Possibility of Predicting Serotonin Transporter Occupancy From the In Vitro Inhibition Constant for Serotonin Transporter, the Clinically Relevant Plasma Concentration of Unbound Drugs, and Their Profiles for Substrates of Transporters.

abstract：:Personalized medicine aims to determine the most adequate treatment and dose regimen to obtain the maximum efficacy and minimum side effect by taking into account patients' characteristics. For numerous reasons, one being ethical and methodological hurdles in including specific populations in clinical trials, innovati...

journal_title：Journal of pharmaceutical sciences

authors： Marsousi N,Desmeules JA,Rudaz S,Daali Y

更新日期：2017-09-01 00:00:00

abstract：:Two nonporous and three porous amorphous silicas were used as dispersion media to convert corticoid solutions into free-flowing powders. The corticoids (prednisone, prednisolone, and hydrocortisone) were dissolved in N,N-dimethylacetamide-polyethylene glycol 400 (7:3 v/v) and their 10% (w/v) solutions were mixed with ...

journal_title：Journal of pharmaceutical sciences

authors： Liao CC,Jarowski CI

更新日期：1984-03-01 00:00:00

abstract：:A novel process based on solvent extraction was developed to produce drug-loaded polyanhydride microspheres for controlled-release applications. The technique consists of adding a chloroform solution of polyanhydride and drug into a stirred silicone oil phase containing suspended droplets of surfactant. No chemical re...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Leong K,Mathiowitz E,Langer R

更新日期：1988-08-01 00:00:00

abstract：:Pharmaceutical scientists are often asked to assess the impact of modifications to the illumination in the manufacturing and product packaging environment on product quality. To assess the impact of switching light sources, four model compounds were exposed to standard fluorescent light, LED, and "yellow light" and th...

journal_title：Journal of pharmaceutical sciences

authors： Wasylaschuk W,Pierce B,Geng X,Socia A,Kim D,Wuelfing WP,Abend A

更新日期：2020-11-01 00:00:00

abstract：:Reported estrone pKa and solubility data show wide variation. Improved experimental procedures were designed and used to obtain reproducible results. The pKa values for several estrogens and related compounds also were determined to assess the effects of structural differences on ionization. No evidence was obtained f...

journal_title：Journal of pharmaceutical sciences

authors： Hurwitz AR,Liu ST

更新日期：1977-05-01 00:00:00

abstract：:A stereoselective and sensitive method for the determination of nilvadipine, a new dihydropyridine calcium antagonist, in human plasma was developed. An internal standard, the deuterated analogue of racemic nilvadipine, was added to the plasma and extracted with an n-hexane:ethyl acetate (92.5:7.5) mixture under alkal...

journal_title：Journal of pharmaceutical sciences

authors： Tokuma Y,Fujiwara T,Noguchi H

更新日期：1987-04-01 00:00:00

abstract：:The P-glycoprotein (Pgp), a drug efflux pump, is expressed in intestinal epithelial cells, where it constitutes a barrier against xenobiotics. In inflammatory bowel disease, a dysregulation in the production of tumor necrosis factor (TNF)alpha and interferon (IFN)gamma, and an alteration of Pgp expression and activity...

journal_title：Journal of pharmaceutical sciences

authors： Belliard AM,Lacour B,Farinotti R,Leroy C

更新日期：2004-06-01 00:00:00

abstract：:Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

journal_title：Journal of pharmaceutical sciences

authors： Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

更新日期：2010-09-01 00:00:00

abstract：:A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...

journal_title：Journal of pharmaceutical sciences

authors： Ghanekar AG,Das Gupta V

更新日期：1978-06-01 00:00:00

abstract：:A high-performance liquid chromatographic method for the simultaneous determination of propranolol and 4-hydroxypropranolol in plasma is presented. The method involves plasma extraction at basic pH with ethyl column, and fluorescence detection. The within-run a reversed-phase column coefficient of variation were 3.0-7...

journal_title：Journal of pharmaceutical sciences

authors： Rosseel MT,Bogaert MG

更新日期：1981-06-01 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

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:Investigation of the leaves of Montanoa tomentosa Cerv. ssp. microcephala (Sch.-Bip.) Funk (Compositae) resulted in the isolation of three novel guaianolide sesquiterpenes, montacephalin (1), tomencephalin (2), and 5-hydroxytomencephalin (3), which were shown to be cytotoxic (P-388). The structures of these sesquiterp...

journal_title：Journal of pharmaceutical sciences

authors： Topcu G,Cordell GA,Farnsworth NR,Fong HH

更新日期：1988-06-01 00:00:00

abstract：:A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...

journal_title：Journal of pharmaceutical sciences

authors： Thornhill DP,Schwerzel E

更新日期：1985-05-01 00:00:00

abstract：:Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...

journal_title：Journal of pharmaceutical sciences

authors： Schantz S,Hoppu P,Juppo AM

更新日期：2009-05-01 00:00:00

abstract：:A GLC determination of cyclobenzaprine in human plasma and urine is described. After extraction from alkalinized samples with heptane-isopentyl alcohol (97:3), the drug and internal standard were back-extracted into 0.1 N HCl and then reextracted into ether. Use of a lower homolog of the drug as an internal standard w...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Stauffer SC

更新日期：1976-08-01 00:00:00

abstract：:Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...

journal_title：Journal of pharmaceutical sciences

authors： Almarsson O,Kaufman MJ,Stong JD,Wu Y,Mayr SM,Petrich MA,Williams JM

更新日期：1998-05-01 00:00:00

abstract：:Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

journal_title：Journal of pharmaceutical sciences

authors： Segarra I,Movshin DA,Zarif L

更新日期：2002-08-01 00:00:00

abstract：:The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...

journal_title：Journal of pharmaceutical sciences

authors： Nakano NI,Oshio T,Fujimoto Y,Amiya T

更新日期：1978-07-01 00:00:00

abstract：:The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

journal_title：Journal of pharmaceutical sciences

authors： Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

更新日期：2004-06-01 00:00:00

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

authors： Pandey P,Bindra DS

更新日期：2014-11-01 00:00:00

abstract：:Bacmecillinam is an amdinocillin prodrug designed to be easily hydrolyzed in biological materials, so special procedures were developed for the collection of blood specimens. Whole blood was collected in tubes containing bacampicillin as an adsorption inhibitor and kept at -70 degrees; the extracting solvent, hexane-m...

journal_title：Journal of pharmaceutical sciences

authors： Westerlund D,Pettersson B,Carlqvist J

更新日期：1982-10-01 00:00:00

abstract：:We report the preparation and structural characterization of a family of primary alcohol solvates of a small-molecule hydrochloride salt. The structures of the solvates are probed by powder and single crystal X-ray diffraction, and the compounds were additionally characterized by polarized light microscopy, thermograv...

journal_title：Journal of pharmaceutical sciences

authors： Vasudevan KV,Peterson ML

更新日期：2018-06-01 00:00:00

abstract：:Application of low-frequency ultrasound has been shown to enhance transdermal transport of drugs (low-frequency sonophoresis). In this paper, we show that the efficacy of low-frequency ultrasound in enhancing transdermal transport can be further increased by its combination with sodium lauryl sulfate (SLS), a well-kno...

journal_title：Journal of pharmaceutical sciences

authors： Mitragotri S,Ray D,Farrell J,Tang H,Yu B,Kost J,Blankschtein D,Langer R

更新日期：2000-07-01 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

authors： Wiseman EH,McIlhenny HM,Bettis JW

更新日期：1975-09-01 00:00:00

abstract：:In pharmaceutical development alternative drug delivery modalities are being increasingly employed. One example is an implant, which achieves gradual drug release in patients over a period of many months or years. Due to the complexity of these long-acting formulations, advanced physical characterization methods are d...

journal_title：Journal of pharmaceutical sciences

authors： Skomski D,Liu Z,Su Y,John CT,Doty A,Forster SP,Teller R,Barrett SE,Xu W

更新日期：2020-09-01 00:00:00

abstract：:The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

journal_title：Journal of pharmaceutical sciences

authors： Shaik N,Pan G,Elmquist WF

更新日期：2008-12-01 00:00:00

abstract：:A round-robin study compared four methods of residual ethylene oxide analysis. Results from the six participating laboratories, along with a statistical treatment of the data, are presented. ...

journal_title：Journal of pharmaceutical sciences

authors： Romano SJ,Renner JA

更新日期：1975-08-01 00:00:00

abstract：:The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the t...

journal_title：Journal of pharmaceutical sciences

authors： Kawakami S,Nishida K,Mukai T,Yamamura K,Kobayashi K,Sakaeda T,Nakamura J,Nakashima M,Sasaki H

更新日期：2001-12-01 00:00:00

abstract：:Free radical polymerization converts aqueous solutions of methacrylated inulin into cross-linked hydrogels. The purpose of this work was to study the hydrogel formation and to characterize the fully cured hydrogels. The gelation process of aqueous solutions of methacrylated inulin was monitored as a function of time b...

journal_title：Journal of pharmaceutical sciences

authors： Vervoort L,Vinckier I,Moldenaers P,Van den Mooter G,Augustijns P,Kinget R

更新日期：1999-02-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00