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pharmacokinetics

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https://www.readbyqxmd.com/read/29679708/the-impact-of-polymers-on-3d-microstructure-and-controlled-release-of-sildenafil-citrate-from-hydrophilic-matrices
#1
Anna Krupa, Zbisław Tabor, Jacek Tarasiuk, Beata Strach, Krzysztof Pociecha, Elżbieta Wyska, Sebastian Wroński, Ewelina Łyszczarz, Renata Jachowicz
Sildenafil citrate has short biological half-life in humans. Thus, matrix tablets of controlled release were designed and prepared by compaction on the basis of hydrophilic polymers, i.e. HPMC, sodium alginate, carbomer, poloxamer and their mixtures. The impact of these polymers on sildenafil release in vitro and its pharmacokinetics in vivo was evaluated. Since drug release rate from hydrophilic matrices can be govern by the porosity of the matrix, the microstructure of tablets was studied using X-ray microcomputed tomography...
April 18, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29679590/phase-i-ii-pharmacokinetic-and-pharmacodynamic-evaluation-of-two-levonorgestrel-only-contraceptive-patches-in-a-multicenter-randomized-trial
#2
Carolyn L Westhoff, Beatrice A Chen, Jeffrey T Jensen, Kurt Barnhart, Michael Thomas, Stephanie Teal, Diana Blithe
OBJECTIVES: To evaluate the pharmacokinetic and pharmacodynamic effects of two novel levonorgestrel (LNG)-only contraceptive patches. STUDY DESIGN: This multi-center Phase I/II trial randomized participants to use a 7-day transdermal patch designed to deliver a 40 mcg or 75 mcg daily LNG dose for 11 consecutive weeks; randomization was stratified by body mass index (BMI) <32 or 32-40kg/m2 . Evaluations occurred twice weekly for 5weeks, then once weekly with supplemental visits for participants reporting a urinary LH surge...
April 18, 2018: Contraception
https://www.readbyqxmd.com/read/29679536/curcumin-formulated-in-solid-lipid-nanoparticles-has-enhanced-efficacy-in-hodgkin-s-lymphoma-in-mice
#3
Jacob Guorgui, Ruixue Wang, George Mattheolabakis, Gerardo G Mackenzie
Curcumin reduces Hodgkin's lymphoma (HL) cell growth in vitro, but its unfavorable pharmacokinetics highlight the need for novel in vivo delivery systems. Thus, we explored whether formulation of curcumin in solid lipid nanoparticles (SLN-curc) or d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) nanoparticles (TPGS-curc) could enhance its efficacy in mice. Curcumin formulated in SLN and in TPGS resulted in higher curcumin plasma levels in mice. Compared to vehicle-treated controls, SLN-curc and TPGS-curc reduced HL xenograft growth by 50...
April 18, 2018: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29679509/pharmacokinetic-properties-of-wogonin-and-its-herb-drug-interactions-with-docetaxel-in-rats-with-mammary-tumors
#4
Ting Wang, Fangyi Long, Gang Jiang, Hong Cai, Qian Jiang, Kai Cheng, Zhiqiang Hu, Yuxi Wang
Docetaxel, frequently used for the treatment of breast cancer, is mainly metabolized via hepatic cytochrome P450 (CYP) 3A in humans and is also a substrate of P-glycoprotein (P-gp). Wogonin has been shown to be able to modulate the activities of CYPs and P-gp, and it could be served as an adjuvant chemotherapeutic agent. However, the impacts of co-administration of wogonin and docetaxel on their pharmacokinetics have not been studied for lacking analytical method of their simultaneous measurement. In the present study, we established an HPLC-MS/MS method for simultaneous measurement of wogonin and docetaxel in rat plasma, and it was then utilized to explore the pharmacokinetics of wogonin and the herb-drug interactions between wogonin and docetaxel after the combined administration in rats with mammary tumors...
April 21, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29679478/randomized-controlled-study-of-bleselumab-askp1240-pharmacokinetics-and-safety-in-patients-with-moderate-to-severe-plaque-psoriasis
#5
Mysore S Anil Kumar, Kim Papp, Ryo Tainaka, Udaya Valluri, Xuegong Wang, Tong Zhu, Christian Schwabe
This study evaluated pharmacokinetics (PK), efficacy, safety, and tolerability of bleselumab - a fully-human anti-CD40 monoclonal recombinant IgG4. Patients with moderate-to-severe psoriasis were randomized on Day 1 to receive bleselumab or placebo on Days 1, 15, and 29 in a dose-escalation of bleselumab 0.1, 0.3, 1.0, or 3.0mg/kg. The safety-analysis set (SAF) and full-analysis set (FAS) included all patients who received bleselumab or placebo, and the PK-analysis set (PKAS) included patients in the SAF with ≥1 quantifiable serum bleselumab concentration...
April 21, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29679474/population-pharmacokinetics-of-gliclazide-in-normal-and-diabetic-rabbits
#6
Mastan Shaik, Shabana Shaik, Eswar Kumar Kilari
Gliclazide is a second-generation sulphonylurea drug widely used in the treatment of type 2 diabetes. However, there is no single report to describe the population pharmacokinetics of gliclazide in animal models. This study was aimed to evaluate the population pharmacokinetics (PK) of gliclazide in normal and alloxan-induced diabetic rabbits using nonlinear mixed effects modeling. A total of 90 New Zealand white rabbits were administered with 3 doses (4.13, 8.27 and 16.53 mg/kg b.wt) of gliclazide by an oral route...
April 21, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29679445/development-of-coumarin-and-benzofuran-conjugated-hybrids-as-the-versatile-multi-targeted-compounds-for-the-treatment-of-alzheimer-s-disease
#7
Asha Hiremathad, Karam Chand, Rangappa S Keri
Alzheimer's disease (AD), the most common cause of dementia, is a neurodegenerative disorder characterized by progressive deterioration of memory and cognition. The evidenced multi-factorial nature of AD has been considered the main reason for the absence of cure so far. Therefore, the development of novel hybrids to treat the disease is very much essential. Focusing on this, a novel series of coumarin-benzofuran conjugated hybrids have been designed and screened as anti-Alzheimer's disease agents. The strategy is to obtain an effective mimetic of donepezil, which is acetylcholnesterase inhibitor...
April 20, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29679387/the-pharmacokinetics-and-pharmacodynamics-of-carfentanil-after-recreational-exposure-a-case-report
#8
Uvaraj Uddayasankar, Colin Lee, Curtis Oleschuk, Gregg Eschun, Robert E Ariano
Carfentanil and related fentanyl analogues have been linked to a number of overdose deaths from drug users in several cities across North America. Diagnosis of carfentanil exposure requires a very high index of clinical suspicion, especially because available laboratory narcotic screens do not detect this agent. We describe a 34-year-old male admitted with depressed level of consciousness and in respiratory failure after recreational exposure to a white powder later inferred to contain carfentanil. Urine and whole blood samples were obtained for conventional preliminary drug screen immunoassays for unknown exposures; in addition to utilizing high pressure liquid chromatography tandem mass spectrometry assay for quantification of carfentanil and its metabolite...
April 20, 2018: Pharmacotherapy
https://www.readbyqxmd.com/read/29679349/timeline-bioavailability-of-magnesium-compounds-in-hours-which-magnesium-compound-works-best
#9
Nazan Uysal, Servet Kizildag, Zeynep Yuce, Guven Guvendi, Sevim Kandis, Basar Koc, Aslı Karakilic, Ulas M Camsari, Mehmet Ates
Magnesium is an element of great importance functioning because of its association with many cellular physiological functions. The magnesium content of foods is gradually decreasing due to food processing, and magnesium supplementation for healthy living has become increasingly popular. However, data is very limited on the bioavailability of various magnesium preparations. The aim of this study is to investigate the bioavailability of five different magnesium compounds (magnesium sulfate, magnesium oxide, magnesium acetyl taurate, magnesium citrate, and magnesium malate) in different tissues...
April 21, 2018: Biological Trace Element Research
https://www.readbyqxmd.com/read/29679234/clinical-pharmacokinetics-and-dose-recommendations-for-posaconazole-in-infants-and-children
#10
Sophida Boonsathorn, Iek Cheng, Frank Kloprogge, Carlos Alonso, Charmion Lee, Bilyana Doncheva, John Booth, Robert Chiesa, Adam Irwin, Joseph F Standing
OBJECTIVES: The objectives of this study were to investigate the population pharmacokinetics of posaconazole in immunocompromised children, evaluate the influence of patient characteristics on posaconazole exposure and perform simulations to recommend optimal starting doses. METHODS: Posaconazole plasma concentrations from paediatric patients undergoing therapeutic drug monitoring were extracted from a tertiary paediatric hospital database. These were merged with covariates collected from electronic sources and case-note reviews...
April 20, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29679228/recovery-time-after-oral-and-maxillofacial-ambulatory-surgery-with-dexmedetomidine-an-observational-study
#11
Belen Hernando, Antonio Martinez-Simon, Elena Cacho-Asenjo, Iñaki F Troconiz, Cristina Honorato-Cia, Alfredo Panadero, Luis L Naval, Jorge M Nuñez-Cordoba
OBJECTIVES: To evaluate the relationship between pharmacokinetic descriptors of dexmedetomidine (predicted area under the curve during the procedure, predicted plasma level at the end of the procedure, and duration of procedure) and sedation depth (proportion of time with bispectral index < 85 during the procedure) with recovery time after ambulatory procedures. MATERIALS AND METHODS: Clinical observational study of patients undergoing oral and maxillofacial ambulatory surgery with dexmedetomidine as sole sedative agent...
April 20, 2018: Clinical Oral Investigations
https://www.readbyqxmd.com/read/29679159/notch-1-sirna-and-methotrexate-towards-a-multifunctional-approach-in-rhematoid-arthritis-management-a-nanomedicine-approach
#12
Guang Zhao, Haifei Zhang
PURPOSE: Rheumatoid arthritis (RA) is a chronic inflammatory disease and Notch pathway plays a pivotal role in synoviocytes involved in progression of RA. METHODS: Herein, we have designed a self-assembled polymeric micelles based on polycaprolactone-polyethylene glycol (PCL-PEG) and polyethylenimine-polyethylene glycol (PEI-PEG) was prepared and loaded with methotrexate and Notch-1 siRNA for the effective treatment of rheumatoid arthritis. RESULTS: The MTX/siRNA-loaded polymeric micelles (siM-PM) showed appreciable cellular uptake in Raw264...
April 20, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29679046/impact-of-antenatal-corticosteroids-in-preterm-neonates-based-on-maternal-body-mass-index
#13
Maheer Faden, Sarah D McDonald, Prakeshkumar S Shah, Amit Mukerji
OBJECTIVE: Impact of antenatal corticosteroid (ACS) in context of maternal body mass index (BMI) as it relates to neonatal outcomes remains unclear. We sought to evaluate effects of ACS on clinical outcomes of preterm infants based on maternal BMI. METHODS: We performed a retrospective cohort study among neonates 23-33 weeks' GA at a tertiary neonatal intensive care unit from 2011 to 2015. Outcomes of neonates exposed to any ACS and pre-pregnancy maternal BMI ≥ 25 (N = 491) were compared with maternal BMI < 25 (N = 484)...
April 20, 2018: Journal of Perinatology: Official Journal of the California Perinatal Association
https://www.readbyqxmd.com/read/29678733/pharmacokinetics-of-lipid-drug-conjugates-loaded-into-liposomes
#14
REVIEW
Rea D Signorell, Paola Luciani, Davide Brambilla, Jean-Christophe Leroux
Drugs that are neither lipophilic nor suitable for encapsulation via remote loading procedures are generally characterized by low entrapment efficiencies and poor retention in liposomes. One approach to circumvent this problem consists in covalently linking a lipid to the drug molecule in order to permit its insertion into the vesicle membrane. The nature of the conjugated lipid and linker, as well as the composition of the liposomal bilayer were found to have a profound impact on the pharmacokinetic properties and biodistribution of the encapsulated drugs as well as on their biological activity...
April 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29678659/association-of-cyp3a4-1b-genotype-with-cyclosporin-a-pharmacokinetics-in-renal-transplant-recipients-a-meta-analysis
#15
Cai-E Wang, Ke-Peng Lu, Zhao Chang, Meng-Li Guo, Hai-Ling Qiao
OBJECTIVE: Cyclosporine (CsA) is a substrate of cytochrome P450 (CYP) 3A4 with a narrow therapeutic index and large individual difference. CYP3A4*1B is reported to be associated with CsA pharmacokinetics parameters, but the relevance is still in dispute. Therefore, a meta-analysis was employed to evaluate the influence of CYP3A4*1B on CsA pharmacokinetics at different post-transplantation times in adult renal transplant recipients. METHODS: Studies on evaluating the CYP3A4*1B genotype and CsA pharmacokinetics were retrieved through a systematical search of relevant database including PubMed, Emabase, Web of science, the Cochrane Library, Clinical Trials...
April 17, 2018: Gene
https://www.readbyqxmd.com/read/29678547/pamam-dendrimers-as-a-carbamazepine-delivery-system-for-neurodegenerative-diseases-a-biophysical-and-nanotoxicological-characterization
#16
Daniela E Igartúa, Carolina S Martinez, C Facundo Temprana, Silvia Del V Alonso, M Jimena Prieto
Carbamazepine (CBZ) is an antiepileptic drug, which also could be used in the treatment of neurodegenerative diseases, such as the Alzheimer's disease. However, its use has been limited due to its low solubility, inefficient pharmacokinetic profiles, and multiple side effects. PAMAM dendrimers, ethylenediamine core, generation 4.0 (amine terminal groups) and 4.5 (carboxylate terminal groups) (DG4.0 and DG4.5 respectively) are polymers that can increase drug solubility through complexation. Thus, the aim of this work was to obtain and characterize complexes between CBZ and dendrimers...
April 17, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29678262/tolfenamic-acid
#17
Sofia Ahmed, Muhammad Ali Sheraz, Iqbal Ahmad
Tolfenamic acid (TA) is a nonsteroidal antiinflammatory drug and belongs to the group of fenamates. It is used as a potent pain reliever in the treatment of acute migraine attacks, and disorders like dysmenorrhea, rheumatoid, and osteoarthritis. TA has shown excellent in vitro antibacterial activity against certain ATCC strains of bacteria when complexed with bismuth(III). It has also been reported to block pathological processes associated with Alzheimer's disease. In the recent past, TA has also been used as a novel anticancer agent for the treatment of various cancers...
2018: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/29678261/mirtazapine
#18
Abdulrahman Al-Majed, Ahmed H Bakheit, Raed M Alharbi, Hatem A Abdel Aziz
Mirtazapine is one of antidepression which is used mainly in the treatment of depression, moreover, it is sometimes used in the treatment of anxiety disorders, insomnia, nausea, and vomiting, and to produce weight gain when desirable. The action of mirtazapine is an antagonist of certain adrenergic and serotonin receptors, and, furthermore, the drug is used strong as antihistamine, and it is occasionally defined as a noradrenergic and specific serotonergic antidepressant (NaSSA). The comprehensive profile of mirtazapine gives more detailed information about nomenclature, formulae, elemental analysis, and appearance...
2018: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/29678260/ganciclovir
#19
Abdullah A Al-Badr, Tariq D S Ajarim
Ganciclovir is synthetic nucleoside analog of guanine closely related to acyclovir but has greater activity against cytomegalovirus. This comprehensive profile on ganciclovir starts with a description of the drug: nomenclature, formulae, chemical structure, elemental composition, and appearance. The uses and application of the drug are explained. The methods that were used for the preparation of ganciclovir are described and their respective schemes are outlined. The methods which were used for the physical characterization of the dug are: ionization constant, solubility, X-ray powder diffraction pattern, crystal structure, melting point, and differential scanning calorimetry...
2018: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/29677683/application-of-solid-phase-microextraction-followed-by-liquid-chromatography-mass-spectrometry-in-the-determination-of-antibiotic-drugs-and-their-metabolites-in-human-whole-blood-and-tissue-samples
#20
Malgorzata Szultka-Mlynska, Pawel Pomastowski, Boguslaw Buszewski
A sensitive, rapid and specific analytical method using high performance liquid chromatography coupled with mass spectrometry (HPLC-QqQ-MS) was developed to determine selected antibiotic drugs and their metabolites (amoxicillin, cefotaxime, ciprofloxacin, clindamycin and metronidazole; amoxycilloic acid, 4-hydroxyphenyl glycyl amoxicillin, desacetyl cefotaxime, 3-desacetyl cefotaxime lactone, ciprofloxacin N-oxide, N-demethylclindamycin, clindamycin sulfoxide, and hydroxy metronidazole) in human whole blood and vascularized tissue after single oral administration...
April 12, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
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