collection
https://read.qxmd.com/read/24634842/prediction-of-pharmacokinetic-parameters-using-a-genetic-algorithm-combined-with-an-artificial-neural-network-for-a-series-of-alkaloid-drugs
#21
JOURNAL ARTICLE
Majid Zandkarimi, Mohammad Shafiei, Farzin Hadizadeh, Mohammad Ali Darbandi, Kaveh Tabrizian
An important goal for drug development within the pharmaceutical industry is the application of simple methods to determine human pharmacokinetic parameters. Effective computing tools are able to increase scientists' ability to make precise selections of chemical compounds in accordance with desired pharmacokinetic and safety profiles. This work presents a method for making predictions of the clearance, plasma protein binding, and volume of distribution for alkaloid drugs. The tools used in this method were genetic algorithms (GAs) combined with artificial neural networks (ANNs) and these were applied to select the most relevant molecular descriptors and to develop quantitative structure-pharmacokinetic relationship (QSPkR) models...
January 2014: Scientia Pharmaceutica
https://read.qxmd.com/read/24634843/qsar-and-molecular-docking-studies-of-oxadiazole-ligated-pyrrole-derivatives-as-enoyl-acp-coa-reductase-inhibitors
#22
JOURNAL ARTICLE
Kalyani D Asgaonkar, Ganesh D Mote, Trupti S Chitre
A quantitative structure-activity relationship model was developed on a series of compounds containing oxadiazole-ligated pyrrole pharmacophore to identify key structural fragments required for anti-tubercular activity. Two-dimensional (2D) and three-dimensional (3D) QSAR studies were performed using multiple linear regression (MLR) analysis and k-nearest neighbour molecular field analysis (kNN-MFA), respectively. The developed QSAR models were found to be statistically significant with respect to training, cross-validation, and external validation...
January 2014: Scientia Pharmaceutica
https://read.qxmd.com/read/24636040/dose-selection-method-for-pharmacokinetic-study-in-hemodialysis-patients-using-a-subpharmacological-dose-oseltamivir-as-a-model-drug
#23
JOURNAL ARTICLE
Dong Ki Kim, Jay Wook Lee, Kwang-Hee Shin, Sejoong Kim, Kook-Hwan Oh, Myounghee Kim, Kyung-Sang Yu, Jung Pyo Lee, Chun-Soo Lim, Yon Su Kim, Kwon Wook Joo
BACKGROUND: Dose selection is an important step in pharmacokinetic (PK) studies of hemodialysis patients. We propose a simulation-based dose-selection method for PK studies of hemodialysis patients using a subpharmacological dose of oseltamivir as a model drug. METHODS: The concentrations of oseltamivir and its active metabolite, oseltamivir carboxylate (OC), were measured by liquid chromatography-tandem mass spectrometry. To determine a low oseltamivir dose exhibiting PK linearity, a pilot low dose determination investigation (n = 4) was performed using a single administration dose-escalation study...
2014: BMC Nephrology
https://read.qxmd.com/read/24647103/development-of-a-physiologically-based-pharmacokinetic-model-of-the-rat-central-nervous-system
#24
JOURNAL ARTICLE
Raj K Singh Badhan, Marylore Chenel, Jeffrey I Penny
Central nervous system (CNS) drug disposition is dictated by a drug's physicochemical properties and its ability to permeate physiological barriers. The blood-brain barrier (BBB), blood-cerebrospinal fluid barrier and centrally located drug transporter proteins influence drug disposition within the central nervous system. Attainment of adequate brain-to-plasma and cerebrospinal fluid-to-plasma partitioning is important in determining the efficacy of centrally acting therapeutics. We have developed a physiologically-based pharmacokinetic model of the rat CNS which incorporates brain interstitial fluid (ISF), choroidal epithelial and total cerebrospinal fluid (CSF) compartments and accurately predicts CNS pharmacokinetics...
2014: Pharmaceutics
https://read.qxmd.com/read/24647104/application-of-pharmacokinetic-and-pharmacodynamic-analysis-to-the-development-of-liposomal-formulations-for-oncology
#25
JOURNAL ARTICLE
Sihem Ait-Oudhia, Donald E Mager, Robert M Straubinger
Liposomal formulations of anticancer agents have been developed to prolong drug circulating lifetime, enhance anti-tumor efficacy by increasing tumor drug deposition, and reduce drug toxicity by avoiding critical normal tissues. Despite the clinical approval of numerous liposome-based chemotherapeutics, challenges remain in the development and clinical deployment of micro- and nano-particulate formulations, as well as combining these novel agents with conventional drugs and standard-of-care therapies. Factors requiring optimization include control of drug biodistribution, release rates of the encapsulated drug, and uptake by target cells...
2014: Pharmaceutics
https://read.qxmd.com/read/24658499/largazole-pharmacokinetics-in-rats-by-lc-ms-ms
#26
JOURNAL ARTICLE
Mingming Yu, Lilibeth A Salvador, Sherwin K B Sy, Yufei Tang, Ravi S P Singh, Qi-Yin Chen, Yanxia Liu, Jiyong Hong, Hartmut Derendorf, Hendrik Luesch
A highly sensitive and specific LC-MS/MS method for the quantitation of largazole thiol, the active species of the marine-derived preclinical histone deacetylase inhibitor, largazole (prodrug), was developed and validated. Largazole thiol was extracted with ethyl acetate from human or rat plasma along with the internal standard, harmine. Samples were separated on an Onyx Monolithic C18 column by a stepwise gradient elution with 0.1% formic acid in methanol and 0.1% aqueous formic acid employing multiple reaction monitoring (MRM) detection...
March 2014: Marine Drugs
https://read.qxmd.com/read/24658827/the-influence-of-cyp3a-ppara-and-por-genetic-variants-on-the-pharmacokinetics-of-tacrolimus-and-cyclosporine-in-renal-transplant-recipients
#27
JOURNAL ARTICLE
Ingrid Lunde, Sara Bremer, Karsten Midtvedt, Beata Mohebi, Miriam Dahl, Stein Bergan, Anders Åsberg, Hege Christensen
PURPOSE: Tacrolimus (Tac) and cyclosporine (CsA) are mainly metabolized by CYP3A4 and CYP3A5. Several studies have demonstrated an association between the CYP3A5 genotype and Tac dose requirements. Recently, CYP3A4, PPARA, and POR gene variants have been shown to influence CYP3A metabolism. The present study investigated potential associations between CYP3A5*3, CYP3A4*22, PPARA c.209- 1003G>A and c.208+3819A>G, and POR*28 alleles and dose-adjusted concentrations (C/D) of Tac and CsA in 177 renal transplant patients early post-transplant...
June 2014: European Journal of Clinical Pharmacology
https://read.qxmd.com/read/24672114/bioavailability-study-of-fixed-dose-tablet-versus-capsule-formulation-of-amlodipine-plus-benazepril-a-randomized-single-dose-two-sequence-two-period-open-label-crossover-study-in-healthy-volunteers
#28
JOURNAL ARTICLE
Kuo-Liong Chien, Chia-Lun Chao, Ta-Cheng Su
BACKGROUND: In the treatment of hypertension, combination therapy is important10 because antihypertensive monotherapy is effective in only 40% of patients worldwide. Amlodipine is a dihydropyridine calcium channel blocker with a slow onset and long duration of action. Benazepril hydrochloride is a prodrug hydrolyzed by esterase to the active metabolite benazeprilat, an angiotensin-converting enzyme inhibitor. In 1995, the US Food and Drug Administration approved the use of a capsule formulation of combination amlodipine-benazepril for hypertension...
March 2005: Current Therapeutic Research, Clinical and Experimental
https://read.qxmd.com/read/24282510/pharmacokinetics-of-drugs-in-cachectic-patients-a-systematic-review
#29
REVIEW
Katja Trobec, Mojca Kerec Kos, Stephan von Haehling, Jochen Springer, Stefan D Anker, Mitja Lainscak
Cachexia is a weight-loss process caused by an underlying chronic disease such as cancer, chronic heart failure, chronic obstructive pulmonary disease, or rheumatoid arthritis. It leads to changes in body structure and function that may influence the pharmacokinetics of drugs. Changes in gut function and decreased subcutaneous tissue may influence the absorption of orally and transdermally applied drugs. Altered body composition and plasma protein concentration may affect drug distribution. Changes in the expression and function of metabolic enzymes could influence the metabolism of drugs, and their renal excretion could be affected by possible reduction in kidney function...
2013: PloS One
https://read.qxmd.com/read/24660066/preparation-and-the-biopharmaceutical-evaluation-for-the-metered-dose-transdermal-spray-of-dexketoprofen
#30
JOURNAL ARTICLE
Wangding Lu, Huafei Luo, Zhuangzhi Zhu, Yubo Wu, Jing Luo, Hao Wang
The objective of the present work was to develop a metered dose transdermal spray (MDTS) formulation for transdermal delivery of dexketoprofen (DE). DE release from a series of formulations was assessed in vitro. Various qualitative and quantitative parameters like spray pattern, pump seal efficiency test, average weight per metered dose, and dose uniformity were evaluated. The optimized formulation with good skin permeation and an appropriate drug concentration and permeation enhancer (PE) content was developed incorporating 7% (w/w, %) DE, 7% (v/v, %) isopropyl myristate (IPM), and 93% (v/v, %) ethanol...
2014: Journal of Drug Delivery
https://read.qxmd.com/read/24670388/physiologically-based-pharmacokinetic-modeling-framework-for-quantitative-prediction-of-an-herb-drug-interaction
#31
JOURNAL ARTICLE
S J Brantley, B T Gufford, R Dua, D J Fediuk, T N Graf, Y V Scarlett, K S Frederick, M B Fisher, N H Oberlies, M F Paine
Herb-drug interaction predictions remain challenging. Physiologically based pharmacokinetic (PBPK) modeling was used to improve prediction accuracy of potential herb-drug interactions using the semipurified milk thistle preparation, silibinin, as an exemplar herbal product. Interactions between silibinin constituents and the probe substrates warfarin (CYP2C9) and midazolam (CYP3A) were simulated. A low silibinin dose (160 mg/day × 14 days) was predicted to increase midazolam area under the curve (AUC) by 1%, which was corroborated with external data; a higher dose (1,650 mg/day × 7 days) was predicted to increase midazolam and (S)-warfarin AUC by 5% and 4%, respectively...
March 26, 2014: CPT: Pharmacometrics & Systems Pharmacology
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