Abstract：
:Hepatic clearance (CLh) of carvedilol (CAR), which is eliminated via stereoselective metabolism by the CYP2D subfamily of cytochromes P450 (CYPs), was predicted using liver microsomes and hepatocytes from Sprague-Dawley (SD) rats and CYP2D-deficient Dark Agouti (DA) rats to determine the usefulness of prediction method. Plasma concentrations of CAR following intravenous injection to DA rats were higher than those in SD rats. The volume of distribution at steady state and total clearance (CLtot) of S-CAR were approximately two times greater than those of R-CAR in both strains. CLh predicted from in vitro studies using DA rat liver microsomes was different from that obtained from in vivo studies. In contrast, in vitro CLh prediction using DA rat hepatocytes was nearly identical to the CLh observed in DA rats in vivo, and was lower than that in SD rats. The predicted CLh in vitro using hepatocytes correlated well with the observed CLtot in vivo, which is expected to be nearly the same as CLh. These results suggest that in vitro metabolic studies using hepatocytes are more relevant with regard to stereoselectively predicting CLh of CAR than those using liver microsomes.
journal_name
J Pharm Pharm Sciauthors
Iwaki M,Niwa T,Tanaka H,Kawase A,Komura Hdoi
10.18433/jpps30237subject
Has Abstractpub_date
2019-01-01 00:00:00pages
72-84issue
1issn
1482-1826journal_volume
22pub_type
杂志文章abstract：PURPOSE:To study the effect of encapsulation of recombinant adenovirus type 5 encoding Beta-galactosidase (Ad5-Betagal) in poly (D,Llactic-co-glycolic acid) (PLGA) microspheres on viral delivery to professional antigen presenting cells (APCs) in vitro, viral dissemination in vivo, and induction of protective immune res...
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:The purpose of our study was to optimize lipid-lowering therapy in patients undergoing coronary revascularization and to determine whether the percentage change in low-density lipoprotein-cholesterol (LDL-C) level in the 3 months after coronary revascularization could be used as a predictor of the time to recur...
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/j3hg6q
更新日期：2010-01-01 00:00:00
abstract：PURPOSE:To establish structural equation model (SEM) of subjected quality of life (QOL) in cancer patients taking into account qualification of pharmacists. METHOD:The SEM model was constructed from correlation matrix of the scores of answers of questions to both patients and pharmacists. Data were collected from 15 c...
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：2005-10-04 00:00:00
abstract：PURPOSE:The aim of this work was to prepare the stable water/oil/water multiple emulsions (MEs), to investigate the usage of poloxamine 908, to observe the influence of surfactant percentage on the properties of MEs. METHOD:MEs were prepared by liquid paraffin, cetyl dimethicone copolyol and poloxamine 908 by a two-st...
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：2005-08-11 00:00:00
abstract：PURPOSE:To study the influence of inspiratory flow rate on the fine particle mass and the particle size distribution for metered dose inhaler (MDI) and dry powder inhaler (DPI) glucocorticoid products, in vitro. To compare the performance of MDI and DPI inhalers containing the same drug and strength at an impaction flo...
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：2000-09-01 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：: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:Regular exercise training and metformin medication are widely considered to increase insulin sensitivity and protect against type 2 diabetes, however, evaluating the effect of exercise training on the disposition and pharmacokinetics of metformin is unclear. METHODS:We investigated the effect of a 4-wk swim tr...
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/j3tg7w
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:To review microbial contamination rates about preparation of individual and batch doses using aseptic techniques within pharmaceutical (controlled) and clinical (ward and theatre) environments. METHODS:Systematic review, involving amalgamation of data using a random effect model and metaanalysis. RESULTS:A to...
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,meta分析,评审
doi：10.18433/j3jp4b
更新日期：2009-01-01 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：:The microneedles technology has found applications in many health-related fields. For example, their application in drugs and vaccines delivery as well, as the determination of biomarkers, has been reported. They also have a place in the dermatology and cosmetic areas such as the treatment of wounds from burns, scars,...
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/jpps29610
更新日期：2018-01-01 00:00:00
abstract：:Alzheimer's disease (AD) is an irreversible neurodegenerative disease characterized by a progressive decline in cognition and memory, leading to significant impairment in daily activities and ultimately death. It is the most common cause of dementia, the prevalence of which increases with age; however, age is not the ...
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/J3VS8P
更新日期：2017-01-01 00:00:00
abstract：PURPOSE:To determine if there is sufficient evidence to recommend the addition of pentoxifylline to standard ACE inhibitor and ARB therapy in chronic kidney disease patients to reduce proteinuria and preserve kidney function. METHODS:A search of the literature was conducted using the PubMed.gov and ClinicalTrials.gov...
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/J3K020
更新日期：2016-01-01 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:To assess the predicted rate and the factors associated with bleeding events among patients with non-valvular atrial fibrillation (NVAF) receiving dabigatran therapy. METHODS:This retrospective cohort study includes adult patients of two tertiary hospitals in Malaysia. Potential study subjects were identified ...
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/J3TP9Q
更新日期：2017-01-01 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
abstract：PURPOSE:A series of delta-valerolactones has been synthesized in good yields, by reaction of ethyl acetoacetate with several aldehydes in presence of LDA. METHODS AND RESULTS:The in vivo analgesic activity of these compounds has been evaluated. The results indicate that the lactones synthesized showed an important ant...
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：2005-04-08 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:Aim of this study is to investigate the mechanism of self-emulsification through rheological analysis of intermediate liquid crystalline (LC) phase formed during self-emulsification process. METHODS:Binary system of tween 80 (T80) and imwitor 742 (I742) was used and different SES were prepared with I742 at 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/j30w2p
更新日期：2009-01-01 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 predict Caco-2 permeability is a valuable target for pharmaceutical research. Most of the Caco-2 prediction models are based on commercial or special software which limited their practical value. This study represents the relationship between Caco-2 permeability and molecular descriptors totally based on ope...
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:To determine the possible mechanism of poor bioavailability of bicyclol, and clarify the respective contribution of P- glycoprotein (P-gp) and Cytochrome 3A (CYP3A). METHODS:Rat in situ single-pass intestinal perfusion and Caco-2 cell monolayer model with selective inhibitors of CYP3A and P-gp were employed. ...
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/j3b88v
更新日期：2008-01-01 00:00:00
abstract：PURPOSE:Comparison of the effects of one year treatment with sibutramine compared to placebo on insulin resistance parameters, body weight, glycemic control, and lipid profile, in type 2 diabetic patients. METHODS:Two hundred and forty-six patients with uncontrolled type 2 diabetes mellitus in therapy with different o...
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,多中心研究,随机对照试验
doi：10.18433/j3388p
更新日期：2010-01-01 00:00:00
abstract：:A simple and efficient method for radiolabeling preformed liposomes was developed using hepatobiliary imaging agent (99m)Tc-diisopropyl iminodiacetic acid ((99m)Tc-DISIDA). Chloroform extraction of (99m)Tc-DISIDA from aqueous solutions results in 80% radioactivity in the organic phase due to its lipophilic properties....
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：1998-01-01 00:00:00
abstract：PURPOSE:To design a buccal mucoadhesive system for systemic delivery of acyclovir using a novel mucoadhesive, copolymers of acrylic acid and poly(ethylene glycol), and to determine the feasibility of transbuccal delivery of acyclovir using this system. METHODS:The buccal delivery system was prepared using an adhesive,...
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：1998-05-01 00:00:00
abstract：:PURPOSE. Animal-derived drugs are the major source of biological products and traditional medicine, but they are often difficult to identify, causing confusion in the clinical application. Among these medicinal animals, a number of animal species are endangered, leading to the destruction of biodiversity. The identifi...
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/j3n017
更新日期：2011-01-01 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：:Years after the first report on 1,4-dihydropyridines (1,4-DHPs) and 1,2,3,4-tetrahydropyrimidines (1,2,3,4-THPMs) appeared, they are revisited as plausible therapeutic agents. This is mainly due to the convenient methods that exist for their synthesis and the diverse pharmacologic properties that these scaffolds prese...
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/j3q01v
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:Organic anion-transporting polypeptide (OATP) 1B1 and OATP1B3 contribute to hepatic uptake of numerous drugs. Thus, reduced OATP1B1 and OATP1B3 activity in chronic kidney disease (CKD) may have a major impact on the hepatic clearance of drugs. The effect of drug-uremic toxin interactions on OATP1B1 and OATP1B3 ...
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/j3m89q
更新日期：2014-01-01 00:00:00
abstract：PURPOSE:Monoclonal antibodies (mAbs) are commonly administered by subcutaneous (SC) route. However, bioavailability is often reduced after SC administration. In addition, the sequential transfer of mAbs through the SC tissue and lymphatic system is not completely understood. Therefore, major objectives of this study we...
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/jpps30028
更新日期：2018-01-01 00:00:00
