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https://www.readbyqxmd.com/read/28822220/eremophilane-type-sesquiterpenes-from-fungi-and-their-medicinal-potential
#1
Kamila Tomoko Yuyama, Diana Fortkamp, Wolf-Rainer Abraham
Eremophilanes are sesquiterpenes with a rearranged carbon skeleton formed both by plants and fungi, however, almost no plant eremophilanes are found in fungi. These eremophilanes possess mainly phytotoxic, antimicrobial, anticancer and immunomodulatory properties and in this review fungal eremophilanes with bioactivities of potential medicinal applications are reviewed and discussed. A special focus is set on natural products bearing highly functionalized fatty acids at C-1 or C-3 position of the eremophilane backbone...
August 28, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28822201/-pharmacokinetic-research-strategies-of-compatibilities-and-synergistic-effects-of-classical-danshen-herb-pairs-based-on-pharmacokinetics-of-danshen-bingpian-and-danshen-honghua
#2
Cui-Ying Zhang, Wei-Guang Ren
Herb pairs are usual clinical compatibility forms and one of compound prescription sources in Chinese medicine. Pharmacokinetic research in vivo is one of the important items in elucidating the mechanism for synergistic and attenuated mechanisms of herb pairs. The paper comprehensively summarized and systemized the pharmacokinetic researches of marker-ingredients about Danshen-Honghua and Danshen-Bingpian in order to elucidate the rationality and scientificity of herb pairs and provide some feasible suggestions on the pharmacokinetics of drugs in the future...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822195/-pharmacokinetics-of-%C3%AE-asarone-after-intranasal-and-intravenous-administration-with-pla-%C3%AE-asarone-nanoparticles
#3
Jin Lu, Li-Wei Guo, Ting-Ming Fu, Guo-Long Zhu, Zhen-Nan Dai, Guan-Jun Zhan, Li-Li Chen
PLA-α-asarone nanoparticles were prepared by using organic solvent evaporation method, and their in vivo distribution and brain targeting after intranasal administration were studied as compared with intravenous administration. The results showed that brain targeting coefficient of PLA-α-asarone nanoparticles after intranasal and intravenous administration was 1.65 and 1.16 respectively. The absolute bioavailability, brain-targeting efficiency and the percentage of nasal-brain delivery of PLA-α-asarone nanoparticles were 74...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822164/-analysis-on-microdialysis-probe-recovery-of-baicalin-in-vitro-and-in-vivo-based-on-lc-ms-ms
#4
Teng-Fei Chen, Jian-Xun Liu, Ying Zhang, Li Lin, Wen-Ting Song, Ming-Jiang Yao
To further study the brain behavior and the pharmacokinetics of baicalin in intercellular fluid of brain, and study the recovery rate and stability of brain and blood microdialysis probe of baicalin in vitro and in vivo. The concentration of baicalin in brain and blood microdialysates was determined by LC-MS/MS and the probe recovery for baicalin was calculated. The effects of different flow rates (0.50, 1.0, 1.5, 2.0,3.0 μL•min⁻¹) on recovery in vitro were determined by incremental method and decrement method...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822161/-synergistic-mechanism-of-traditional-chinese-medicine-based-on-target-combination-of-pept1-and-ppar%C3%AE
#5
Lian-Sheng Qiao, Yan-Kun Chen, Gang-Gang Luo, Fang Lu, Si-Jia Liu, Gong-Yu Li, Yan-Ling Zhang
Synergistic effect is main pharmacological mechanism of traditional Chinese medicine(TCM). The research method based on the key targets combination is an important method to explore the synergistic effect of TCM. Peptide transporter 1 (PepT1) is an essential target for drug uptake into the bloodstream, accounting for about 50% of the total transporter protein content from the small intestine. Peroxisome proliferator-activated receptor α(PPARα) is the lipid-lowering target of fibrates, which have a good hypolipidemic effect by activating PPARα...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822051/new-basal-insulins-a-clinical-perspective-of-their-use-in-the-treatment-of-type-2-diabetes-and-novel-treatment-options-beyond-basal-insulin
#6
REVIEW
Patrick F Frias, Juan Pablo Frias
PURPOSE OF REVIEW: The purpose of this review was to review advances in basal insulin formulations and new treatment options for patients with type 2 diabetes not achieving glycemic targets despite optimized basal insulin therapy. RECENT FINDINGS: Advances in basal insulin formulations have resulted in products with increasingly favorable pharmacokinetic and pharmacodynamic properties, including flatter, peakless action profiles, less inter- and intra-patient variability, and longer duration of activity...
August 18, 2017: Current Diabetes Reports
https://www.readbyqxmd.com/read/28822046/body-mass-index-and-clinical-response-to-intravenous-or-subcutaneous-abatacept-in-patients-with-rheumatoid-arthritis
#7
Maria-Antonietta D'Agostino, Rieke Alten, Eduardo Mysler, Manuela Le Bars, June Ye, Bindu Murthy, Julia Heitzmann, Radu Vadanici, Gianfranco Ferraccioli
This post hoc analysis of ACQUIRE (NCT00559585) explored the effect of baseline body mass index (BMI) on the pharmacokinetics of and clinical response to subcutaneous (SC) or intravenous (IV) abatacept in patients with rheumatoid arthritis (RA). ACQUIRE was a phase 3b, 6-month, double-blind, double-dummy study in which patients with RA were randomized (1:1) to SC (fixed - dose; 125 mg/week) or IV (weight-tiered; ~ 10 mg/kg/month) abatacept plus methotrexate. In this analysis, minimum abatacept plasma concentration (Cmin) was measured at 3 and 6 months, and clinical remission over 6 months was assessed by Disease Activity Score 28 (C-reactive protein; DAS28 [CRP], < 2...
August 18, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28821484/measurement-and-mathematical-characterization-of-cell-level-pharmacokinetics-of-antibody-drug-conjugates-a-case-study-with-trastuzumab-vc-mmae
#8
Aman P Singh, Dhaval K Shah
The main objective of this work was to understand and mathematically characterize the cellular disposition of a tool ADC, trastuzumab-vc-MMAE (T-vc-MMAE). Towards this goal, three different analytical methods were developed to measure the concentrations of different ADC related analytes in the media and cell lysate. An LC-MS/MS method was developed to quantify unconjugated drug (i.e. MMAE) concentrations, a forced deconjugation method was developed to quantify total drug concentrations, and an ELISA method was developed to quantify total antibody (i...
August 18, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28821462/ferritin-nanocage-with-intrinsically-disordered-proteins-and-affibody-a-platform-for-tumor-targeting-with-extended-pharmacokinetics
#9
Na Kyeong Lee, Eun Jung Lee, Soyoun Kim, Gi-Hoon Nam, Minwoo Kih, Yeonsun Hong, Cherlhyun Jeong, Yoosoo Yang, Youngro Byun, In-San Kim
Ferritin nanocages are of particular interest as a novel platform for drug and vaccine delivery, diagnosis, biomineralization scaffold and more, due to their perfect and complex symmetry, ideal physical properties, high biocompatibility, low toxicity profiles as well as easy manipulation by genetic or chemical strategies. However, a short half-life is still a hurdle for the translation of ferritin-based nanomedicines into the clinic. Here, we developed a series of rationally designed long circulating ferritin nanocages (LCFNs) with 'Intrinsically Disordered Proteins (IDP)' as a stealth layer for extending the half-life of ferritin nanocages...
August 15, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28821438/effect-of-lipid-emulsion-infusion-on-paliperidone-pharmacokinetics-in-the-acute-overdose-rat-model-a-potential-emergency-treatment-for-paliperidone-intoxication
#10
Tomoyuki Enokiya, Erquan Zhang, Kenji Ikemura, Yuichi Muraki, Yoshiaki Iwashita, Takuya Iwamoto, Hiroshi Imai, Kazuo Maruyama, Masahiro Okuda
Paliperidone prolongs cardiac repolarization in a concentration-dependent manner. Meanwhile, continuous infusion of intravenous lipid emulsion (ILE) has been established as a detoxification therapy for lipophilic drugs. However, this change in pharmacokinetics of various drugs following ILE administration remains to be clarified. Our objective is to clarify the effect of continuous intravenous infusion of lipid emulsion (ILE) on the pharmacokinetics of overdosed paliperidone in rats. Paliperidone (20mg/kg) was administered orally to free-moving male Wistar rats...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28821026/ultrahigh-antibacterial-efficacy-of-meropenem-loaded-chitosan-nanoparticles-in-a-septic-animal-model
#11
Ayat Abdelkader, Mohamed A El-Mokhtar, Ola Abdelkader, Mostafa A Hamad, Mahmoud Elsabahy, Omaima N El-Gazayerly
Antimicrobial resistance is one of the most significant health challenges worldwide. Meropenem is a broad spectrum beta-lactam antibiotic that possesses high activity against Gram-positive and Gram-negative bacteria. However, it has a short plasma half-life, and thus requiring frequent administration of high doses. For the first time, meropenem-loaded chitosan nanoparticles were prepared and evaluated as a potential tool to overcome antimicrobial resistance and to improve pharmacokinetics of the drug. Spherical nanosized particles were prepared and demonstrated ultrahigh encapsulation efficiency of meropenem (i...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28820966/reactive-oxygen-species-responsive-polymeric-nanoparticles-for-alleviating-sepsis-induced-acute-liver-injury-in-mice
#12
Gan Chen, Hongzhang Deng, Xiang Song, Mingzi Lu, Lian Zhao, Sha Xia, Guoxing You, Jingxiang Zhao, Yulong Zhang, Anjie Dong, Hong Zhou
Sepsis-associated acute liver injury contributes to the pathogenesis of multiple organ dysfunction syndrome and is associated with increased mortality. Currently, no specific therapeutics for sepsis-associated liver injury are available. With excess levels of reactive oxygen species (ROS) being implicated as key players in sepsis-induced liver injury, we hypothesize that ROS-responsive nanoparticles (NPs) formed via the self-assembly of diblock copolymers of poly(ethylene glycol) (PEG) and poly(propylene sulfide) (PPS) may function as an effective drug delivery system for alleviating sepsis-induced liver injury by preferentially releasing drug molecules at the disease site...
August 11, 2017: Biomaterials
https://www.readbyqxmd.com/read/28820457/role-of-cyp2c9-cyp2c19-and-ephx-polymorphism-in-the-pharmacokinetic-of-phenytoin-a-study-on-uruguayan-caucasian-subjects
#13
Natalia Guevara, Cecilia Maldonado, Manuel Uría, Raquel González, Manuel Ibarra, Silvana Alvariza, Antonella Carozzi, Carlos Azambuja, Pietro Fagiolino, Marta Vázquez
Phenytoin (PHT) oxidative route leads to its main metabolite p-hydroxyphenytoin (p-HPPH), by means of CYP2C9 and CYP2C19. Formation of p-HPPH proceeds via a reactive arene-oxide intermediate. This intermediate can also be converted into PHT dihydrodiol by microsomal epoxide hydrolase (EPHX). The three enzymes are polymorphically expressed and the genetic variants are responsible for changes in the enzyme activity. In order to evaluate the effect that these polymorphisms have on PHT metabolism, PHT and p-HPPH plasma concentrations were measured and the genotype for the three enzymes was assessed in 50 Uruguayan epileptic patients...
August 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28820428/pharmacokinetic-analysis-of-an-oral-multicomponent-joint-dietary-supplement-phycox-%C3%A2-in-dogs
#14
Stephanie E Martinez, Ryan Lillico, Ted M Lakowski, Steven A Martinez, Neal M Davies
Despite the lack of safety, efficacy and pharmacokinetic (PK) studies, multicomponent dietary supplements (nutraceuticals) have become increasingly popular as primary or adjunct therapies for clinical osteoarthritis in veterinary medicine. Phycox(®) is a line of multicomponent joint support supplements marketed for joint health in dogs and horses. Many of the active constituents are recognized anti-inflammatory and antioxidant agents. Due to a lack of PK studies in the literature for the product, a pilot PK study of select constituents in Phycox(®) was performed in healthy dogs...
August 18, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28820390/small-molecule-inhibitors-of-dna-pk-for-tumor-sensitization-to-anticancer-therapy
#15
M Pospisilova, M Seifrtova, M Rezacova
The most sensitive cell structure - a DNA molecule, is the common target of cancer therapy. DNA damage response (controlled by enzymes from the phosphatidylinositol 3-kinase-related kinases family - PIKK) presents many encouraging targets for improving both conventional cytotoxic anticancer therapy and individualized monotherapy. DNA-dependent protein kinase (DNA-PK) is a member of the PIKK superfamily and plays an important role in the detection and repair of DNA double-strand breaks via the non-homologous end-joining pathway...
June 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28820269/reaction-phenotyping-to-assess-victim-drug-drug-interaction-risks
#16
Li Di
Reaction phenotyping provides critical information regarding the fraction metabolized (fm) of drug candidates. It has become increasingly important in drug discovery and development as it can be used to assess victim drug-drug interaction potential, guide structural modification to reduce fm, inform clinical study design, predict individual variability in pharmacokinetics, and evaluate the impact of genetic polymorphisms. Areas covered: The currently available in vitro and in vivo methods for reaction phenotyping are summarized along with their advantages, limitations and timings for application during the different stages of drug discovery and development...
August 18, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28820026/pilot-validation-of-an-individualised-pharmacokinetic-algorithm-for-protamine-dosing-after-systemic-heparinisation-for-cardiopulmonary-bypass
#17
Lachlan F Miles, Paolo Marchiori, Florian Falter
INTRODUCTION: This manuscript represents a pilot study assessing the feasibility of a single-compartment, individualised, pharmacokinetic algorithm for protamine dosing after cardiopulmonary bypass. METHODS: A pilot cohort study in a specialist NHS cardiothoracic hospital targeting patients undergoing elective cardiac surgery using cardiopulmonary bypass. Patients received protamine doses according to a pharmacokinetic algorithm (n = 30) or using an empirical, fixed-dose model (n = 30)...
September 2017: Perfusion
https://www.readbyqxmd.com/read/28819873/similarities-and-differences-between-doxycycline-and-minocycline-clinical-and-antimicrobial-stewardship-considerations
#18
REVIEW
B A Cunha, J Baron, C B Cunha
Doxycycline and, to a lesser extent, minocycline, have been used for decades to treat various serious systemic infections, but many physicians remain unfamiliar with their spectrum, interpretation of susceptibility results, pharmacokinetic/pharmacodynamic (PK/PD) properties, optimal dosing regimens, and their activity against MRSA, VRE, and multidrug-resistant (MDR) Gram-negative bacilli, e.g., Acinetobacter sp. This article reviews the optimal use of doxycycline and minocycline to treat a variety of infections and when minocycline is preferred instead of doxycycline...
August 17, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28819760/effect-of-alisertib-an-investigational-aurora-a-kinase-inhibitor-on-the-qtc-interval-in-patients-with-advanced-malignancies
#19
Xiaofei Zhou, John Nemunaitis, Shubham Pant, Todd M Bauer, Manish Patel, John Sarantopoulos, A Craig Lockhart, Daniel Goodman, Dirk Huebner, Diane R Mould, Karthik Venkatakrishnan
Aims A primary objective of this study was to investigate the effect of single and multiple doses of alisertib, an investigational Aurora A kinase inhibitor, on the QTc interval in patients with advanced malignancies. The dose regimen used was the maximum tolerated dose which was also the recommended phase 3 dose (50 mg twice daily [BID] for 7 days in 21-day cycles). Methods Patients received a single dose of alisertib (50 mg) on Day 1, and multiple doses of alisertib (50 mg BID) on Days 4 through to the morning of Day 10 of the first cycle of treatment...
August 18, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28819726/population-pharmacokinetics-of-stiripentol-in-paediatric-patients-with-dravet-syndrome-treated-with-stiripentol-valproate-and-clobazam-combination-therapy
#20
Sophie Peigné, Stéphanie Chhun, Michel Tod, Elisabeth Rey, Christelle Rodrigues, Catherine Chiron, Gérard Pons, Vincent Jullien
AIM: The aim of this study was to describe the pharmacokinetics of stiripentol in children with Dravet syndrome and to determine the concentrations of stiripentol achieved in this population for the usual 25 mg/kg twice-daily dose. METHODS: Thirty-five children with epilepsy were included in a prospective population pharmacokinetic study (using MONOLIX software). Four blood samples were drawn per patient. Stiripentol area under the plasma concentration-time curve (AUC) values and trough concentrations were simulated for 7000 theoretical children weighing between 10 and 70 kg for the 25 mg/kg twice-daily dose...
August 17, 2017: Clinical Pharmacokinetics
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