Ocular absorption behavior of palmitoyl tilisolol, an amphiphilic prodrug of tilisolol, for ocular drug delivery.

abstract：:The dissolution kinetics of theophylline monohydrate and anhydrous theophylline were investigated with a rotating-disk apparatus in buffer solutions at 298 K under sink conditions. The observed dissolution rate of theophylline monohydrate under various conditions agreed well with predictions based on the Extended Simu...

journal_title：Journal of pharmaceutical sciences

authors： de Smidt JH,Fokkens JG,Grijseels H,Crommelin DJ

更新日期：1986-05-01 00:00:00

abstract：:Lipid-based dose forms, which encompass a wide variety of compositional and functional characteristics, can be advantageously utilized for the formulation of lipophilic drugs. There has been a traditional reluctance to develop lipid-based dose forms due to potential problems of chemical and physical instability, and a...

journal_title：Journal of pharmaceutical sciences

authors： Charman WN

更新日期：2000-08-01 00:00:00

abstract：:Magnetic resonance imaging (MRI) with chemical shift resolution is a recent extension of MRI and it provides information about species resolved molecular transport on the macroscopic scale in complex systems. In this contribution, we show that by using this novel method, one can predict the behavior of drug and food m...

journal_title：Journal of pharmaceutical sciences

authors： Lafitte G,Thuresson K,Söderman O

更新日期：2007-02-01 00:00:00

abstract：:To characterize and evaluate human serum albumin-encapsulated nanoparticles for drug delivery of a tyrosine kinase inhibitor combined with induction of photothermal ablation combination therapy of renal cell carcinoma (RCC), nanoparticles of varying preparations and concentrations were characterized via zeta potential...

journal_title：Journal of pharmaceutical sciences

authors： Callaghan C,Peralta D,Liu J,Mandava SH,Maddox M,Dash S,Tarr MA,Lee BR

更新日期：2016-01-01 00:00:00

abstract：:Pyrimethamine, an antimalarial drug, was found to be able to inhibit both enzymes (DHFR-TS and PTR1) of the leishmanial folate pathway, although this effect in vivo appears only in relatively high concentrations. To reach the parasites inside macrophage cells, where they are sheltered, targeted drugs of pyrimethamine,...

journal_title：Journal of pharmaceutical sciences

authors： De Carvalho PB,Ramos DC,Cotrim PC,Ferreira EI

更新日期：2003-10-01 00:00:00

abstract：:The kinetics of irreversible aggregation of bovine Granulocyte-Colony Stimulating Factor (bG-CSF) in solution were investigated as a function of temperature (T), concentration, and pH, and analyzed in terms of an Extended Lumry-Eyring model of protein aggregation proceeding via a non-native conformational state. In th...

journal_title：Journal of pharmaceutical sciences

authors： Roberts CJ,Darrington RT,Whitley MB

更新日期：2003-05-01 00:00:00

abstract：:Protein higher order structure (HOS) is an essential quality attribute to ensure protein stability and proper biological function. Protein HOS characterization is performed during comparability assessments for product consistency as well as during forced degradation studies for structural alteration upon stress. Circu...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Meengs B,Meyer J,Bongers J,Ludwig R,Tao L,Das TK,Leone A,Kar SR

更新日期：2018-10-01 00:00:00

abstract：:The quantitative determinations of phenol in phenolated calamine lotion USP and of phenol and resorcinol in phenol-resorcinol-boric acid solution by high-pressure liquid chromatography are reported. The procedures are simple, rapid (no special preliminary treatment is required), and accurate. There is no interference ...

journal_title：Journal of pharmaceutical sciences

authors： Das Gupta V

更新日期：1976-11-01 00:00:00

abstract：:A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic c...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Bellini AM,Mencini E,Minutello A,Fini A,Guarneri M

更新日期：1992-03-01 00:00:00

abstract：:The adsorption of quinidine onto kaolin was studied as a function of pH in aqueous solutions in which the ionic strength was adjusted to 0.1. The interaction of quinidine with pectin also was investigated in water and in phosphate buffer; the buffer pH and ionic strength were adjusted to 6.5 and 0.1, respectively. The...

journal_title：Journal of pharmaceutical sciences

authors： Bucci AJ,Myre SA,Tan HS,Shenouda LS

更新日期：1981-09-01 00:00:00

abstract：:Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanopartic...

journal_title：Journal of pharmaceutical sciences

authors： Tsai MJ,Huang YB,Wu PC,Fu YS,Kao YR,Fang JY,Tsai YH

更新日期：2011-02-01 00:00:00

abstract：:The survival of Staphylococcus aureus was studied in 30 oral administration liquid medicaments (15 syrups and 15 solutions) to determine the effectiveness of the preservatives, the influence of the culture medium used in the enumeration of the surviving microorganisms, and the loss of the enzyme coagulase, phosphatase...

journal_title：Journal of pharmaceutical sciences

authors： Vivar C,de la Rosa C,Mosso A

更新日期：1993-02-01 00:00:00

abstract：:Pelrinone HCl is essentially nonhygroscopic. The pH-solubility profile exhibits a U-shaped curve, while the octanol-water partition coefficient-pH profile shows a bell-shaped curve. Two ionizable functions, with a pKa1 value of 4.71 and a pKa2 value of 8.94, produce the cationic and anionic forms, respectively. A weak...

journal_title：Journal of pharmaceutical sciences

authors： Hajdu J,Adams G,Lee HK

更新日期：1988-11-01 00:00:00

abstract：:The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

journal_title：Journal of pharmaceutical sciences

authors： Soliman FS,Shafik RM,Darwish M

更新日期：1982-02-01 00:00:00

abstract：:Low-density lipoproteins (LDLs), the physiological vehicles for lipids, are potentially useful drug delivery devices for (hydrophobic) drugs. The physicochemical characteristics of LDL loaded with the adriamycin derivative AD 32 or the N-mustard derivative WB 4291 were compared to that of native and reconstituted LDL ...

journal_title：Journal of pharmaceutical sciences

authors： Westesen K,Gerke A,Koch MH

更新日期：1995-02-01 00:00:00

abstract：:The insidious nature of Zika virus (ZIKV) infections can have a devastating consequence for fetal development. Recent reports have highlighted that chloroquine (CQ) is capable of inhibiting ZIKV endocytosis in brain cells. We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an...

journal_title：Journal of pharmaceutical sciences

authors： Olafuyi O,Badhan RKS

更新日期：2019-01-01 00:00:00

abstract：:SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 receptor. Ivermectin has shown antiviral activity by inhibiting the formation of the importin-α (IMPα) and IMPβ1 subunits as well as dissociating the IMPα/β1 heterodimer and has in vitro efficacy agains...

journal_title：Journal of pharmaceutical sciences

authors： Jermain B,Hanafin PO,Cao Y,Lifschitz A,Lanusse C,Rao GG

更新日期：2020-12-01 00:00:00

abstract：:The concept of cosolvent exclusion was developed by a group of Timasheff's laboratory in 1970-1990 and is currently used widely to explain the effects of a variety of cosolvents on the stability and solubility of macromolecules. Not surprisingly, these concepts have had substantial influence in the fields of formulati...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Gagnon P

更新日期：2018-09-01 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：:Ensuring the health of street-involved children is a growing public health challenge. These children are vulnerable, neglected, and rarely a priority for basic service providers and governments. Sizable populations of street-involved children are present in major urban areas worldwide and current trends in urbanizatio...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Twum JA,Wasan KM

更新日期：2012-10-01 00:00:00

abstract：:3D cultures of primary human hepatocytes (PHH) are emerging as a more in vivo-like culture system than previously available hepatic models. This work describes the characterisation of drug metabolism in 3D PHH spheroids. Spheroids were formed from three different donors of PHH and the expression and activities of impo...

journal_title：Journal of pharmaceutical sciences

authors： Kanebratt KP,Janefeldt A,Vilén L,Vildhede A,Samuelsson K,Milton L,Björkbom A,Persson M,Leandersson C,Andersson TB,Hilgendorf C

更新日期：2021-01-01 00:00:00

abstract：:Uncharged, lipophilic, low molecular weight copper complexes labeled with generator-produced copper-62 are of interest as potential radiopharmaceutials for imaging the brain with positron emission tomography (PET). We report here the synthesis and biodistribution of a series of [67Cu]copper(II) complexes with tetraden...

journal_title：Journal of pharmaceutical sciences

authors： John EK,Bott AJ,Green MA

更新日期：1994-04-01 00:00:00

abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...

journal_title：Journal of pharmaceutical sciences

authors： Heiman AS,Taraporewala IB,McLean HM,Hong D,Lee HJ

更新日期：1990-07-01 00:00:00

abstract：:A high-performance liquid chromatographic method for the determination of (Z)- and (E)-doxepin hydrochloride isomers was developed. The analysis employs a column packed with spherical silica microparticles (5-6 mum), and a mobile phase of acetonitrile-chloroform-diethylamine (750:250:0.2) permits baseline resolution a...

journal_title：Journal of pharmaceutical sciences

authors： Whall TJ,Dokladalova J

更新日期：1979-11-01 00:00:00

abstract：:Bile acid (BA) retention within hepatocytes is an underlying mechanism of cholestatic drug-induced liver injury (DILI). We previously developed an assay using sandwich-cultured human hepatocytes (SCHHs) to evaluate drug-induced hepatocyte toxicity accompanying intracellular BA accumulation. However, due to shortcoming...

journal_title：Journal of pharmaceutical sciences

authors： Susukida T,Sekine S,Nozaki M,Tokizono M,Oizumi K,Horie T,Ito K

更新日期：2016-04-01 00:00:00

abstract：:The kinetics of decomposition of the following conformationally restricted N-chloro-alpha-amino acids were studied: 1-amino-1-cyclopentanecarboxylic acid (2), 1-amino-1-cyclohexanecarboxylic acid (4), 2-amino-2-norbornanecarboxylic acid (6), and 2-amino-2-benzonorbornanecarboxylic acid (8). The first-order rate consta...

journal_title：Journal of pharmaceutical sciences

authors： Awad R,Hussain A,Crooks PA

更新日期：1990-12-01 00:00:00

abstract：:The tissue penetration and distribution of antibiotics is of great importance, since most of the infections occur in the tissue. At the infection site, the free, unbound fraction of the antibiotic is responsible for the antiinfective effect. These free extracellular concentrations can be measured by microdialysis. It ...

journal_title：Journal of pharmaceutical sciences

authors： Nolting A,Costa TD,Vistelle R,Rand KH,Derendorf H

更新日期：1996-04-01 00:00:00

abstract：:Experimental solubilities are reported for anthracene in binary solvent mixtures containing p-dioxane with n-hexane, cyclohexane, n-heptane, methylcyclohexane, n-octane, cyclooctane, and isooctane at 25 degrees C. Results of these measurements, used in conjunction with the nearly ideal binary solvent (NIBS) model, ena...

journal_title：Journal of pharmaceutical sciences

authors： Procyk AD,Bissell M,Street KW Jr,Acree WE Jr

更新日期：1987-08-01 00:00:00

abstract：:There has been a growing interest in predicting in vivo metabolic drug-drug interactions from in vitro systems. High-throughput screening methods aimed at assessing the potential of drug candidates for drug interactions are widely used in industry. However, at present, there is no consensus on methodologies that would...

journal_title：Journal of pharmaceutical sciences

authors： Yao C,Levy RH

更新日期：2002-09-01 00:00:00

abstract：:Poly(D,L-lactide-co-glycolide, 50:50) samples of similar molecular weight were obtained from three commercial sources and were characterized by gel permeation chromatography, differential scanning calorimetry, X-ray powder diffraction, viscometry, and proton nuclear magnetic resonance spectroscopy. Pellets were prepar...

journal_title：Journal of pharmaceutical sciences

authors： Schmitt EA,Flanagan DR,Linhardt RJ

更新日期：1993-03-01 00:00:00