Binding of metronidazole and its derivatives to plasma proteins: an assessment of drug binding phenomenon.

abstract：:Electron donor-acceptor complexes for a group of quinolines and naphthalenes with 9-(dicyanomethylene)-2,4,7-trinitrofluorene in 1,2-dichloroethane were studied by optical absorption methods. Association constants, molar absorptivities, and charge-transfer transition energies were evaluated for each system, together w...

journal_title：Journal of pharmaceutical sciences

authors： Webb NE,Thompson CC

更新日期：1978-02-01 00:00:00

abstract：:The present study aimed to develop optimized quercetin (QT)-loaded self-nanoemulsifying drug delivery system (SNEDDS) that offers protective effect against liver damage. Solubility study of QT in different oils, surfactants, and cosurfactants was performed. Ternary phase mixtures of the selected components were constr...

journal_title：Journal of pharmaceutical sciences

authors： Ahmed OA,Badr-Eldin SM,Tawfik MK,Ahmed TA,El-Say KM,Badr JM

更新日期：2014-02-01 00:00:00

abstract：:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone. ...

journal_title：Journal of pharmaceutical sciences

authors： Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

更新日期：1980-08-01 00:00:00

abstract：:We studied the effects of pH and solution additives on freezing-induced perturbations in the tertiary structure of a monoclonal antibody (mAb) by intrinsic tryptophan fluorescence spectroscopy. In general, freezing caused perturbations in the tertiary structure of the mAb, which were reversible or irreversible dependi...

journal_title：Journal of pharmaceutical sciences

authors： Liu L,Braun LJ,Wang W,Randolph TW,Carpenter JF

更新日期：2014-07-01 00:00:00

abstract：:This work involves the study of the solid-phase and solution crystallization behavior of the N-methylephedrine enantiomers. A systematic investigation of the melt phase diagram of the enantiomeric N-methylephedrine system was performed considering polymorphism. Two monotropically related modifications of the enantiome...

journal_title：Journal of pharmaceutical sciences

authors： Tulashie SK,Polenske D,Seidel-Morgenstern A,Lorenz H

更新日期：2016-11-01 00:00:00

abstract：:The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, an...

journal_title：Journal of pharmaceutical sciences

authors： Sasaki Y,Shinohara Y,Baba S

更新日期：1990-02-01 00:00:00

abstract：:4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...

journal_title：Journal of pharmaceutical sciences

authors： Schwan TJ,Honkomp LJ,Snyder HR Jr,Watson EJ

更新日期：1978-03-01 00:00:00

abstract：:Pharmacokinetic profiles of pentylenetetrazol in the dog were studied following rapid intravenous and oral administrations of a convulsant dose (15-20 mg/kg). Plasma level-time curves after a rapid intravenous injection showed biexponential decline, indicating that the disposition of this drug in the dog follows a two...

journal_title：Journal of pharmaceutical sciences

authors： Jun HW

更新日期：1976-07-01 00:00:00

abstract：:Mathematical relationships describing the delivery of drug to a target organ after intra-arterial, intravenous, and oral administration are presented. This discussion clearly demonstrates that administration into a blood vessel leading to the target organ often is superior to intravenous administration. However, this ...

journal_title：Journal of pharmaceutical sciences

authors： Oie S,Huang JD

更新日期：1981-12-01 00:00:00

abstract：:A stereoselective and sensitive method for the determination of nilvadipine, a new dihydropyridine calcium antagonist, in human plasma was developed. An internal standard, the deuterated analogue of racemic nilvadipine, was added to the plasma and extracted with an n-hexane:ethyl acetate (92.5:7.5) mixture under alkal...

journal_title：Journal of pharmaceutical sciences

authors： Tokuma Y,Fujiwara T,Noguchi H

更新日期：1987-04-01 00:00:00

abstract：:6-Amino-2-mercapto-5-methylpyrimidine-4-carboxylic acid proved to be a potent hypolipidemic agent in rodents at the low dose of 20 mg/kg/d. The agent effectively reduced the liver enzyme activities required for the synthesis of triglycerides and cholesterol. Lower lipid levels in tissue were observed in mice but not i...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Cocolas GH,Murthy AR,Rhyne KA,Knowles M

更新日期：1985-07-01 00:00:00

abstract：:The hypothermic response following intraperitoneal doses (6.25, 12.5, and 25 mg/kg) of cobaltous chloride was investigated in Swiss albino mice. The magnitude and duration of rectal temperature depression were dose related. In each case, maximal hypothermia was evident within 30 min after injection. Body temperature d...

journal_title：Journal of pharmaceutical sciences

authors： Burke DH

更新日期：1978-06-01 00:00:00

abstract：:Sodium salicylate improves the rectal absorption of drugs which exhibit molecular self-association; it is suggested that salicylate may improve drug bioavailability by altering the drug self-association pattern. Methylene blue was chosen as a model molecule for investigating the interference of salicylate with drugs u...

journal_title：Journal of pharmaceutical sciences

authors： Touitou E,Fisher P

更新日期：1986-04-01 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 solubility of a drug is ultimately governed by its chemical potential as it is present in the undissolved solute. For a pharmaceutical amorphous solid dispersion (ASD), its solubility depends on the state and composition of the undissolved solute when the ASD is equilibrated with water. Concerning the undissolved ...

journal_title：Journal of pharmaceutical sciences

authors： Huang S,Mao C,Williams RO 3rd,Yang CY

更新日期：2016-12-01 00:00:00

abstract：:Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebr...

journal_title：Journal of pharmaceutical sciences

authors： Villesen HH,Foster DJ,Upton RN,Somogyi AA,Martinez A,Grant C

更新日期：2006-08-01 00:00:00

abstract：:The analysis of corticosteroid prodrugs in pharmacokinetic (PK) studies poses the risk of overestimation of corticosteroid concentrations due to in vitro hydrolysis of prodrugs after sample collection. This study tests the effectiveness of enzyme inhibitors as stabilizers for betamethasone sodium phosphate (BSP) in pr...

journal_title：Journal of pharmaceutical sciences

authors： Samtani MN,Schwab M,Nathanielsz PW,Jusko WJ

更新日期：2004-03-01 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：:The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results s...

journal_title：Journal of pharmaceutical sciences

authors： de la Luz Reus Medina M,Kumar V

更新日期：2007-02-01 00:00:00

abstract：:The recently introduced four-parameter extended Hansen approach was used to study the solubility of p-hydroxybenzoic acid and methyl p-hydroxybenzoate in 32 and 35 individual solvents, respectively. The results are compared with those for benzoic acid in 40 solvents. Seventeen of the thirty-two or 53% of the calculate...

journal_title：Journal of pharmaceutical sciences

authors： Martin A,Wu PL,Beerbower A

更新日期：1984-02-01 00:00:00

abstract：:This whitepaper highlights current challenges and opportunities associated with continuous synthesis, workup, and crystallization of active pharmaceutical ingredients (drug substances). We describe the technologies and requirements at each stage and emphasize the different considerations for developing continuous proc...

journal_title：Journal of pharmaceutical sciences

authors： Baxendale IR,Braatz RD,Hodnett BK,Jensen KF,Johnson MD,Sharratt P,Sherlock JP,Florence AJ

更新日期：2015-03-01 00:00:00

abstract：:Azo compounds are commonly used to study radical-mediated degradation of pharmaceutical compounds. The favorable chemical and physical properties of 2,2'-azobis(2-methylpropanenitrile) (AIBN) have made it one of the most widely used compound for these type of studies. This article describes the characterization of a s...

journal_title：Journal of pharmaceutical sciences

authors： Wells-Knecht KJ,Dunn D

更新日期：2019-09-01 00:00:00

abstract：:The particle sizing performance of a Next Generation Pharmaceutical Impactor (NGI) was compared to that of an Andersen cascade impactor (ACI). A single lot of Vanceril MDIs containing beclomethasone dipropionate (BDP) was used throughout. MDIs were sampled into NGI and ACI in accordance with USP recommendations, at 30...

journal_title：Journal of pharmaceutical sciences

authors： Kamiya A,Sakagami M,Hindle M,Byron PR

更新日期：2004-07-01 00:00:00

abstract：:Solubilization of nonpolar drugs constitutes one of the most important tasks in parenteral formulations design. This study investigates and assesses the solubility enhancement of Fluasterone by various techniques including cosolvency, micellization, and complexation. Of the solubilizing agents used, the modified beta-...

journal_title：Journal of pharmaceutical sciences

authors： Zhao L,Li P,Yalkowsky SH

更新日期：1999-10-01 00:00:00

abstract：:A Modified Crisp Equation, describing the differential Gibbs free energy of the adsorption process, is being proposed, which considers multiple sites available on the surface for adsorption and their relative fractions. The differential Gibbs free energy can be calculated by the van't Hoff Equation, which depends on t...

journal_title：Journal of pharmaceutical sciences

authors： Yu P,Wurster DE

更新日期：2018-04-01 00:00:00

abstract：:Phenytoin has been decreasingly used because of the high interindividual variability in drug concentration and the narrow therapeutic window. Despite such drawbacks, phenytoin is still essential as a second-line therapy for status epilepticus when patients are resistant to benzodiazepines. This study aimed to develop ...

journal_title：Journal of pharmaceutical sciences

authors： Guk J,Lee SG,Chae D,Kim JH,Park K

更新日期：2019-08-01 00:00:00

abstract：:Previously, 1 mL of purified water (hyposmotic) or saline (isosmotic) which dissolved 200 μM of FITC-dextran (FD-4), a nonabsorbable marker, was orally administered to rats, and luminal concentration-time profile of FD-4 was directly measured. In this study, at first, luminal FD-4 concentration was measured after oral...

journal_title：Journal of pharmaceutical sciences

authors： Tanaka Y,Higashino H,Kataoka M,Yamashita S

更新日期：2020-06-01 00:00:00

abstract：:A method for the measurement, in human plasma, of all tertiary and secondary tricyclic antidepressants prescribed in the United States is described. The method uses electron beam ionization GLC-mass spectrometry, employing a computer-controlled multiple-ion detector. This method, mass fragmentography, is used with int...

journal_title：Journal of pharmaceutical sciences

authors： Biggs JT,Holland WH,Chang S,Hipps PP,Sherman WR

更新日期：1976-02-01 00:00:00

abstract：:The molecular connectivity indexes of various aliphatic alcohols, ketones, ethers, and esters were used to describe structural features influencing chromatographic retention indexes. Good correlations were obtained within chemical classes for a particular stationary phase. ...

journal_title：Journal of pharmaceutical sciences

authors： Kier LB,Hall LH

更新日期：1979-01-01 00:00:00

abstract：:The preformulation, solubilization and pharmacokinetic evaluation of antalarmin, a stress inhibitor, have been conducted. Antalarmin has a poor water solubility of less than 1 microg/mL and is weakly basic with an experimentally determined pK(a) of 5.0. Multiple solubilization approaches including pH-control either al...

journal_title：Journal of pharmaceutical sciences

authors： Sanghvi R,Mogalian E,Machatha SG,Narazaki R,Karlage KL,Jain P,Tabibi SE,Glaze E,Myrdal PB,Yalkowsky SH

更新日期：2009-01-01 00:00:00