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Oral liquid compounding

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https://www.readbyqxmd.com/read/29145890/pharmacokinetic-study-of-single-and-multiple-dosing-with-metolazone-tablets-in-healthy-chinese-population
#1
Xueqing Li, Rutao Wang, Yang Liu, Yun Liu, Heng Zheng, Yabo Feng, Na Zhao, Hongbin Geng, Wanzhi Zhang, Aidong Wen
BACKGROUND: Metolazone is a diuretic, saluretic and antihypertensive chemical compound from the quinazoline category that possesses medicinal features similar to those of other thiazide diuretic drugs. However, the pharmacokinetics of metolazone in the Chinese population has rarely been studied. This study aimed to examine the pharmacokinetic characteristics, safety characteristic, and tolerability of metolazone in healthy Chinese subjects after single and multiple doses taken orally as well as the effects that food and gender have on oral metolazone pharmacokinetic parameters...
November 16, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29142437/docking-based-screening-of-ficus-religiosa-phytochemicals-as-inhibitors-of-human-histamine-h2-receptor
#2
Amit Chaudhary, Birendra Singh Yadav, Swati Singh, Pramod Kumar Maurya, Alok Mishra, Shweta Srivastva, Pritish Kumar Varadwaj, Nand Kumar Singh, Ashutosh Mani
Background: Ficus religiosa L. is generally known as Peepal and belongs to family Moraceae. The tree is a source of many compounds having high medicinal value. In gastrointestinal tract, histamine H2 receptors have key role in histamine-stimulated gastric acid secretion. Their over stimulation causes its excessive production which is responsible for gastric ulcer. Objective: This study aims to screen the range of phytochemicals present in F. religiosa for binding with human histamine H2 and identify therapeutics for a gastric ulcer from the plant...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29135439/biological-cleavage-of-the-c-p-bond-in-perfluoroalkyl-phosphinic-acids-in-male-sprague-dawley-rats-and-the-formation-of-persistent-and-reactive-metabolites
#3
Shira Joudan, Leo W Y Yeung, Scott A Mabury
BACKGROUND: Perfluoroalkyl phosphinic acids (PFPiAs) have been detected in humans, wildlife, and various environmental matrices. These compounds have been used with perfluoroalkyl phosphonic acids (PFPAs) as surfactants in consumer products and as nonfoaming additives in pesticide formulations. Unlike the structurally related perfluoroalkyl sulfonic and carboxylic acids, little is known about the biological fate of PFPiAs. OBJECTIVES: We determined the biotransformation products of PFPiAs and some pharmacokinetic parameters in a rat model...
November 3, 2017: Environmental Health Perspectives
https://www.readbyqxmd.com/read/29113958/comparison-of-two-jatropha-species-euphorbiaceae-used-popularly-to-treat-snakebites-in-northeastern-brazil-chemical-profile-inhibitory-activity-against-bothrops-erythromelas-venom-and-antibacterial-activity
#4
Juliana Félix-Silva, Jacyra A S Gomes, Júlia M Fernandes, Angela K C Moura, Yamara A S Menezes, Elizabeth C G Santos, Denise V Tambourgi, Arnóbio A Silva-Junior, Silvana M Zucolotto, Matheus F Fernandes-Pedrosa
ETHNOPHARMACOLOGICAL RELEVANCE: Jatropha species (Euphorbiaceae) are largely used in traditional medicine to treat different pathologies in Africa, Asia and Latin America. In Northeastern Brazilian folk medicine, several Jatropha species, such as Jatropha gossypiifolia L. and Jatropha mollissima (Pohl) Baill., are indistinctly used to treat snakebites. AIM OF THE STUDY: To compare two of the Brazilian most used Jatropha species for snakebites (J. gossypiifolia and J...
November 4, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29113503/effects-of-crystalline-state-and-self-nanoemulsifying-drug-delivery-system-snedds-on-oral-bioavailability-of-the-novel-anti-hiv-compound-6-benzyl-1-benzyloxymethyl-5-iodouracil-in-rats
#5
Ying-Yuan Lu, Wen-Bing Dai, Xin Wang, Xiao-Wei Wang, Jun-Yi Liu, Pu Li, Ya-Qing Lou, Chuang Lu, Qiang Zhang, Guo-Liang Zhang
The objective of this study was to investigate the effect of crystalline state and a formulation of self-nanoemulsifying drug delivery system (SNEDDS) on oral bioavailability of 6-benzyl-1-benzyloxymethyl-5-iodouracil (W-1), a novel non-nucleoside reverse transcriptase inhibitor, in rats. The crystalline states of W-1 were characterized by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). The SNEDDS was formulated by medium-chain lipids, characterized by droplet particle size...
November 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29112179/green-ultrasound-versus-conventional-synthesis-and-characterization-of-specific-task-pyridinium-ionic-liquid-hydrazones-tethering-fluorinated-counter-anions-novel-inhibitors-of-fungal-ergosterol-biosynthesis
#6
Nadjet Rezki, Salsabeel A Al-Sodies, Sheikh Shreaz, Rayees Ahmad Shiekh, Mouslim Messali, Vaseem Raja, Mohamed R Aouad
A series of specific task ionic liquids (ILs) based on a pyridiniumhydrazone scaffold in combination with hexafluorophosphate (PF₆(-)), tetrafluoroboron (BF₄(-)) and/or trifluoroacetate (CF₃COO(-)) counter anion, were designed and characterized by IR, NMR and mass spectrometry. The reactions were conducted under both conventional and green ultrasound procedures. The antifungal potential of the synthesized compounds 2-25 was investigated against 40 strains of Candida (four standard and 36 clinical isolates)...
November 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29104273/study-of-absorption-characteristics-of-the-total-saponins-from-radix-ilicis-pubescentis-in-an-in-situ-single-pass-intestinal-perfusion-spip-rat-model-by-using-ultra-performance-liquid-chromatography-uplc
#7
Guojun Kuang, Huan Yi, Mingjuan Zhu, Jie Zhou, Xueying Shang, Zhongxiang Zhao, Chenchen Zhu, Qiongfeng Liao, Shixia Guan, Lei Zhang
In contrast to the extensively reported therapeutic activities, far less attention has been paid to the intestinal absorption of the total saponins from Radix Ilicis Pubescentis (in Chinese Mao-Dong-Qing, MDQ). This study aimed to investigate the intestinal absorption characteristics of ilexgenin A (C1), ilexsaponin A1 (C2), ilexsaponin B1 (C3), ilexsaponin B2 (C4), ilexsaponin B3 (DC1), and ilexoside O (DC2) when administrated with the total saponins from MDQ (MDQ-TS). An UPLC method for simultaneous determination of C1, C2, C3, C4, DC1, and DC2 in intestinal outflow perfusate was developed and validated...
November 1, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29095657/redispersible-spray-dried-lipid-core-nanocapsules-intended-for-oral-delivery-the-influence-of-the-particle-number-on-redispersibility
#8
Diego Fontana de Andrade, Branko Vukosavljevic, Edilson Valmir Benvenutti, Adriana Raffin Pohlmann, Sílvia Stanisçuaski Guterres, Maike Windbergs, Ruy Carlos Ruver Beck
This study proposes a new approach to produce easily redispersible spray-dried lipid-core nanocapsules (LNC) intended for oral administration, evaluating the influence of the particle number density of the fed sample. The proposed approach to develop redispersible spray-dried LNC formulations intended for oral route is innovative, evidencing the needing of an optimization of the initial particle number density in the liquid suspension of nanocapsules. A mixture of maltodextrin and L-leucine (90:10 w/w) was used as drying adjuvant...
November 2, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29084165/simultaneous-determination-of-twenty-five-compounds-in-rat-plasma-using-ultra-high-performance-liquid-chromatography-polarity-switching-tandem-mass-spectrometry-and-its-application-to-a-pharmacokinetic-study
#9
Na Zhang, Yueting Li, Jing Sun, Chun Li, Yuelin Song, Jun Li, Pengfei Tu, Yunfang Zhao
An attempt was made to characterize the pharmacokinetic profiles of Qishen Keli (QSKL) that has been widely proved to be effective in clinical practice. A method using ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS/MS) for the simultaneous determination of 25 analytes in rat plasma was developed and validated. Satisfactory chromatographic separation was achieved on an ACQUITY UPLC HSS T3 column with gradient elution using mobile phase consisting of 0.02% aqueous formic acid (A) and acetonitrile fortified with 0...
October 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29078252/analysis-of-new-psychoactive-substances-in-oral-fluids-by-means-of-microextraction-by-packed-sorbent-followed-by-uhplc-ms-ms
#10
Rachele Rocchi, Maria Chiara Simeoni, Camilla Montesano, Gabriele Vannutelli, Roberta Curini, Manuel Sergi, Dario Compagnone
In recent years, new drugs, commonly known as "new psychoactive substances" (NPS), appeared on the market, which include, among others, synthetic cannabinoids, cathinones and tryptamine analogs of psilocin. The aim of this work was to develop and validate a new method for simultaneous screening and quantification of 31 NPS in oral fluid by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). The chosen target analytes represented different chemical and toxicological NPS classes, such as synthetic cathinones, piperazines, phenethylamines, synthetic cannabinoids and their metabolites...
October 27, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29055030/identification-of-absorbed-constituents-and-in-vivo-metabolites-in-rats-after-oral-administration-of-physalisalkekengi-var-franchetii-by-ultrahigh-pressure-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry
#11
Xinchi Feng, Xiaoguang Huo, Hongxia Liu, Liwei Chai, Liqin Ding, Feng Qiu
The calyces of Physalisalkekengi var. franchetii (Chinese Lantern, JDL) are well-known traditional Chinese medicine owing to its various therapeutic effects. However, the bioactive constituents responsible for the pharmacological effects of JDL and their metabolites in vivo are still unclear to date. In this paper, an ultrahigh-pressure liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF-MS/MS) method was established to identify absorbed constituents and in vivo metabolites in rat biological fluids after oral administration of JDL...
October 20, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29045620/determination-and-pharmacokinetics-of-wga-in-rat-plasma-by-lc-ms-after-oral-administration-of-xanthoceras-sorbifolia-bunge-extract
#12
Junhong Ling, Nan Wang, Shaoning Wang, Yingchun Liu, Dandan Xia, Kaishun Bi
3-O-(3-O-angeloyl-6-O-β-D-glucopyranosyl)-β-D-glucopyranosyl-28-O-(2-α-L-rhamnopyranosyl-6-O-β-D-glucopyranosyl)-β-D-glucopyranosyl-16-deoxybarringtogenol A (WGA) is a potential anti-AD (Alzheimer's disease) active compound isolated from the husks of Xanthoceras sorbifolia Bunge. A rapid and accurate high-performance liquid chromatography-mass spectrometry (LC-MS) method was developed and validated for the quantification of WGA in rat plasma. Digoxin was used as internal standard (IS). Sample preparation was performed by liquid-liquid extraction using ethyl acetate-isopropanol (1:1, v/v)...
October 17, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29043410/determination-of-the-absolute-oral-bioavailability-of-niraparib-by-simultaneous-administration-of-a-14-c-microtracer-and-therapeutic-dose-in-cancer-patients
#13
L van Andel, H Rosing, Z Zhang, L Hughes, V Kansra, M Sanghvi, M M Tibben, A Gebretensae, J H M Schellens, J H Beijnen
INTRODUCTION: Niraparib (Zejula™) is a poly(ADP-ribose) polymerase inhibitor recently approved by the US Food and Drug Administration for the maintenance treatment of patients with recurrent platinum-sensitive epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. The pivotal phase III clinical trial has shown improved progression-free survival in patients receiving niraparib compared with those receiving placebo...
October 17, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29036309/chiral-analysis-of-methamphetamine-in-oral-fluid-samples-a-method-to-distinguish-licit-from-illicit-drug-use
#14
Damon Borg, Elizabeth Kolb, Cindy Lantigua, Richard Stripp
Methamphetamine (MAMP) is a popular illicit drug abused for its central nervous system stimulating effects. MAMP is also used therapeutically in the treatment of overeating disorders, narcolepsy, attention deficit disorder, in over-the-counter (OTC) products to ease nasal congestion. MAMP exists in two enantiomeric forms, dextrorotary (d-MAMP) or levorotary (l-MAMP). The compounds are similar in chemical structure, simply differing in the orientation of functional groups around the asymmetric carbon. In part because of the availability of l-MAMP in OTC nasal inhalers, forensic guidelines require a sample to contain greater than 20% d-MAMP to consider illicit drug use when interpreting results...
September 25, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29027933/dpph-radical-scavenging-and-postprandial-hyperglycemia-inhibition-activities-and-flavonoid-composition-analysis-of-hawk-tea-by-uplc-dad-and-uplc-q-tof-ms-e
#15
Xuan Xiao, Lijia Xu, Huagang Hu, Yinjun Yang, Xinyao Zhang, Yong Peng, Peigen Xiao
Hawk tea (Litsea coreana Lévl. var. Lanuginosa (Migo) Yen C. Yang & P.H. Huang), a very popular herbal tea material, has attracted more and more attention due to its high antioxidant properties and possible therapeutic effect on type II diabetes mellitus. The raw materials of Hawk tea are usually divided into three kinds: bud tea (BT), primary leaf tea (PLT) and mature leaf tea (MLT). In this study, the DPPH radical scavenging activity and the antimicrobial properties of these three kinds of Hawk tea from different regions were comparatively investigated, and a ultra-high performance liquid chromatographic coupled with a photodiode array detector (UPLC-DAD) method was employed for comparison of the three major flavonoid constituents, including hyperoside, isoquercitrin and astragalin, in different samples of Hawk tea...
October 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29021702/biotransformation-of-panax-ginseng-extract-by-rat-intestinal-microflora-identification-and-quantification-of-metabolites-using-liquid-chromatography-tandem-mass-spectrometry
#16
Wei-Wei Dong, Jinhua Zhao, Fei-Liang Zhong, Wen-Jing Zhu, Jun Jiang, Songquan Wu, Deok-Chun Yang, Donghao Li, Lin-Hu Quan
BACKGROUND: In general, after Panax ginseng is administered orally, intestinal microbes play a crucial role in its degradation and metabolization process. Studies on the metabolism of P. ginseng by microflora are important for obtaining a better understanding of their biological effects. METHODS: In vitro biotransformation of P. ginseng extract by rat intestinal microflora was investigated at 37°C for 24 h, and the simultaneous determination of the metabolites and metabolic profile of P...
October 2017: Journal of Ginseng Research
https://www.readbyqxmd.com/read/28994740/antibacterial-and-antitubercular-activities-of-cinnamylideneacetophenones
#17
Carlos R Polaquini, Guilherme S Torrezan, Vanessa R Santos, Ana C Nazaré, Débora L Campos, Laíza A Almeida, Isabel C Silva, Henrique Ferreira, Fernando R Pavan, Cristiane Duque, Luis O Regasini
Cinnamaldehyde is a natural product with broad spectrum of antibacterial activity. In this work, it was used as a template for design and synthesis of a series of 17 cinnamylideneacetophenones. Phenolic compounds 3 and 4 exhibited MIC (minimum inhibitory concentration) and MBC (minimum bactericidal concentration) values of 77.9 to 312 µM against Staphylococcus aureus, Streptococcus mutans, and Streptococcus sanguinis. Compounds 2, 7, 10, and 18 presented potent effects against Mycobacterium tuberculosis (57...
October 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28991379/a-target-and-non-target-strategy-for-identification-or-characterization-of-the-chemical-ingredients-in-chinese-herb-preparation-shuang-huang-lian-oral-liquid-by-ultra-performance-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry
#18
Feng-Xiang Zhang, Min Li, Zhi-Hong Yao, Chang Li, Li-Rui Qiao, Xiu-Yu Shen, Kate Yu, Yi Dai, Xin-Sheng Yao
A target and non-target strategy based on in-house chemical components library was developed for rapid and comprehensive analysis of complicated components from traditional Chinese medicine (TCM) preparation Shuang-Huang-Lian oral liquid (SHL). The sample was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC/Qtof MS) using generic acquisition parameters. Automated detection and data filtering were performed on the UNIFI(TM) software and the detected peaks were evaluated against an in-house library...
October 9, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28990851/stability-study-of-a-clonidine-oral-solution-in-a-novel-vehicle-designed-for-pediatric-patients
#19
Arnaud Potier, Julien Voyat, Alain Nicolas
Clonidine hydrochloride is administered to opioid-addicted mothers' neonates to reduce neonatal abstinence syndrome. It is prescribed off-label to neonates at 0.5-1 µg/kg/6 h, alone or in combination. The commercially injectable form of clonidine-Catapressan(®) 0.15 mg/mL-is being orally given after an appropriate dilution in water. However, this practice is not suitable for a perfectly safe and accurate administration. The objectives were to design a 10 µg/mL oral solution of clonidine hydrochloride in Inorpha(®) and to study the stability of this solution by a validated stability-indicating liquid chromatography (LC) method...
October 24, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28990207/a-review-of-bioanalytical-quantitative-methods-for-selected-sphingosine-1-phosphate-s1p1-receptor-modulators
#20
REVIEW
Ranjeet Prasad Dash, Nuggehally R Srinivas, Rana Rais
Sphingosine 1-phosphate (S1P1 ) modulators provide an emerging therapeutic approach for various autoimmune disorders such as multiple sclerosis and psoriasis. Fingolimod is the first approved orally active, selective and potent drug of this class. Other drugs belonging to this class include siponimod, ponesimod, ceralifimod, amiselimod, CS-0777 and GSK2018682. However, due to the high protein binding, polarity and zwitter-ionic nature of the phosphate metabolite of parent drugs, it becomes challenging to optimize the extraction method for this class of compounds...
October 9, 2017: Biomedical Chromatography: BMC
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