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Oral liquid drug

Ping-Ping Lin, Xue-Ning Li, Fei Yuan, Wei-Li Chen, Meng-Jie Yang, Hong-Rong Xu
Huperzine A (HupA), one of the reversible and selective acetylcholinesterase inhibitors derived from Chinese herb Huperzia Serrata, possesses affirmative action of ameliorating cognitive dysfunction of Alzheimer's disease. Up to now, the effects of HupA on human cytochrome P450s (CYPs) have not been fully elucidated. The purpose of the present study was to clarify the metabolic pathway of HupA in vitro and in vivo, and to evaluate the CYPs inhibition/induction profile of HupA in vitro. The catalytic activity of CYP enzymes (CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A4) was measured by the quantification of specific enzyme substrates using validated liquid chromatography-tandem mass spectrometry (LC/MS/MS) methods...
October 14, 2016: Biochemical and Biophysical Research Communications
Elena Puris, Markku Pasanen, Mikko Gynther, Merja R Häkkinen, Jussi Pihlajamäki, Tapani Keränen, Paavo Honkakoski, Hannu Raunio, Aleksanteri Petsalo
Cocktail phenotyping using specific probe drugs for cytochrome P450 (CYP) enzymes provides information on the real-time activity of multiple CYPs. We investigated different sample preparation techniques and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method with simple protein precipitation for the analysis of nine CYP probe drugs and their metabolites in human serum and urine. Specific CYP probe drugs (melatonin, CYP1A2; nicotine, CYP2A6; bupropion, CYP2B6; repaglinide, CYP2C8; losartan, CYP2C9; omeprazole, CYP2C19 and CYP3A4; dextromethorphan, CYP2D6; chlorzoxazone, CYP2E; midazolam, CYP3A4) and their main metabolites, with the exception of 3'-hydroxyrepaglinide, were quantified in human serum and urine using the developed LC-MS/MS method...
October 12, 2016: Analytical and Bioanalytical Chemistry
Mihaela Friciu, Sarra Zaraa, V Gaëlle Roullin, Grégoire Leclair
The objective of this study was to evaluate the stability of diazoxide in extemporaneously compounded oral suspensions. Oral suspensions of diazoxide 10 mg/mL were prepared from either bulk drug or capsules dispersed in either Oral Mix or Oral Mix Sugar Free. These suspensions were stored at 5°C and 25°C/60%RH in bottles and oral syringes for a total of 90 days. At predetermined time intervals, suspensions were inspected for homogeneity, color or odor change; the pH was measured and the concentration of diazoxide was evaluated by ultraviolet detection using a stability-indicating high pressure liquid chromatography method...
2016: PloS One
Georgina Balcells, Xavier Matabosch, Rosa Ventura
Stanozolol (STAN) is one of the most frequently detected anabolic androgenic steroids in sports drug testing. STAN misuse is commonly detected by monitoring metabolites excreted conjugated with glucuronic acid after enzymatic hydrolysis or using direct detection by liquid chromatography tandem mass spectrometry (LC-MS/MS). It is well known that some of the previously described metabolites are the result of the formation of sulfate conjugates in C17, which are converted to their 17-epimers in urine. Therefore, sulfation is an important phase II metabolic pathway of STAN that has not been comprehensively studied...
October 7, 2016: Drug Testing and Analysis
Hai-Lang He, Dan Wang, Jie Tang, Xian-Mei Zhou, Jian-Xin Li, Ling Xu
Lung cancer is the leading cause of cancer-related deaths worldwide. Jin Fu Kang (JFK), an oral liquid prescription of Chinese herbal drugs, has been clinically available for the treatment of non-small cell lung cancer (NSCLC). Lymphangiogenesis is a primary event in the process of cancer development and metastasis, and the formation and migration of lymphatic endothelial cells (LECs) play a key role in the lymphangiogenesis. To assess the activity of stromal cell-derived factor-1 (SDF-1) and the coeffect of SDF-1 and vascular endothelial growth factor-C (VEGF-C) on the formation and migration of LECs and clarify the inhibitory effects of JFK on the LECs, the LECs were differentiated from CD34(+)/VEGFR-3(+) endothelial progenitor cells (EPCs), and JFK-containing serums were prepared from rats...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
Anna Leonidova, Mireille Vargas, Jörg Huwyler, Jennifer Keiser
One of the major neglected tropical diseases, schistosomiasis, is currently treated and controlled with a single drug, praziquantel. The quest for an alternative drug is fueled by its lack of activity against juvenile Schistosoma and the fear of emerging resistance. The synthetic ozonide OZ418 has shown high activity against Schistosoma mansoni, S. haematobium and S. japonicum in vivo, but its drug disposition remains unknown. To bridge this gap, our study determined the basic pharmacokinetic (PK) parameters of a single oral dose (400 mg/kg) of OZ418 in uninfected mice...
October 3, 2016: Antimicrobial Agents and Chemotherapy
Hidenori Kamiguchi, Masashi Yamaguchi, Mika Murabayashi, Ikuo Mori, Akira Horinouchi
Urinary hippuric acid (HA) and phenylacetylglycine (PAG) are biomarker candidates for drug-induced phospholipidosis (PLD). To confirm their utility in preclinical and clinical settings, it is essential to develop and validate their quantification method in advance. In this study, we have applied liquid chromatography-tandem mass spectrometry (LC/MS/MS) for simultaneous quantification of HA and PAG in rat urine, and matrix based ion suppression was assessed by post-column infusion assay. Effective sample dilution reduced matrix effect of urine to be negligible level and calibration curves showed good correlation between those in urine diluent and buffer alone...
November 1, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
B Lebkowska-Wieruszewska, G Barsotti, A Lisowski, A Gazzano, H Owen, M Giorgi
AIMS: To assess the effect of food intake on the pharmacokinetics of grapiprant administered orally at 2 mg/kg, and to estimate its oral bioavailability in dogs. METHODS: Eight healthy female Labrador Retriever dogs, aged 4-10 years were used. In the initial trial two dogs were administered a 0.5 mg/kg I/V bolus of grapiprant dissolved in ethanol. In the second trial, six dogs were assigned to two treatment groups, using a randomised cross-over design, and received 2 mg/kg of grapiprant orally, as pure powder, after fasting for 12 hours or after being fed...
October 2, 2016: New Zealand Veterinary Journal
Bappaditya Chatterjee, Samah Hamed Almurisi, Ather Ahmed Mahdi Dukhan, Uttam Kumar Mandal, Pinaki Sengupta
Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug...
August 15, 2016: Drug Delivery
Carmen Belmonte, Dolores Ochoa, Manuel Román, Teresa Cabaleiro, Maria Talegón, Sergio Daniel Sánchez-Rojas, Francisco Abad-Santos
AIMS: The aim of this study was the evaluation of the possible relationship between pharmacokinetics and the safety of aripiprazole as well as its influence on blood pressure (BP), heart rate (HR), and corrected QT (QTc) interval. METHODS: The study population comprised 157 healthy volunteers from 6 bioequivalence clinical trials. Subjects were administered a single 10-mg oral dose of each formulation separated by a 28-day washout period. Plasma concentrations were measured using high-performance liquid chromatography coupled to mass spectrometry...
September 28, 2016: Journal of Clinical Psychopharmacology
Camille Cohier, Bruno Mégarbane, Olivier Roussel
Driving after illicit drug use is a worldwide growing concern requiring rapid and sensitive screening at the roadside. It is noteworthy that the sampling method used to collect oral fluid (OF) may significantly influence drug concentrations in the collected sample and thus alter the accuracy of the measurement. We evaluated two OF collection devices, Quantisal(®) and Certus(®) collectors, for their suitability for collecting samples to allow laboratory confirmation of driving after illicit drug use. Four parameters were studied including (i) the collected OF volume; (ii) the recovery efficiency using OFs spiked with opiates, cannabinoids, amphetamines, cocaine and its metabolites; (iii) drug stability after storage for 1, 7 and 14 days at -20°C, +4°C and room temperature; and (iv) the impact of mouth cells present in the collected OF on drug stability...
September 27, 2016: Journal of Analytical Toxicology
Kenneth K Mugwanya, Craig W Hendrix, Nelly R Mugo, Mark Marzinke, Elly T Katabira, Kenneth Ngure, Nulu B Semiyaga, Grace John-Stewart, Timothy R Muwonge, Gabriel Muthuri, Andy Stergachis, Connie L Celum, Jared M Baeten
BACKGROUND: As pre-exposure prophylaxis (PrEP) becomes more widely used in heterosexual populations, an important consideration is its safety in infants who are breastfed by women taking PrEP. We investigated whether tenofovir and emtricitabine are excreted into breast milk and then absorbed by the breastfeeding infant in clinically significant concentrations when used as PrEP by lactating women. METHODS AND FINDINGS: We conducted a prospective short-term, open-label study of daily oral emtricitabine-tenofovir disoproxil fumarate PrEP among 50 HIV-uninfected breastfeeding African mother-infant pairs between 1-24 wk postpartum (ClinicalTrials...
September 2016: PLoS Medicine
G Kampf
Chlorhexidine digluconate (CHG) is an antimicrobial agent used for different types of applications in hand hygiene, skin antisepsis, oral care, and patient washing. Increasing use raises concern regarding development of acquired bacterial resistance. Published data from clinical isolates with CHG minimum inhibitory concentrations (MICs) were reviewed and compared to epidemiological cut-off values to determine resistance. CHG resistance is rarely found in Escherichia coli, Salmonella spp., Staphylococcus aureus or coagulase-negative staphylococci...
August 26, 2016: Journal of Hospital Infection
Mouna Chakroun, Bassem Khemakhem, Hazem Ben Mabrouk, Hanen El Abed, Mohamed Makni, Mohamed Bouaziz, Noureddine Drira, Naziha Marrakchi, Hafedh Mejdoub
Among various chronic disorders, cancer and diabetes mellitus are the most common disorders. This study was designed to evaluate the effectiveness of hydroalcoholic extract of Phoenix dactylifera L. leaves (HEPdL) in animal models of type II diabetes in vitro/in vivo and in a human melanoma-derived cell line (IGR-39). A liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis was also performed to determine the amount of phenolic and flavonoid compounds in this plant. The physicochemical results by LC-MS/MS analysis of HEPdL showed the presence of 10 phenolic compounds...
September 23, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Jin Ren, Zhengjie Fang, Liqun Jiang, Qian Du
The purpose of this study was to develop a liquid self-assemble proliposome for quercetin oral delivery. This liquid proliposome was prepared by dissolving phospholipids, surfactants and drug in ethanol. There was only one step in the preparation process of this liquid self-assemble proliposome and no special devices were required. The mechanism about proliposome transformation was discussed. Quercetin proliposomes with different cremorphor RH40 concentrations (0%, 20%, 23%, 26%, 30%) were prepared. The particle size and polydispersity index decreased as cremorphor RH40 concentration increased...
September 25, 2016: Journal of Liposome Research
Shuhua Deng, Wencan Huang, Xiaojia Ni, Ming Zhang, Haoyang Lu, Zhanzhang Wang, Jinqing Hu, Xiuqing Zhu, Chang Qiu, Dewei Shang, Yuefeng Zhang, Linghui Xiong, Yuguan Wen
1. A new oral liquid formulation combining guaifenesin, pseudoephedrine and hydrocodone is effective in improving the symptoms of common cold. The pharmacokinetic properties of the individual components were evaluated in a randomized, open-label, 4-period study in 12 healthy Chinese volunteers following single and multiple doses. The data were compared with data for the individual ingredients in Antuss(®). 2. In the single-dose period, exposure levels (AUC and Cmax) for guaifenesin, pseudoephedrine and hydrocodone increased directly as the dose of the oral liquid formulation increased from 5 to 15 mL...
September 23, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Atsuko Tanaka, Ikuko Yano, Keiko Shinsako, Eriko Sato, Masahide Fukudo, Satohiro Masuda, Toshinari Yamasaki, Tomomi Kamba, Osamu Ogawa, Kazuo Matsubara
BACKGROUND: Everolimus has been used for the treatment of unresectable or metastatic renal cell carcinoma (RCC). Here, we measured blood concentrations of everolimus to obtain the population pharmacokinetic parameters and to examine the relationship between blood concentration and clinical outcomes. METHODS: Twenty-two Japanese patients were enrolled. Blood samples were collected before and 2, 4, 8, and 24 h after drug administration on days 1 and 8 of everolimus therapy (5 or 10 mg) for inpatients; occasional samples were collected for outpatients...
September 19, 2016: Therapeutic Drug Monitoring
Najmul Hasan, Mathurot Chaiharn, Umair Ali Toor, Zulfiqar Ali Mirani, Ghulam Sajjad, Nawab Sher, Mubashir Aziz, Farhan Ahmed Siddiqui
In this article we describe development and validation of stability indicating, accurate, specific, precise and simple Ion-pairing RP-HPLC method for simultaneous determination of paracetamol and cetirizine HCl along with preservatives i.e. propylparaben, and methylparaben in pharmaceutical dosage forms of oral solution and in serum. Acetonitrile: Buffer: Sulfuric Acid (45:55:0.3 v/v/v) was the mobile phase at flow rate 1.0 mL min(-1) using a Hibar(®) Lichrosorb(®) C18 column and monitored at wavelength of 230nm...
2016: Open Medicinal Chemistry Journal
Hong Sun, Yunhai Bo, Mingjie Zhang, Xiao Wu, Mingyang Zhou, Longshan Zhao, Zhili Xiong
In the present work, a simple, rapid and reliable ultra high performance liquid chromatography -tandem mass spectrometric (UHPLC-MS/MS) method was developed and validated to simultaneously determine epalrestat (EPA) and puerarin (PUE) in rat plasma for evaluation the pharmacokinetic interaction of this two drugs. Both the analytes and glipizide (IS) were extracted using protein precipitation method. The separation was performed on C18 reversed phase column using acetonitrile and 5 mmol/L ammonium acetate in water as mobile phase with a gradient elution program...
September 21, 2016: Biomedical Chromatography: BMC
Madeleine J Swortwood, Matthew N Newmeyer, Maria Andersson, Osama A Abulseoud, Karl B Scheidweiler, Marilyn A Huestis
Oral fluid (OF) is an important matrix for monitoring drugs. Smoking cannabis is common, but vaporization and edible consumption also are popular. OF pharmacokinetics are available for controlled smoked cannabis, but few data exist for vaporized and oral routes. Frequent and occasional cannabis smokers were recruited as participants for four dosing sessions including one active (6.9% Δ(9) -tetrahydrocannabinol, THC) or placebo cannabis-containing brownie, followed by one active or placebo cigarette, or one active or placebo vaporized cannabis dose...
September 19, 2016: Drug Testing and Analysis
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