Abstract：
:It is shown that a suitable dosage interval, tau, can be estimated by a factor times the sum of the mean residence time (MRT) of the central compartment (MRTC) and the MRT of the absorption site (MRTA). This value of tau will provide a ratio, maximum steady-state plasma concentration: minimum steady-state plasma concentration, which averages approximately 2, such that the percent variation of the steady-state drug concentration is +/- 33%. It is shown that this approach produces vastly improved steady-state concentrations compared with those obtained when the tau value is chosen as equal to the apparent elimination half-life, which, classically, has been the approach usually used. When the drug is administered intravenously, the MRT of the absorption site in the above relationship is equal to zero. Suitable values of the "factor" in the above relationship were found to be 0.75 for the two-compartment open models with bolus iv administration, unity for the one-compartment open model with first-order absorption and elimination, and 1.35 for the classical two-compartment open model with first-order absorption.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Wagner JGdoi
10.1002/jps.2600760111subject
Has Abstractpub_date
1987-01-01 00:00:00pages
35-8issue
1eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47331-9journal_volume
76pub_type
杂志文章abstract：:Taxanes such as paclitaxel (Taxol) and docetaxel (Taxotere) are promising agents for use against ovarian cancer and other malignancies. Recently, SB-T-1011, a semisynthetic taxane, has been prepared from 14-hydroxy-10-deacetylbaccatin III. SB-T-1011 shows similar or greater in vitro cytostatic activity than paclitaxel...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600841204
更新日期：1995-12-01 00:00:00
abstract：:The tissue:plasma partition coefficients (Kp ) are good indicators of the extent of tissue distribution. Therefore, advanced tissue composition-based models were used to predict the Kp values of drugs under in vivo conditions on the basis of in vitro and physiological input data. These models, however, focus on animal...
journal_title：Journal of pharmaceutical sciences
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更新日期：2015-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670542
更新日期：1978-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.21697
更新日期：2009-11-01 00:00:00
abstract：:The acidic, neutral, and alkaline degradations of six therapeutically useful cephalosporins (cephalothin, cephaloridine, cephaloglycin, cephalexin, cephradine, and cefazolin), 7-amino-cephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and some 7-substituted derivatives were followed by high-pressure liquid ch...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600651104
更新日期：1976-11-01 00:00:00
abstract：:Flightless I (Flii) is an actin remodeling protein important for cytoskeletal regulation and cellular processes including migration, proliferation, and adhesion. Previous studies have clearly identified Flii as a novel therapeutical target for improved wound repair and have demonstrated Flii regulation using Flii neut...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2017.03.012
更新日期：2017-07-01 00:00:00
abstract：:The degradation kinetics of moricizine hydrochloride (1) were examined over a pH range of 0.6 to 6.0 at an ionic strength of 0.3 and 60 degrees C. The disappearance of intact 1 was followed by a stability-indicating HPLC assay. The degradation products, which had approximate solubilities of less than 100 micrograms/mL...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600810625
更新日期：1992-06-01 00:00:00
abstract：:The interaction of L-tryptophan with alpha-cyclodextrin was investigated in a 0.1 M phosphate buffer at pH 7.4 with a LKB 2277 microcalorimeter, using flow mixed mode at 25 degrees C. The thermodynamic parameters for inclusion complex formation obtained are as follows; DeltaG(0) = - 7.03 kJ/mol (K = 17.0), DeltaH(0) =...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/1520-6017(200102)90:2<134::aid-jps4>3.0.co
更新日期：2001-02-01 00:00:00
abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600790716
更新日期：1990-07-01 00:00:00
abstract：:A high-performance liquid chromatographic (HPLC) method for the simultaneous determination of pralidoxime chloride (I) and its major decomposition products in an injectable formulation is described. I and its decomposition products were detected and quantitated by their UV absorbances at 270 nm, after being separated ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600720710
更新日期：1983-07-01 00:00:00
abstract：:A simple enzyme immunoassay for the determination of captopril was developed. A specific antibody for captopril was produced in rabbits that were immunized with a hapten-bovine immunoglobulin G conjugate, which was prepared by using 4-(maleimidomethyl)cyclohexane carboxylic acid as a spacer group. The limit of detecti...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600750720
更新日期：1986-07-01 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
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doi：10.1002/jps.22766
更新日期：2012-01-01 00:00:00
abstract：:The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/1520-6017(200102)90:2<234::aid-jps14>3.0.c
更新日期：2001-02-01 00:00:00
abstract：:The development of an ocular dosage form containing xanthan gum and capable of interacting with mucin in the precorneal area is a challenge. The polymer concentration that can be applied is restricted because of the limited patient acceptability of highly viscous preparations. The precorneal mucin concentration is low...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.10106
更新日期：2002-04-01 00:00:00
abstract：:The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.24391
更新日期：2015-09-01 00:00:00
abstract：:The effects of physical aging and antiplasticization on the water transport properties of glassy cellulose acetate film-coated tablets were investigated. The gradual approach toward thermodynamic equilibrium during physical aging decrease the free volume of the polymers. This decrease in free volume is accompanied by ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600830337
更新日期：1994-03-01 00:00:00
abstract：:The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24575
更新日期：2016-02-01 00:00:00
abstract：:An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble parti...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23891
更新日期：2014-04-01 00:00:00
abstract：:This edition of the Journal of Pharmaceutical Sciences is dedicated to the wonderful career of Per Artursson from the Uppsala University. My Commentary focusses on Per's major contributions to the Caco-2 cell literature over the past 30 years. Two especially influential papers have been cited more than 1000 times out ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.08.016
更新日期：2021-01-01 00:00:00
abstract：:In this paper, we establish a mechanistic model for the prediction of amorphous solid dispersion (ASD) stability. The novel approach incorporates fundamental physical parameters, principally supersaturation, diffusivity, and interfacial energy, to model crystallization in ASDs accounting for both kinetic and thermodyn...
journal_title：Journal of pharmaceutical sciences
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abstract：:This study describes the synthesis of a new generation of immunotoxins made by a noncovalent interaction between a monoclonal antibody derivatized with a dichlorotriazinic dye and the ribosomal inhibitor protein gelonin. The scheme of preparation has several advantages with respect to the traditional methods, which us...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600830218
更新日期：1994-02-01 00:00:00
abstract：:The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.1080
更新日期：2001-09-01 00:00:00
abstract：:Pancreatic islet transplantation is a promising advanced therapy that has been used to treat patients suffering from diabetes type 1. Traditionally, pancreatic islets are infused via the portal vein, which is subsequently intended to engraft in the liver. Severe immunosuppressive treatments are necessary, however, to ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2019.10.028
更新日期：2020-01-01 00:00:00
abstract：:Nosocomial diarrhea and pseudomembranous colitis causing toxins A and B from Clostridium difficile were studied at pH 5-8 and over the temperature range of 10-85 degrees C. The proteins were crosslinked with formaldehyde to inactivate them to toxoid forms and permit their use as vaccines. Structural changes and aggreg...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.21261
更新日期：2008-09-01 00:00:00
abstract：:A α-helical GALA peptide (WEAALAEALAEALAEHLAEALAEALEALAA) has been found to possess dual functions: a pH-dependent inducer of endosomal escape, and a ligand that targets lung endothelium. In the present study, the flexibility of GALA was improved by modifying the edge with polyethylene glycol linker, to increase lung-...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2017.04.075
更新日期：2017-09-01 00:00:00
abstract：:Methods were developed for the determination of octanoic acid and N-acetyl-DL-tryptophan, which are used as stabilizers in the human blood-derived therapeutic products normal serum albumin and plasma protein fraction. The method for octanoic acid uses GC; quantitation is achieved using heptanoic acid as the internal s...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600730122
更新日期：1984-01-01 00:00:00
abstract：:A modification of wet agglomeration technique is developed and demonstrated by agglomerative crystallization process for a nonapeptide (ABT-510) to improve processing of needle like crystals. Our procedure involves exploiting partial miscibility of the crystallization solvent system for in situ generation of a wetting...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.21063
更新日期：2008-03-01 00:00:00
abstract：:Flexible manufacturing technologies for solid oral dosage forms with a continuous adjustability of the manufactured dose strength are of interest for applications in personalized medicine. This study explored the feasibility of using microvalve technology for the manufacturing of different solid oral dosage form conce...
journal_title：Journal of pharmaceutical sciences
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更新日期：2018-03-01 00:00:00
abstract：:The synthesis, characterization, and therapeutic evaluation of a series of partially esterified derivatives of pentetic (diethylenetriaminepentaacetic) acid are reported. These compounds were prepared in an attempt to promote increased decorporation of insoluble colloidal forms of plutonium, which are removed by pente...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600680219
更新日期：1979-02-01 00:00:00
abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...
journal_title：Journal of pharmaceutical sciences
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更新日期：2020-12-03 00:00:00
