Carrier-Mediated Transport of Nicotine Across the Inner Blood-Retinal Barrier: Involvement of a Novel Organic Cation Transporter Driven by an Outward H(+) Gradient.

abstract：:Each of three harmala alkaloids, harmine, harmaline, and harmalol, decreased heart rate and increased pulse pressure, peak aortic flow, and myocardial contractile force in intact normotensive anesthetized dogs. Harmine reduced systemic arterial blood pressure and total peripheral vascular resistance; harmaline-evoked ...

journal_title：Journal of pharmaceutical sciences

authors： Aarons DH,Rossi GV,Orzechowski RF

更新日期：1977-09-01 00:00:00

abstract：:We investigated the effect of cytochrome P450 (CYP) 2C9 polymorphism on the inhibition of methylhydroxylation activity of tolbutamide, a typical CYP2C9 substrate, by triazole antifungal agents, fluconazole and voriconazole. Although the Michaelis constants (Km), maximal velocities (Vmax), and Vmax/Km values for CYP2C9...

journal_title：Journal of pharmaceutical sciences

authors： Niwa T,Hata T

更新日期：2016-03-01 00:00:00

abstract：:During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...

journal_title：Journal of pharmaceutical sciences

authors： Deiringer N,Haase C,Wieland K,Zahler S,Haisch C,Friess W

更新日期：2020-12-09 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...

journal_title：Journal of pharmaceutical sciences

authors： Wong BK,Bruhin PJ,Lin JH

更新日期：1999-02-01 00:00:00

abstract：:This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

journal_title：Journal of pharmaceutical sciences

authors： Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

更新日期：2011-06-01 00:00:00

abstract：:Regional permeability coefficients of 19 drugs with different physicochemical properties were determined using excised segments from three regions of rat intestine: jejunum, ileum, and colon. The results are discussed in relation to the characteristics of the drug, i.e., MW (range 113-1071 Da), pKa, log D (octanol/wat...

journal_title：Journal of pharmaceutical sciences

authors： Ungell AL,Nylander S,Bergstrand S,Sjöberg A,Lennernäs H

更新日期：1998-03-01 00:00:00

abstract：:Stent implantation following angioplasty is the standard treatment of coronary artery disease necessitating interventional procedures. The use of stents as a platform for local drug delivery is a popular strategy to achieve local pharmacological treatment to the diseased artery. Drug eluting stents (DES) are now large...

journal_title：Journal of pharmaceutical sciences

authors： Sharkawi T,Cornhill F,Lafont A,Sabaria P,Vert M

更新日期：2007-11-01 00:00:00

abstract：:Liposomes containing sodium ioxitalamate were prepared by sonication. Suitable amounts of purified soybean phosphatidylcholine and cholesterol were used at various molar ratios. Stearylamine or dicetylphosphate were added to this lipid composition when charged liposomes were required. After sonication and removal of u...

journal_title：Journal of pharmaceutical sciences

authors： Benita S,Poly PA,Puisieux F,Delattre J

更新日期：1984-12-01 00:00:00

abstract：:Montelukast, a cysteinyl leukotriene type 1 receptor antagonist, exhibits secondary anti-inflammatory properties when used at higher concentrations. Low-molecular-weight heparin (LMWH) evokes pronounced anti-inflammatory effects by interrupting leukocyte adhesion and migration. We hypothesized that inhalable particles...

journal_title：Journal of pharmaceutical sciences

authors： Patel B,Rashid J,Gupta N,Ahsan F

更新日期：2017-04-01 00:00:00

abstract：:Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

journal_title：Journal of pharmaceutical sciences

authors： Betker JL,Anchordoquy TJ

更新日期：2017-03-01 00:00:00

abstract：:High-throughput lyophilization process was designed and developed for protein formulations using a single-step drying approach at a shelf temperature (Ts) of ≥40°C. Model proteins were evaluated at different protein concentrations in amorphous-only and amorphous-crystalline formulations. Single-step drying resulted in...

journal_title：Journal of pharmaceutical sciences

authors： Pansare SK,Patel SM

更新日期：2019-04-01 00:00:00

abstract：:Anhydrotetracycline (AHTC), one of the major toxic decomposition products of the antibiotic tetracycline, contains several potential binding sites to metal ions. The acidity constants of the ligand were calculated in aqueous medium (I = 0.1 M) at 25 and 37 degrees C. We found pKa1 = 3.23 +/- 0.08, pKa2 = 5.94 +/- 0.09...

journal_title：Journal of pharmaceutical sciences

authors： de Siqueira JM,Carvalho S,Paniago EB,Tosi L,Beraldo H

更新日期：1994-03-01 00:00:00

abstract：:The delamination of glass contact surfaces because of hydrolytic instability has been well documented. However, the lack of glass surface integrity can also lead to other undesirable outcomes prior to visible glass delamination. This work shows how the early stages of delamination, namely, glass corrosion, can influen...

journal_title：Journal of pharmaceutical sciences

authors： Watkins MA,Iacocca RG,Shelbourn TL,Dong X,Stobba-Wiley C

更新日期：2014-08-01 00:00:00

abstract：:Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...

journal_title：Journal of pharmaceutical sciences

authors： Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

更新日期：1979-10-01 00:00:00

abstract：:In pharmacokinetic evaluation of mice, using serial sampling methods rather than a terminal blood sampling method could reduce the number of animals needed and lead to more reliable data by excluding individual differences. In addition, using serial sampling methods can be valuable for evaluation of the drug-drug inte...

journal_title：Journal of pharmaceutical sciences

authors： Watanabe A,Watari R,Ogawa K,Shimizu R,Tanaka Y,Takai N,Nezasa K,Yamaguchi Y

更新日期：2015-03-01 00:00:00

abstract：:The solubility equation of Yalkowsky was used to estimate the aqueous solubility of 33 barbiturates in the temperature range of 5 to 45 degrees C. The equation was extended by adding a term which accounts for the effect of pH on the solubility of the drug. The extended equation is successful in estimating the aqueous ...

journal_title：Journal of pharmaceutical sciences

authors： Pinal R,Yalkowsky SH

更新日期：1987-01-01 00:00:00

abstract：:A series of substituted 3-(benzylideneamino) coumarins was synthesized and evaluated for anti-inflammatory activity against carrageenan-induced edema in rats. Halogenated derivatives 4g and 4c, at oral doses of 100 mg/kg, showed 75 and 60% antiedmatous activity, respectively (phenylbutazone antiedematous activity, 58%...

journal_title：Journal of pharmaceutical sciences

authors： Maddi V,Raghu KS,Rao MN

更新日期：1992-09-01 00:00:00

abstract：:Anthrax remains a serious threat worldwide as a bioterror agent. A second-generation anthrax vaccine currently under clinical evaluation consists of a recombinant Protective Antigen (rPA) of Bacillus anthracis. We have previously demonstrated that complete protection against inhalational anthrax can be achieved in a r...

journal_title：Journal of pharmaceutical sciences

authors： Jiang G,Joshi SB,Peek LJ,Brandau DT,Huang J,Ferriter MS,Woodley WD,Ford BM,Mar KD,Mikszta JA,Hwang CR,Ulrich R,Harvey NG,Middaugh CR,Sullivan VJ

更新日期：2006-01-01 00:00:00

abstract：:The cyclopropyl amine moiety in GSK2879552 (1) degrades hydrolytically in high pH conditions. This degradation pathway was observed during long-term stability studies and impacted the shelf life of the drug product. This article describes the work to identify the degradation impurities, elucidate the degradation mecha...

journal_title：Journal of pharmaceutical sciences

authors： Campbell JM,Lee M,Clawson J,Kennedy-Gabb S,Bethune S,Janiga A,Kindon L,Leach KP

更新日期：2019-09-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

journal_title：Journal of pharmaceutical sciences

authors： Schieffer GW,Palermo PJ,Pollard-Walker S

更新日期：1984-01-01 00:00:00

abstract：:The interaction between sulfadimethoxine and tolbutamide in sheep involving displacement from protein binding sites was investigated quantitatively. A 52% increase in the unbound plasma concentration of tolbutamide was observed in vitro at 37 degrees after the addition of sulfadimethoxine (100 microgram/ml) to sheep p...

journal_title：Journal of pharmaceutical sciences

authors： Thiessen JJ,Rowland M

更新日期：1977-08-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 00:00:00

abstract：:It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled man...

journal_title：Journal of pharmaceutical sciences

authors： Matsumoto K,Kimura SI,Noguchi S,Itai S,Kondo H,Iwao Y

更新日期：2019-06-01 00:00:00

abstract：:A GLC method is presented for the quantitative determination of menthol, phenol, benzocaine, and pyrilamine maleate. The propellent was exhausted from a pressurized can, and an aliquot of the alcoholic base was weighed. After the addition of the internal standard diluted with chloroform, 1 microliter of the mixture wa...

journal_title：Journal of pharmaceutical sciences

authors： De Fabrizio F

更新日期：1981-10-01 00:00:00

abstract：:The purpose of this study was to develop a nanocarrier system for codelivery of paclitaxel (PTX) and piperlongumine (PL) and investigate the therapeutic potential of improving efficacy and reducing toxicity. PTX and PL were formulated into poly lactic-co-glycolic acid and D-α-tocopheryl polyethylene glycol succinate v...

journal_title：Journal of pharmaceutical sciences

authors： Liu Q,Zhao D,Zhu X,Chen H,Yang Y,Xu J,Zhang Q,Fan A,Li N,Guo C,Kong Y,Lu Y,Chen X

更新日期：2017-10-01 00:00:00

abstract：:The mechanism of drug loading in cross-linked polymers was studied by X-ray photoelectron spectroscopy (XPS). This gave the atomic composition of the surface layers of the loaded polymeric particles so that the exact location of the drug molecules could be identified. Three different lots of popcorn crospovidone and a...

journal_title：Journal of pharmaceutical sciences

authors： Carli F,Garbassi F

更新日期：1985-09-01 00:00:00

abstract：:Accurate partition coefficients K = Corg/Caq in chloroform-ammonia can be obtained by measuring the absorbance of the aqueous layer, replenishing with fresh aqueous solvent, and remeasuring the absorption after reequilibration. Provided the solute has a reasonably strong UV absorption, only 0.1-5 mg of material is req...

journal_title：Journal of pharmaceutical sciences

authors： Rummens FH,Bujaczek RF,Peters M,Green RD

更新日期：1984-02-01 00:00:00

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

authors： Lévy MC,Rambourg P,Lévy J,Potron G

更新日期：1982-07-01 00:00:00