by design approach

AbstractThe two chemical components Escitalopram (ESC) and Etizolam (ETZ) are beneficial for the health of individuals because it helps to treat anxiety. The study mainly illustrated that a green approach is essential in the medical sector with the help of “Green Analytical quality by design”. According to AQbD, the techniques of HPTLC have become eco-friendly, and decided to use “ESC” and “ETZ”. Hence, ethanol and phosphate buffer pH 3.5 adjusted with 1% “orthophosphoric acid”. After the retardation factor, the product ESC was found at 0.34 min and ETZ was found at 0.53 min. The linearity of ETZ the range varies from 300 to 1800 μg mL−1 and for ESC it varies from 100 to 600 μg mL−1. The validation parameter of R2 Values ranged from 0.9997 to 0.9994 for both ESC and ETZ. The study also demonstrated that different other methods were also useful for the medical sector to make it more convenient and eco-friendly. Some of those approaches are “GAPI”, “AGMS”, “NEMI”, and “AGREE”. The outcome of the study helped to find that the technique “HPTLC” is a green analytic design that helps to maintain the stability of the medicine and it was also approved as a quality design and also a novel approach in the pharmaceutical sector.

Impact of Baduanjin exercise combined with rational emotive behavior therapy on sleep and mood in patients with poststroke depression: A randomized controlled trial.

Poststroke depression (PSD) is one of the most common stroke complications. It not only leads to a decline in patients' quality of life but also increases the mortality of patients. In this study, the method of combining Chinese traditional exercise Baduanjin with psychotherapy was used to intervene in patients with PSD and to explore the improvement of sleep, mood, and serum levels of brain-derived neurotrophic factor (BDNF), 5-hydroxytryptamine (5-HT), and interleukin-6 (IL-6) levels in patients with PSD by combined treatment. A total of 100 patients with PSD who met the inclusion criteria were randomly assigned to Baduanjin group (n = 50) or control group (n = 50). The control group received treatment with escitalopram oxalate and rational emotive behavior therapy, while the experimental group received Baduanjin training in addition to the treatment given to the control group. Changes in sleep efficiency, sleep total time, sleep latency, arousal index, Hamilton Anxiety Rating Scale, Hamilton Depression Scale score, serum BDNF, 5-HT, IL-6 levels, and Modified Barthel Index were measured at baseline, 4 weeks and 8 weeks after intervention, and the results were compared between the 2 groups. Significantly improvements in the sleep efficiency, sleep total time, serum 5-HT, BDNF levels, and Modified Barthel Index score were detected at week 4 in the Baduanjin group than in the control group (P < .05). Additionally, the sleep latency, arousal index, Hamilton Anxiety Rating Scale, Hamilton Depression Scale scores and IL-6 levels in the Baduanjin group were lower than those in the control group (P < .05). After 8 weeks of treatment, the above indexes in the Baduanjin group were further improved compared with the control group (P < .05), and the above indexes of the 2 groups were significantly improved compared with the baseline (P < .001). Baduanjin exercise combined with rational emotive behavior therapy effectively improves the mood and sleep status of patients with PSD; It increases the serum levels of 5-HT and BDNF while reducing the level of serum proinflammatory factor IL-6; additionally, the intervention alleviates the degree of neurological impairment, upgrades the ability of daily living, and improves the quality of life.

DESIGN AND OPTIMIZATION OF ESCITALOPRAM OXALATE ORAL DISSOLVING FILMS BY RESPONSE SURFACE METHODOLOGY

Objective: To develop and optimise the oral dissolving films of escitalopram oxalate by response surface methodology. Methods: Oral dissolving film compositions were optimized by central composite design. The films are prepared by solvent casting method. Initially, different polymers were screened and based on the results polyvinyl alcohol was selected as polymer, propylene glycol was selected as plasticizer. Concentration of polymer and concentration of plasticizer were fixed as independent variables; tensile strength, percent elongation, elastic modulus and amount dissolved up to 5 min (%D5 min) were taken as responses. Results: The prepared films exhibited good surface characteristics. The thickness, uniformity of weight, surface pH and drug content are within acceptable range. The mechanical properties like tensile strength, folding endurance, percent elongation and elastic modulus were determined. The statistical analysis showed that polymer concentration has a positive effect on disintegration time and the plasticizer concentration has a significant effect on folding endurance. The prepared film relesases nearly 95% at the end of 5 min. The design space was used to optimize the quantities of polymer and plasticizer. The comparison of checkpoint experiment batch responses are corelating with the predicted responses. Conclusion: Escitalopram oxalate oral dissolving films was successfully designed and optimized by response surface method. It was concluded that the prepared films exhibit good mechanical properties and maximum release within 10 min.

Unveiling potential adverse events associated with escitalopram oxalate: A real-world analysis based FDA adverse event reporting system database.

The study aimed to conduct a multidimensional evaluation of potential adverse events (AEs) of escitalopram oxalate based on the FDA adverse event reporting system (FAERS) database. This study utilized the reporting odds ratio (ROR), proportional reporting ratio (PRR), Bayesian confidence propagation neural network (BCPNN), and multi-item gamma-poisson shrinker (MGPS) to mine and analyze data from the FAERS database from the first quarter of 2004 to the second quarter of 2023. There was a total of 19,854 AE reports related to escitalopram oxalate, extracting 625 preferred terms (PTs), and covering 27 system organ classes (SOCs). The results showed that the number of reports by females was significantly higher than males, accounting for 57.68%. The reporting number was higher in 2018 and 2019, accounting for 9.50% and 10.18% of the total reports, respectively. The main reporters were consumers and other health professionals, accounting for 26.99% and 26.75% respectively. The majority of the reports were primarily from the United States. Newly emerging AE signals such as intentional overdose (n = 691, ROR 8.51, PRR 8.45, IC 3.05, Empirical Bayesian Geometric Mean (EBGM) 8.35), suicide attempt (n = 665, ROR 8.58, PRR 8.52, IC 3.06, EBGM 8.42), serum serotonin (n = 5, ROR 1044.78, PRR 1044.71, IC 2.56, EBGM 392.39), anti-actin antibody positive (n = 5, ROR 626.87, PRR 626.83, IC 2.56, EBGM 313.91), among others, were not mentioned in the drug's label. While escitalopram oxalate has clear benefits in the treatment of depression and other mental health disorders, the presence of AEs also suggests risks associated with its use. Particularly concerning are risks of suicide and changes in serum serotonin levels.

Fabrication of Ion selective PVC Membrane Sensor for Potentiometric Determination of Escitalopram Oxalate in its Pure Form and Pharmaceutical Tablet

Fabrication of Ion selective PVC Membrane Sensor for Potentiometric Determination of Escitalopram Oxalate in its Pure Form and Pharmaceutical Tablet

Assessing Pharmacokinetic Correlates of Escitalopram-Related Adverse Drug Reactions.

To assess the pharmacokinetic correlates of reported adverse drug reactions (ADRs) under antidepressant treatment with escitalopram (ESC) using a large therapeutic drug monitoring database. A large naturalistic sample of inpatients and outpatients prescribed ESC was analyzed. ADRs were classified using the Udvalg for Kliniske Undersogelser side effect rating scale. We compared ESC-treated patients with (n = 35) and without ADRs (n = 273) using ESC plasma concentrations as the primary outcome. We also compared ADR rates in the 2 groups based on 2 cut-off ESC levels reflecting the recommended upper thresholds of the therapeutic reference range of 80 ng/mL, suggested by the consensus therapeutic drug monitoring guidelines, and 40 ng/mL, based on recent meta-analysis data. The effects of age, sex, smoking, daily ESC dose, plasma concentrations, and concentrations corrected for daily dose were included in a binary logistic regression model to predict ADRs. No differences in clinical, demographic, or pharmacokinetic parameters were observed between patients with and without ADRs ( P > 0.05). Patients with ESC-related ADRs were more frequently diagnosed with psychotic disorders than those without (25% vs. 7.1%, P = 0.004). None of the variables was associated with ADR risk. Overall, ADR rates were not significantly different in patients above versus below thresholds of ESC concentrations (ESC concentrations >40 [n = 59] vs. ≤40 ng/mL [n = 249] and >80 [n = 8] vs. ≤80 ng/mL [n = 300]; P = 0.56 and P = 1.0, respectively). No distinct pharmacokinetic patterns underlying ESC-associated ADRs were observed. Further studies with more specific assessments of ADRs in larger cohorts are required to better identify potential underlying patterns.

Electroacupuncture versus Escitalopram for mild to moderate Post-Stroke Depression: A randomized non-inferiority trial.

To explore the efficacy of electroacupuncture in treating post-stroke depression (PSD) by modulating the inflammatory response pathway. One hundred and fifty participants with mild or moderate PSD were randomly divided into 75 cases each in the electroacupuncture group (EA group) and escitalopram group (ESC group). In the EA group, 30 sessions of electroacupuncture were performed on the Baihui (GV 20), Yintang (GV 29), and the ipsilateral Taichong (LR 3) and Hegu (LI 4), simultaneous oral placebo for 40 days. The ESC group received oral escitalopram oxalate tablets 10mg to 20mg for 40 days, plus 30 sessions of sham electroacupuncture. The effectiveness of the treatment was evaluated by the Hamilton Depression Scale (HAMD-17), Self-Depression Scale (SDS), Modified Barthel Index Score (MBI), and the serum levels of IL-1β, IL-6, IL-10, TNF-α, and INF-γ. There was no statistically significant difference in the baseline data, HAMD-17, SDS, MBI scores, and serum IL-1β, IL-6, IL-10, TNF-α, and INF-γ levels between the two groups of participants before the intervention (P >0.05). After treatment, HAMD-17 and SDS scores continued to decrease and MBI scores continued to increase in both groups. The differences were statistically significant at the 6th week and baseline, the 10th week and baseline, and the 10th week and the 6th week (all P <0.001). The differences in HAMD-17, SDS, and MBI scores between the two groups at the 6th week were not statistically significant (P=0.110, 0.115, 0.516, respectively); HAMD-17 scores and SDS scores in the EA group were lower than those in the ESC group at the 10th week, and the differences were statistically significant (P=0.002,0.026, respectively). In the 6th week, the serum levels of pro-inflammatory factors such as IL-1β, IL-6, TNF-α, and INF-γ were significantly lower in both groups compared with the baseline, while the level of anti-inflammatory factor IL-10 was significantly higher. The difference between the pre-and post-intervention intra-group comparisons was statistically significant (P <0.001), and the difference between the inter-group comparisons was not statistically significant (P >0.05). No serious adverse events occurred throughout the trial. Both therapies could safely and effectively improve HAMD-17, SDS, and MBI scores and modulate neuroinflammatory responses in PSD participants. After the treatment was stopped, some parameters were better in the EA group than the ESC group in a short time. Electroacupuncture is an effective, alternative to escitalopram for the treatment of mild-to-moderate PSD. Chinese Clinical Trial Registry (ChiCTR2300072576).

Continuous Spherical Crystallization of Escitalopram Oxalate without Additives

Continuous Spherical Crystallization of Escitalopram Oxalate without Additives

Development and Evaluation of an Orodispersible Tablet Formation for the Delivery of a Hydrophobic Drug.

Orodispersible tablet (ODT) is a promising avenue for drug delivery, offering a dosage form that can be disintegrated instantaneously in the mouth and released the drug that dissolves or disperses in the saliva without the addition of water. ODT can effectively boost the dissolution rate and consequently the bioavailability of several hydrophobic drugs. Additionally, ODT is very attractive and suitable for specific patients who are unable to swallow the traditional tablet. The basic approach in the fabrication of oral tablets for hydrophobic drugs relies on the utilization of superdisintegrants which allow prompt disintegration of tablets after swallowing. In the present investigation, escitalopram oxalate was chosen as a model drug, which is a hydrophobic, antidepressant, selective serotonin reuptake inhibitor (SSRI) drug. Nine formulas of escitalopram oxalate ODTs were prepared by varying the concentrations of three different superdisintegrants: sodium starch glycolate, croscarmellose sodium, and crospovidone to improve the dissolution and release of escitalopram oxalate. Each was used in three different concentrations (2.5%, 5%, and 7.5%), and all the ODTs were prepared by the direct compression method. The micrometric characterization of the powder blend used in the formulations was investigated such as angle of repose, bulk and tapped densities, compressibility percent (Carr's index), and Hausner ratio. Furthermore, the prepared ODTs were characterized in terms of weight variation, thickness, diameter, hardness, friability, in vitro disintegration, wetting time, water absorption ratio, drug content, in vitro dissolution, and accelerated stability study. The results showed that the formula (ODT9) that contained 7.5% of the superdisintegrant sodium starch glycolate had superior characteristics in almost all the tests, with a dissolution rate of 100% after 6 minutes. Also, it was stable under the accelerated stability conditions.

IPSC‐derived hindbrain spheroids to evaluate drug responses targeting neuropsychiatric symptoms in Alzheimer’s disease

AbstractBackgroundAlzheimer’s disease (AD), a neurodegenerative disorder, is the most common cause of dementia. The gradual deterioration of brain function eventually leads to death. Almost all AD patients eventually suffer from neuropsychiatric symptoms (NPS; e.g., agitation, depression) whose emergence correlates with dysfunctional serotonergic systems. Our aim is to generate hindbrain spheroids containing serotonergic neurons using induced Pluripotent Stem Cells (iPSCs) from healthy volunteers or AD patients with and without NPS. The spheroids can be used to study AD, NPS, and to evaluate individual differences in disease progression, NPS development, and/or pharmacological treatment response.MethodHuman peripheral blood mononuclear cells from healthy volunteers (n = 3), an AD patient without NPS (n = 1), and AD patients with NPS (n = 2) were reprogrammed into iPSCs and subsequently differentiated into hindbrain spheroids. The presence of serotonergic neurons was confirmed by quantitative reverse transcription PCR, flow cytometry, immunocytochemistry, and detection of serotonin (5‐HT) secreted in the extracellular environment. To assess patient‐specific treatment effects, spheroids were treated with different concentrations of escitalopram oxalate, a medication widely prescribed for the treatment of NPS.ResultHindbrain spheroids containing serotonergic neurons were successfully generated and characterized from these 6 individual iPSC lines. Changes in 5‐HT levels before and after treatment with escitalopram were dose‐dependent and variable across patients.ConclusionIt is possible to generate hindbrain spheroids from human iPSCs to study inter‐patient variability using a precision medicine approach. Since hindbrain spheroids from different people respond differently to the application of escitalopram in vitro this may reveal subgroups of AD patients who may be more or less likely to benefit from the drug in vivo. We propose that this 3D platform might be effectively used for drug screening purposes to predict patients with NPS most likely to respond to treatment with escitalopram.

Development and Validation of Analytical Method by Reverse Phase HPLC for the Estimation of Escitalopram oxalate in Bulk and Dosage form

Development and Validation of Analytical Method by Reverse Phase HPLC for the Estimation of Escitalopram oxalate in Bulk and Dosage form

Comparison of tandospirone and escitalopram as a symptomatic treatment in Multiple System Atrophy-cerebellar ataxia: An open-label, non-controlled, 4 weeks observational study

BackgroundMultiple system atrophy (MSA) is a neurodegenerative disorder characterized by autonomic failure and motor dysfunction in parkinsonism and/or cerebellar ataxia. Patients with MSA usually present with depression and anxiety symptoms. This observational study of patients with MSA-cerebellar subtype (MSA-C) with subthreshold depression/anxiety symptoms aimed to compare the efficacy of escitalopram oxalate (an antidepressant drug) and tandospirone citrate (an anxiolytic drug). MethodsFifty-six MSA-C patients were included, with 28 patients in each treatment group. One group received escitalopram oxalate 10 mg/day and the other group received tandospirone citrate 30 mg/day. The patients were evaluated at baseline and after 4 weeks. Several psychiatric and neurological tests were performed, including the Hamilton Anxiety Rating Scale (HAMA), Hamilton Depression Rating Scale (HAMD), Scale for the Assessment and Rating of Ataxia (SARA), and the Scale for Outcomes in Parkinson's Disease for Autonomic Symptoms (SCOPA-AUT). Furthermore, post-void residual urine volume (PVR) and blood pressure were measured. ResultsThere was a more substantial reduction in the HAMA/HAMD, scores of stance, finger tracking, and finger nose test in the SARA, and PVR in the tandospirone group. There was a more substantial reduction in scores of dysuria, light-headed when standing up, syncope and hyperhidrosis in the SCOPA-AUT in the escitalopram group (p's < 0.05). ConclusionsTandospirone citrate was more effective in improving depression/anxiety and some cerebellar ataxia symptoms, whereas escitalopram was more effective in improving some autonomic symptoms in MSA-C patients over a short-term period in an open-label observational study without a control group. Further research is needed to evaluate the long-term effects of tandospirone and escitalopram in MSA-C in long-term placebo controlled trials.