Abstract：
:The tissue penetration and distribution of antibiotics is of great importance, since most of the infections occur in the tissue. At the infection site, the free, unbound fraction of the antibiotic is responsible for the antiinfective effect. These free extracellular concentrations can be measured by microdialysis. It was the aim of the study to correlate free levels of the beta-lactam antibiotic piperacillin in blood with those in tissue. In vivo microdialysis sampling was used to study the tissue distribution patterns of piperacillin in anesthetized rats after single dose iv administration of the drug. The pharmacokinetics of piperacillin in plasma were consistent with a two-compartment body model. Comparisons between calculated free concentrations in the peripheral compartment and measured free extracellular concentrations revealed excellent agreement. Microdialysis is a suitable method to evaluate unbound drug concentrations in the tissues. In case of piperacillin, predictions of the concentration time profiles of free drug in the peripheral compartment can be made on the basis of plasma data.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Nolting A,Costa TD,Vistelle R,Rand KH,Derendorf Hdoi
10.1021/js950304xsubject
Has Abstractpub_date
1996-04-01 00:00:00pages
369-72issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)50047-6journal_volume
85pub_type
杂志文章abstract：:The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...
journal_title：Journal of pharmaceutical sciences
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abstract：:Single-walled carbon nanotubes (SWCNTs) attract great interest in biomedical applications including drug and gene delivery. In this study, we developed a novel delivery system using SWCNTs associated with designed polycationic and amphiphilic peptides. Wrapping of SWCNTs with H-(-Lys-Trp-Lys-Gly-)7-OH [(KWKG)7] result...
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更新日期：1981-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600671126
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更新日期：1997-03-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2010-03-01 00:00:00
abstract：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23913
更新日期：2014-05-01 00:00:00
abstract：:The geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...
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更新日期：1992-12-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js970137w
更新日期：1997-09-01 00:00:00
abstract：:During stability studies at high temperature (70 degrees C) and low relative humidity ( approximately 0%), the recovery of an asparagine containing hexapeptide (VYPNGA) and its known deamidation products from solid polyvinylpyrrolidone (PVP) matrices was incomplete. To determine the causes of this mass loss, formulati...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.10316
更新日期：2003-03-01 00:00:00
abstract：:Most anticancer drugs are intended to function in the nuclei of cancer cells. If an anticancer drug could be delivered to mitochondria, the source of cellular energy, this organelle would be destroyed, resulting in the arrest of the energy supply and the killing of the cancer cells. To achieve such an innovative strat...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.04.058
更新日期：2017-09-01 00:00:00
abstract：:This in vitro study evaluated the extent of the absorption and metabolism of propranolol in human skin from four sources. Between 10.4 +/- 3.1 and 36.6 +/- 2.6% of the applied dose was absorbed; however, only a small portion (between 4.1 +/- 0.9 and 16.1 +/- 1.3%) of the dose permeated through the skin. Naphthoxyaceti...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600820802
更新日期：1993-08-01 00:00:00
abstract：:Analytical methods based on the title reactions are reviewed, and the malonic acid-acetic anhydride system was selected for detailed study. It is postulated that carbon suboxide, O = C = C = C = O, formed by the action of acetic anhydride on malonic acid, is the effective reactive species in this system. Carbon suboxi...
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pub_type： 杂志文章
doi：10.1002/jps.2600761018
更新日期：1987-10-01 00:00:00
abstract：:A method has been developed for the estimation of the distribution coefficient (D), which considers the microspecies of a compound. D is calculated from the microscopic dissociation constants (microconstants), the partition coefficients of the microspecies, and the counterion concentration. A general equation for the ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js960177k
更新日期：1997-07-01 00:00:00
abstract：:Two novel series of benzimidazole derivatives bearing structural modifications of certain drugs were prepared for evaluation for potential anticancer activity. The first series was a group of alkylating agents, and the second series was a variety of 4-substituted-1-thioacetyl-3-thiosemicarbazides. The tests of some re...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600691130
更新日期：1980-11-01 00:00:00
abstract：:A series of gem-cichlorocyclopropyl and cyclopropyl analogs of stilbene congeners was synthesized and examined for estrogenic and antiestrogenic activity using the uterotropic assay in the immature mouse. The relative receptor affinity in vitro was determined by measuring [3H]estradiol displacement from the rat uterin...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600711012
更新日期：1982-10-01 00:00:00
abstract：:The binding of representative chemical classes of nonsteroidal anti-inflammatory drugs (NSAIDs) to human serum albumin (HSA) was investigated by equilibrium dialysis. Warfarin enantiomers were used as specific markers in displacement studies. Data were analyzed by a computerized nonlinear least squares approach design...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600770314
更新日期：1988-03-01 00:00:00
abstract：:Microparticles are of considerable interest for drug delivery, vaccination and diagnostic imaging. In order to obtain microparticles with long circulation times, or to provide the prerequisite for tissue specific targeting through decoration with suitable ligands, their surfaces need to be modified such that they beco...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
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更新日期：2008-11-01 00:00:00
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更新日期：1998-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20091
更新日期：2004-07-01 00:00:00
abstract：:Cephalosporins are among the most frequently used broad-spectrum antimicrobial agents. Ceftazidime is a semisynthetic β-lactam antibiotic for parenteral administration widely used in the clinical practice, which has been categorized as a third-generation cephalosporin antibiotic. This drug crystallizes as a pentahydra...
journal_title：Journal of pharmaceutical sciences
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更新日期：2020-03-01 00:00:00
abstract：:Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonst...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600750324
更新日期：1986-03-01 00:00:00
abstract：:Tritium-labeled progesterone was administered to mature female rats in the proestrous stage by three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600661223
更新日期：1977-12-01 00:00:00
abstract：:HPLC analysis confirmed a difference in the chemical composition of commercial versus NF reference standard potassium guaiacolsulfonate. After separation by fractional crystallization, the two constituents comprising the former sample were identified by 1H-NMR as potassium guaiacol-4- and -5-sulfonate, respectively. T...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730911
更新日期：1984-09-01 00:00:00
abstract：:Lipids were extracted from human stratum corneum and the remaining corneocytes were reaggregated with different lyotropic liquid crystals. Water transport through the reaggregated stratum corneum was determined using a diffusion chamber according to Smith and Blank. The permeability constant for the reaggregated strat...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800506
更新日期：1991-05-01 00:00:00
abstract：:We extend and modify the Noyes-Whitney equation and the Hixon-Crowell cube root law to include surface roughness effects on the dissolution rate of drugs. The problem is treated theoretically in terms of the fractal reaction dimension, DR, of the effective surface which undergoes dissolution. Effects of changes in DR ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810111
更新日期：1992-01-01 00:00:00
abstract：:The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800113
更新日期：1991-01-01 00:00:00
abstract：:A sensitive and specific GLC method is described to determine therapeutic levels of tilidine and its two main metabolites, nortilidine and bisnortilidine, in plasma and urine. The method involves the extraction of the compounds and an internal standard with cyclohexane from alkalinized samples, followed by back-extrac...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600671237
更新日期：1978-12-01 00:00:00
abstract：:Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.02.021
更新日期：2018-07-01 00:00:00
