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 the oral doses of CPT. Mice were administered orally one of three single doses of CZ48 (50, 200 and 1000 mg/kg) and two single doses of CPT (1.5 mg/kg and 6.0 mg/kg). Blood samples were collected from all mice at the defined time points after drug administration for assessment of plasma CZ48 and CPT concentrations. RESULTS:The study showed that CZ48 was very stable in mouse blood and the majority of this agent stayed intact as the lactone form when in circulation, with only a small fraction of the CZ48 molecules metabolized into CPT. The concentration of the metabolite CPT measured in the mouse blood was only 3% of the concentration found for the maximum tolerated dose (6.0 mg/kg) of plain CPT. The stability difference between CZ48 and CPT in blood was structurally explained by the geometry of these two molecules. CONCLUSION:The lack of toxicity of CZ48 at effective doses in mice is attributed to its enhanced stability in their blood.
journal_name
J Pharm Pharm Sciauthors
Liu X,Wang Y,Cao Z,Zhan M,Vardeman D,Giovanella Bdoi
10.18433/j3b604subject
Has Abstractpub_date
2013-01-01 00:00:00pages
115-24issue
1issn
1482-1826journal_volume
16pub_type
杂志文章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:Breast cancer resistance protein (BCRP/ABCG2) is a drug efflux transporter expressed at the blood cerebrospinal fluid barrier (BCSFB), and influences distribution of drugs into the central nervous systems (CNS). Current inhibitors have failed clinically due to neurotoxicity. Novel approaches are needed to ident...
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/j3p31k
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:Vigabatrin, an anti-epileptic drug with poor UV absorptivity, is used as a model drug to investigate parameters affecting quantitative determination of cationic drugs using capillary zone electrophoresis with indirect UV detection. METHODS:All experiments were performed on a HP 3D CE instrument equipped with a...
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：2005-08-03 00:00:00
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 metho...
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/jpps30237
更新日期：2019-01-01 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：: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：: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：: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:The precise role of carnitine as the key regulator of lipid metabolism in sepsis is unclear. In this review, available experimental as well as clinical evidences regarding the probable beneficial effects of carnitine in sepsis were evaluated. METHOD:A comprehensive literature search was performed in the relate...
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/j3js4c
更新日期：2013-01-01 00:00:00
abstract：:In noncompartmental analysis, poor characterization of the terminal elimination rate constant (Kel) will lead to biased results for half-life and total exposure (AUCinf), providing incorrect relative bioavailability and bioequivalence conclusions. We set out to determine if the sampling scheme duration was crucial for...
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/j3fg63
更新日期：2011-01-01 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 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: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 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 aim of this study was to investigate the excretion of irinotecan hydrochloride (CPT-11) and its metabolites into the gastrointestinal lumen via the biliary route after intravenous administration of lactone and carboxylate forms of CPT-11. METHODS:Biliary excretions of CPT-11 and its metabolites, SN-38 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
doi：
更新日期：2004-01-23 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:A randomized cross-over, double blind placebo controlled study of smoked cannabis was carried out on occasional cannabis smokers. The objective of this research was to describe the pharmacokinetic parameters of THC and its metabolites in plasma, oral fluid and urine, from samples obtained simultaneously to prov...
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,随机对照试验
doi：10.18433/J3F31D
更新日期：2016-01-01 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 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:Drug release from nanosystems at the sites of either absorption or effect biophase is a major determinant of its biological action. Thus, in vitro drug release is of paramount importance in gaining insight for the systems performance in vivo. METHODS:A novel in vitro in vivo correlation, IVIVC, model denoted a...
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/j3np5n
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:The present study was undertaken to investigate the effect of plastic, hydrophilic and hydrophobic types of polymers and their content level on the release profile of drug from matrix systems. As the physico-chemical nature of the active ingredients influence the drug retarding ability of these polymers, three ...
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：2003-05-01 00:00:00
abstract：:Cannabis has been used for its medicinal purposes since ancient times. Its consumption leads to the activation of Cannabis receptors CB1 and CB2 that, through specific mechanisms can lead to modulation and progression of inflammation or repair. The novel findings are linked to the medical use of Cannabis in gastrointe...
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/jpps31242
更新日期：2020-01-01 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:To examine the inhibitory effects of star fruit (Averrhoa carambola) juice towards seven major cytochrome P450 (CYP) isoforms and NADPH-cytochrome P450 reductase (CPR). METHODS:The inhibitory effects of star fruit juice (0.5 to 5%, v/v) against the activities of seven CYP isoforms including CYP1A2, CYP2A6, CYP...
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/j30593
更新日期：2007-01-01 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：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: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:We have previously reported that the Australian Northern Kaanju (Kuuku I'yu) medicinal plant Dodonaea polyandra has anti-inflammatory activity. This is attributed largely to the presence of clerodane diterpenoids contained within the leaf resin. We envisaged developing a topical preparation to treat indications...
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/j38p57
更新日期：2015-01-01 00:00:00
abstract：BACKGROUND:To perform a review describing the pharmacokinetic (PK) parameters and covariates of interest of the eight first choice β-lactams (BL) antibiotics for treatment of severe infections in pediatric population. Pediatric sepsis and septic shock reportedly affect 30% of children admitted to pediatric intensive ca...
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/jpps30927
更新日期：2020-01-01 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
