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https://www.readbyqxmd.com/read/28231522/novel-2-3-disubstituted-quinazoline-4-3h-one-molecules-derived-from-amino-acid-linked-sulphonamide-as-a-potent-malarial-antifolates-for-dhfr-inhibition
#1
Tarosh S Patel, Satish F Vanparia, Urmila H Patel, Ritu B Dixit, Chaitanya J Chudasama, Bhavesh D Patel, Bharat C Dixit
An optimization of a modified Grimmel's method for N-heterocyclization of Leucine linked sulphonamide leading to 2,3-disustituted-4-quinazolin-(3H)-ones was accomplished. Further, nineteen hybrid quinazolinone motifs (5a-5s) were synthesized by N-heterocyclization reaction under microwave irradiation using TEAA (IL) as green solvent as well as catalyst. The in vitro screening of the hybrid entities against the plasmodium species P. falciparum yielded five antimalarial potent molecules 5g, 5l, 5m, 5n &5p owing comparable activity to the reference drugs...
February 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231051/short-communication-challenges-relating-to-comparison-of-flavonoid-glycosides-dissolution-profiles-from-sutherlandia-frutescens-products
#2
Oluchi N Mbamalu, James Syce, Halima Samsodien
Unlike the case of conventional drug formulations, dissolution tests have hitherto not been required for herbal medicinal products commercially available in South Africa. This study investigated dissolution of the South African Sutherlandia frutescens using selected flavonoid glycosides as marker compounds. Dissolution of markers was assessed in three dissolution media at pH 1.2, 4.5 and 6.8, and samples were analysed using a validated HPLC method. The dissolution profile of each marker varied for the different materials investigated...
March 1, 2017: Acta Pharmaceutica
https://www.readbyqxmd.com/read/28231003/utilization-of-gastrointestinal-simulator-gis-an-in-vivo-predictive-dissolution-methodology-coupled-with-computational-approach-to-forecast-oral-absorption-of-dipyridamole
#3
Kazuki Matsui, Yasuhiro Tsume, Susumu Takeuchi, Amanda Searls, Gordon L Amidon
Weakly basic drugs exhibit a pH-dependent dissolution profile in the gastrointestinal (GI) tract, making it difficult to predict their oral absorption profile. The aim of this study was to investigate the utility of the Gastrointestinal Simulator (GIS), a novel in vivo predictive dissolution (iPD) methodology, in predicting the in vivo behavior of the weakly basic drug, dipyridamole, when coupled with in silico analysis. The GIS is a multi-compartmental dissolution apparatus, which represents physiological gastric emptying in the fasted state...
February 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28230986/design-synthesis-and-evaluation-of-a-novel-series-of-oxadiazine-gamma-secretase-modulators-for-familial-alzheimer-s-disease
#4
Matthew G Bursavich, Bryce A Harrison, Raksha Acharya, Donald E Costa, Emily A Freeman, Hilliary E Hodgdon, Lori A Hrdlicka, Hong Jin, Sudarshan Kapadnis, Jeffrey S Moffit, Deirdre A Murphy, Scott Nolan, Holger Patzke, Cuyue Tang, Melody Wen, Gerhard Koenig, Jean-François Blain, Duane A Burnett
Herein we describe the design, synthesis and evaluation of a novel series of oxadiazine-based gamma secretase modulators obtained via isosteric amide replacement and critical consideration of conforma-tional restriction. Oxadiazine lead 47 possesses good in vitro potency with excellent predicted CNS drug-like properties and desirable ADME/PK profile. This lead compound demonstrated robust Aβ42 reductions and subsequent Aβ37 increases in both rodent brain and CSF at 30 mg/kg dosed orally.
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230972/paclitaxel-biosynthesis-adenylation-and-thiolation-domains-of-an-nrps-tyca-pheat-module-produce-various-arylisoserine-coa-thioesters
#5
Ruth Muchiri, Kevin D Walker
Structure-activity relationship studies show that the phenylisoserinyl moiety of paclitaxel is largely necessary for the effective anticancer activity. Several paclitaxel analogs with a variant isoserinyl sides chain have improved pharmaceutical properties over the parent drug. To produce the isoserinyl CoAs as intermediates needed for enzyme catalysis on a semibiosynthetic pathway to paclitaxel analogs, we repurposed the adenylation and thiolation domains of a non-ribosomal peptide synthetase (Phe-AT) to function as a CoA ligase...
February 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28230445/benchmarking-insulin-treatment-persistence-among-patients-with-type-2-diabetes-across-different-u-s-payer-segments
#6
Wenhui Wei, Jenny Jiang, Youbei Lou, Sohini Ganguli, Mark S Matusik
BACKGROUND: Treatment persistence with basal insulins is crucial to achieving sustained glycemic control, which is associated with a reduced risk of microvascular disease and other complications of type 2 diabetes (T2D). However, studies suggest that persistence with basal insulin treatment is often poor. OBJECTIVE: To measure and benchmark real-world basal insulin treatment persistence among patients with T2D across different payer segments in the United States...
March 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28230322/comparative-effectiveness-and-safety-of-different-basal-insulins-in-a-real-world-setting
#7
Linong Ji, Puhong Zhang, Dongshan Zhu, Juming Lu, Xiaohui Guo, Yangfeng Wu, Xian Li, Jiachao Ji, Weiping Jia, Wenying Yang, Dajin Zou, Zhiguang Zhou, Yan Gao, Satish K Garg, Changyu Pan, Jianping Weng, Sanjoy K Paul
AIMS: To compare glucose control and safety of different basal insulin (BI, including Insulin NPH, glargine and detemir) therapies in real-life clinical settings based on a large-scale registry study. METHODS: In this multi-center 6-month prospective observational study, patients with type 2 diabetes uncontrolled (HbA1c≥7%) by oral anti-diabetic drugs (OADs) and willing to initiate BI were enrolled from 209 hospitals of eight regions of China. Type and dose of BI were at the physician's discretion and patients' willingness...
February 23, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28230176/antithrombotic-therapy-for-patients-with-stemi-undergoing-primary-pci
#8
REVIEW
Francesco Franchi, Fabiana Rollini, Dominick J Angiolillo
Antithrombotic therapy, including antiplatelet and anticoagulant agents, is the cornerstone of pharmacological treatment to optimize clinical outcomes in patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary percutaneous coronary intervention (PPCI). Intravenous anticoagulant drugs available for PPCI include the indirect thrombin inhibitors unfractionated heparin and low-molecular-weight heparin, and the direct thrombin inhibitor bivalirudin. Intravenous antiplatelet drugs mainly include glycoprotein IIb/IIIa inhibitors and the P2Y12-receptor inhibitor cangrelor...
February 23, 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/28230172/evidence-for-critical-role-of-lymphocyte-cytosolic-protein-1-in-oral-cancer
#9
Nao Koide, Atsushi Kasamatsu, Yosuke Endo-Sakamoto, Sho Ishida, Toshihiro Shimizu, Yasushi Kimura, Isao Miyamoto, Shusaku Yoshimura, Masashi Shiiba, Hideki Tanzawa, Katsuhiro Uzawa
Lymphocyte cytosolic protein 1 (LCP1), a member of actin-binding protein of the plastin family, has been identified in several malignant tumors of non-hematopoietic sites, such as the colon, prostate, and breast. However, little is known about the roles of LCP1 in oral squamous cell carcinomas (OSCCs). This present study sought to clarify the clinical relevance of LCP1 in OSCCs and investigate possible clinical applications for treating OSCCs by regulating LCP1 expression. We found up-regulation of LCP1in OSCCs compared with normal counterparts using real-time quantitative reverse transcription polymerase chain reaction (qRT-PCR), immunoblotting, and immunohistochemistry (P < 0...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28230041/gefitinib-single-drug-in-treatment-of-advanced-esophageal-cancer
#10
Yingjun Xu, Zhihui Xie, Yan Shi, Mengwei Zhang, Jia Pan, Yanming Li, Hong Lu
OBJECTIVE: The objective of this study is to evaluate the clinical efficacy and toxicity of gefitinib single drug in treatment of advanced esophageal cancer. MATERIALS AND METHODS: Forty-one case of advanced esophageal cancer were included from February 2012 to June 2016 in the Department of Oncology, Huaihe Hospital of Henan University. All of the included 41 cases were pathology or cytology confirmed of esophageal cancer with advanced stage with previously chemotherapy regimen of cisplatin or fluorouracil...
December 2016: Journal of Cancer Research and Therapeutics
https://www.readbyqxmd.com/read/28229944/development-and-in-vivo-evaluation-of-an-innovative-hydrochlorothiazide-in-cyclodextrins-in-solid-lipid-nanoparticles-formulation-with-sustained-release-and-enhanced-oral-bioavailability-for-the-hypertension-treatment-in-pediatrics
#11
Marzia Cirri, Natascia Mennini, Francesca Maestrelli, Paola Mura, Carla Ghelardini, Lorenzo di Cesare Mannelli
An innovative pediatric oral formulation of hydrochlorothiazide (HCT) (2mg/mL), endowed with improved bioavailability and sustained release properties and suitable for the hypertension treatment in pediatric patients, was developed by combining the drug-cyclodextrin complexation and the incorporation of the complex into Solid Lipid Nanoparticles (SLN). Precirol(®)ATO5-based SLN, with two different surfactants (Pluronic(®)F68 and Tween(®)80) loaded with the drug as such or as binary system with hydroxypropyl-beta-cyclodextrin (HPβCd) and sulfobutyl-ether-beta-cyclodextrin (SBEβCd) both as physical mixture (P...
February 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28229907/expression-and-functional-evaluation-of-biopharmaceuticals-made-in-plant-chloroplasts
#12
REVIEW
Bei Zhang, Balamurugan Shanmugaraj, Henry Daniell
After approval of the first plant-made biopharmaceutical by FDA for human use, many protein drugs are now in clinical development. Within the last decade, significant advances have been made in expression of heterologous complex/large proteins in chloroplasts of edible plants using codon optimized human or viral genes. Furthermore, advances in quantification enable determination of in-planta drug dosage. Oral delivery of plastid-made biopharmaceuticals (PMB) is affordable because it eliminates prohibitively expensive fermentation, purification processes addressing major challenges of short shelf-life after cold storage...
February 21, 2017: Current Opinion in Chemical Biology
https://www.readbyqxmd.com/read/28229819/dabigatran-aggravates-topoisomerase-i-peptide-loaded-dendritic-cells-induced-lung-and-skin-fibrosis
#13
Heena Mehta, Philippe-Olivier Goulet, Jade Desjardins, Gemma Pérez, Martial Koenig, Jean-Luc Senécal, Marika Sarfati
OBJECTIVES: Dysregulated coagulation cascade has been implicated in development of fibrosis in systemic sclerosis (SSc). Thrombin, a key mediator of the coagulation pathway, has both proinflammatory and procoagulant properties. Here, we evaluated the efficacy of oral dabigatran, a direct thrombin inhibitor, on topoisomerase I dendritic cells (TOPOIA DCs)-induced lung and skin fibrosis, an experimental model of SSc. METHODS: Mice were repeatedly immunized with TOPOIA DCs...
February 8, 2017: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/28229530/an-audit-of-anticholinergic-medication-changes-in-older-hospitalised-patients-using-the-anticholinergic-drug-scale
#14
Michele Lee, Hugh Carl Hanger
OBJECTIVE: In patients discharged from an Older Person's Health hospital, we assessed 1) the prevalence of anticholinergic medications in this study population and 2) changes in anticholinergic drug burden during admission using the Anticholinergic Drug Scale (ADS). METHODS: Cases were identified between September 2010 and January 2011 using discharge coding data. Clinical notes were reviewed to determine which regular oral medications were commenced, altered or ceased during admission with their respective ADS level...
February 23, 2017: Internal Medicine Journal
https://www.readbyqxmd.com/read/28229376/the-pharmacogenetics-of-tacrolimus-in-corticosteroid-sparse-pediatric-and-adult-kidney-transplant-recipients
#15
Mads Juul Madsen, Troels K Bergmann, Kim Brøsen, Helle Charlotte Thiesson
INTRODUCTION: Tacrolimus is a calcineurin inhibitor used as an immunosuppressant drug in solid organ transplantation, and is mainly metabolized by cytochrome P450 (CYP) 3A4 and CYP3A5. Studies have shown an association between the CYP3A5 genotype and tacrolimus dose-adjusted trough concentrations. Variants in the genes PPARA, POR and CYP3A4 have recently been shown to influence tacrolimus metabolism. Furthermore, pharmacokinetic interaction between corticosteroid treatment and tacrolimus has been shown...
February 22, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28229374/effect-of-short-term-fasting-on-systemic-cytochrome-p450-mediated-drug-metabolism-in-healthy-subjects-a-randomized-controlled-crossover-study-using-a-cocktail-approach
#16
Laureen A Lammers, Roos Achterbergh, Ron H N van Schaik, Johannes A Romijn, Ron A A Mathôt
BACKGROUND AND OBJECTIVE: Short-term fasting can alter drug exposure but it is unknown whether this is an effect of altered oral bioavailability and/or systemic clearance. Therefore, the aim of our study was to assess the effect of short-term fasting on oral bioavailability and systemic clearance of different drugs. METHODS: In a randomized, controlled, crossover trial, 12 healthy subjects received a single administration of a cytochrome P450 (CYP) probe cocktail, consisting of caffeine (CYP1A2), metoprolol (CYP2D6), midazolam (CYP3A4), omeprazole (CYP2C19) and warfarin (CYP2C9), on four occasions: an oral (1) and intravenous (2) administration after an overnight fast (control) and an oral (3) and intravenous (4) administration after 36 h of fasting...
February 22, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28229274/oral-antiplatelet-drugs-in-patients-with-chronic-kidney-disease-ckd-a-review
#17
REVIEW
Homam Ibrahim, Sunil V Rao
Oral Antiplatelet Drugs (OAD) have a proven track record in the risk reduction of major cardiovascular events in patients with cardiovascular disease and normal kidney function. However, major gaps exist in our understanding of their effects on thrombosis and bleeding in chronic kidney disease (CKD). Clinical practice guidelines are ambiguous about use of such drugs in CKD patients, because patients with moderate to severe CKD were systematically excluded from clinical trials evaluating the efficacy and safety of OAD...
February 22, 2017: Journal of Thrombosis and Thrombolysis
https://www.readbyqxmd.com/read/28229223/levodopa-carbidopa-intestinal-gel-lcig-infusion-as-mono-or-combination-therapy
#18
Carsten Buhmann, R Hilker, P Lingor, C Schrader, J Schwarz, M Wolz, H Reichmann
Levodopa/carbidopa intestinal gel (LCIG) infusion is an effective escalating therapy in patients with Parkinson disease (PD) suffering from motor fluctuations and dyskinesia. Levodopa/carbidopa given continuously as infusion provides an optimized application of the most effective and best tolerable antiparkinsonian drug. It has been proven to have a superior motor effect compared with oral levodopa and to improve also non-motor symptoms. However, invasiveness, discomfort resulting from carrying an external device, and side effects associated with the way of administration limit its application in PD patients...
February 22, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28228783/-atypical-atypical-femur-fractures-and-use-of-bisphosphonates
#19
Denise M van de Laarschot, Matthijs P Somford, Agnes Jager, Edwin H Oei, P Koen Bos, M Carola Zillikens
BACKGROUND: Atypical femur fractures (AFFs) present a rare but serious condition associated with use of bisphosphonates. Underlying mechanisms and clinical risk factors remain unclear. According to the diagnostic criteria formulated by the ASBMR, a lateral localization of an AFF is required. CASE HISTORY: We present a patient who developed bilateral leg pain while using an oral bisphosphonate and aromatase inhibitor in the course of adjuvant treatment for breast cancer...
September 2016: Clinical Cases in Mineral and Bone Metabolism
https://www.readbyqxmd.com/read/28228617/silkworm-fungal-infection-model-for-identification-of-virulence-genes-in-pathogenic-fungus-and-screening-of-novel-antifungal-drugs
#20
Masaki Ishii, Yasuhiko Matsumoto, Ikuko Nakamura, Kazuhisa Sekimizu
The silkworm infection model has the potential to replace conventional animal models for evaluation of the efficacy and toxicity of investigational antifungal agents. Silkworms are relatively inexpensive, can be simply grown in large numbers and can be easily infected with pathogenic fungi, including mutant strains. Antifungal agents can then be injected into the silkworm either via the hemolymph to mimic intravenous administration or directly into the gut for oral administration, and their antifungal effect can be evaluated...
February 21, 2017: Drug Discoveries & Therapeutics
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