Controlled delivery of basal insulin from phase-sensitive polymeric systems after subcutaneous administration: in vitro release, stability, biocompatibility, in vivo absorption, and bioactivity of insulin.

abstract：:Present study aims to improve efficiency and capacity of in vivo rat pharmacokinetic studies for rapid assessment of systemic exposure (AUC and C(max)) of new chemical entities. Plasma concentration-time profiles in rats from structurally diverse compounds were extracted from the Pfizer database. AUC(0-8) was calculat...

journal_title：Journal of pharmaceutical sciences

authors： Han HK,Sadagopan N,Reichard GA,Yapa U,Zhu T,Hubbel A,Johnson K,Brodfuehrer J

更新日期：2006-08-01 00:00:00

abstract：:Nipecotic acid (1), one of the most potent in vitro inhibitors of neuronal and glial gamma-amino butyric acid (GABA) uptake, is inactive as an anticonvulsant when administered systemically. To obtain in vivo active prodrugs of (1), we synthesized four new nipecotic acid esters (3-6), which were obtained by chemical co...

journal_title：Journal of pharmaceutical sciences

authors： Bonina FP,Arenare L,Palagiano F,Saija A,Nava F,Trombetta D,de Caprariis P

更新日期：1999-05-01 00:00:00

abstract：:In this paper we describe the synthesis and characterization of magnetic microcapsules, intended for use in vivo, and which contain polyethyleneimine nucleophilic targets capable of trapping electrophilic carcinogens. The microcapsules, 15-50 microns in diameter, consist of a semipermeable cross-linked nylon membrane ...

journal_title：Journal of pharmaceutical sciences

authors： Povey AC,Bartsch H,Nixon JR,O'Neill IK

更新日期：1986-09-01 00:00:00

abstract：:The plasma protein binding of zomepirac, a new nonnarcotic analgesic, was studied using equilibrium dialysis. Experiments were performed using human plasma and plasma from mice, rats, and rhesus monkeys, all species of pharmacological or toxicological interest. At concentrations approximating those achieved in vivo, t...

journal_title：Journal of pharmaceutical sciences

authors： O'Neill PJ

更新日期：1981-07-01 00:00:00

abstract：:The solubility of butamben has been measured gravimetrically in pure methanol, 1-propanol, 2-propanol, 1-butanol, and toluene over the temperature range 268-298 K. Polymorph transition and melting temperatures, associated enthalpy changes, and the heat capacity of the solid forms and the supercooled melt have been mea...

journal_title：Journal of pharmaceutical sciences

authors： Svärd M,Zeng L,Valavi M,Krishna GR,Rasmuson ÅC

更新日期：2019-07-01 00:00:00

abstract：:Angiogenesis--process of new blood-vessel growth from existing vasculature--is an integral part of both normal developmental processes and numerous pathologies such as cancer, ischemic diseases and chronic inflammation. Angiogenesis plays a crucial role facilitating tumour growth and the metastatic process, and it is ...

journal_title：Journal of pharmaceutical sciences

authors： Mauriz JL,González-Gallego J

更新日期：2008-10-01 00:00:00

abstract：:Characterizing and quantifying subvisible particles in protein drug products is critical to ensuring product quality. A variety of analytical methods are used to detect and make meaningful measurements of subvisible particles. Resonant mass measurement (RMM) is a novel technology that characterizes the subvisible part...

journal_title：Journal of pharmaceutical sciences

authors： Krueger AB,Hadley J,Cheney PP,Markova N,Carpenter JF,Fradkin AH

更新日期：2019-05-01 00:00:00

abstract：:The thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, beca...

journal_title：Journal of pharmaceutical sciences

authors： Juhász V,Beéry E,Nagy Z,Bui A,Molnár E,Zolnerciks JK,Magnan R,Jani M,Krajcsi P

更新日期：2013-05-01 00:00:00

abstract：:A physiologic pharmacokinetic model describing percutaneous absorption of topically applied compounds in the isolated perfused porcine skin flap (IPPSF) is presented. As an extension of a previously reported hybrid physiologically relevant compartmental model of uptake of intra-arterially administered drug in the IPPS...

journal_title：Journal of pharmaceutical sciences

authors： Williams PL,Carver MP,Riviere JE

更新日期：1990-04-01 00:00:00

abstract：:The area under the plasma concentration-time curve (AUC) was measured after an intravenous injection of sodium salicylate and after intragastric administration of aspirin, using either an intermittent sampling and the trapezoid rule (AUC-trapezoid) or the recently introduced constant blood withdrawal method (AUC-integ...

journal_title：Journal of pharmaceutical sciences

authors： Kowarski CR,Kowarski AA

更新日期：1978-06-01 00:00:00

abstract：:The Setschenow constant, K(salt), of a nonelectrolyte in a NaCl solution is shown to be related to the logarithm of its octanol-water partition coefficient, log K(ow), determined by K(salt) = A log K(ow) + B, where K(ow) is the octanol-water partition coefficient of the solute and the coefficients A and B are constant...

journal_title：Journal of pharmaceutical sciences

authors： Ni N,El-Sayed MM,Sanghvi T,Yalkowsky SH

更新日期：2000-12-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 00:00:00

abstract：:The present work employs recent advances in high-resolution real-time magnetic resonance imaging (MRI) to investigate the disintegration process of tablets containing disintegrants. A temporal resolution of 75 ms and a spatial resolution of 80 × 80 µm with a section thickness of only 600 µm were achieved. The histogra...

journal_title：Journal of pharmaceutical sciences

authors： Quodbach J,Moussavi A,Tammer R,Frahm J,Kleinebudde P

更新日期：2014-01-01 00:00:00

abstract：:Phosphate is specifically adsorbed by aluminum hydroxycarbonate by anion ligand exchange. IR analysis indicated that phosphate exchanged with specifically adsorbed carbonate. Adsorption is favored by low pH and is inversely related to particle size. Adsorption of phosphate decreases the rate of acid neutralization of ...

journal_title：Journal of pharmaceutical sciences

authors： Liu JC,Feldkamp JR,White JL,Hem SL

更新日期：1984-10-01 00:00:00

abstract：:The new concept developed in this study is the design of poly(ethylene glycol) (PEG)-coated biodegradable nanoparticles coupled to folic acid to target the folate-binding protein; this molecule is the soluble form of the folate receptor that is overexpressed on the surface of many tumoral cells. For this purpose, a no...

journal_title：Journal of pharmaceutical sciences

authors： Stella B,Arpicco S,Peracchia MT,Desmaële D,Hoebeke J,Renoir M,D'Angelo J,Cattel L,Couvreur P

更新日期：2000-11-01 00:00:00

abstract：:The dissolution behavior and absorption of mefenamic acid following oral and rectal administration from drug:egg albumin solid dispersions have been studied in comparison with those of the drug alone. The interaction of drug with egg albumin in aqueous solution and solid state were examined by solubility analysis, dia...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Nohdomi K,Acartürk F,Otagiri M

更新日期：1991-05-01 00:00:00

abstract：:A high-performance liquid chromatographic (HPLC) method for the simultaneous determination of pralidoxime chloride (I) and its major decomposition products in an injectable formulation is described. I and its decomposition products were detected and quantitated by their UV absorbances at 270 nm, after being separated ...

journal_title：Journal of pharmaceutical sciences

authors： Prue DG,Johnson RN,Kho BT

更新日期：1983-07-01 00:00:00

abstract：:Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...

journal_title：Journal of pharmaceutical sciences

authors： Yamashita F,Wanchana S,Hashida M

更新日期：2002-10-01 00:00:00

abstract：:Polyspecific organic cation transporters in the basolateral and brush border membrane of the kidney play a role in the elimination of many clinically important drugs and endogenous compounds. In this study we report the functional expression of organic cation transport activity in Xenopus laevis oocytes injected with ...

journal_title：Journal of pharmaceutical sciences

authors： Chun JK,Piquette-Miller M,Zhang L,Giacomini KM

更新日期：1997-06-01 00:00:00

abstract：:Chitosan microspheres were evaluated for sustained-release of recombinant human interleukin-2 (rIL-2) in this study. In addition, the effects of different formulation factors, such as chitosan and protein concentrations, the volume of sodium sulfate solution, addition technique of rIL-2, and presence of glutaraldehyde...

journal_title：Journal of pharmaceutical sciences

authors： Ozbaş-Turan S,Akbuğa J,Aral C

更新日期：2002-05-01 00:00:00

abstract：:As part of a series of articles in this special issue evaluating model IgG1-Fc glycoforms for biosimilarity analysis, 3 well-defined IgG1-Fc glycoforms (high mannose-Fc, Man5-Fc, and N-acetylglucosamine-Fc) and a nonglycosylated Fc protein (N297Q-Fc) were examined in this work to elucidate chemical degradation pathway...

journal_title：Journal of pharmaceutical sciences

authors： Mozziconacci O,Okbazghi S,More AS,Volkin DB,Tolbert T,Schöneich C

更新日期：2016-02-01 00:00:00

abstract：:The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

更新日期：1982-11-01 00:00:00

abstract：:It is shown that tricalcium phosphate follows a simple Heckel relationship in pressures of usual tablet compression, only if a density of 1.92 g/mL is used. This coincides with the density obtained by wet pycnometry, whereas the crystallographical density is 3.1 g/mL. The interpretation is that some of the pore space ...

journal_title：Journal of pharmaceutical sciences

authors： Hou XP,Carstensen JT

更新日期：1985-04-01 00:00:00

abstract：:The goal of this research was to evaluate the effectiveness of cationic liposomes for intranasal administration of proteins to the brain. Cationic liposomes were loaded with a model protein, ovalbumin (OVAL), and a 50 microg dose was administered intranasally to rats. In qualitative studies, liposomes were loaded with...

journal_title：Journal of pharmaceutical sciences

authors： Migliore MM,Vyas TK,Campbell RB,Amiji MM,Waszczak BL

更新日期：2010-04-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs in the world, primarily for symptoms associated with osteoarthritis and other chronic musculoskeletal conditions. However, adverse effects caused by oral administration, such as local or systemic disturbance in the gastrointestinal ...

journal_title：Journal of pharmaceutical sciences

authors： Cheng Y,Man N,Xu T,Fu R,Wang X,Wang X,Wen L

更新日期：2007-03-01 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

authors： Schuhmacher J,Kohlsdorfer C,Bühner K,Brandenburger T,Kruk R

更新日期：2004-04-01 00:00:00

abstract：:The axial and radial tensile strengths were compared to the hardness of compressed tablets containing various concentrations of lubricants. Since radial tensile strength measurement considers the thickness of a tablet, and only tensile stress and axial tensile strength express the strength in the direction in which ca...

journal_title：Journal of pharmaceutical sciences

authors： Jarosz PJ,Parrott EL

更新日期：1982-06-01 00:00:00

abstract：:The presence of subvisible particles in formulations of therapeutic proteins is a risk factor for adverse immune responses. Although the immunogenic potential of particulate contaminants likely depends on particle structural characteristics (e.g., composition, size, and shape), exact structure-immunogenicity relations...

journal_title：Journal of pharmaceutical sciences

authors： Daniels AL,Randolph TW

更新日期：2018-05-01 00:00:00

abstract：:Synthetic peptides corresponding to the variable tandem repeat domain of the cancer-associated antigen MUC1 mucin are candidates for cancer vaccines. In our investigation mice were immunized via subcutaneous injection with poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres containing a MUC1 mucin peptide. It was hy...

journal_title：Journal of pharmaceutical sciences

authors： Newman KD,Sosnowski DL,Kwon GS,Samuel J

更新日期：1998-11-01 00:00:00

abstract：:(-)-1-Cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo [a,d]cyclohepten-5-ylidene)piperidine (MK-160) was extracted from human plasma and urine with petroleum ether and quantitated by GLC using a nitrogen-sensitive detector. A homologue of the drug served as the internal standard. The method is specific for the d...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Hutt JE

更新日期：1983-07-01 00:00:00