Abstract：
:The reaction of chlorthalidone with methanol to give the corresponding methyl ether was investigated. The kinetics are pseudo-first-order in chlorthalidone, but the observed pseudo-first-order rate constants show an unexpected dependence on the initial chlorthalidone concentration, attributable to the presence of trace catalytic impurities in commercial chlorthalidone. Evidence is presented to show that trace heavy metals are probably responsible for the primary catalytic effect. Trace quantities of acetic acid are also present and show a smaller secondary catalytic effect. Kinetics in the presence of added heavy metals and acetic acid were examined. EDTA and povidone reduce the degradation rate. Stabilization by EDTA is due to its ability to chelate heavy metals. Stabilization by povidone is also primarily due to its ability to complex heavy metals; complexation data of ferric and nickel ions with povidone and with 1-methyl-2-pyrrolidinone as a monomer model are presented. In addition, complexation constants were calculated for the interaction of povidone with chlorthalidone, which may also play a role in stabilization.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Pandit NK,Hinderliter JSdoi
10.1002/jps.2600740811subject
Has Abstractpub_date
1985-08-01 00:00:00pages
857-61issue
8eissn
0022-3549issn
1520-6017pii
S0022-3549(15)46825-Xjournal_volume
74pub_type
杂志文章abstract：:The absorption of propicillin from the rat stomach and small intestine in situ was examined as a function of recirculating solution pH. The in vitro interphase transport from an aqueous buffer of various pH values to the octanol phase was also studied for several penicillins by the use of a two-phase rolling cell. The...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600671219
更新日期：1978-12-01 00:00:00
abstract：:Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.2600840214
更新日期：1995-02-01 00:00:00
abstract：:The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600821005
更新日期：1993-10-01 00:00:00
abstract：:Griseofulvin/cyclodextrin interactions were investigated in aqueous environment and in solid state. Two cyclodextrin derivatives (beta-cyclodextrin and 2-hydroxypropyl beta-cyclodextrin) were used to prepare different physical mixtures and kneaded systems, and the drug/cyclodextrin ratios were 1:1 and 1:2 mol/mol. Sca...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js970233x
更新日期：1998-07-01 00:00:00
abstract：:The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600801116
更新日期：1991-11-01 00:00:00
abstract：:The pharmaceutical industry has large investments in compound library enrichment, high throughput biological screening, and biopharmaceutical (ADME) screening. As the number of compounds submitted for in vitro ADME screens increases, data analysis, interpretation, and reporting will become rate limiting in providing A...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20020
更新日期：2004-05-01 00:00:00
abstract：:The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680208
更新日期：1979-02-01 00:00:00
abstract：:The new concept developed in this study is the design of poly(ethylene glycol) (PEG)-coated biodegradable nanoparticles coupled to folic acid to target the folate-binding protein; this molecule is the soluble form of the folate receptor that is overexpressed on the surface of many tumoral cells. For this purpose, a no...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/1520-6017(200011)89:11<1452::aid-jps8>3.0.
更新日期：2000-11-01 00:00:00
abstract：:The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23517
更新日期：2013-06-01 00:00:00
abstract：:We investigate the presence of a surface species for the active pharmaceutical ingredient (API) AZD9496 with dynamic nuclear polarization surface enhanced nuclear spectroscopy (DNP SENS). We show that using DNP we can elucidate the presence of an amorphous form of the API at the surface of crystalline particles of the...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.12.037
更新日期：2021-01-05 00:00:00
abstract：:Polymer shielded liposomes were investigated as detoxifying agents for the weak bases imipramine and dosulepin and the diprotic drug opipramol. In vitro binding measurements in the presence of human serum samples revealed that the liposomes reduced the free drug concentration of the weak bases (corrected for protein b...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21683
更新日期：2009-10-01 00:00:00
abstract：:In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different re...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731038
更新日期：1984-10-01 00:00:00
abstract：:A theoretical analysis of a proposed drug delivery device is presented. The device is of cylindrical shape with an opening on its side surface. Analytical expressions for the temporal variations in the amount of drug released and the size of the unreleased portion of the device are derived. The result of numerical sim...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810905
更新日期：1992-09-01 00:00:00
abstract：:It is shown that the existence of the second peak on the drug plasma concentration time curve C(p)(t) after iv bolus dosing can be explained by considering the traditional multi-compartmental linear pharmacokinetics. It was found that a direct solution of the general three-compartment model yields the second peak of C...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21151
更新日期：2008-06-01 00:00:00
abstract：:The effects of five conventional film-coating materials on tablet hardness were studied. Placebos showed apparently linear increases in hardness as coatings were applied. Completely coated samples exhibited hardness increases from 50 to 140%, with a corresponding 3% increase in tablet weight. Equations were derived re...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650908
更新日期：1976-09-01 00:00:00
abstract：:Magnetic resonance imaging (MRI) with chemical shift resolution is a recent extension of MRI and it provides information about species resolved molecular transport on the macroscopic scale in complex systems. In this contribution, we show that by using this novel method, one can predict the behavior of drug and food m...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20749
更新日期：2007-02-01 00:00:00
abstract：:A method for the simultaneous determination of etoricoxib and its carbon-13 analog ((13)C(6)-etoricoxib) from human plasma has been developed and used to support bioavailability studies. Plasma samples (0.5 mL) were extracted by using a 3M Empore 96-well plate (C(8)) and the resulting extracts were analyzed by using a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10038
更新日期：2002-02-01 00:00:00
abstract：:(14)N nuclear quadrupole resonance (NQR) in two known polymorphs of famotidine was measured. At room temperature, seven quadrupolar sets of transition frequencies (ν(+), ν(-), and ν(0)) corresponding to seven different nitrogen sites in the crystal structure of each of the two polymorphs were found. This confirms the ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23956
更新日期：2014-09-01 00:00:00
abstract：:The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS). Intranasal delivery is a noninvasive method that targets drugs to the brain and spinal cord along olfactory and trigeminal neural pathways, bypassing the BBB and minimizing systemic expo...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21604
更新日期：2009-07-01 00:00:00
abstract：:Correlations between the bioavailability parameters for erythromycin stearate tablets from five manufacturers and in vitro tests of these tablets were examined using forward (stepwise), multiple linear regression analysis. Bioavailability parameters were determined in clinical studies employing a balanced, incomplete ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：
更新日期：1980-11-01 00:00:00
abstract：:A series of even numbered fatty acid esters (C2-C18) of p-[N,N-bis(2-chloroethyl)amino]phenol were synthesized and evaluated as to acute toxicity as well as effectiveness against L-1210 mouse leukemia. The acetate through the decanoate derivatives demonstrated toxicity between 2 and 3 times that of phenol mustard in H...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710713
更新日期：1982-07-01 00:00:00
abstract：:A simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23296
更新日期：2012-11-01 00:00:00
abstract：:Trimethoprim undergoes thermally and photochemically catalyzed hydrolysis or oxidation to give rise to at least five products. The structures of these compounds were determined by physical methods and it was found that the resonance of C-5 in the 13C NMR spectrum is indicative of the substitution pattern of the result...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600780418
更新日期：1989-04-01 00:00:00
abstract：:Hyperlipidemia (HL) was previously shown to lower liver uptake of the more potent (-) enantiomer of ketoconazole (KTZ) in rat. The current study examined the possible modifying influence of experimental HL on a KTZ pharmacokinetic interaction with midazolam (MDZ). Normolipidemic and hyperlipidemic rats were administer...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22675
更新日期：2011-11-01 00:00:00
abstract：:In 2005, the World Health Organization (WHO) proposed that provided an active pharmaceutical ingredient could meet certain criteria, bioequivalence could be evaluated with a set of laboratory tests, obviating the need for expensive and time-consuming pharmacokinetic studies in humans. The aim of this work was to deter...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22349
更新日期：2011-03-01 00:00:00
abstract：:This article shows how milling can be used to explore the phase diagram of pharmaceuticals. This process has been applied to sulindac. A short milling has been found to trigger a polymorphic transformation between form II and form I upon heating which is not seen in the nonmilled material. This possibility was clearly...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.03.017
更新日期：2019-08-01 00:00:00
abstract：:In the present study, the interaction between phenobarbital and activated carbons which is driven by hydrophobic bonding was evaluated. The Two-Mechanism Langmuir-Like Equation was proposed to describe the isotherms for phenobarbital adsorbing to activated carbons. The parameters in the Two-Mechanism Langmuir-Like Equ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.06.018
更新日期：2019-01-01 00:00:00
abstract：:Three polymorphs (forms I-III), a monohydrate (form S2), and three new solvates [4:1 hydrate (form S1), monohydrate (form S3), and methanol half-solvate (form S4)] were isolated and characterized by X-ray powder diffractometry (XRPD), IR spectroscopy, differential scanning calorimetry (DSC), hot stage microscopy, solu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600841007
更新日期：1995-10-01 00:00:00
abstract：:Insight into the stratum corneum (SC) permeation pathway for hydrophilic compounds is gained by comparing experimental measurements of permeability and lag time (tlag) with the predictions of a finite element (FE) model. A database of permeability and lag time measurements (n=27) of hydrophilic compounds was compiled ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20695
更新日期：2006-10-01 00:00:00
abstract：:Methods for monitoring mechanical events occurring within particulate solids systems in a dynamic state are described. The electrical conductance and capacitance characteristics of such systems, as they relate to the degree of bed dilation or expansion, extent of interparticulate contact, and intensity of particle mot...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670825
更新日期：1978-08-01 00:00:00
