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https://www.readbyqxmd.com/read/28738608/a-fast-bioanalytical-method-based-on-microextraction-by-packed-sorbent-and-uplc-ms-ms-for-determining-new-psychoactive-substances-in-oral-fluid
#1
A M Ares, P Fernández, M Regenjo, A M Fernández, A M Carro, R A Lorenzo
The emergence in recent years of potentially dangerous new psychoactive substances (NPS) that are not under international control has led to the development of multi-analyte procedures for their unequivocal quantification. A fast ultra-performance liquid chromatography-tandem mass spectrometry method (UPLC-MS/MS), in combination with a sample pretreatment based on microextraction by packed sorbent (MEPS), was for the first time used in this work for the simultaneous determination of NPS in oral fluid. This matrix is an effective alternative to typical biological samples for drug control in substitution therapy programs, and also for the prevention and reduction of traffic accidents...
November 1, 2017: Talanta
https://www.readbyqxmd.com/read/28738003/pharmacokinetics-and-egg-residues-after-oral-administration-of-a-single-dose-of-meloxicam-in-domestic-chickens-gallus-domesticus
#2
Marcy J Souza, Joan B Bergman, Molly S White, Kristen I Gordon, Lillian E Gerhardt, Sherry K Cox
OBJECTIVE To determine the pharmacokinetics of meloxicam in domestic hens and duration and quantity of drug residues in their eggs following PO administration of a single dose (1 mg of meloxicam/kg). ANIMALS 8 healthy adult White Leghorn hens. PROCEDURES Hens were administered 1 mg of meloxicam/kg PO once. A blood sample was collected immediately before and at intervals up to 48 hours after drug administration. The hens' eggs were collected for 3 weeks after drug administration. Samples of the hens' plasma, egg whites (albumen), and egg yolks were analyzed by high-performance liquid chromatography...
August 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28737445/preclinical-pharmacokinetics-and-biodistribution-studies-of-asenapine-maleate-using-novel-and-sensitive-rp-hplc-method
#3
Renuka S Managuli, Karthik Gourishetti, Rekha R Shenoy, Kunnatur B Koteshwara, Meka Sreenivasa Reddy, Srinivas Mutalik
AIM: Asenapine maleate (ASPM) is a newer antipsychotic drug available as a sublingual tablet in the market. EXPERIMENTAL: To investigate the pharmacokinetic and tissue distribution study of ASPM following oral administration in rats, reversed-phase HPLC method was developed and validated. RESULTS: ASPM was extracted from plasma and tissue matrix by liquid-liquid extraction technique and analyzed using mobile phase consisted of phosphate buffer pH 3...
July 24, 2017: Bioanalysis
https://www.readbyqxmd.com/read/28737409/low-buffer-capacity-and-alternating-motility-along-the-human-gastrointestinal-tract-implications-for-in-vivo-dissolution-and-absorption-of-ionizable-drugs
#4
Bart Hens, Yasuhiro Tsume, Marival Bermejo, Paulo Paixao, Mark Koenigsknecht, Jason R Baker, William L Hasler, R Lionberger, Jianghong Fan, Joseph Dickens, Kerby A Shedden, Bo Wen, Jeffrey Wysocki, Raimar Löbenberg, Allen Lee, Ann F Fioritto, Gregory E Amidon, Alex Yu, Gail Benninghoff, Niloufar Salehi, Arjang Talattof, Duxin Sun, Gordon L Amidon
In this study, we determined the pH and buffer capacity of human gastrointestinal (GI) fluids (aspirated from the stomach, duodenum, proximal jejunum and mid/distal jejunum) as a function of time, from 37 healthy subjects after oral administration of an 800 mg immediate-release tablet of ibuprofen (reference listed drug; RLD) under typical prescribed bioequivalence (BE) study protocol conditions in both fasted and fed state (simulated by ingestion of a liquid meal). Simultaneously, motility was continuously monitored using water-perfused manometry...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28719376/stability-of-spironolactone-oral-suspension-in-pcca-base-suspendit
#5
Richard Graves, Kelly V Phan, Levon A Bostanian, Tarun K Mandal, Yashoda V Pramar
Spironolactone (Aldactone) is a potassium-sparing diuretic used to treat hypertension and heart failure and may also be used to treat edema resulting from kidney disease, low potassium levels, or excess aldosterone. No commercial liquid dosage form of spironolactone exists. An extemporaneously compounded suspension from pure drug powder or commercial tablets would provide an alternative option to meet unique patient needs. The purpose of this study was to determine the physicochemical stability of spironolactone in the PCCA base SuspendIt...
July 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28715789/quantification-of-idp-73152-a-novel-antibiotic-in-plasma-from-mice-rats-and-humans-using-an-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-method-for-use-in-pharmacokinetic-studies
#6
Myongjae Lee, Dohee Kim, Jeongcheol Shin, Hee-Yeol Lee, Soobong Park, Hong-Sub Lee, Jae-Hoon Kang, Suk-Jae Chung
IDP-73152, a novel inhibitor of a bacterial peptide deformylase, was recently approved as a new, investigational drug in Korea for the clinical management of infections caused by Gram positive bacteria. The objective of this study was to develop/validate a simple and robust analytical method for the determination of IDP-73152 in plasma samples from rodents and humans, and to assess the feasibility of the assay for use in pharmacokinetic studies using animal models. Plasma samples were processed using a standard method for protein precipitation and an aliquot of the extract then injected onto an UHPLC-MS/MS system...
July 6, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28711713/surprisingly-high-stability-of-the-a%C3%AE-oligomer-eliminating-all-d-enantiomeric-peptide-d3-in-media-simulating-the-route-of-orally-administered-drugs
#7
Anne Elfgen, Beatrix Santiago-Schübel, Lothar Gremer, Janine Kutzsche, Dieter Willbold
The aggregation of the amyloid β protein (Aβ) plays an important role in the pathology of Alzheimer's disease. Previously, we have developed the all-d-enantiomeric peptide D3, which is able to eliminate neurotoxic Aβ oligomers in vitro and improve cognition in a transgenic Alzheimer's disease mouse model in vivo even after oral administration. d-Peptides are expected to be more resistant against enzymatic proteolysis compared to their l-enantiomeric equivalents, and indeed, a pharmacokinetic study with tritiated D3 revealed the oral bioavailability to be about 58%...
July 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28708440/model-calculations-of-regional-deposition-and-disposition-for-single-doses-of-inhaled-liposomal-and-dry-powder-ciprofloxacin
#8
Andrew R Martin, Warren H Finlay
BACKGROUND: Model predictions of regional deposition in the respiratory tract are useful in assessing factors that influence the effectiveness of aerosol delivery. Regional deposition models have previously been coupled with models of mucous production and clearance to estimate initial concentrations of drug deposited in the airway surface liquid (ASL) lining tracheobronchial airways. METHODS: Established models of regional deposition and ASL volumes were used to provide input to a new model evaluating the disposition of drug resulting from dissolution or release, absorption, and mucociliary clearance...
July 14, 2017: Journal of Aerosol Medicine and Pulmonary Drug Delivery
https://www.readbyqxmd.com/read/28706399/comparative-effect-of-divided-doses-of-adult-solid-and-liquid-oral-formulations-of-antiepileptic-drugs-in-the-management-of-pediatric-epilepsy
#9
Ravi Prasad Nidanapu, Bascarane Tamijarassy, Subramanian Mahadevan, Batmanabane Gitanjali
OBJECTIVE: To compare the differences in the efficacy and safety of the commonly prescribed AEDs in the management of epilepsy in children when using divided doses of adult solid oral formulations (DDSF) with the liquid oral formulations (LFs). MATERIALS AND METHODS: Patients who had one or more seizures per month and prescribed with DDSF were recruited. Initially the patients were continued on DDSF for 4 months following which they were switched over to LF for the subsequent 4 months...
April 2017: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/28693970/development-of-a-sedation-protocol-using-orally-administered-tiletamine-zolazepam-acepromazine-in-free-roaming-dogs
#10
Hsiao-Chun Huang, Shih-Wei Huang, Kuan-Hua Yu, Jiann-Hsiung Wang, Jui-Te Wu
OBJECTIVE: To investigate the sedative effects in dogs of tiletamine-zolazepam-acepromazine (TZA) or ketamine-flunitrazepam (KF) administered orally and to evaluate the effectiveness of encapsulated TZA for capturing free-roaming dogs. STUDY DESIGN: Experimental study followed by a field trial. ANIMALS: Six research dogs and 27 free-roaming dogs. METHODS: In a pilot study, six research dogs were administered liquid TZA (20 mg kg(-1) tiletamine-zolazepam and 2 mg kg(-1) acepromazine) or liquid KF (50 mg kg(-1) ketamine and 2 mg kg(-1) flunitrazepam) orally: treatment 1, forcefully squirting liquid medication into the mouth; treatment 2, encapsulating liquid medication for administration in canned food; treatment 3, administering liquid medication mixed with gravy...
April 14, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28685696/an-in-vivo-rat-d-glucose-stable-isotope-homeostasis-drug-discovery-screen-a-targeted-metabolomics-approach
#11
G Caldwell, Wensheng Lang
We have developed a targeted metabolomics screen which consists of using two isotopically labeled glucose compounds to conduct a dual oral glucose tolerance test in rats. This dual isotopic oral glucose tolerance test (DIS-OGTT) can be used to select drug candidates that have "on"-target or have "off"-target effects on oral glucose absorption, hepatic glucose production or glucose disposal. The DIS-OGTT assay utilized intravenously administered [6-13C1-6, 6'-2H2]-glucose and orally administered [U-13C6] glucose to monitor glucose homeostasis...
July 7, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685625/preparation-and-characterization-of-self-nano-emulsifying-drug-delivery-system-snedds-for-oral-delivery-of-heparin-using-hydrophobic-complexation-by-cationic-polymer-of-%C3%AE-cyclodextrin
#12
Yasaman Soltani, Navid Goodarzi, Reza Mahjub
OBJECTIVE: The aim of this study was the preparation of a self nano-emulsifying drug delivery system (SNEDDS) for oral delivery of heparin. SIGNIFICANCE: Preparation of hydrophobic complexes between heparin as the hydrophilic macromolecule and cationic polymer of β-cyclodextrin (CPβCD) was considered for preparation of orally administered SNEDDS in which the drug incorporated in internal oil phase of O/W nano-droplets. METHOD: Hydrophobic complexes of heparin-CPβCD were prepared by electrostatic interaction...
July 7, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28674061/assessment-of-clinical-pharmacokinetic-drug-drug-interaction-of-antimalarial-drugs-%C3%AE-%C3%AE-arteether-and-sulfadoxine-pyrimethamine
#13
Y S Chhonker, V V Bhosale, S K Sonkar, H Chandasana, D Kumar, S Vaish, S C Choudhary, S Bhadhuria, S Sharma, R K Singh, G K Jain, A K Vaish, S P S Gaur, R S Bhatta
The antimalarial drugs combination therapy is now being widely used for treatment of uncomplicated malaria. The objective of the present study was to investigate the effects of co-administration of intramuscular α/β-arteether (AE) and oral sulfadoxine-pyrimethamine (SP) on the pharmacokinetic properties of each drug as a drug-drug interaction study to support developing the fixed-dose combination therapy. Single-dose, open-label, crossover clinical trial was conducted in healthy adult Indian male volunteers (18-45 years, n=13), received single dose of AE, SP and combination dose of AE and SP...
July 3, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28671393/top-20-research-studies-of-2016-for-primary-care-physicians
#14
Mark H Ebell, Roland Grad
This article summarizes the top 20 original research studies and four practice guidelines of 2016, based on regular literature surveillance and as selected by members of the Canadian Medical Association. The studies, known as POEMs (patient-oriented evidence that matters), were rated highly because of their relevance, validity, and potential to change practice. Key hypertension treatment findings include reduced mortality (a benefit not demonstrated in lower-risk persons or persons with diabetes mellitus) but also an increase in harms with a more aggressive blood pressure target in high-risk persons with hypertension and without diabetes...
May 1, 2017: American Family Physician
https://www.readbyqxmd.com/read/28652732/preparation-characterization-and-evaluation-of-amphotericin-b-loaded-mpeg-pcl-g-pei-micelles-for-local-treatment-of-oral-candida-albicans
#15
Li Zhou, Peipei Zhang, Zhuo Chen, Shaona Cai, Ting Jing, Huihui Fan, Fei Mo, Jiye Zhang, Rong Lin
Fatal Candida albicans infections in the mucosal system can occur in association with immune-compromised diseases and dysbacteriosis. Currently, amphotericin B (AmB) is considered to be the most effective antibiotic in the treatment of C. albicans infections, but its clinical application is limited by side effects and poor bioavailability. In order to use AmB in the local treatment of oral C. albicans infections, AmB/MPEG-PCL-g-PEI (monomethoxy poly(ethylene glycol)-poly(epsilon-caprolactone)-graft-polyethylenimine, MPP) micelles were prepared...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28649076/renal-clearance-and-urinary-excretion-of-omeprazole-in-healthy-female-volunteers-in-pakistan
#16
Nazia Qadir, Tanweer Khaliq, Rai Altaf Hussain, Ghulam Abbas Shah, Sadia Asharaf, Ahmad Raza, Nadia Noor
Omeprazole is a widely prescribed proton pump inhibitor to treat various gastric acid hyper secretion disorders. The present study was designed to evaluate the renal clearance and urinary excretion of omeprazole in eight healthy female volunteers to increase the understanding of the contributing factors such as demographics variability in the renal clearance and urinary excretion of omeprazole under indigenous conditions. The urine and blood samples were collected 0.5, 1, 1.5, 2, 3, 4, 6, 8 hours after oral administration of enteric coated omeprazole (20 mg) and drug concentration in the samples was determined by High Performance Liquid Chromatography (HPLC) with C18 column and UV detector...
March 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28649075/hypouricemic-and-nephroprotective-effects-of-total-flavonoids-from-the-residue-of-supercritical-co2-extraction-of-humulus-lupulus-in-potassium-oxonate-induced-mice
#17
Zhen Jing Li, Zhuan Li, Xiao Ying Dong, Lai Feng Lu, Chang Lu Wang
Total flavonoids of Humulus lupulus (TFHL) were prepared using ethanol extraction, liquid-liquid partition and purification with polyamide resin. Different dose of TFHL were orally administered to normal and hyperuricemic mice for 7 days. The xanthine oxidase (XOD) inhibitory activity and hypouricemic effects of TFHL on potassium oxonate-induced hyperuricemic mice were examined. The TFHL showed very potent XOD inhibitory activity with IC50=66.8 μg/mL. At a single oral dose of 100mg/kg TFHL, the serum uric acid levels of hyperuricemic mice significantly decreased (P<0...
March 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28648070/magnetic-resonance-imaging-quantification-of-fasted-state-colonic-liquid-pockets-in-healthy-humans
#18
Kathryn Murray, Caroline L Hoad, Deanna M Mudie, Jeff Wright, Khaled Heissam, Nichola Abrehart, Susan E Pritchard, Salem Al Atwah, Penny A Gowland, Martin C Garnett, Gregory E Amidon, Robin C Spiller, Gordon L Amidon, Luca Marciani
The rate and extent of drug dissolution and absorption from solid oral dosage forms is highly dependent on the volume of liquid in the gastrointestinal tract (GIT). However, little is known about the time course of GIT liquid volumes after drinking a glass of water (8 oz), particularly in the colon, which is a targeted site for both locally and systemically acting drug products. Previous magnetic resonance imaging (MRI) studies offered novel insights on GIT liquid distribution in fasted humans in the stomach and small intestine, and showed that freely mobile liquid in the intestine collects in fairly distinct regions or "pockets"...
July 6, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28641022/a-randomized-single-dose-parallel-study-on-enhancement-of-nitric-oxide-in-serum-and-saliva-with-the-use-of-natural-sports-supplement-in-healthy-adults
#19
Joby Jacob, Sreeraj Gopi, Chandradhara Divya
Sports supplements that stimulate the production of nitric oxide (NO) are widely promoted agents in the sports nutrition domain, and nitric oxide plays an important role to enhance the cardiovascular and physical fitness of the sports participants. The purpose of the study is to investigate whether oral intake of a sports nutritional supplement (Fitnox) is able to increase nitrate (NO3(-)) and nitrite (NO2(-)) levels in blood serum and saliva of healthy adults. Fitnox is a unique blend of Kaempferia parviflora methoxy flavones, pomegranate peel polyphenols, and Moringa oleifera leaf saponins...
June 22, 2017: Journal of Dietary Supplements
https://www.readbyqxmd.com/read/28636208/a-phase-i-trial-of-prn1008-a-novel-reversible-covalent-inhibitor-of-bruton-s-tyrosine-kinase-in-healthy-volunteers
#20
Patrick F Smith, Janakan Krishnarajah, Philip A Nunn, Ron J Hill, Dane Karr, D Tam, Mohammad Masjedizadeh, Jens O Funk, Steve G Gourlay
AIM: To evaluate the safety, tolerability, and PK/PD of PRN1008, a novel BTK inhibitor, in healthy volunteers, and thus determine the dose range for future clinical studies. METHODS: This was a two-part randomized, placebo controlled study in healthy volunteers using a liquid formulation. Part I was a single ascending dose design with dose levels of 50 to 1200 mg (n=6 active, 2 placebo per cohort); Part II was a multiple ascending dose design, with dose regimens ranging from 300 mg to 900 mg daily, either qd or bd for 10 days...
June 21, 2017: British Journal of Clinical Pharmacology
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