Indolizines II: search for potential oral hypoglycemic agents.

abstract：:Three families of alloxan derivatives, 5-arylthiobarbituric, 5-aryliminobarbituric, and 5-aryldialuric acids, were prepared as prospective radioiodine-transporting radiopharmaceuticals for the delineation of pancreatic insulinomas. Members of each class were screened for effects on blood sugar levels in a rat glucose ...

journal_title：Journal of pharmaceutical sciences

authors： Adams WE,Heindel ND,Tutwiler G,Fawthrop H

更新日期：1984-03-01 00:00:00

abstract：:A model based on heat transport control was developed to describe the uptake of water on a deliquescent solid in an atmosphere of pure water vapor. The model assumes the presence of a saturated liquid film on the surface of the solid. The decrease in the vapor pressure of water over the surface, brought about by the c...

journal_title：Journal of pharmaceutical sciences

authors： Van Campen L,Amidon GL,Zografi G

更新日期：1983-12-01 00:00:00

abstract：:A set of nonionic cellulose ethers with varying hydrophobicity and molecular weight has been investigated by principal component analysis (PCA). Several experimental variables such as dynamic surface tension, diffusion coefficient, microviscosity as monitored by a fluorescence probe technique, and intrinsic viscosity ...

journal_title：Journal of pharmaceutical sciences

authors： Persson B,Evertsson H,Bergman R,Sundelöf LO

更新日期：1999-08-01 00:00:00

abstract：:Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

journal_title：Journal of pharmaceutical sciences

authors： Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

更新日期：2013-10-01 00:00:00

abstract：:The effects of physical aging and antiplasticization on the water transport properties of glassy cellulose acetate film-coated tablets were investigated. The gradual approach toward thermodynamic equilibrium during physical aging decrease the free volume of the polymers. This decrease in free volume is accompanied by ...

journal_title：Journal of pharmaceutical sciences

authors： Guo JH

更新日期：1994-03-01 00:00:00

abstract：:Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

journal_title：Journal of pharmaceutical sciences

authors： Francis L,Harrell A,Hallifax D,Galetin A

更新日期：2020-09-01 00:00:00

abstract：:In liver microsomes, selexipag (NS-304; ACT-293987) mainly undergoes hydrolytic removal of the sulfonamide moiety by carboxylesterase 1 (CES1) to yield the pharmacologically active metabolite MRE-269 (ACT-333679). However, it is not known how much CES in the liver and intestine contributes to the hydrolysis of selexip...

journal_title：Journal of pharmaceutical sciences

authors： Imai S,Ichikawa T,Sugiyama C,Nonaka K,Yamada T

更新日期：2019-02-01 00:00:00

abstract：:The benzenesulfonate salt of an anti-methicillin-resistant Staphylococcus aureus carbapenem antibiotic studied is a crystalline, nonhygroscopic powder which is stable at room temperature, making it an ideal compound for long-term storage. However, the limited aqueous solubility of this salt prohibits parenteral admini...

journal_title：Journal of pharmaceutical sciences

authors： Antonucci V,Yen D,Kelly J,Crocker L,Dienemann E,Miller R,Almarrsson O

更新日期：2002-04-01 00:00:00

abstract：:A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or...

journal_title：Journal of pharmaceutical sciences

authors： Aoyama T,Kotaki H,Honda Y,Nakagawa F

更新日期：1990-06-01 00:00:00

abstract：:Hydrastine, canadine, and berberine were determined by the acid-dye technique. At pH 5.6, both the tertiary and the quaternary hydrastis alkaloids formed ion-pairs with bromcresol purple. The liberated hydrastine and canadine from the alkaloid-dye complexes were determined spectrophotometrically in the presence of ber...

journal_title：Journal of pharmaceutical sciences

authors： El-Masry S,Korany MA,Abou-Donia AH

更新日期：1980-05-01 00:00:00

abstract：:Maintaining a native-like structure of protein pharmaceuticals during lyophilization is an important aspect of formulation. Infrared spectroscopy can be used to evaluate the effectiveness of formulations in protecting the secondary structural integrity of proteins in the dried solid. This necessitates making quantitat...

journal_title：Journal of pharmaceutical sciences

authors： Kendrick BS,Dong A,Allison SD,Manning MC,Carpenter JF

更新日期：1996-02-01 00:00:00

abstract：:The pharmacokinetics of valproic acid after oral administration of sustained-release formulations were studied in 12 healthy volunteers. The objective of the present study was to find an appropriate mathematical model to describe the complex drug intake process. The concentration of valproic acid in plasma was measure...

journal_title：Journal of pharmaceutical sciences

authors： Bressolle F,Gomeni R,Alric R,Royer-Morrot MJ,Necciari J

更新日期：1994-10-01 00:00:00

abstract：:Two multisample laboratory powder diffractometers have been evaluated for the purpose of pattern indexing in the context of physical form screening. Both diffractometers utilise foil transmission geometry, primary monochromated radiation, and a position-sensitive detector. Data collected from six compounds (sotalol hy...

journal_title：Journal of pharmaceutical sciences

authors： Florence AJ,Baumgartner B,Weston C,Shankland N,Kennedy AR,Shankland K,David WI

更新日期：2003-09-01 00:00:00

abstract：:Sugars and polyols have been used routinely with lyophilized proteins and peptides as bulking agents, cryoprotectants, and lyoprotectants. However, reducing sugars may present a problem as excipients since they are potentially reactive with proteins. In this stability study of recombinant human relaxin (Rix) with vari...

journal_title：Journal of pharmaceutical sciences

authors： Li S,Patapoff TW,Overcashier D,Hsu C,Nguyen TH,Borchardt RT

更新日期：1996-08-01 00:00:00

abstract：:The diffusion model for percutaneous absorption is developed for the specific case of delivery to the skin being limited by the application of a finite amount of solute. Two cases are considered; in the first, there is an application of a finite donor (vehicle) volume, and in the second, there are solvent-deposited so...

journal_title：Journal of pharmaceutical sciences

authors： Anissimov YG,Roberts MS

更新日期：2001-04-01 00:00:00

abstract：:The elementary osmotic pump is a new delivery system for drugs or other active agents; it delivers the agent by an osmotic process at a controlled rate. Control resides in the: (a) water permeation characteristics of a semipermeable membrane surrounding the formulated agent, and (b) osmotic properties of the formulati...

journal_title：Journal of pharmaceutical sciences

authors： Theeuwes F

更新日期：1975-12-01 00:00:00

abstract：:Alpha-Hydroxyaryl ketones such as 2-hydroxypropiophenone and 1-(2,4-difluorophenyl)-2-hydroxy-1-propanone, the key intermediates in the preparation of antifungal agents, decompose into oxidized, rearranged, and condensed products. These products were isolated and characterized. The possible mechanisms for the formatio...

journal_title：Journal of pharmaceutical sciences

authors： Gala D,Puar MS,Das PR,Kugelman M,DiBenedetto DJ

更新日期：1992-12-01 00:00:00

abstract：:The bioavailability of three different brands and three different dosage forms of doxycycline was studied in normal subjects. Single doses, equivalent to 200 mg of doxycycline, were administered to six subjects in a crossover design as the innovator's intravenous solution given orally (Treatment A), the innovator's ca...

journal_title：Journal of pharmaceutical sciences

authors： Antal EJ,Jaffe JM,Poust RI,Colaizzi JL

更新日期：1975-12-01 00:00:00

abstract：:Water evaporation rates were measured from thin samples of a model layered structure of stratum corneum lipids with 32% water. A model with only free fatty acids present gave the lowest evaporation rates, while a model with only oleic acid gave values approximately 50% higher. Using the total lipid spectrum of stratum...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Kayali I

更新日期：1989-08-01 00:00:00

abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has received considerable attention as a potential anticancer agent. However, recombinant Apo2L/TRAIL has several limitations, which include a weak pharmacokinetic profile, namely, a short biological half-life and rapid renal clearance, and an inability t...

journal_title：Journal of pharmaceutical sciences

authors： Kim TH,Jiang HH,Youn YS,Park CW,Lim SM,Jin CH,Tak KK,Lee HS,Lee KC

更新日期：2011-02-01 00:00:00

abstract：:The objective of the current study was to develop and evaluate VLDL-resembling phospholipid-submicron emulsion (PSME) as a carrier system for new cholesterol-based compounds for targeted delivery to cancer cells. BCH, a boronated cholesterol compound, was originally developed in our laboratory to mimic the cholesterol...

journal_title：Journal of pharmaceutical sciences

authors： Shawer M,Greenspan P,ØIe S,Lu DR

更新日期：2002-06-01 00:00:00

abstract：:A high-performance liquid chromatographic method using a linear elution gradient has been developed for the analysis of sulindac, sulindac sulfone, and sulindac sulfide in plasma, urine, bile, and gastric fluid. The methodology uses reverse-phase, radial compression chromatography with gradient elution, and UV detecti...

journal_title：Journal of pharmaceutical sciences

authors： Musson DG,Vincek WC,Constanzer ML,Detty TE

更新日期：1984-09-01 00:00:00

abstract：:The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...

journal_title：Journal of pharmaceutical sciences

authors： Gay B,Cardot JM,Schnell C,van Hoogevest P,Gygax D

更新日期：1993-10-01 00:00:00

abstract：:A specific and reproducible high-performance liquid chromatographic (HPLC) procedure was developed for the quantitative analysis of carboplatin (JM-8) in dog plasma ultrafiltrate. Plasma ultrafiltrate samples were generated using Amicon Centrifree micropartition systems or Amicon Centriflo cones, and injected onto a m...

journal_title：Journal of pharmaceutical sciences

authors： Duncan GF,Faulkner HC 3rd,Farmen RH,Pittman KA

更新日期：1988-03-01 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：:Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitr...

journal_title：Journal of pharmaceutical sciences

authors： Stange U,Scherf-Clavel M,Gieseler H

更新日期：2013-11-01 00:00:00

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：:Drug-induced phototoxic skin responses involves photoirritation, photoallergy, and photogenotoxicity. In the present study, we attempted to develop effective analytical tools to predict the photogenotoxic potential of pharmaceutical substances on the basis of their photobiological and DNA-binding properties. Photoclea...

journal_title：Journal of pharmaceutical sciences

authors： Onoue S,Seto Y,Oishi A,Yamada S

更新日期：2009-10-01 00:00:00

abstract：:Transformation of polymorph I of clopidogrel hydrogen sulfate (CHS) to polymorph II of CHS during the crystallization was monitored by using in situ measurement of ultrasonic velocity. Drowning-out crystallization using methanol as a solvent and isopropyl alcohol as nonsolvent was carried out. The polymorphs were iden...

journal_title：Journal of pharmaceutical sciences

authors： Kim HJ,Kim KJ

更新日期：2008-10-01 00:00:00

abstract：:Respirable crystals of cromoglycic acid (CA) were prepared by precipitation of CA with hydrochloric acid from aqueous solutions of cromolyn sodium and subsequent recrystallization from hot water or mixtures of dimethyl sulphoxide and water. The properties of the materials were established by melting point measurements...

journal_title：Journal of pharmaceutical sciences

authors： Chan HK,Gonda I

更新日期：1989-02-01 00:00:00