Abstract：
:Hypochlorhydria is a condition where the production of hydrochloric acid in the stomach is decreased. As a result, the intragastric pH is elevated. This condition can be due to a series of causes, such as disease (gastric mucosal infection caused by Helicobacter pylori and is prominent in AIDS patients), ethnicity, age and also the use of antisecretory agents. This may significantly impact the absorption of other drugs that have pH-dependent solubility, such as ketoconazole, a weak base. Within this context, the purpose of this study was to demonstrate how GastroPlusTM - a physiological based software program- can be used to predict clinical pharmacokinetics of ketoconazole in a normal physiological state vs. elevated gastric pH. A simple physiologically based pharmacokinetic model was built and validated to explore the impact that different physiologic conditions in the stomach (hypochlorhydria, drug administered with water and Coca Cola®) had on ketoconazole's bioavailability. The developed model was able to accurately predict the impact of increased pH and beverage co-administration on dissolution and absorption of the drug, and confirmed that complete gastric dissolution is essential. Particle size only mattered in hypochlorhydric conditions due to the incomplete gastric dissolution, as its absorption would depend on intestinal dissolution, which corroborates with previous studies. Therefore, in silico approaches are a potential tool to assess a pharmaceutical product's performance and efficacy under different physiological and pathophysiological states supporting the assessment of different dosing strategies in clinical practice.
journal_name
J Pharm Pharm Sciauthors
Silva DA,Duque MD,Davies NM,Löbenberg R,Ferraz HGdoi
10.18433/jpps30227subject
Has Abstractpub_date
2018-01-01 00:00:00pages
242s-253sissue
1sissn
1482-1826journal_volume
21pub_type
杂志文章abstract：PURPOSE:Because oxytocin (OT) is potentially useful in cardiovascular therapy but has hormonal roles on the cardiovascular and renal systems, we characterized its pharmacokinetic (PK) properties as a function of dose. METHODS:A single intravenous bolus of OT was given at doses of 200, 300, 500, 1000, 3000, 5000 and 10...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3pk5x
更新日期：2008-01-01 00:00:00
abstract：:Purpose - The CEIBA cocktail consisting of caffeine (CAF), omeprazole (OZ), dextromethorphan (DM) and losartan (LOS) was previously proposed for the clinical phenotyping of five major human cytochrome P450 (CYP) isoenzymes. This work aimed to assess the usefulness of CEIBA cocktail to study non-clinical drug interacti...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/J3D313
更新日期：2016-01-01 00:00:00
abstract：:Cardiac ischemia-reperfusion stimulates the renin-angiotensin system (RAS) associated with elevated levels of circulating angiotensin II. Numerous studies demonstrate that the antagonist for the angiotensin II type 1 receptor, losartan improves cardiac function in animal models of ischemia-reperfusion. Molecular mecha...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/j3nw2k
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:The purpose of this study was to determine if Disodium Ascorbyl Phytostanol Phosphates (FM-VP4) alters animal body weight and plasma lipid levels in a dietary-induced obese mouse model. METHODS:Twenty-four C57BL6 mice (28 days old) were housed individually and fed a standard mouse diet for 2 weeks upon arrival...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2005-08-24 00:00:00
abstract：BACKGROUND:Drug-induced lung injury leads to serious lung diseases, such as pulmonary fibrosis. We demonstrated in an alveolar epithelial cell line A549/ABCA3 that certain microRNAs were associated with bleomycin induced epithelial-mesenchymal transition (EMT) which is closely related to pulmonary fibrosis. In this stu...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps31448
更新日期：2020-01-01 00:00:00
abstract：PURPOSE:The extent of palmitate uptake by hepatocytes is dependent upon the surface charge of the extracellular binding protein. Specifically, hepatocyte uptake is greater when palmitate is bound to cationic binding proteins than when it is bound to anionic proteins. To further understand the role of protein surface ch...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3bc8w
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:The primary aim of this work was to establish a radiolabeling procedure of vinblastine, a vinca alkaloid widely used in chemotherapy, with the positron-emitter carbon-11 for application in positron-emission-tomography (PET) studies in cancer patients. The optimized reaction conditions were transferred to an aut...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2007-01-01 00:00:00
abstract：PURPOSE:To determine the merits of a robot at the community pharmacy in a quasi-experiment. METHOD:The applied methods for data-collection were barcode-time measurements, direct observations, time-interval studies, and tally at a Dutch community pharmacy. The topics consisted of workload, waiting times, congestion, sl...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2006-01-01 00:00:00
abstract：PURPOSE:The adrenoceptor family, as one of the main contributors in regulating the noradrenergic system, has been studied in involvement of depression and its treatment. A functional polymorphism of G1165C on beta adrenoceptor (βAR) enhances post receptor signalling and is assumed to be involved in pharmacotherapy of d...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/J3W31F
更新日期：2017-01-01 00:00:00
abstract：PURPOSE:An improved HPLC method with fluorescence detection was developed and validated for determination of glucosamine in human and rat biological samples. METHOD:Aliquot of 0.1 mL plasma was spiked with mannosamine HCl as the internal standard (IS); proteins were precipitated with acetonitrile; the clear layer was ...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3t01s
更新日期：2010-01-01 00:00:00
abstract：:Chitosan has prompted the continuous movement for the development of safe and effective drug delivery systems because of its unique physicochemical and biological characteristics. The primary hydroxyl and amine groups located on the backbone of chitosan allow for chemical modification to control its physical propertie...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/j3jc7c
更新日期：2010-01-01 00:00:00
abstract：PURPOSE:The gastrointestinal damage induced by xenobiotics is occurring more frequently and with greater toxicological significance than previously thought. Although there are some preliminary clinical studies and reports, there does not appear to be an extensive examination of gastrointestinal toxicity of various chem...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2003-09-01 00:00:00
abstract：PURPOSE:The purpose of this study was to develop an artificial neural network (ANN) model to predict drug removal during dialysis based on drug properties and dialysis conditions. Nine antihypertensive drugs were chosen as model for this study. METHODS:Drugs were dissolved in a physiologic buffer and dialysed in vitro...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j35c8b
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:To synthesize current knowledge about the effectiveness and the magnitude of the effect, of Academic Detailing (AD), as a stand-alone intervention, at modifying drug prescription behavior of Family Physicians (FPs) in primary care settings. METHODS:A search of MEDLINE, EMBASE, CENTRAL, and Web of Science datab...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/j3kk6c
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:A few studies have shown that normothermic hepatic ischemia-reperfusion (IR) injury may affect the mRNA and/or protein levels of canalicular transporters P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (Mrp2). However, the effects of the injury on the functions of these canalicular transport...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3ms40
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:The aim of the study was the prediction of human intestinal permeability and fraction absorbed of oral dose using single-pass intestinal perfusion technique (SPIP) in rats. METHODS:Permeability coefficients in anaesthetized rats were determined for 14 compounds. Drug solution in phosphate buffered saline (PBS)...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2007-01-01 00:00:00
abstract：PURPOSE:Gabapentin, a drug for neuropathic pain, exerts its therapeutic effect via inhibition of the a2d subunit of N-type Ca2+ channels. Thus, finding peptides that specifically displace gabapentin from its binding site may lead to the development of new drugs. METHODS:Displacement of bound [3H]-gabapentin in membran...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps30358
更新日期：2019-01-01 00:00:00
abstract：PURPOSE:The aim of this study was to correlate the relationship between the pharmacokinetic behaviors and the toxicity of a new investigational anticancer agent CZ48, a C20-propionate ester of camptothecin (CPT) in mice. METHODS:In this study, the safety and pharmacokinetics of oral doses of CZ48 were compared with th...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3b604
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:The plasma membrane localization and transport activity of multidrug resistance- associated protein 2 (MRP2/ABCC2) and P-glycoprotein (P-gp/ABCB1) efflux transporters are governed by transporter-associated proteins. Phosphatidylinositol 4,5-bisphosphate (PIP2) formed by phosphatidylinositol 4-phosphate 5-kinase...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps30444
更新日期：2019-01-01 00:00:00
abstract：:Dry eye disease (DED) is a common inflammatory disorder of the ocular surface. Millions of people are affected by DED worldwide. Lifitegrast is a novel drug designed to inhibit DED-associated ocular inflammation. Four clinical trials have shown that lifitegrast is well tolerated and effective in improving symptoms and...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/jpps29895
更新日期：2019-01-01 00:00:00
abstract：PURPOSE:A high performance liquid chromatographic method was developed for the determination of glucosamine (GlcN) in rat plasma. METHOD:Internal standard, galactosamine, was added to 100 micro L of plasma containing GlcN followed by precipitation of plasma proteins with acetonitrile. Evaporation of the decanted super...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2002-05-01 00:00:00
abstract：PURPOSE:Oseltamivir is a prodrug that requires metabolic activation but there is little information on whether natural health products interact to prevent the biotransformation by the carboxylesterase. METHODS:HPLC-DAD-ESI-MSD and fluorometric assays were used to determine if 50-pooled mixed gender human liver microso...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3zp42
更新日期：2010-01-01 00:00:00
abstract：BACKGROUND:The identification of fragment sequences, or motifs, within a therapeutic protein that may elicit an immune response when processed by T-cells can be provided by computer-aided approaches. Immunogenicity is a significant problem associated with protein therapeutics and should be investigated in the early sta...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps29800
更新日期：2018-01-01 00:00:00
abstract：PURPOSE:Patients with type 2 diabetes are generally treated with various pharmacological compounds and are exposed to a high risk of drug-drug interactions. However, alterations of pharmacokinetics in a type 2 diabetes model have been obscure. The present study was undertaken to investigate the effects of type 2 diabet...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3mc70
更新日期：2014-01-01 00:00:00
abstract：:Clearance concepts were introduced into the pharmacokinetics discipline in the 1970s and since then have played a major role in characterization of the pharmacokinetic behavior of drugs. These concepts are based on the relationship between organ extraction ratio or clearance and physiologic parameters such as the orga...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/jpps29896
更新日期：2018-01-01 00:00:00
abstract：PURPOSE:Concomitant use of nutraceuticals with chemotherapy is very common. Cancer patients self-medicate to relieve the side effects associated with chemotherapy, improve disease outcome and to regain control of their medical care. However, there is limited empirical evidence on potential drug-nutraceutical interactio...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3m30k
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:The aim of this study was to determine the cause of the decline in phenolsulfonphthalein (PSP) excretion in Long-Evans Cinnamon (LEC) rats. METHODS:The uptake of PSP into rat renal basolateral membrane vesicles (BLMV) was studied. Cyclosporin A (CYA) was used to modulate an ATP-dependent primary active transpo...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2004-07-13 00:00:00
abstract：PURPOSE:To develop a high performance liquid chromatography system for the determination of a new 1,4-dihydropyridine, mebudipine, in rabbit plasma. METHODS:To 1 ml of rabbit plasma was added internal standard (dibudipine) and 0.5 ml of 1 M NaOH. Mebudipine and internal standard were extracted to 5 ml ethyl acetate, e...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2001-09-01 00:00:00
abstract：PURPOSE:Clinical studies have suggested that proton pump inhibitors may decrease levothyroxine absorption and an in vitro study suggested that the effect of pH on dissolution may differ with formulation. To determine the impact of formulation on the pharmacokinetics of levothyroxine in altered gastric pH conditions, th...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j36p5m
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:To evaluate the inhibitory activity of active compounds isolated from Cinnamomum cassia bark against lens aldose reductase and compare to that of three commercially available compounds (cinnamyl alcohol, trans -cinnamic acid, and eugenol) and quercitrin as aldose reductase inhibitors. The IC (50) value of cinna...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2002-09-01 00:00:00
