Phosphodiesterase inhibition by succinic and related acid biphenylalkyl monoesters.

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 development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...

journal_title：Journal of pharmaceutical sciences

authors： Aboul-Enein N,Sam J

更新日期：1976-09-01 00:00:00

abstract：:A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug-delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at sufficiently high local concentrations for desirable therapeutic effects. HAP cements loaded with antibiotics can be formed in situ and c...

journal_title：Journal of pharmaceutical sciences

authors： Yu D,Wong J,Matsuda Y,Fox JL,Higuchi WI,Otsuka M

更新日期：1992-06-01 00:00:00

abstract：:Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibio...

journal_title：Journal of pharmaceutical sciences

authors： Ceschan NE,Rosas MD,Olivera ME,Dugour AV,Figueroa JM,Bucalá V,Ramírez-Rigo MV

更新日期：2020-09-01 00:00:00

abstract：:A general method for predicting the intestinal absorption of a wide range of drugs using multiple regression analysis of their physicochemical properties and the drug-membrane electrostatic interaction was developed. The absorption rates of tested drugs from rat jejunum were measured by the in situ single-pass perfusi...

journal_title：Journal of pharmaceutical sciences

authors： Sugawara M,Takekuma Y,Yamada H,Kobayashi M,Iseki K,Miyazaki K

更新日期：1998-08-01 00:00:00

abstract：:Eprosartan mesylate (SKF 108566-J; EM) is an antihypertensive agent approved for marketing in the USA. EM dihydrate was prepared by three methods, one of which included suspending the anhydrous drug in an aqueous solution of 1.0 M methanesulfonic acid to form a slurry, followed by filtration. The dehydration kinetics ...

journal_title：Journal of pharmaceutical sciences

authors： Sheng J,Venkatesh GM,Duddu SP,Grant DJ

更新日期：1999-10-01 00:00:00

abstract：:The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ce...

journal_title：Journal of pharmaceutical sciences

authors： Hashimoto N,Hirano K

更新日期：1998-09-01 00:00:00

abstract：:Oil-frozen water-in-oil-in-water (W₁/O/W₂) double emulsions (DE) containing ethanol up to 40% (w/v) in the external aqueous W₂ phase exhibited external coalescence upon thawing of the oil phase, releasing up to 85% of the encapsulated protein of the internal aqueous phase. These emulsions were studied in vitro as pote...

journal_title：Journal of pharmaceutical sciences

authors： Jaimes-Lizcano YA,Lawson LB,Papadopoulos KD

更新日期：2011-04-01 00:00:00

abstract：:The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...

journal_title：Journal of pharmaceutical sciences

authors： Tromelin A,Gnanou JC,Andrès C,Pourcelot Y,Chaillot B

更新日期：1996-09-01 00:00:00

abstract：:Three polymorphs (forms I-III), a monohydrate (form S2), and three new solvates [4:1 hydrate (form S1), monohydrate (form S3), and methanol half-solvate (form S4)] were isolated and characterized by X-ray powder diffractometry (XRPD), IR spectroscopy, differential scanning calorimetry (DSC), hot stage microscopy, solu...

journal_title：Journal of pharmaceutical sciences

authors： Chang LC,Caira MR,Guillory JK

更新日期：1995-10-01 00:00:00

abstract：:Meglumine labeled with carbon-14 was administered orally as 14C-meglumine salicylate to rats and dogs to study its distribution and excretion. The compound was incompletely absorbed; that which was absorbed was rapidly excreted in the urine. Peak blood levels were about 5-10 mug/ml in rats and 2-8 mug/ml in dogs. Tiss...

journal_title：Journal of pharmaceutical sciences

authors： Heeg JF,Born GS,Kessler WV,Shaw SM,Lange WE

更新日期：1977-01-01 00:00:00

abstract：:The development of multiple drug modalities over the past 20 years has dramatically expanded the therapeutic space for intervention in disease processes. Rather than being alternative therapeutic approaches, these modalities tend to be complimentary both in the scope of target space and the biological mechanisms harne...

journal_title：Journal of pharmaceutical sciences

authors： Hochman JH

更新日期：2021-01-01 00:00:00

abstract：:Understanding the coating unit operation is imperative to improve product quality and reduce output risks for coated solid dosage forms. Three batches of sustained-release tablets coated with the same process parameters (pan speed, spray rate, etc.) were subjected to terahertz pulsed imaging (TPI) analysis followed by...

journal_title：Journal of pharmaceutical sciences

authors： Ho L,Müller R,Gordon KC,Kleinebudde P,Pepper M,Rades T,Shen Y,Taday PF,Zeitler JA

更新日期：2009-12-01 00:00:00

abstract：:99mTc-N-(3-bromo-2,4,6-trimethylacetanilide)iminodiacetat e (I) and 99mTc-N-pyridoxyl-5-methyl-tryptophan (II) have been described as having optimal properties as hepatobiliary radiopharmaceuticals. This study compared specificity for hepatobiliary excretion, blood disappearance, rates of biliary appearance, and pharm...

journal_title：Journal of pharmaceutical sciences

authors： Fritzberg AR,Bloedow DC,Eshima D,Johnson DL

更新日期：1984-12-01 00:00:00

abstract：:Regular insulin, NPH insulin, glargine insulin, calcitonin, and human growth hormone were administered to rats nasally with 0.125% tetradecyl-beta-D-maltoside (TDM), or at various times after TDM treatment. Absorption of all five peptides was enhanced initially and diminished in a time-dependent manner as the interval...

journal_title：Journal of pharmaceutical sciences

authors： Arnold JJ,Fyrberg MD,Meezan E,Pillion DJ

更新日期：2010-04-01 00:00:00

abstract：:Male and female rats treated with a single 20-mg/kg ip dose of pregnenolone-16alpha-carbonitrile (PCN) produced parallel increases in hepatic cytochrome P-450 and aniline hydroxylase activity. However, the onset of increase in aniline hydroxylase activity and cytochrome P-450 content was slower in male than female ani...

journal_title：Journal of pharmaceutical sciences

authors： Stohs SJ,Rosenberg H

更新日期：1976-04-01 00:00:00

abstract：:Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2003-07-01 00:00:00

abstract：:Carboxy group-terminated synthetic polymers--branched poly(ethylene glycol), poly(acryloylmorpholine), and poly(vinylpyrrolidone)--were made amphiphilic by derivatization with phosphatidyl ethanolamine via the terminal carboxy group and then incorporated into lecithin-cholesterol liposomes prepared by the detergent di...

journal_title：Journal of pharmaceutical sciences

authors： Torchilin VP,Trubetskoy VS,Whiteman KR,Caliceti P,Ferruti P,Veronese FM

更新日期：1995-09-01 00:00:00

abstract：:The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...

journal_title：Journal of pharmaceutical sciences

authors： Hauptstein S,Bonengel S,Griessinger J,Bernkop-Schnürch A

更新日期：2014-02-01 00:00:00

abstract：:This edition of the Journal of Pharmaceutical Sciences is dedicated to the wonderful career of Per Artursson from the Uppsala University. My Commentary focusses on Per's major contributions to the Caco-2 cell literature over the past 30 years. Two especially influential papers have been cited more than 1000 times out ...

journal_title：Journal of pharmaceutical sciences

authors： Brayden DJ

更新日期：2021-01-01 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：: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：:It is shown that the existence of the second peak on the drug plasma concentration time curve C(p)(t) after iv bolus dosing can be explained by considering the traditional multi-compartmental linear pharmacokinetics. It was found that a direct solution of the general three-compartment model yields the second peak of C...

journal_title：Journal of pharmaceutical sciences

authors： Berezhkovskiy LM

更新日期：2008-06-01 00:00:00

abstract：:Treatment of systemic diseases by means of the inhalation route is hampered by uncertainties of the drug dose applied by inhalation. In this study, the hypothesis was tested that by standardization of the breathing maneuver used for inhalation, the interindividual variability of the dose deposited intrathoracically ca...

journal_title：Journal of pharmaceutical sciences

authors： Brand P,Friemel I,Meyer T,Schulz H,Heyder J,Häubetainger K

更新日期：2000-06-01 00:00:00

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 00:00:00

abstract：:Simultaneously Manufactured Nano-In-Micro (SIMANIM) particles for the pulmonary delivery of antibodies have been prepared by the spray-drying of a double-emulsion containing human IgG (as a model antibody), lactose, poly(lactide-co-glycolide) (PLGA) and dipalmitoylphosphatidylcholine (DPPC). The one-step drying proces...

journal_title：Journal of pharmaceutical sciences

authors： Kaye RS,Purewal TS,Alpar HO

更新日期：2009-11-01 00:00:00

abstract：:The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 14 2-(3-alkylaminoalkylamido)-pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, with seven showing comparable or greater activity than lidocaine. Most compounds also exhibite...

journal_title：Journal of pharmaceutical sciences

authors： Sowell JW Sr,Block AJ,Derrick ME,Freeman JJ,Kosh JW,Mubarak PF,Tenthorey PA

更新日期：1981-05-01 00:00:00

abstract：:Previous studies from this laboratory suggested that a solution model (Flory-Huggins equation) modified by a free volume model (Vrentas equation) could satisfactorily describe water absorption into an amorphous solid composed of a sugar or a polymer. This paper has extended the studies of single solutes to binary mixt...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2001-09-01 00:00:00

abstract：:An approach to analyzing and interpreting kinetic data from stability studies using factorial designs is presented. This may be useful for screening purposes or as an aid in identifying significant effects in complex systems. A typical 2n factorial experiment is discussed, and methods of variance estimation and statis...

journal_title：Journal of pharmaceutical sciences

authors： Bolton S

更新日期：1983-04-01 00:00:00

abstract：:In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...

journal_title：Journal of pharmaceutical sciences

authors： Krueger AB,Carnell P,Carpenter JF

更新日期：2016-04-01 00:00:00