Inactivation of gamma-glutamylcysteine synthetase by SAPH-3 disulfide: role of the histaminyl moiety.

abstract：:The binding of representative chemical classes of nonsteroidal anti-inflammatory drugs (NSAIDs) to human serum albumin (HSA) was investigated by equilibrium dialysis. Warfarin enantiomers were used as specific markers in displacement studies. Data were analyzed by a computerized nonlinear least squares approach design...

journal_title：Journal of pharmaceutical sciences

authors： Li KL,Thakur AK,Kapoor AL

更新日期：1988-03-01 00:00:00

abstract：:This study aims at investigating factors influencing humidity-induced recrystallization of amorphous lactose, produced by co-spray drying with particles of cellulose nanocrystals or sodium montmorillonite. In particular, the focus is on how the nanoparticle shape and surface properties influence the nanometer to micro...

journal_title：Journal of pharmaceutical sciences

authors： Hellrup J,Mahlin D

更新日期：2017-01-01 00:00:00

abstract：:The pharmacokinetics of aniracetam (AP), a new cognitive performance enhancer, and its main metabolites was investigated after intravenous (iv) and oral administrations to rat. The plasma levels of AP, 4-p-anisamidobutyric acid (ABA), and p-anisic acid (AA) were determined simultaneously by the HPLC method. The plasma...

journal_title：Journal of pharmaceutical sciences

authors： Ogiso T,Iwaki M,Tanino T,Ikeda K,Paku T,Horibe Y,Suzuki H

更新日期：1998-05-01 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：:A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...

journal_title：Journal of pharmaceutical sciences

authors： Acree WE Jr,McHan DR,Rytting JH

更新日期：1983-08-01 00:00:00

abstract：:The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...

journal_title：Journal of pharmaceutical sciences

authors： Gu CH,Grant DJ

更新日期：2001-09-01 00:00:00

abstract：:The rapid hydrolysis of epoprostenol to 6-keto-prostaglandin F1 alpha is hydronium ion-catalyzed even at pH 10 or higher. In the presence of 1.0% hexadecyltrimethylammonium chloride, the rate was reduced significantly (1580-fold at pH 2 and 283-fold at a physiological pH). This decrease in the hydrolysis rate is attri...

journal_title：Journal of pharmaceutical sciences

authors： Cho MJ

更新日期：1982-04-01 00:00:00

abstract：:Acrylic acid-esterified starch was produced by reacting starch with acrylic acid chloride. This reaction was rapid and easy to control. Introduction of acrylic groups into starch reduced the enzymatic degradability of starch (e.g., with 12 acrylic groups/100 glucose residues, approximately 75% of the degradation produ...

journal_title：Journal of pharmaceutical sciences

authors： Laakso T,Sjöholm I

更新日期：1987-12-01 00:00:00

abstract：:The antifungal activity of amphotericin B (AmB) incorporated in three cholesteryl carbonate esters (CCEs), sodium cholesteryl carbonate, cholesteryl palmityl carbonate, and dicholesteryl carbonate, was examined to assess their potential for use in a dry powder aerosol. Formulations containing dissolved AmB were stable...

journal_title：Journal of pharmaceutical sciences

authors： Chuealee R,Wiedmann TS,Srichana T

更新日期：2011-05-01 00:00:00

abstract：:Nasal drug delivery is an interesting route of administration for dihydroergotamine in migraine therapy. The currently available formulation contains dihydroergotamine at 4 mg/mL. For a nasal dose of 2 mg, a volume of 0.5 mL has to be administered, which sometimes leads to spillage of the formulation. The aim of the p...

journal_title：Journal of pharmaceutical sciences

authors： Marttin E,Romeijn SG,Verhoef JC,Merkus FW

更新日期：1997-07-01 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 pharmacokinetics of drug delivery from transdermal controlled-release devices consisting of (a) a membrane plus a reservoir or (b) a monolithic slab are examined. For the period when the devices act as if the drug reservoir were infinite, simple relationships for the steady-state slope and time lag are derived and...

journal_title：Journal of pharmaceutical sciences

authors： Berner B

更新日期：1985-07-01 00:00:00

abstract：:The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...

journal_title：Journal of pharmaceutical sciences

authors： Rayfield WJ,Kandula S,Khan H,Tugcu N

更新日期：2017-08-01 00:00:00

abstract：:The phase behavior of two series of phosphatidylcholines (PC) possessing carbamyloxy-linked fatty acids has been studied by differential scanning calorimetry. These non-natural phosphatidylcholines are of interest because they possess the capability of forming interlipid hydrogen bonds via the carbamyloxy function and...

journal_title：Journal of pharmaceutical sciences

authors： Curatolo W,Bali A,Gupta CM

更新日期：1985-12-01 00:00:00

abstract：:The pharmacokinetics of tamsulosin (TAM) was investigated using male Sprague-Dawley rats in which plasma alpha(1)-acid glycoprotein (alpha(1)-AGP) levels were elevated by the subcutaneous injection of 0.2 mL/kg of turpentine oil. alpha(1)-AGP levels increased about eight times after turpentine oil treatment, causing a...

journal_title：Journal of pharmaceutical sciences

authors： Matsushima H,Watanabe T,Higuchi S

更新日期：2000-04-01 00:00:00

abstract：:Our objective was to characterize, by DSC and XRD, the equilibrium thermal behavior of frozen aqueous solutions containing polyethylene glycol (PEG) and sucrose. Aqueous solutions of (i) PEG (2.5-50% w/w), (ii) sucrose (10% w/v) with different concentrations of PEG (1-20% w/v), and (iii) PEG (2% or 10% w/v) with diffe...

journal_title：Journal of pharmaceutical sciences

authors： Bhatnagar BS,Martin SM,Teagarden DL,Shalaev EY,Suryanarayanan R

更新日期：2010-11-01 00:00:00

abstract：:The objective of this study was to investigate product performance of freeze dried l-arginine/sucrose-based formulations under variation of excipient weight ratios, l-arginine counter ions and formulation pH as a matrix to stabilize a therapeutic monoclonal antibody (MAb) during freeze drying and shelf life. Protein a...

journal_title：Journal of pharmaceutical sciences

authors： Stärtzel P,Gieseler H,Gieseler M,Abdul-Fattah AM,Adler M,Mahler HC,Goldbach P

更新日期：2015-07-01 00:00:00

abstract：:To reduce the risk of immunogenicity that may be caused by therapeutic protein products, it is important to properly characterize subvisible particles and to develop strategies to reduce the levels of particles delivered to patients. In the present study, by using state-of-the-art methods to quantify particle levels, ...

journal_title：Journal of pharmaceutical sciences

authors： Ueda T,Nakamura K,Abe Y,Carpenter JF

更新日期：2019-01-01 00:00:00

abstract：:The physicochemical properties of A-75998, a synthetic antagonist of luteinizing hormone releasing hormone with potential for treatment of hormone-sensitive cancers and endometriosis, are described. An accelerated solution stability study indicated that the compound is relatively stable and showed a U-shaped pH-rate p...

journal_title：Journal of pharmaceutical sciences

authors： Cannon JB,Krill SL,Porter WR

更新日期：1995-08-01 00:00:00

abstract：:The objective of this study was to determine if a high Tg polymer (Eudragit(®) S100) could be used to stabilize amorphous domains of polyethylene oxide (PEO) and hence improve the stability of binary polymer systems containing celecoxib (CX). We propose a novel method of stabilizing the amorphous PEO solid dispersion ...

journal_title：Journal of pharmaceutical sciences

authors： Jones DS,Tian Y,Li S,Yu T,Abu-Diak OA,Andrews GP

更新日期：2016-10-01 00:00:00

abstract：:The objective of this study was to determine the primary formulation properties that affect the dissolution rate of poorly soluble nondisintegrating drugs. This work focused on compression of orally administered acidic drugs with ionizable buffers. Naproxen was used as the poorly soluble model drug, and calcium salts ...

journal_title：Journal of pharmaceutical sciences

authors： Chakrabarti S,Southard MZ

更新日期：1997-04-01 00:00:00

abstract：:The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level Box-Behnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X(1)), Tween 20 (X(2)), and Transcutol HP (X(3)...

journal_title：Journal of pharmaceutical sciences

authors： Marasini N,Yan YD,Poudel BK,Choi HG,Yong CS,Kim JO

更新日期：2012-12-01 00:00:00

abstract：:A rapid, sensitive, and accurate reversed-phase HPLC method has been developed for the analysis and quantification of pharmaceutical formulations containing tyrothricin (1), an antibiotic used in antiseptic buccal compressed tablets for local application. The assay has been carried out under isocratic conditions, usin...

journal_title：Journal of pharmaceutical sciences

authors： Caraballo I,Fernandez-Arevalo M,Holgado MA,Vela MT,Rabasco AM

更新日期：1994-08-01 00:00:00

abstract：:The use of various synthetic lipids and polymers to deliver DNA for gene therapy applications has been the subject of intense examination for the last 15 years. Our understanding of the processes involved in the delivery of DNA, although still limited, can be described in terms of specific physical and chemical barrie...

journal_title：Journal of pharmaceutical sciences

authors： Wiethoff CM,Middaugh CR

更新日期：2003-02-01 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：:The delivery of active agents to the skin by liposome carriers is an interdisciplinary topic of great interest today. Data accumulated over the last decade strongly point to important advantages of these drug delivery systems. A symposium devoted to classic and new approaches in the use of liposomal systems was organi...

journal_title：Journal of pharmaceutical sciences

authors： Touitou E,Junginger HE,Weiner ND,Nagai T,Mezei M

更新日期：1994-09-01 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 dissolution of the 60-85-mesh fraction os recording, flow-through dissolution apparatus equipped with a dissolution cell; it was particularly suitable for kinetic analysis of multiparticulate systems. By using a time-scaling approach, experimental data are compared with theoretical calculations to evaluate, quanti...

journal_title：Journal of pharmaceutical sciences

authors： Pedersen PV,Brown KF

更新日期：1976-10-01 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：:The correlation between dynamic surface properties of drug molecules and drug absorption in two common in vitro models of the intestinal wall (Caco-2 monolayers and rat intestinal segments) has been investigated. A homologous series of beta-adrenoreceptor antagonists were used as model compounds. Dynamic molecular sur...

journal_title：Journal of pharmaceutical sciences

authors： Palm K,Luthman K,Ungell AL,Strandlund G,Artursson P

更新日期：1996-01-01 00:00:00