Abstract:
:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbitrary compounds.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
van de Waterbeemd H,van Bakel P,Jansen Adoi
10.1002/jps.2600700930subject
Has Abstractpub_date
1981-09-01 00:00:00pages
1081-2issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(15)43893-6journal_volume
70pub_type
杂志文章abstract::This review addresses a major question of importance to pharmaceutical scientists: how can novel drug delivery systems play a role in maximizing the UV protection of sunscreens? Because more and more people are being diagnosed with skin cancer each year than all other cancers combined, adequate sun protective measures...
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abstract::Apparent micellar molecular weights were determined with the antibiotic fusidate sodium by ultracentrifugation in varying counterion concentrations (Na+). The effects of buffer salts, pH, sodium chloride concentration, and drug concentration were studied. The results strongly support the concept of the formation of pr...
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abstract::The entropy of fusion of 84 disubstituted benzenes was essentially constant and independent of the participation of the compounds in intramolecular or intermolecular hydrogen bonding. It was also independent of the shapes, sizes, and dipole moments of the rigid molecules studied. While the entropy of fusion was indepe...
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abstract::Present study aims to improve efficiency and capacity of in vivo rat pharmacokinetic studies for rapid assessment of systemic exposure (AUC and C(max)) of new chemical entities. Plasma concentration-time profiles in rats from structurally diverse compounds were extracted from the Pfizer database. AUC(0-8) was calculat...
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abstract::Hyperthermia (HT)-dependent cisplatin (CDDP) release and tumor CDDP level increase after the administration of thermosensitive, large unilamellar vesicles (LUVs: LUV-1 and LUV-2) and a thermosensitive, small unilamellar vesicle (SUV: SUV-1) were examined in comparison with those following administration of a non-therm...
journal_title:Journal of pharmaceutical sciences
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abstract::Nasal administration as a means of delivering therapeutic agents preferentially to the brain has gained significant recent interest. While some substrates appear to be delivered directly to the brain via this route, the mechanisms governing overall brain uptake and exposure remain unclear. Some substrates utilize the ...
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更新日期:1976-11-01 00:00:00
abstract::Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...
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更新日期:1984-11-01 00:00:00
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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更新日期:2013-03-01 00:00:00
abstract::The pharmacokinetics of atropine in three healthy male volunteers after intravenous administration of 1.35 and 2.15 mg of the drug was determined. Pharmacodynamic effects of atropine were measured simultaneously. All the data were fitted to a novel integrated kinetic-dynamic model. Plasma concentrations of atropine an...
journal_title:Journal of pharmaceutical sciences
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更新日期:1985-07-01 00:00:00
abstract::A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22766
更新日期:2012-01-01 00:00:00
abstract::A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...
journal_title:Journal of pharmaceutical sciences
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更新日期:2021-01-22 00:00:00
abstract::The dissolution rates of a number of drug-urethan solid-state dispersion systems were studied. A marked enhancement of the initial dissolution rates of several poorly water-soluble drugs was found when they were incorporated into a urethan matrix by heat fusion. These differences were considerable when pure substances...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670332
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abstract::The pre-equilibrium capillary zone electrophoretic (pre-eq CZE) method to determine association constants of active anionic forms of antithyroid drugs: 6-n-propyl-2-thiouracil (PTU), 6-methyl-2-thiouracil (MTU), 2-thiouracil (TU) with bovine serum albumin (BSA) under physiological pH 7.4 has been developed for the fir...
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journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
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更新日期:2020-10-07 00:00:00
abstract::The aim of the present study was to investigate the mechanism of aqueous degradation of Salinosporamide A (NPI-0052; 1), a potent proteasome inhibitor that is currently in Phase I clinical trials for the treatment of cancer and is characterized by a unique beta-lactone-gamma-lactam bicyclic ring structure. The degrada...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
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更新日期:2007-08-01 00:00:00
abstract::Plasma levels were determined frequently after single doses of perfluorooctyl bromide were administered to beagle dogs at doses of either 30.8 g/kg po or 3.9 g/kg intratracheally. The apparent first-order half-life during the terminal elimination phase was about 1 day after oral medication and about 7 days after intra...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
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abstract::After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...
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pub_type: 杂志文章
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abstract::The disposition of the beta-blocking drug talinolol is controlled by P-glycoprotein in man. Because talinolol is marketed as a racemate, we reevaluated the serum-concentration time profiles of talinolol of a previously published study with single intravenous (30 mg) and repeated oral talinolol (100 mg for 14 days) bef...
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更新日期:1999-02-01 00:00:00
abstract::The estimation of Michaelis-Menten pharmacokinetic parameters in patients with epilepsy receiving phenytoin continues to be a vexing problem. The various approximate methods suggested in the literature have serious shortcomings, primarily due to the role of the error term in the statistical model. In this report we pr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
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更新日期:1989-05-01 00:00:00
abstract::The use of enzymes as therapeutics is very promising because of their catalytic activity and specificity. However, intracellular delivery of active enzymes is challenging due to their low stability and large size. The production of protein-enzyme nanoparticles was investigated with the goal of developing a protein car...
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更新日期:2014-06-01 00:00:00
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journal_title:Journal of pharmaceutical sciences
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更新日期:1995-12-01 00:00:00
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journal_title:Journal of pharmaceutical sciences
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更新日期:1997-07-01 00:00:00
abstract::Tissue-specific ultrasonic enhancement can be used for the detection and characterization of atherosclerosis. We have previously demonstrated the generation of inherently echogenic (acoustically reflective) liposomes solely by varying lipid composition and controlling the method of production. In this study, echogenic...
journal_title:Journal of pharmaceutical sciences
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doi:10.1021/js9603515
更新日期:1997-02-01 00:00:00
abstract::Racemic and homochiral sodium ibuprofen were characterized by thermal analysis and powder X-ray diffractometry. The melting point phase diagram was constructed and thermodynamic calculation was performed. In contrast to racemic ibuprofen, which is a racemic compound, racemic sodium ibuprofen forms both a racemic congl...
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journal_title:Journal of pharmaceutical sciences
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