Abstract：
:The pharmacokinetics of cefixime, a new orally active cephalosporin, was studied after an intravenous dose of 50 mg/kg to four beagle dogs. Cefixime was shown to exhibit concentration dependent serum protein binding and saturable tubular reabsorption. The drug was excreted mainly in the urine, the net result of glomerular filtration and saturable tubular reabsorption. The experimental results were analyzed by model independent pharmacokinetic equations and with theoretical models describing renal clearance. Modification of the models, based on observed data, was proposed. The experimental methods employed and the pharmacokinetic approach offered in this study can be applied to drugs that exhibit concentration dependent protein binding and saturable renal elimination processes.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Tonelli AP,Bialer M,Look ZM,Carson S,Yacobi Adoi
10.1023/A:1016309923717subject
Has Abstractpub_date
1986-06-01 00:00:00pages
150-5issue
3eissn
0724-8741issn
1573-904Xjournal_volume
3pub_type
杂志文章abstract：PURPOSE:To characterize the electrochemical behavior of the photodegradation product of nifedipine, i.e., 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridine-carboxylic acid dimethyl ester (NPD) in different electrolytic media. We also evaluated the interaction between free radicals generated from NPD and xeno/endobiotics. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015112216360
更新日期：2002-04-01 00:00:00
abstract：PURPOSE:The purpose of this study was to determine the existence of insulin-degrading enzyme (EC 3.4.22.11) (IDE) in rat intestinal enterocytes. METHODS:Subcellular fractionation, biochemical characterization, immunoprecipitation, and western blots were employed. RESULTS:Insulin-degrading activity was localized in th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016263926946
更新日期：1995-08-01 00:00:00
abstract：:The possible mechanism of hepatic uptake of colchicine (CLC), a microtubule system disrupting agent, was examined using isolated rat hepatocytes. The existence of a carrier-mediated active transport system for CLC was demonstrated. This transport system is saturable, is affected by metabolic inhibitors (dinitrophenol,...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015917601349
更新日期：1989-03-01 00:00:00
abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9139-6
更新日期：2007-01-01 00:00:00
abstract：PURPOSE:This paper aims to investigate the immunoinhibitory properties of a lymph nodes-targeting suppressive oligonucleotide (ODN) for the potential treatment of autoimmune diseases or chronic inflammation. METHODS:Synthetic suppressive ODN engineered with an albumin-binding diacyl lipid at the 5'-terminal (lipo-ODN)...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2344-2
更新日期：2018-02-08 00:00:00
abstract：:A reverse-phase HPLC method for the analysis of tryptic digests of recombinant porcine growth hormone (pGH) has been developed and validated. Digestion was performed at 4 degrees C for a 20-hr period with TPCK-treated trypsin at a 1:20 (w/w) trypsin:pGH ratio. Gradient elution HPLC, using an Aquapore RP300 C8 column, ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018927426268
更新日期：1993-10-01 00:00:00
abstract：:Assessment of bioavailability/bioequivalence generally relies on the comparison of rate and extent of drug absorption between products. Rate of absorption is commonly expressed by peak concentration (C(max)) and time to peak concentration (T(max)), although these parameters are indirect measures of absorption rate. Re...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-011-0421-x
更新日期：2011-08-01 00:00:00
abstract：PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9301-9
更新日期：2007-09-01 00:00:00
abstract：:New generation vaccines, particularly those based on recombinant proteins and DNA, are likely to be less reactogenic than traditional vaccines but are also less immunogenic. Therefore, there is an urgent need for the development of new and improved vaccine adjuvants. Adjuvants can be broadly separated into two classes...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1016104910582
更新日期：2002-06-01 00:00:00
abstract：:Moisture sorption characteristics and the effect of moisture content on the compression properties of two dextrose-based directly compressible diluents, namely, Emdex (diluent A) and Sweetrex (diluent B) were studied. Both diluents sorbed moisture rapidly at relative humidities greater than 60%. For both the diluents,...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015889414533
更新日期：1991-03-01 00:00:00
abstract：PURPOSE:To develop novel bioactive-chylomicrons to solve oral delivery obstacles of Berberine chloride and target the lymphatic system. METHODS:Berberine-loaded bioactive-chylomicrons were prepared and underwent full in vitro characterization. Intestinal permeability was appraised via both non-everted gut sac model an...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2307-z
更新日期：2018-01-05 00:00:00
abstract：:We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018920118631
更新日期：1993-05-01 00:00:00
abstract：PURPOSE:The purpose of this study was to use a replicate designed trial to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters of CGP 33101 after oral administration of tablets relative to that of powder suspended in water, and to determine the relative proportion of the intra-subje...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1023/a:1016275402723
更新日期：1995-12-01 00:00:00
abstract：PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1716-0
更新日期：2015-10-01 00:00:00
abstract：PURPOSE:Low temperature sensitive liposome (LTSL) encapsulated docetaxel were combined with mild hyperthermia (40-42°C) to investigate in vivo biodistribution and efficacy against a castrate resistant prostate cancer. METHOD:Female athymic nude mice with human prostate PC-3 M-luciferase cells grown subcutaneously into...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1971-8
更新日期：2016-10-01 00:00:00
abstract：PURPOSE:To evaluate the mechanism of renal transport of quinolone antibacterial drugs, we examined the interaction of levofloxacin with p-aminohippurate (PAH) transport systems and the transport of levofloxacin in renal epithelial cells. METHODS:Transport of [14C]PAH or [14C]levofloxacin was measured using OK cell mon...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011012822437
更新日期：2001-05-01 00:00:00
abstract：PURPOSE:The aim was to evaluate fluorescent molecular rotors (DCVJ and CCVJ), which are mainly sensitive to viscosity, for the characterization of polysorbate-containing IgG formulations and compare them to the polarity-sensitive dyes ANS, Bis-ANS and Nile Red. METHODS:IgG formulations with polysorbate 20 or 80 were s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-0020-2
更新日期：2010-02-01 00:00:00
abstract：PURPOSE:The aim of this study was to investigate the effect of hepatic or renal insufficiency on the pharmacokinetics of paclitaxel in rats. METHODS:Rats were treated with carbon tetrachloride (CCl4; 0.5 ml/kg) to induce hepatic failure or were subjected to 5/6 nephrectomy (5/6 Nx) to induce renal failure. Paclitaxel ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-1190-6
更新日期：2005-02-01 00:00:00
abstract：PURPOSE:To analyze the effects of chemical enhancers and iontophoresis on the buccal transmucosal delivery of lidocaine and nicotine. METHODS:Porcine oral mucosal samples were pretreated with chemical enhancers before conducting 8-hr Franz diffusion-cell experiments. In studies addressing the influence of iontophoresi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0636-x
更新日期：2012-04-01 00:00:00
abstract：:Effects of protease inhibitors and absorption enhancers on the absorption of salmon calcitonin (sCT) were evaluated after intratracheal coadministration to rats using the plasma Ca level as an index. Remarkable absorption enhancement could be attained with unsaturated fatty acids such as oleic acid and polyoxyethylene...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018926007902
更新日期：1994-09-01 00:00:00
abstract：PURPOSE:To identify the mechanism behind the unexpected bio-performance of two amorphous solid dispersions: BMS-A/PVP-VA and BMS-A/HPMC-AS. METHODS:Solubility of crystalline BMS-A in PVP-VA and HPMC-AS was measured by DSC. Drug-polymer interaction parameters were obtained by Flory-Huggins model fitting. Drug dissoluti...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0695-7
更新日期：2012-10-01 00:00:00
abstract：PURPOSE:Stable transformants expressing human multidrug resistance 1 (MDR1), monkey MDR1, canine MDR1, rat MDR1a, rat MDR1b, mouse mdr1a, and mouse mdr1b in LLC-PK1 were established to investigate species differences in P-glycoprotein (P-gp, ABCB1) mediated efflux activity. METHODS:The seven cDNAs of MDR1 from five an...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0285-7
更新日期：2006-07-01 00:00:00
abstract：PURPOSE:Understanding the mechanism of protein-excipient interaction and illuminating the influencing factors on protein stability are key steps in the rational design of protein formulations. The objective of this study was to assess effects of preferential interaction type of excipient and surface aromatic hydrophobi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2152-0
更新日期：2017-07-01 00:00:00
abstract：PURPOSE:To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks. METHODS:Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loade...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2059-1
更新日期：2017-02-01 00:00:00
abstract：PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1579-9
更新日期：2015-05-01 00:00:00
abstract：:An open, randomized, six-way crossover study was conducted in 12 healthy males to assess pharmacokinetics and bioinversion of ibuprofen enantiomers. The mean plasma terminal half-life (t1/2) of R(-)ibuprofen was 1.74 hr when intravenously infused as a racemic mixture and was 1.84 hr when intravenously infused alone. T...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1023/a:1018969506143
更新日期：1994-06-01 00:00:00
abstract：PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2117-3
更新日期：2017-05-01 00:00:00
abstract：PURPOSE:Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS:A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacte...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018908421434
更新日期：1999-07-01 00:00:00
abstract：:Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling fac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015942013413
更新日期：1988-09-01 00:00:00
abstract：PURPOSE:Short linear peptides have a high potential for delivering various drugs with therapeutic potential, including nucleic acids. Recently, we have shown that the cationic amphipathic histidine-rich peptide LAH4 (KKALLALALHHLAHLALHLALALKKA) possesses high plasmid DNA delivery capacities. Since such peptides are tho...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0138-2
更新日期：2010-07-01 00:00:00
