Bioequivalence of long half-life drugs--informative sampling determination--using truncated area in parallel-designed studies for slow sustained-release formulations.

abstract：:Boron analogues of carbamoylcholine and thiocholine and esters of these analogues were prepared. These compounds were fairly stable toward hydrolysis and demonstrated moderate anti-inflammatory and hypolipidemic activities in mice. The hypolipidemic activity of the compounds at a dose of 8 mg/kg/day was equivalent in ...

journal_title：Journal of pharmaceutical sciences

authors： Sood A,Sood CK,Spielvogel BF,Hall IH,Wong OT

更新日期：1992-05-01 00:00:00

abstract：:The crystal structures of the analgesic compounds anhydrous naloxone and naltrexone hydrochloride were determined ab initio from high resolution laboratory X-ray powder diffraction data. Both compounds crystallize in the orthorhombic space group P2(1)2(1)2(1) with lattice parameters of a = 14.6588(10) A, b = 17.4363(9...

journal_title：Journal of pharmaceutical sciences

authors： Sugimoto K,Dinnebier RE,Zakrzewski M

更新日期：2007-12-01 00:00:00

abstract：:In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Kita Y

更新日期：2000-05-01 00:00:00

abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2004-01-01 00:00:00

abstract：:Uptake of the fluorescent probe, 1-anilino-8-naphthalene-sulfonate (I) into isolated rat liver cells was studied using both fluorescence and filtration methods. The time course of the fluorescence enhancement of I after addition to the isolated liver cells was analyzed in terms of rapid, medium, and slow phases. The s...

journal_title：Journal of pharmaceutical sciences

authors： Sugiyama Y,Kimura S,Lin JH,Izukura M,Awazu S,Hanano M

更新日期：1983-08-01 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

authors： Rippie EG,Kriesel DC,Rettig H

更新日期：1978-08-01 00:00:00

abstract：:It is shown that a suitable dosage interval, tau, can be estimated by a factor times the sum of the mean residence time (MRT) of the central compartment (MRTC) and the MRT of the absorption site (MRTA). This value of tau will provide a ratio, maximum steady-state plasma concentration: minimum steady-state plasma conce...

journal_title：Journal of pharmaceutical sciences

authors： Wagner JG

更新日期：1987-01-01 00:00:00

abstract：:The aim of this study is to prepare novel pH-sensitive beads to obtain a gastric mucosa protective formulation and to ensure drug delivery into the intestine. Diclofenac sodium was used as a model drug. Bead formation was achieved by ionotropic gelation method using three-component gel system containing sodium alginat...

journal_title：Journal of pharmaceutical sciences

authors： Fenyvesi Z,Auner A,Schmalz D,Pásztor E,Csóka G,Gyires K,Marton S,Klebovich I,Antal I

更新日期：2009-11-01 00:00:00

abstract：:Numerous case reports have documented that phenylpropanolamine (PPA) stimulates the central nervous system with symptoms ranging from anxiety and hallucinations to grand mal seizures produced by overdoses. Most of these reports have occurred following concomitant use of caffeine which in high doses is known to cause s...

journal_title：Journal of pharmaceutical sciences

authors： Walker JS

更新日期：1989-12-01 00:00:00

abstract：:To study if electrostatic charge initially present in mannitol powder plays a role in the generation of aerosols, mannitol was unipolarly charged to varying magnitudes by tumbling the powder inside containers of different materials. The resulting charge in the powder was consistent with predictions from the triboelect...

journal_title：Journal of pharmaceutical sciences

authors： Adi H,Kwok PC,Crapper J,Young PM,Traini D,Chan HK

更新日期：2010-05-01 00:00:00

abstract：:The pharmacokinetics and safety of TY-11345 [(+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt], a novel gastric proton pump inhibitor, were studied in healthy male volunteers after single (20, 40, and 80 mg) and repeated oral doses (60 mg, once daily for 7 day...

journal_title：Journal of pharmaceutical sciences

authors： Uematsu T,Nakano M,Kosuge K,Nagai A,Sato A,Nakashima M

更新日期：1994-10-01 00:00:00

abstract：:In spite of the recent advances in technology to optimize the absorption, distribution, metabolism and elimination (ADME) properties of new and promising medicinal products to reduce clinical failures, the investigation of drug disposition in the pediatric and elderly populations continues to be under evaluated. With ...

journal_title：Journal of pharmaceutical sciences

authors： Chien JY,Ho RJ

更新日期：2011-01-01 00:00:00

abstract：:A rapid solubility-screening assay was developed with a focus on Biopharmaceutic Classification Scheme (BCS) class II drug solubility in animal and simulated human gastrointestinal (GI) fluids. The assay enables biologically promising drug leads to be evaluated for solubility limitations earlier in the drug developmen...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Elzinga PA,Hageman MJ,Herron JN

更新日期：2008-04-01 00:00:00

abstract：:Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...

journal_title：Journal of pharmaceutical sciences

authors： Borne RF,Law SJ,Kapeghian JC,Masten LW

更新日期：1980-09-01 00:00:00

abstract：:The widespread use of butylated hydroxyanisole (I) and butylated hydroxytoluene (II) as food antioxidants recently has been criticized by the Food and Drug Administration because of their pharmacological and toxicological effects. Interest also has arisen recently in the use of these compounds as anticancer agents. Th...

journal_title：Journal of pharmaceutical sciences

authors： El-Rashidy R,Niazi S

更新日期：1980-12-01 00:00:00

abstract：:CAM2038, FluidCrystal injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physio...

journal_title：Journal of pharmaceutical sciences

authors： Liu T,Gobburu JVS

更新日期：2018-03-01 00:00:00

abstract：:Ambrisentan is a nonsulfonamide, ET(A)-selective endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), and tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor under investigation for treatment of PAH. Due to the potential combination use, the pharmacokinetic (P...

journal_title：Journal of pharmaceutical sciences

authors： Spence R,Mandagere A,Harrison B,Dufton C,Boinpally R

更新日期：2009-12-01 00:00:00

abstract：:Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs...

journal_title：Journal of pharmaceutical sciences

authors： Rao VM,Haslam JL,Stella VJ

更新日期：2001-07-01 00:00:00

abstract：:Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...

journal_title：Journal of pharmaceutical sciences

authors： Risaliti L,Ambrosi M,Calamante M,Bergonzi MC,Lo Nostro P,Bilia AR

更新日期：2020-10-01 00:00:00

abstract：:An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...

journal_title：Journal of pharmaceutical sciences

authors： Metzler CM

更新日期：1987-07-01 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

authors： Strauch S,Jantratid E,Stahl M,Rägo L,Dressman JB

更新日期：2011-03-01 00:00:00

abstract：:Phospholipids have been extensively evaluated as an anchor for both PEGylation and receptor-targeting in liposomal formulations. However, cholesterol, another important component in biomembranes, has not been fully investigated as an alternative anchor. In this study, the potential role of cholesterol for anchoring PE...

journal_title：Journal of pharmaceutical sciences

authors： Zhao XB,Muthusamy N,Byrd JC,Lee RJ

更新日期：2007-09-01 00:00:00

abstract：:Maintaining good content uniformity (CU) is a significant challenge for low-dose oral tablets in particular when using direct compression (DC). Using 6 model active pharmaceutical ingredients, we show that a platform DC tablet formulation suitable for developing low-dose API with excellent CU can be developed. This pl...

journal_title：Journal of pharmaceutical sciences

authors： Sun WJ,Aburub A,Sun CC

更新日期：2017-07-01 00:00:00

abstract：:The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...

journal_title：Journal of pharmaceutical sciences

authors： Nagy ZK,Balogh A,Drávavölgyi G,Ferguson J,Pataki H,Vajna B,Marosi G

更新日期：2013-02-01 00:00:00

abstract：:Health interventions developed for wealthy nations are difficult to introduce in developing countries due to a lack of sufficient technological, financial, political, or infrastructural resources. Increasingly, however, product developers are creating new technologies that meet the needs of low-resource settings. Expe...

journal_title：Journal of pharmaceutical sciences

authors： Harner-Jay C,Sherris J

更新日期：2008-12-01 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

authors： Kadir R,Stempler D,Liron Z,Cohen S

更新日期：1987-10-01 00:00:00

abstract：:The release of potassium chloride from hydroxypropyl methylcellulose matrices was investigated for tablets prepared with several different compression forces. It was determined that the release kinetics for these systems deviates significantly from the classical t1/2 dependence. This behavior was attributed to air ent...

journal_title：Journal of pharmaceutical sciences

authors： Korsmeyer RW,Gurny R,Doelker E,Buri P,Peppas NA

更新日期：1983-10-01 00:00:00

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

authors： Boryczka S,Jastrzebska M,Bębenek E,Kusz J,Zubko M,Kadela M,Michalik E

更新日期：2012-12-01 00:00:00

abstract：:Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...

journal_title：Journal of pharmaceutical sciences

authors： Wu B,Sun YN

更新日期：2014-01-01 00:00:00

abstract：:There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...

journal_title：Journal of pharmaceutical sciences

authors： Ochsner AB,Sokoloski TD

更新日期：1985-06-01 00:00:00