Abstract：
:Current drug level predictions in nonlinear pharmacokinetics are based on specific pharmacokinetic models in contrast to the model-independent (structureless), dose-linearity, and superposition principles used in linear pharmacokinetics. Such model-dependent methods may not provide reliable predictions due to their inherent nonuniqueness, computational complexity, and often unrealistic kinetic assumptions. Some novel model-independent methods for predicting the steady-state drug levels of extravascular, intravenous bolus, and intravenous infusion administrations are presented that should overcome such disadvantages. The methods only assume an autonomic nonlinear kinetic behavior, which implies that following an intravenous bolus administration the derivatives of the drug concentration-time profile at arbitrary drug levels are independent of the dose given. Such a kinetic behavior is found for any nonlinear pharmacokinetic system when the rate of change of the drug level following an intravenous bolus administrations depends only on the drug level, i.e., dC/dt = -q(C), where q can be any function dependent only on C and time-invariant kinetic parameters. The basic approach presented represents a novel alternative which avoids the very difficult and often impractical task of identifying and incorporating the numerous kinetic parameters and processes responsible for the observed drug concentration data into a useful pharmacokinetic model. The focus in the kinetic analysis is instead on two much simpler processes: (a) fitting empirical functions to estimate the mean drug disposition behavior of the subject or population and (b) testing the validity of the assumptions involved.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Veng-Pedersen Pdoi
10.1002/jps.2600730614subject
Has Abstractpub_date
1984-06-01 00:00:00pages
761-5issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(15)46184-2journal_volume
73pub_type
杂志文章abstract：:A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690318
更新日期：1980-03-01 00:00:00
abstract：:Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24544
更新日期：2015-10-01 00:00:00
abstract：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730136
更新日期：1984-01-01 00:00:00
abstract：:The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22428
更新日期：2011-05-01 00:00:00
abstract：:The highly lipid soluble, free-base form of halofantrine (Hf base; approximately 50 mg/mL in triglyceride lipids), a highly lipophilic (calculated log P approximately 8.5) antimalarial, has recently been shown to undergo significant intestinal lymphatic transport (54% of administered dose) after postprandial administr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10045
更新日期：2002-03-01 00:00:00
abstract：:The axial and radial tensile strengths were compared to the hardness of compressed tablets containing various concentrations of lubricants. Since radial tensile strength measurement considers the thickness of a tablet, and only tensile stress and axial tensile strength express the strength in the direction in which ca...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710625
更新日期：1982-06-01 00:00:00
abstract：:In this paper, we demonstrate that by employing a combination of sedimentation field-flow fractionation (sedFFF) and other characterization techniques, such as photon correlation spectroscopy (PCS) and freeze-fracture electron microscopy (EM), it is possible to show that commercial fat emulsions of similar overall che...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600831114
更新日期：1994-11-01 00:00:00
abstract：:A GLC method is presented for the quantitative determination of menthol, phenol, benzocaine, and pyrilamine maleate. The propellent was exhausted from a pressurized can, and an aliquot of the alcoholic base was weighed. After the addition of the internal standard diluted with chloroform, 1 microliter of the mixture wa...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600701015
更新日期：1981-10-01 00:00:00
abstract：:Inclusion complexes between beta-cyclodextrin derivatives and 1, 2-dithione-3-thiones were studied in aqueous solution and in the solid state. Phase solubility study was used to evaluate the complexation in solution, at 37 degrees C, of three cyclodextrins, i. e., beta-cyclodextrin (betaCD), hydroxypropyl-beta-cyclode...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js990067o
更新日期：1999-09-01 00:00:00
abstract：:The recently developed hydrogen-bonding propensity tool in the Cambridge Structural Database software package (Mercury) was tested to predict polymorphs. The compounds for the study were chosen from a list of approximately 300 pharmaceutically important compounds, for which multiple crystal forms had not been previous...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24449
更新日期：2015-06-01 00:00:00
abstract：:Near infrared (NIR) spectroscopy was used for quantitatively monitoring polymorph conversion of an active pharmaceutical ingredient (API) in wet granulation. The API under pharmaceutical development has two different polymorphs. Polymorph A is the stable form for drug development and polymorph B is the undesired form ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20501
更新日期：2005-12-01 00:00:00
abstract：:A procedure was developed for the separation and selective quantitative determination of the (S)(+)- and (R)(-)-enantiomers of the racemic anti-inflammatory drug carprofen as their diastereomeric l-(-)-alpha-methylbenzylamides. These derivatives are obtained in equivalent yields by reacint purified 14C-carprofen from ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600681021
更新日期：1979-10-01 00:00:00
abstract：:The objective of this study was to establish the optimal blood concentrations of the potent P-glycoprotein (P-gp) inhibitor GF120918 (Elacridar) required to achieve maximal knockout of this efflux transporter in the blood-brain barrier (BBB) of mice, rats, and guinea pigs. Genetic mdr1a/b(-/-) knockout mice and "chemi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20658
更新日期：2006-09-01 00:00:00
abstract：:The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23094
更新日期：2012-06-01 00:00:00
abstract：:A rapid and simple high-performance liquid chromatographic (HPLC) method for the analysis of dichlorophen in raw material and in dichlorophen-toluene soft gelatin capsules for veterinary use was developed using a reverse-phase technique. This HPLC system was shown to isolate dichlorophen from its major impurity (the t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730629
更新日期：1984-06-01 00:00:00
abstract：:One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.09.055
更新日期：2021-01-01 00:00:00
abstract：:Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9504245
更新日期：1996-07-01 00:00:00
abstract：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24253
更新日期：2015-02-01 00:00:00
abstract：:This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24646
更新日期：2015-12-01 00:00:00
abstract：:Mathematical models were determined relating preservative concentration and D values (decimal reduction times at 25 degrees C; pH 6.9-7.1) against Escherichia coli in aqueous medium. Preservatives investigated were 2-bromo-2-nitro-1,3-propanediol (Bronopol), N-(hydroxymethyl)-N-(1,3-dihydroxymethyl-2, 5-dioxo-4-imidaz...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740820
更新日期：1985-08-01 00:00:00
abstract：:The aims of this study were to evaluate the pharmacokinetics of doripenem (Finibax®, Doribax®, S-4661), a parenteral carbapenem antibiotic, in pediatric patients based on concentrations of doripenem in plasma after administration of 20 mg/kg 2 or 3 times daily and to evaluate the dosing regimens by using Monte-Carlo p...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.04.002
更新日期：2019-09-01 00:00:00
abstract：:Poly(D,L-lactide-co-glycolide, 50:50) samples of similar molecular weight were obtained from three commercial sources and were characterized by gel permeation chromatography, differential scanning calorimetry, X-ray powder diffraction, viscometry, and proton nuclear magnetic resonance spectroscopy. Pellets were prepar...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600820322
更新日期：1993-03-01 00:00:00
abstract：:Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ. Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680706
更新日期：1979-07-01 00:00:00
abstract：:Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24085
更新日期：2014-10-01 00:00:00
abstract：:A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731245
更新日期：1984-12-01 00:00:00
abstract：:Jet-milling as the common way for micronization of drugs shows several disadvantages. Drug powder properties are decisive for pulmonary use because, besides a small particle size, a good deagglomeration behavior is required. In this study, several anti-inflammatory drugs [beclomethasone-17,21-dipropionate (BDP), betam...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10274
更新日期：2003-01-01 00:00:00
abstract：:The human immunodeficiency virus has infected millions of people and the epidemic continues to grow rapidly in some parts of the world. Antiretroviral (ARV) therapy has provided improved treatment and prolonged the life expectancy of patients. Moreover, there is growing interest in using ARVs to protect against new in...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1016/j.xphs.2016.09.015
更新日期：2016-12-01 00:00:00
abstract：:A method is presented for encapsulating high molecular weight biological materials such as viral antigen, concanavalin A, and other proteins with cellulose acetate phthalate. The method is simple, inexpensive, and rapid; the process takes approximately 15 min. Capsules generated by this method are produced as microsph...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730110
更新日期：1984-01-01 00:00:00
abstract：:Chromatographic gel filtration matrixes used in various separation techniques are subject to microbial contamination. The need for a microbe-free column is critical when preparing materials that require a low or zero microbial count. This report proposes two alternative washing systems: 0.02 N HCl containing 0.81% NaC...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690205
更新日期：1980-02-01 00:00:00
abstract：:Polymethyl [1-14C]methacrylate nanoparticles were administered orally to bile cannulated rats. Ten to fifteen percent of the administered radioactivity was absorbed and found in the bile and urine. Within 48 h, 94-97% of the absorbed radioactivity had been eliminated from the body. After 8 d, the highest residual radi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730934
更新日期：1984-09-01 00:00:00
