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https://www.readbyqxmd.com/read/28944986/development-and-in-vitro-in-vivo-evaluation-of-a-novel-benznidazole-liquid-dosage-form-using-a-quality-by-design-approach
#1
Higo Fernando Santos Souza, Daniel Real, Darío Leonardi, Sandra Carla Rocha, Victoria Alonso, Esteban Serra, Ariel Mariano Silber, Claudio Javier Salomon
OBJECTIVES: To develop an alcohol-free solution suitable for children of benznidazole, the drug of choice for treatment of Chagas disease. METHODS: In a quality-by-design approach a systematic optimization procedure was carried out in order to estimate the values of the factors leading to the maximum drug concentration. The formulations were analyzed in terms of chemical and physical stability and drug content. The final preparation was subjected to an in-vivo palatability assay...
September 25, 2017: Tropical Medicine & International Health: TM & IH
https://www.readbyqxmd.com/read/28930747/quantification-of-bisoprolol-and-metoprolol-in-simultaneous-human-serum-and-cerebrospinal-fluid-samples
#2
Ali Sigaroudi, Martina Kinzig, Oliver Wahl, Christoph Stelzer, Michael Schroeter, Uwe Fuhr, Ulrike Holzgrabe, Fritz Sörgel
BACKGROUND: Bisoprolol and metoprolol are moderately lipophilic, beta(1)-selective betablockers reported to cause adverse effects in the central nervous system (CNS), such as sleep disturbance, suggesting that both drugs may reach relevant concentrations in the brain. CNS beta(2)-receptor blockade has been suspected to be related to such effects. The higher molecular size of bisoprolol (325 Dalton) and the higher beta(1)-selectivity compared to metoprolol (267 Dalton) would suggest a lower rate of CNS effects...
September 21, 2017: Pharmacology
https://www.readbyqxmd.com/read/28923870/associations-between-voriconazole-therapeutic-drug-monitoring-toxicity-and-outcome-in-liver-transplant-patients-an-observational-study
#3
Zahra Hashemizadeh, Parisa Badiee, Seyed Ali Malekhoseini, Hadi Raeisi Shahraki, Bita Geramizadeh, Hashem Montaseri
The aim of this study was to investigate the variability of voriconazole plasma level and its relationship with clinical outcomes and adverse events, among liver transplant recipients to optimize the efficacy and safety of their treatment. Liver transplant recipients treated with voriconazole were included and voriconazole trough levels were quantified by the validated high-performance liquid chromatography method. Cytochrome P450 genotypes of CYP2C19 were evaluated in allograft liver tissues. A total of 832 voriconazole trough levels from 104 patients were measured...
September 18, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28917081/evaluation-of-the-ecstasy-influence-on-tramadol-and-its-main-metabolite-plasma-concentration-in-rats
#4
Bardia Jamali, Behjat Sheikholeslami, Yalda Hosseinzadeh Ardakani, Hoda Lavasani, Mohammad-Reza Rouini
BACKGROUND: Tramadol is prone to be abused alone, or in combination with 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy). It was reported that 95% of people with a history of substance abuse in the United States used tramadol in 2004. According to the WHO report in 2016, there was a growing number of tramadol abusers alone or in combination with psychoactive substances such as MDMA in particular in some Middle East countries. Higher concentrations of tramadol in plasma may lead to adverse drug reactions or lethal intoxication...
September 16, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28911678/averrhoa-bilimbi-fruits-attenuate-hyperglycemia-mediated-oxidative-stress-in-streptozotocin-induced-diabetic-rats
#5
Surya B Kurup, S Mini
Hyperglycemia-mediated oxidative stress plays a major role in the development of diabetic complications. Averrhoa bilimbi Linn. (Oxalidaceae) is a medicinal plant with fruits reported to possess antidiabetic activity. This study evaluated the beneficial effects of the ethyl acetate fraction of A. bilimbi fruit (ABAEE) on the antioxidant/oxidant status in diabetes mellitus. Diabetic rats were treated orally with the ethyl acetate fraction of A. bilimbi fruits at a dose of 25 mg/kg body weight for 60 days. Serum glucose, glycated hemoglobin, plasma insulin, hepatic toxicity markers, antioxidant enzymes, lipid peroxidation products, and liver histopathology were assayed checked after 60 days of extract treatment...
April 2017: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28911626/high-throughput-liquid-chromatography-tandem-mass-spectrometry-method-for-simultaneous-determination-of-fampridine-paroxetine-and-quinidine-in-rat-plasma-application-to-in%C3%A2-vivo-perfusion-study
#6
Suneetha Achanti, Raja Rajeswari Katta
A selective and high-throughput liquid chromatography-mass spectrometry method has been developed and validated for the simultaneous quantification of paroxetine, fampridine, and quinidine in rat plasma using imipramine as an internal standard. Following protein precipitation extraction, the analytes and internal standard were run on XBridge C18 column (150 mm × 4.6 mm, 5 μm) using a gradient mobile phase consisting of 5mM ammonium formate in water (pH 9.0) and acetonitrile in a flow gradience program...
October 2016: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28905202/drug-interactions-in-users-of-tablet-vs-oral-liquid-levothyroxine-formulations-a-real-world-evidence-study-in-primary-care
#7
Valeria Guglielmi, Alfonso Bellia, Elisa Bianchini, Gerardo Medea, Iacopo Cricelli, Paolo Sbraccia, Davide Lauro, Claudio Cricelli, Francesco Lapi
PURPOSE: Several medications may interact with levothyroxine (LT4) intestinal absorption or metabolism, thus reducing its bioavailability. We investigated the variability of thyroid stimulating hormone (TSH) levels and prescribed daily dosages (PDDs) of LT4 before and during potential drug-drug interactions (DDIs) in users of tablets vs. oral liquid LT4 formulations. METHODS: By using the Italian general practice Health Search Database (HSD), we retrospectively selected adult patients with at least one LT4 prescription from 2012 to 2015 and at least 1 year of clinical history recorded...
September 14, 2017: Endocrine
https://www.readbyqxmd.com/read/28890266/in-line-coupling-of-supported-liquid-membrane-extraction-to-capillary-electrophoresis-for-simultaneous-analysis-of-basic-and-acidic-drugs-in-urine
#8
Pavla Pantůčková, Pavel Kubáň
Simultaneous extraction of basic and acidic drugs across thin supported liquid membrane (SLM) and direct injection of the extracted drugs from SLM surface into capillary electrophoresis (CE) were demonstrated. A microextraction device compatible with injection system of commercial CE instrument was filled with 20μL of sample and 10μL of acceptor solution, which were interspaced by the SLM impregnated with 5μL of organic solvent. Extractions of three basic drugs (nortriptyline, haloperidol and loperamide) and two acidic drugs (ketoprofen and naproxen) were achieved at optimized conditions including 1-ethyl-2-nitrobenzene as SLM solvent, natural pH of sample solution, 2...
October 13, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28888975/solvent-responsive-floating-liquid-crystalline-molecularly-imprinted-polymers-for-gastroretentive-controlled-drug-release-system
#9
Li-Ping Zhang, Xiao-Lin Wang, Qian-Qian Pang, Yan-Ping Huang, Lei Tang, Meng Chen, Zhao-Sheng Liu
Liquid crystalline-molecularly imprinted polymer (LC-MIP) particles were first found to possess the floating behavior on the aqueous medium. Combined with molecular recognition, the LC-MIP was fabricated as a novel class of the controlled-release gastric retentive DDS. The LC-MIP was made using co-polymerization of methacrylic acid, 4-methyl phenyl dicyclohexyl ethylene (LC monomer with vinyl group), and ethylene glycol dimethacrylate with S-amlodipine (S-AML) as model template drug. The optimum condition of the preparation of LC-MIP has been obtained relying on release behaviors of S-AML from the LC-MIP...
September 6, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28884840/hydroxycarbamide-in-children-with-sickle-cell-anemia-after-first-dose-vs-chronic-therapy-pharmacokinetics-and-predictive-models-for-drug-exposure
#10
Jeremie H Estepp, Paweł Wiczling, Joseph Moen, Guolian Kang, Joana Marie Mack, Robert Liem, Julie A Panepinto, Uttam Garg, Gregory Kearns, Kathleen A Neville
AIMS: The purpose of this work was to (1) compare pharmacokinetic (PK) parameters for hydroxycarbamide in children receiving their first dose (HCnew ) versus those receiving chronic therapy (HCchronic ), (2) assess the external validity of a published PK dosing strategy, and (3) explore the accuracy of dosing strategies based on a limited number of HC measurements. METHODS: Utilizing data from two prospective, multicenter trials of hydroxycarbamide (Pharmacokinetics of Liquid Hydroxyurea in Pediatric Patients with Sickle Cell Anemia; NCT01506544 and Single-Dose (SD) and Steady-State (SS) Pharmacokinetics of Hydroxyurea in Children and Adolescents with Sickle Cell Disease), plasma drug concentration versus time profiles were evaluated with a model independent approach in the HCnew and HCchronic groups...
September 8, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28875060/assessment-of-the-drug-drug-interaction-potential-between-theacrine-and-caffeine-in-humans
#11
Hui He, Dejian Ma, Laura Brooks Crone, Matthew Butawan, Bernd Meibohm, Richard J Bloomer, Charles R Yates
Objective: Theacrine, a methylurate class purine alkaloid, triggers diverse pharmacologic responses, including psychostimulatory activity by modulation of adenosinergic and dopaminergic pathways. In a double-blind, placebo-controlled study, theacrine increased energy, concentration, and mood, while reducing fatigue. Because caffeine, a methylxanthine purine alkaloid, is frequently coadministered with theacrine, we sought to determine if a pharmacokinetic and/or pharmacodynamic interaction existed between theacrine and caffeine...
September 1, 2017: Journal of Caffeine Research
https://www.readbyqxmd.com/read/28867759/development-and-optimization-of-orally-and-topically-applied-liquid-crystal-drug-formulations
#12
Wesam R Kadhum, Tomoki Hada, Ichiro Hijikuro, Hiroaki Todo, Kenji Sugibayashi
Liquid crystal (LC)-forming lipids represent an important class of biocompatible amphiphiles and their application extends to cosmeceutical, dietary, and pharmaceutical technologies. In the present study, we aimed to develop strategies for designing and optimizing oral and topical LC formulations by evaluating their in vitro and in vivo drug absorption performances. C17-Monoglycerol ester (MGE) was used as a LC-forming lipid. p-Amino benzoic acid, methyl PABA, ethyl PABA, and sodium fluorescein were selected as drug models with different physiochemical properties...
2017: Journal of Oleo Science
https://www.readbyqxmd.com/read/28864105/morphine-and-metabolites-plasma-levels-after-administration-of-sustained-release-morphine-in-roux-en-y-gastric-bypass-subjects-versus-matched-control-subjects
#13
Lorry Hachon, Rafael Reis, Laurence Labat, Christine Poitou, Aude Jacob, Xavier Declèves, Celia Lloret-Linares
BACKGROUND: Better knowledge of opioid pharmacology after Roux-en-Y gastric bypass (RYGB) is required for optimizing their use in this growing population. OBJECTIVE: The aim of this case-controlled pharmacokinetic (PK) study was to compare morphine and its glucuronidated metabolites (morphine-3-glucuronide and morphine-6-glucuronide) plasma PKs between patients with RYGB and their controls. SETTINGS: University hospital, Lariboisière Hospital, Paris...
August 3, 2017: Surgery for Obesity and related Diseases: Official Journal of the American Society for Bariatric Surgery
https://www.readbyqxmd.com/read/28862574/steady-state-pharmacokinetics-of-hydroxychloroquine-in-patients-with-cutaneous-lupus-erythematosus
#14
H Al-Rawi, S J Meggitt, F M Williams, S Wahie
Background Hydroxychloroquine (HCQ), a 4-aminoquinolone antimalarial, is regarded as the oral therapy of choice for cutaneous and systemic lupus erythematosus (SLE). It is also licensed for rheumatoid arthritis (RA). Studies of HCQ-treated patients with SLE or RA have demonstrated a positive correlation between whole-blood HCQ levels and clinical response. Such studies have involved measuring whole-blood concentrations at any given time point after HCQ ingestion assuming that steady-state concentrations would undergo limited fluctuation over a daily interval because HCQ has a long half-life...
January 1, 2017: Lupus
https://www.readbyqxmd.com/read/28858753/development-and-validation-of-a-new-hplc-dad-method-for-quantification-of-sofosbuvir-in-human-serum-and-its-comparison-with-lc-ms-ms-technique-application-to-a-bioequivalence-study
#15
Shahram Miraghaei, Bahareh Mohammadi, Atefeh Babaei, Samira Keshavarz, Gholamreza Bahrami
Although for many analyses tandem mass spectrometry (LC-MS/MS) systems have significant advantage over the high-performance liquid chromatography with diode array detection (HPLC-DAD) however, the HPLC methods are easier, cheaper and more available to perform. As no published method is available for quantitative HPLC analysis of sofosbuvir (SOF), an orally administered anti-hepatitis drug in human serum, this study was aimed to evaluate applicability of the HPLC technique to quantify sofosbuvir and comparison of the two methods for analytical performance...
August 28, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28852798/enantioselective-separation-and-determination-of-miconazole-in-rat-plasma-by-chiral-lc-ms-ms-application-in-a-stereoselective-pharmacokinetic-study
#16
Yueying Du, Linda Luo, Shuo Sun, Zhen Jiang, Xingjie Guo
Miconazole has one chiral center, and consists of two enantiomers. In this study, a novel chiral liquid chromatography-tandem mass spectrometry method was developed for enantioselective separation and determination of miconazole in rat plasma. For the first time, the enantioselective pharmacokinetics of miconazole was investigated by the current method. Firstly, attempts were made to separate the enantiomers in reversed-phase mode with a mobile phase that was mass spectrometry compatible. Baseline separation was achieved on a Chiralpak IC column with a mobile phase composed of acetonitrile and aqueous ammonium hydrogen carbonate (5 mM; 80:20, v/v)...
August 29, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28847023/saliva-versus-plasma-bioequivalence-of-valsartan-hydrochlorothiazide-in-humans-validation-of-classes-ii-and-iv-drugs-of-the-salivary-excretion-classification-system
#17
Nasir Idkaidek, Haneen Agha, Tawfiq Arafat
Aim The aim of this study is to investigate the robustness of using non-invasive saliva instead of plasma for bioequivalence of valsartan and hydrochlorothiazide (HCT) in humans based on Salivary Excretion Classification System (SECS). Methods Plasma and resting saliva samples were collected over 24 h after oral administration of single dose 160 mg valsartan and 12.5 mg HCT to 12 healthy male volunteers after 10 h overnight fasting. Plasma and saliva concentrations were determined by validated liquid chromatography-mass spectrometry...
August 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28846866/the-effect-of-deep-eutectic-solvent-on-the-pharmacokinetics-of-salvianolic-acid-b-in-rats-and-its-acute-toxicity-test
#18
Jue Chen, Qi Wang, Mengjun Liu, Liwei Zhang
Deep eutectic solvent (DES), the benign green solvent with uniquely physical properties, has been widely applied in various fields. Our previous study indicated that DES could improve the stability and extraction efficiency of salvianolic acid B (SAB). In this work, with SAB as a model drug, the feasibility of DES as a drug carrier for oral preparation was investigated by evaluating the influence of DES on the pharmacokinetics of SAB and the toxicity of DES. Acute oral toxicity test illustrated that choline chloride-glycerol (ChCl-GL, molar ratio 1:2) was non-toxic with the median lethal dose of 7733mg/kg...
August 19, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28842349/solid-self-nanoemulsifying-drug-delivery-systems-for-oral-delivery-of-polypeptide-k-formulation-optimization-in-vitro-and-in-vivo-antidiabetic-evaluation
#19
Varun Garg, Puneet Kaur, Sachin Kumar Singh, Bimlesh Kumar, Palak Bawa, Monica Gulati, Ankit Kumar Yadav
Development of self-nanoemulsifying drug delivery systems (SNEDDS) of polypeptide-k (PPK) is reported with the aim to achieve its oral delivery. Box-Behnken design (BBD) was adopted to develop and optimize the composition of SNEDDS. Oleoyl polyoxyl-6 glycerides (A), Tween 80 (B), and diethylene glycol monoethyl ether (C) were used as oil, surfactant and co-surfactant, respectively as independent variables. The effect of variation in their composition was observed on the mean droplet size (y1), polydispersity index (PDI) (y2), % drug loading (y3) and zeta potential (y4)...
August 24, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28839365/determination-and-tissue-distribution-comparisons-of-atractylodin-after-oral-administration-of-crude-and-processed-atractylodes-rhizome
#20
Yang-Zhi Liu, Yu-Qiang Liu, Rui Jia, Jun Li, Xiao-Wen Chang, Chen-Xi Xu, Qian Cai
BACKGROUND: Atractylodis rhizoma is one of the most often used drugs in traditional Chinese medicine. Stir frying with wheat bran is the most common processing method. To clarify the principle of processing, an experiment was carried out to compare the tissue distribution of typical constituent after oral administration of raw A. rhizoma and processed ones. OBJECTIVE: To compare the tissues distribution of atractylodin after oral administration of raw and processed A...
July 2017: Pharmacognosy Magazine
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