Abstract:
:A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was injected onto a reversed-phase trimethylsilyl-packed column and eluted with an acetate-acetonitrile mobile phase containing an ion-paired reagent. The method provides an absolute recovery of 71-76% and a day-to-day precision of 5.4-9.1% for each compound at 25 ng/ml. The minimum quantifiable level for all three compounds was 5 ng/ml (RSD greater than 11%), and the detector response was linear up to 500 ng/ml. Fixed-dose steady-state plasma level data for 34 patients are reported.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Suckow RF,Cooper TB,Quitkin FM,Stewart JWdoi
10.1002/jps.2600710812subject
Has Abstractpub_date
1982-08-01 00:00:00pages
889-92issue
8eissn
0022-3549issn
1520-6017pii
S0022-3549(15)44296-0journal_volume
71pub_type
杂志文章abstract::Pinacidil [(+/-)-2-cyano-1-(4-pyridyl)-3-(1,2,2-trimethylpropyl)guanidine monohydrate] is a novel, direct-acting vasodilator antihypertensive agent. The cyano 14C-labeled drug is rapidly and completely absorbed after an oral 12.5-mg dose in solution. The blood:plasma concentration ratios (0.8-0.9) indicate transient p...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600770212
更新日期:1988-02-01 00:00:00
abstract::The distribution conditions in oil-water emulsions prepared by emulsifying a 1:1 eutectic mixture of lidocaine and prilocaine with a nonionic surfactant in water were studied by membrane and gel filtration methods. In this system, the local anesthetics are considered to be freely dissolved, surfactant solubilized, and...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600741112
更新日期:1985-11-01 00:00:00
abstract::Incorporation of starch USP or a modified cornstarch within the granules of several drug formulations was investigated. In general, the formulation containing the modified starch exhibited improved processing characteristics as well as improved tablet properties. A comparison of a granulated and a direct compression f...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600640231
更新日期:1975-02-01 00:00:00
abstract::Several controlled ice nucleation techniques have been developed to increase the efficiency of the freeze-drying process as well as to improve the quality of pharmaceutical products. Owing to the reduction in ice surface area, these techniques have the potential to reduce the degradation of proteins labile during free...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.10.020
更新日期:2018-03-01 00:00:00
abstract::Ascorbic acid (100 mg/ml) and sodium bisulfite (0.5 and 20 mg/ml) prevented more than 10% oxidation of apomorphine hydrochloride in water maintained at room temperature over 1-3 days. Refrigeration at 5 degrees prevented oxidation of apomorphine hydrochloride in aqueous solutions for 1 week. Neither ascorbic acid nor ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600690830
更新日期:1980-08-01 00:00:00
abstract::Modified cyclodextrins (CDs) have shown great promise as non-viral gene and siRNA delivery vectors in a range of in vitro and in vivo studies. In the current study, structural and biophysical characterisation of selected CDs was carried out to enhance our understanding of their interaction with nucleic acids. The meth...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23922
更新日期:2014-05-01 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::A multidisciplinary team approach to identify pharmaceutical impurities is presented in this article. It includes a representative example of the methodology. The first step is to analyze the sample by LC-MS. If the structure of the unknown impurity cannot be conclusively determined by LC-MS, LC-NMR is employed. If th...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20120
更新日期:2004-09-01 00:00:00
abstract::A major impediment of many QSAR-type analyses is that the data show a maximum or minimum and can no longer be adequately described by linear functions that provide unrivaled simplicity and usually give good description over more restricted ranges. Here, a general linearized biexponential (LinBiExp) model is proposed t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20438
更新日期:2005-11-01 00:00:00
abstract::A crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cepha...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600671033
更新日期:1978-10-01 00:00:00
abstract::Quantification of protein binding of new chemical entities is an important early screening step during drug discovery and is of fundamental interest for the estimation of safety margins during drug development. In this publication, we describe the development of a new high-throughput assay for the determination of the...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10588
更新日期:2004-04-01 00:00:00
abstract::Toxin-conjugates, complexes designed from the fusion of tissue toxins and pathology-specific ligands, offer the potential for targeted cytotoxic therapy. Some have postulated that the recurrent failure of these conjugates to exhibit benefit in animal models of vascular injury arose because the timing and frequency of ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980086i
更新日期:1998-11-01 00:00:00
abstract::A multichannel continuous-flow apparatus for dissolution rate measurements is described. Typical data are presented to demonstrate its utility for studies with bulk drug powders as well as with tablets and capsules without any change of setup. Procedures are given for the preparation of powder samples for dissolution ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600641024
更新日期:1975-10-01 00:00:00
abstract::The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24439
更新日期:2015-06-01 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
abstract::Human skin samples are permeable to theophylline delivered from 1.5% solutions in various alkanecarboxylic acids and their mixtures. The respective permeability coefficients of theophylline, calculated from steady-state flux, correlate negatively with the permeability coefficients of the donor carboxylic acids and pos...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600761004
更新日期:1987-10-01 00:00:00
abstract::The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600810216
更新日期:1992-02-01 00:00:00
abstract::Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing metronidazole are reviewed. Metronidazole can be assigned to Biopharmaceutics Classification System Class I. Most BE studies that were identifi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22409
更新日期:2011-05-01 00:00:00
abstract::The intrinsic factor-mediated binding of cyanocobalamin to cholestyramine was studied in vitro under varying conditions of pH, added electrolyte, and bile salt. The intrinsic factor-cyanocobalamin complex was adsorbed strongly by the resin at pH 3 in the presence of neutral salt and low concentrations of glycocholic a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600671132
更新日期:1978-11-01 00:00:00
abstract::A high-performance liquid chromatographic method was developed for the simultaneous determination of azobenzene, hydrazobenzene, and four other decomposition products in phenylbutazone injectable formulations. Separation was achieved on a C18 column, with 0.1 M Tris-citrate buffer (pH 5.25) and acetonitrile (52:48), a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600731211
更新日期:1984-12-01 00:00:00
abstract::The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670446
更新日期:1978-04-01 00:00:00
abstract::The stereospecificity of the metabolic reduction of arylalkylketones was investigated. The ketones, propiophenone (I), phenyl-acetone (III), and 1-phenyl-1,2-propanedione (V) were reduced in vitro and in vivo in rats and rabbits to the corresponding alcohols, 1-phenyl-1-propanol (II), 1-phenyl-2-propanol (IV), and 1-p...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600711220
更新日期:1982-12-01 00:00:00
abstract::Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.09.031
更新日期:2019-01-01 00:00:00
abstract::Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650612
更新日期:1976-06-01 00:00:00
abstract::The free radical scavenger properties of vitamin E (DL-alpha-tocopherol), a natural antioxidant, and derivatives were studied using an original in vitro method consisting of free radical production by photoirradiation of pheomelanin and direct detection of the free radicals by a physical, specific technique, electron ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840124
更新日期:1995-01-01 00:00:00
abstract::Experimental sulfadiazine tablets prepared by direct compression, using a commercially available direct compression tablet mass, were compared with experimental sulfadiazine tablets prepared by fluidized-bed granulation and commercially available sulfadiazine tablets USP. The values for friability and the time require...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600661023
更新日期:1977-10-01 00:00:00
abstract::The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23832
更新日期:2014-02-01 00:00:00
abstract::Mixture response-surface methodology can be used as a technique to predict solubility in mixed solvent systems. The present report shows that if the intent is to predict solubility in nonideal solutions, mixture response-surface methodology is a better technique than one which assumes a particular mechanism to hold tr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600740206
更新日期:1985-02-01 00:00:00
abstract::Corneal permeability data taken from the literature were analyzed for possible quantitative relationships with physicochemical properties. Although a parabolic relationship was obtained with good correlation between lipophilicity, as expressed by the 1-octanol-water partition coefficients, log Poctanol (or the distrib...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js960076m
更新日期:1996-08-01 00:00:00
abstract::To evaluate the regional delivery of conventional aerosol medications, a new whole-lung computational fluid dynamics modeling approach was applied for metered dose inhaler (MDI) and dry powder inhaler (DPI) aerosols delivered to healthy and constricted airways. The computational fluid dynamics approach included comple...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2015.11.027
更新日期:2016-01-01 00:00:00