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https://www.readbyqxmd.com/read/29792353/gastroretentive-raft-liquid-delivery-system-as-a-new-approach-to-release-extension-for-carrier-mediated-drug
#1
Samar M Abouelatta, Ahmed A Aboelwafa, Omaima N El-Gazayerly
Gabapentin (GBP), an antiepileptic and anti-neuropathic agent, suffers from short half-life (5-7 h), has narrow absorption window, and is absorbed via carrier-mediated mechanism resulting in frequent dosing, poor compliance, and poor bioavailability (<60%). Moreover, GBP is a freely water-soluble drug, thus it is considered a challenging candidate to be formulated as extended release dosage form. In this study, raft forming systems were investigated as a potential drug delivery system for prolonging gastric residence time of GBP...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29790010/pectin-and-mucin-enhance-the-bioadhesion-of-drug-loaded-nanofibrillated-cellulose-films
#2
Patrick Laurén, Heli Paukkonen, Tiina Lipiäinen, Yujiao Dong, Timo Oksanen, Heikki Räikkönen, Henrik Ehlers, Päivi Laaksonen, Marjo Yliperttula, Timo Laaksonen
PURPOSE: Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS: Nanofibrillar cellulose and anionic type nanofibrillar cellulose were used as film forming materials with known mucoadhesive components mucin, pectin and chitosan as functional bioadhesion enhancers...
May 22, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29786965/l-and-d-threo-ethylphenidate-concentrations-pharmacokinetics-and-pharmacodynamics-in-horses
#3
Heather K Knych, Dan S McKemie, Kelsey Seminoff, Petra Hartmann, Lynn Hovda, Dionne Benson
Ethylphenidate is a psychostimulant and analogue of the commonly prescribed compound, methylphenidate (Ritalin®). There are a limited number of studies describing the disposition and pharmacologic/toxicological effects of ethylphenidate in any species. The abuse potential in equine athletes along with the limited data available regarding administration in horses necessitates further study. The objectives of the current study were to describe drug concentrations, develop an analytical method that could be used to regulate its use and describe the pharmacodynamic effects of ethylphenidate in horses...
May 22, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29782822/simultaneous-determination-of-intestinal-permeability-and-potential-drug-interactions-of-complex-mixtures-using-caco-2-cells-and-high-resolution-mass-spectrometry-studies-with-rauwolfia-serpentina-extract
#4
Thomas J Flynn, Sanah N Vohra
Caco-2 cells are a commonly used model for estimating the intestinal bioavailability of single chemical entity pharmaceuticals. Caco-2 cells, when induced with calcitriol, also express other biological functions such as phase I (CYP) and phase II (glucuronosyltransferases) drug metabolizing enzymes which are relevant to drug-supplement interactions. Intestinal bioavailability is an important factor in the overall safety assessment of products consumed orally. Foods, including herbal dietary supplements, are complex substances with multiple chemical components...
May 18, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29781217/uhplc-q-tof-ms-based-screening-and-identification-of-main-flavonoids-and-their-metabolites-in-rats-after-oral-administration-of-cirsium-japonicum-dc-extract
#5
Xia Zhang, Man Liao, Xiaoye Cheng, Caijuan Liang, Xinpeng Diao, Lantong Zhang
RATIONALE: Cirsium japonicum DC., a traditional Chinese medicine, has been shown to have antihemorrhagic and antitumour effects. Pharmacological studies have demonstrated that this curative effect may be related to flavonoids. The present work aims to screen and identify the main flavonoids and their corresponding metabolites in rats after oral administration of Cirsium japonicum DC. extract. METHODS: A rapid and simple ultra-high-performance liquid chromatography coupled with triple quadrupole and time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS) method was developed for the identification of the primary absorbing components and metabolites of the principal flavonoids...
May 20, 2018: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29781188/a-novel-anti-malarial-drug-derivative-inhibits-cyclic-gmp-amp-synthase-in-trex1-deficient-mice
#6
Jie An, Joshua J Woodward, Weinan Lai, Mark Minie, Xizhang Sun, Lena Tanaka, Jessica M Snyder, Tomikazu Sasaki, Keith B Elkon
OBJECTIVE: Type I interferon (IFN-I) is strongly implicated in the pathogenesis of Systemic Lupus Erythematosus (SLE) as well as rare monogenic 'interferonopathies' such as Aicardi-Goutieres Syndrome (AGS) caused by mutations in the DNA exonuclease, TREX1. The DNA-activated IFN-I pathway, cyclic GMP-AMP (cGAMP) synthase (cGAS), is linked to subsets of AGS and lupus. We identified inhibitors of DNA-cGAS interaction and tested lead candidate, X6, in a mouse model of AGS. METHODS: Trex1-/- mice were treated orally from birth with either X6 or HCQ for 8 weeks...
May 21, 2018: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29781175/translational-safety-biomarkers-of-colonic-barrier-integrity-in-the-rat
#7
Tim Erkens, Ruud Bueters, Marjolein van Heerden, Filip Cuyckens, Rob Vreeken, Nick Goeminne, Lieve Lammens
The intestinal barrier controls intestinal permeability, and its disruption has been associated with multiple diseases. Therefore, preclinical safety biomarkers monitoring barrier integrity are essential during the development of drugs targeting the intestines, particularly if starting treatment early after onset of disease. Classical toxicology endpoints are not sensitive enough and therefore our objective was to identify non-invasive markers enabling early in vivo detection of colonic barrier perturbation...
May 20, 2018: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29772457/in-vitro-and-in-vivo-metabolic-investigation-of-the-palbociclib-by-uhplc-q-tof-ms-ms-and-in-silico-toxicity-studies-of-its-metabolites
#8
Balasaheb B Chavan, Shristy Tiwari, Shankar G, Rakesh D Nimbalkar, Prabha Garg, Srinivas R, M V N Kumar Talluri
Palbociclib (PAB) is a CDK4/6 inhibitor and U. S Food and Drug Administration (FDA) granted regular approval for the treatment of hormone receptor (HR) positive, metastatic breast cancer in combination with an aromatase inhibitor in postmenopausal women. Metabolite identification is a crucial aspect during drug discovery and development as the drug metabolites may be pharmacologically active or possess toxicological activity. As there are no reports on the metabolism studies of the PAB, the present study focused on investigation of the in vitro and in vivo metabolic fate of the drug...
May 14, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29766657/drug-drug-interaction-and-doping-effect-of-non-prohibited-drugs-on-the-urinary-excretion-profile-of-methandienone
#9
Monica Mazzarino, Franziska L Khevenhüller-Metsch, Ilaria Fiacco, Maria Kristina Parr, Xavier de la Torre, Francesco Botrè
The potential consequences of drug-drug interactions on the excretion profile of the anabolic androgenic steroid methandienone (17β-hydroxy-17α-methylandrosta-1,4-dien-3-one) are discussed here. More specifically, we have evaluated by in vitro and in vivo experiments the effects of seven non-prohibited drugs (fluconazole, ketoconazole, itraconazole, miconazole, fluoxetine, paroxetine and nefazodone) on the main metabolic pathways of methandienone. These are selected among those most commonly used by the athletes...
May 15, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29766610/sensitive-and-simultaneous-quantitation-of-6%C3%AE-hydroxycortisol-and-cortisol-in-human-plasma-by-lc-ms-ms-coupled-with-stable-isotope-dilution-method
#10
Ryohei Hirano, Akitomo Yokokawa, Takashi Furuta, Hiromi Shibasaki
CYP3A phenotyping provide a means for personalized drug therapy. We focused our attention on the plasma 6β-hydroxycortisol (6β-OHF) to cortisol ratio as an index for CYP3A phenotyping. In the present study, we developed a sensitive and reliable method for the simultaneous determination of 6β-OHF and cortisol in human plasma using high-performance liquid chromatography/tandem mass spectrometry (LC-MS/MS) together with picolinylester derivatization or nonderivatization methods and 6β-[9,11,12,12-2 H4 ]hydroxycortisol and [1,2,4,19-13 C4 ]cortisol as internal standards for in vivo CYP3A phenotyping in humans...
May 15, 2018: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/29766296/characterization-of-in-vivo-metabolites-in-rat-urine-following-an-oral-dose-of-masitinib-by-liquid-chromatography-tandem-mass-spectrometry
#11
Adnan A Kadi, Sawsan M Amer, Hany W Darwish, Mohamed W Attwa
Masitinib (MST) is an orally administered drug that targets mast cells and macrophages, important cells for immunity, by inhibiting a limited number of tyrosine kinases. It is currently registered in Europe and USA for the treatment of mast cell tumors in dogs. AB Science announced that the European Medicines Agency has accepted a conditional marketing authorization application for MST to treat amyotrophic lateral sclerosis. In our work, we focused on studying in vivo metabolism of MST in Sprague-Dawley rats...
May 15, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29760572/breath-powered-sumatriptan-dry-nasal-powder-an-intranasal-medication-delivery-system-for-acute-treatment-of-migraine
#12
REVIEW
Stewart J Tepper, Merrilee R Johnstone
There is a need for fast-acting, non-oral medication options for migraine because some attacks develop rapidly and some are accompanied by nausea, vomiting, and gastroparesis, which can hinder oral medication uptake and absorption. The most commonly prescribed migraine medications are oral triptans, with sumatriptan as the most common. However, oral triptans are associated with adverse events (AEs) of atypical sensations that may be problematic for patients. Subcutaneous (SC) injectable sumatriptan and conventional liquid triptan nasal spray formulations are also available, but the frequency of atypical sensations is the highest with SC sumatriptan, and the intense bitter taste of conventional liquid triptan nasal spray discourages use...
2018: Medical Devices: Evidence and Research
https://www.readbyqxmd.com/read/29753212/quantification-of-doping-compounds-in-faecal-samples-from-racing-pigeons-by-liquid-chromatography-tandem-mass-spectrometry
#13
Fernando X Moreira, Renata Silva, Maria B André, Paula G de Pinho, Maria L Bastos, João Ruivo, Patrícia Ruivo, Helena Carmo
The use of performance enhancing drugs is not only common in humans, but also in animal sports, including racing of horses, greyhounds and pigeons. The development of accurate analytical procedures to detect doping agents in sports is crucial in order to protect the fair-play of the game, avoid financial fraud in the attribution of eventual awards and, even more important, to protect the animals from harmful drugs and/or dangerous dosage regimens. The present study aimed to develop and validate, a method that enabled the screening and confirmation of the presence of a beta-agonist (clenbuterol) and three corticosteroids (betamethasone, prednisolone and budesonide) in faeces from pigeons...
May 4, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29751639/novel-neuroprotective-lead-compound-ligustrazine-derivative-mass-spectrometry-fragmentation-rule-and-metabolites-in-rats-by-lc-ltq-orbitrap-ms
#14
Xinyu Zhang, Rui Zhao, Meng Chen, Tao Ma, Gaorong Wu, Nannan Xue, Guoliang Li, Hui Wang, Kang Fang, Wenxi Zhang, Penglong Wang, Haimin Lei
The neuroprotective evaluation of ligustrazine derivatives has become a research focus all over the world. A novel ligustrazine derivative, (3,5,6-Trimethylpyrazin-2-yl)methyl(E)-3-(4-((3,5,6-trimethylpyrazin-2-l)methoxy)phenyl)acrylate (T-CA), has shown protective effects against CoCl₂-induced neurotoxicity in a differentiated PC12 cell model and middle cerebral artery occlusion (MCAO) model in our previous studies. However, nearly none of the parent drugs existed after rapid metabolism due to uncertain reasons...
May 11, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29749718/bioequivalence-evaluation-of-two-oral-formulations-of-acetaminophen-in-healthy-subjects-results-from-a-randomized-single-blind-crossover-study
#15
Luis García Aguirre, Carlos Bohorquez Nassar, Isabel Ruiz Olmedo, Lara Dennie, Araceli G Medina Nolasco
Despite widespread availability of acetaminophen in Mexico, data on its pharmacokinetic properties in Mexican populations are limited. This single-center, single-blind, randomized, 2-period, 2-treatment, crossover, single-dose-per-period, 2-sequence study evaluated the bioequivalence of a test acetaminophen product available in Mexico compared with a reference 500-mg acetaminophen product in 28 healthy adults under fasting conditions. Blood samples were collected predose and at specified intervals across a 16-hour period following administration and were analyzed for acetaminophen using a validated reverse-phase high-performance liquid chromatography method...
May 11, 2018: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29748821/absorption-distribution-metabolism-and-excretion-of-the-novel-helicase-primase-inhibitor-amenamevir-asp2151-in-rodents
#16
Yoshiaki Ohtsu, Yoko Susaki, Kiyoshi Noguchi
BACKGROUND AND OBJECTIVES: The helicase-primase inhibitor amenamevir (ASP2151) is a novel therapeutic agent which has been approved for the treatment of herpes zoster. The present study examined the pharmacokinetic profile of amenamevir in rodents and compared it with data from the literature of past and current established therapies (acyclovir and valaciclovir) to provide additional data to facilitate drug discovery and proper drug use. METHODS: In situ absorption, blood and plasma radioactivity concentrations, tissue distribution, and excretion were determined using liquid scintillation counting...
May 10, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29747645/biopharmaceutical-insights-of-particulate-emulsified-systems-a-prospective-overview
#17
REVIEW
Jyothshna Devi Katamreddy, Prasanna Raju Yalavarthi, Subba Rao D, Sowjanya Battu, Jaya Preethi Peesa
During the twenty-first century, drug discovery is expanding rapidly and a large number of chemical moieties are recognized. Many of them are poorly soluble and hence related biopharmaceutical constraints are to be addressed systematically. Among novel approaches to resolving biopharmaceutical issues, micro- and nano-emulsified systems serve as the best strategy for delivering both hydrophobic and hydrophilic drugs owing to their greater solubilization and transportation capabilities. Of late, the unique physical and biopharmaceutical properties of these liquid isotropic homogenous systems have gained substantive research importance...
May 10, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29745346/orodispersible-films-a-systematic-patent-review
#18
Ashwini Deshpande, Chaitrali Gijare
BACKGROUND: In Recent years, oral film technology is aimed by the research groups. Oral film technology (OFT) has gained much attention among all the oral drug delivery systems. Fast dissolving film, fast disintegrating film and orodispersible film are some alternative words for this dosage form. Without a need of liquid for administration this dosage form dissolves in the mouth. Typically, fast dissolving film dissolves from 1 to 30 seconds. OBJECTIVE: At the root of this originality, many researchers patented their work on the aspect of orodispersible films using different drugs, polymers, excipients and employing methods of preparation...
May 8, 2018: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/29738964/capillary-ultra-performance-liquid-chromatography-tandem-mass-spectrometry-analysis-of-tienilic-acid-metabolites-in-urine-following-intravenous-administration-to-the-rat
#19
Adam M King, Isobelle Grant, Paul D Rainville, Giorgis Isaac, Muireann Coen, Ian D Wilson, Robert S Plumb
Capillary scale (100 mm × 150 μm id) UPLC/MS/MS, performed using reversed-phase gradient chromatography on sub 2 μm particles, has been successfully employed for the characterization of the metabolites of the drug tienilic acid (TA) excreted via the urine following oral administration to the rat. The capillary LC system provided a significant increase (range ca. 11-33-fold) in sensitivity compared with a conventional 150 mm × 2.1 mm id UPLC system. An investigation of the effect of the injection volume and sample mass loading on the capillary column on the results obtained for both endogenous metabolites and TA was performed...
April 26, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29737303/curative-effect-of-oral-ulcer-powder-on-the-treatment-of-recurrent-aphthous-ulcer
#20
Shenshan Zhu, Qiaoyun Shi, Jian Lu
Recurrent aphthous ulcer (RAU) is a common and frequently occurring disease in the Department of Stomatology. The clinical manifestations are localized ulcer of oral mucosa, and the ulcer mask is self limiting and easy to recur. In this paper, by adopting the randomized study method, the author study the effect of oral ulcer powder combined with traditional Chinese drugs on patients with recurrent aphthous ulcer, and analyze its effect on inflammatory factor. Kangfuxin liquid combined with oral ulcer powder helps reduce recurrent aphthous ulcer patients the levels of inflammatory factors, improve the symptoms of pain...
May 2018: Pakistan Journal of Pharmaceutical Sciences
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