Abstract:
:Observed venous plasma concentrations of furosemide, propranolol, griseofulvin, and theophylline at 0.33 and 0.66 min after intravenous bolus injections to unanesthetized dogs were compared with those extrapolated using the instantaneous input hypothesis. At 0.33 min, extrapolated/observed plasma level ratios as high as 20.5, 65.5, 226, and 1.17 were found for these four drugs, respectively. Venous plasma levels peaked at 1 min postinjection in all studies. Total plasma areas (AUC0-->infinity) estimated using the instantaneous input principle were higher by as much as 6.0, 6.8, and 19.6% for propranolol, griseofulvin, and furosemide, respectively, when compared with experimental data. The effect on theophylline was negligible. These results suggest the need for cautious interpretation of some venous pharmacokinetic data. More studies in animals and humans are required to assess the magnitude of deviation from the instantaneous input hypothesis for drugs in general.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Chiou WL,Lam G,Chen ML,Lee MGdoi
10.1002/jps.2600700918subject
Has Abstractpub_date
1981-09-01 00:00:00pages
1037-9issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(15)43858-4journal_volume
70pub_type
杂志文章abstract::Three dimensional terahertz pulsed imaging (TPI) was evaluated as a novel tool for the nondestructive characterization of different solid oral dosage forms. The time-domain reflection signal of coherent pulsed light in the far infrared was used to investigate film-coated tablets, sugar-coated tablets, multilayered con...
journal_title:Journal of pharmaceutical sciences
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abstract::Although significant progress had been made in developing general scale-up rules for an aqueous pan-coating process, there are often scenarios where small-scale experiments are not found to be truly reflective of what may be observed at the large scale. This article reviews some of the methods traditionally used for s...
journal_title:Journal of pharmaceutical sciences
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abstract::The degradation kinetics of gonadorelin were investigated systematically with reversed-phase high-performance liquid chromatography. The stability-indicating properties of this system were checked with photodiode array detection and by comparison with capillary zone electrophoretic analysis. Influences of gonadorelin ...
journal_title:Journal of pharmaceutical sciences
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abstract::Mechanical shock may cause cavitation in vials containing liquid formulations of therapeutic proteins and generate protein aggregates and other particulates. To test whether common formulation components such as protein molecules, air bubbles, or polysorbate 20 (PS20) micelles might nucleate cavitation, a high-speed v...
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abstract::This whitepaper highlights current challenges and opportunities associated with continuous synthesis, workup, and crystallization of active pharmaceutical ingredients (drug substances). We describe the technologies and requirements at each stage and emphasize the different considerations for developing continuous proc...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.24252
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abstract::A sensitive, specific high-performance liquid chromatographic procedure was developed for the determination of plasma ethmozin levels. Basic plasma samples were partitioned with methylene chloride. The organic extract was washed with water and then evaporated to dryness under reduced pressure. The residue was redissol...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700433
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abstract::A titration method was developed for the determination of diphenhydramine, quinine, neostigmine, sparteine, strychnine, homatropine, atropine, physostigmine, and procaine in aqueous solution. Tetraphenylborate was used as a titrant with tetrabromophenolphthalein ethyl ester as an indicator in the presence of organic s...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600701128
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abstract::X-ray diffraction and infrared spectroscopy measurements for the N,N-dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) solvatomorphs of betulonic acid (BA) were investigated. BA [3-oxolup-20(29)-en-28-oic acid, C(30)H(46)O(3)] exhibits a wide spectrum of biological activities and is considered to be a promising na...
journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600780911
更新日期:1989-09-01 00:00:00
abstract::The effect of calcium ions on the structure and stability of recombinant human DNase I (rhDNase) in the aqueous and solid (lyophilized) states was investigated. Fourier transform infrared (FTIR) spectroscopy was used to examine the overall secondary structure, while chemical stability was monitored in terms of deamida...
journal_title:Journal of pharmaceutical sciences
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doi:10.1021/js980273g
更新日期:1999-04-01 00:00:00
abstract::The organic anion-transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs. Although the expression and function of this solute carrier transporter is well characterized in the human liver and other tissues, little i...
journal_title:Journal of pharmaceutical sciences
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abstract::Single crystal structure experiments revealed that the orthorhombic needles of Ciclesonide crystallized in P2(1)2(1)2(1) space group with four independent molecules in the unit cell. Amorphous Ciclesonide was prepared by lyophilization and characterized in comparison with crystalline material by differential scanning ...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.21223
更新日期:2008-09-01 00:00:00
abstract::Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700804
更新日期:1981-08-01 00:00:00
abstract::The heat of precipitation of dl-pseudoephedrine was determined by direct calorimetry using a Tronac isoperibolic calorimeter. The precipitation of dl-pseudoephedrine was induced by mixing aqueous solutions of the two enantiomers, namely, d- and l-pseudoephedrine, directly in the calorimeter. The molar heat of precipit...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600841017
更新日期:1995-10-01 00:00:00
abstract::The total synthesis of d-pilocarpine specifically labeled as N-14CH3 is reported. dl-Homopilopic acid was prepared as a key intermediate and resolved into the d-enantiomer via the alpha-methylbenzylamine salt. The penultimate intermediate, 2-mercaptopilocarpine, was desulfurized by oxidation with dilute hydrogen perox...
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journal_title:Journal of pharmaceutical sciences
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更新日期:2008-12-01 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
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doi:10.1002/jps.2600661223
更新日期:1977-12-01 00:00:00
abstract::A series of unrelated steroids were tested for antimineralocorticoid activity by Kagawa's test in male rats and by modified test in female rats. Adrenalectomized male rats given 12 mcg desoxycorticosterone (DOC) and 2.5 ml normal saline received 1 mg of the test steroid, and their urine was analyzed for sodium and po...
journal_title:Journal of pharmaceutical sciences
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更新日期:1999-07-01 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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更新日期:1979-02-01 00:00:00
abstract::Various novel diesters of pilocarpic acid were synthesized and evaluated as prodrug forms for pilocarpine with the aim of improving the ocular delivery characteristics of the drug. The pilocarpic acid monoesters previously studied cyclized spontaneously to pilocarpine in aqueous solution and although they showed enhan...
journal_title:Journal of pharmaceutical sciences
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abstract::Hemoglobin microcapsules were prepared through cross-linking of hemoglobin itself with various acyldichlorides. Variations in the reticulation conditions were preformed in order to ameliorate the oxygen dissociation curve, the mean diameter, and the possibility for the microcapsules to be lyophilized. With terephthalo...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600710710
更新日期:1982-07-01 00:00:00
abstract::Injectable controlled-release formulations are of increasing interest for the treatment of chronic diseases. This study aims to develop and characterize a polymeric matrix for intramuscular or subcutaneous injection, consisting of two biocompatible polymers, particularly suitable for formulating poorly soluble drugs. ...
journal_title:Journal of pharmaceutical sciences
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更新日期:2012-09-01 00:00:00
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...
journal_title:Journal of pharmaceutical sciences
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abstract::Recently, our laboratory reported that intravenous immunoglobulin (IVIG) treatment increased antiplatelet antibody (7E3) clearance in a rat model of immune thrombocytopenic purpura (ITP). However, due to the multifaceted nature of IVIG therapy, the contribution of this increase in antiplatelet antibody clearance to th...
journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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更新日期:2002-03-01 00:00:00
abstract::Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absor...
journal_title:Journal of pharmaceutical sciences
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更新日期:1975-09-01 00:00:00