Intermolecular contacts influencing the conformational and geometric features of the pharmaceutically preferred mebendazole polymorph C.

abstract：:A series of N1-p-chlorophenyl-N5-alkylbiguanides were synthesized as potential inhibitors of dental plaque. Partition coefficients and pKa values were determined by standard methods. Biological activity was evaluated against Streptococcus mutans, a pure strain of plaque-forming bacteria. All compounds were compared to...

journal_title：Journal of pharmaceutical sciences

authors： Warner VD,Lynch DM,Ajemian RS

更新日期：1976-07-01 00:00:00

abstract：:Flightless I (Flii) is an actin remodeling protein important for cytoskeletal regulation and cellular processes including migration, proliferation, and adhesion. Previous studies have clearly identified Flii as a novel therapeutical target for improved wound repair and have demonstrated Flii regulation using Flii neut...

journal_title：Journal of pharmaceutical sciences

authors： Haidari H,Zhang Q,Melville E,Kopecki Z,Song Y,Cowin AJ,Garg S

更新日期：2017-07-01 00:00:00

abstract：:Cosalane is a potent inhibitor of HIV replication with multiple sites of action. The purposes of this study were to (a) determine the extent and nature of cosalane binding to mucin, alpha(1)-acid glycoprotein (AAG), plasma, and human (HSA) and bovine serum (BSA) albumin, and (b) determine the primary site(s) of cosala...

journal_title：Journal of pharmaceutical sciences

authors： Kuchimanchi KR,Ahmed MS,Johnston TP,Mitra AK

更新日期：2001-05-01 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：:Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

journal_title：Journal of pharmaceutical sciences

authors： Akash MS,Shen Q,Rehman K,Chen S

更新日期：2012-05-01 00:00:00

abstract：:In phenobarbital measurement by GLC with the flash-methylation technique, using trimethylanilinium hydroxide as a methylating reagent, a small amount of water decomposed phenobarbital and interfered with the quantitative analysis. Thus, both the sample and the methylating reagent must be sufficiently dehydrated to att...

journal_title：Journal of pharmaceutical sciences

authors： Kurata K,Takeuchi M,Yoshida K

更新日期：1979-09-01 00:00:00

abstract：:The purpose of the present study was to develop guidance toward rational choice of blenders and processing conditions to make robust and high performing adhesive mixtures for dry-powder inhalers and to develop quantitative experimental approaches for optimizing the process. Mixing behavior of carrier (LH100) and Astra...

journal_title：Journal of pharmaceutical sciences

authors： Sarkar S,Minatovicz B,Thalberg K,Chaudhuri B

更新日期：2017-01-01 00:00:00

abstract：:Compact strength and the particle-size distribution of milled roller compacted compacts were correlated to the slope of the best-fit line through near-infrared spectra for samples prepared under different roll speeds and feed rates. The above correlations were found to hold for compacts prepared from microcrystalline ...

journal_title：Journal of pharmaceutical sciences

authors： Gupta A,Peck GE,Miller RW,Morris KR

更新日期：2004-04-01 00:00:00

abstract：:A dual pH/redox responsive copper-glyglycine-prednisolone succinate-loaded nanoliposomal (NL) sludge was successfully synthesized and optimized using a Box-Behnken design of experiments. Preformulation design variables indicated that relative ratios of phospholipids, considerably influences NL size, thus altering the ...

journal_title：Journal of pharmaceutical sciences

authors： Mavuso S,Marimuthu T,Kumar P,Kondiah PPD,du Toit LC,Choonara YE,Pillay V

更新日期：2018-04-01 00:00:00

abstract：:The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

journal_title：Journal of pharmaceutical sciences

authors： Clausen AE,Bernkop-Schnürch A

更新日期：2000-10-01 00:00:00

abstract：:Fibril formation (aggregation) of human and bovine insulin and six human insulin mutants in hydrochloric acid were investigated by visual inspection, Thioflavin T fluorescence spectroscopy, transmission electron microscopy (TEM), and Fourier transform infrared (FTIR) spectroscopy. The fibrillation tendencies of the wi...

journal_title：Journal of pharmaceutical sciences

authors： Garriques LN,Frokjaer S,Carpenter JF,Brange J

更新日期：2002-12-01 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：:Apparent micellar molecular weights were determined with the antibiotic fusidate sodium by ultracentrifugation in varying counterion concentrations (Na+). The effects of buffer salts, pH, sodium chloride concentration, and drug concentration were studied. The results strongly support the concept of the formation of pr...

journal_title：Journal of pharmaceutical sciences

authors： Richard AJ

更新日期：1975-05-01 00:00:00

abstract：:In this study, we investigated the potential roles of nanoparticles (<100 nm) and submicron (100-1000 nm) particles in the formation of microparticles (>1000 nm) in protein formulations under some pharmaceutically relevant stress conditions. Exposure of intravenous immunoglobulin solutions to the interface-associated ...

journal_title：Journal of pharmaceutical sciences

authors： Pardeshi NN,Zhou C,Randolph TW,Carpenter JF

更新日期：2018-07-01 00:00:00

abstract：:A high-performance liquid chromatographic method has been developed for the simultaneous determination of azobenzene and hydrazobenzene in phenylbutazone and sulfinpyrazone raw materials and formulations. The drug raw material or formulation is shaken with 1N NaOH and n-hexane and centrifuged. The n-hexane layer is in...

journal_title：Journal of pharmaceutical sciences

authors： Matsui F,Lovering EG,Curran NM,Watson JR

更新日期：1983-10-01 00:00:00

abstract：:Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine have been measured over a 2-year period under ambient conditions and under temperature and humidity stress. Hydralazine tablets are stable under ambient conditions, but the hydrazine level in an injectable formulation increased from 4.5 to 10 m...

journal_title：Journal of pharmaceutical sciences

authors： Lovering EG,Matsui F,Curran NM,Robertson DL,Sears RW

更新日期：1983-08-01 00:00:00

abstract：:An analysis of the disintegration-dissolution sequence of drug release from a tablet leads to a mathematical expression relating disintegration to the dissolution profile of the tablet and the dissolution rate of the primary drug particles in the tablet. The equation describing the disintegration of an acetaminophen t...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Wang LY

更新日期：1978-01-01 00:00:00

abstract：:The University of British Columbia (UBC) became the first university in Canada to develop a strategy for enhancing global access to its technologies. UBC's University-Industry Liaison Office, in collaboration with the UBC chapter of Universities Allied for Essential Medicines (UAEM), established a mandate and develope...

journal_title：Journal of pharmaceutical sciences

authors： Wasan KM,Thornton SJ,Bell I,Goulding RE,Gretes M,Gray AP,Hancock RE,Campbell B

更新日期：2009-03-01 00:00:00

abstract：:Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-218 degrees C), molecular weights (135-504) a...

journal_title：Journal of pharmaceutical sciences

authors： Shibata Y,Fujii M,Kokudai M,Noda S,Okada H,Kondoh M,Watanabe Y

更新日期：2007-06-01 00:00:00

abstract：:Dolasetron mesilate (Anzemet) ((2 alpha, 6 alpha, 8 alpha, 9a beta)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1 H-indole-3-carboxylate monomethane-sulfonate) is a 5-HT3 receptor antagonist, which is in development for the treatment of chemotherapy-induced emesis. The ketone moiety of dolasetron is rapidly reduced...

journal_title：Journal of pharmaceutical sciences

authors： Dow J,Francesco GF,Berg C

更新日期：1996-07-01 00:00:00

abstract：:A swellable matrix tablet is described which is partially coated with cellulose acetate (CA) to obtain a film having the shape of a cup, whose permeability to water and solutes was altered by mixing increasing amounts of poly(ethylene glycol) 400 (PEG). The drug-release mechanism from such systems was assessed by carr...

journal_title：Journal of pharmaceutical sciences

authors： Catellani PL,Colombo P,Peppas NA,Santi P,Bettini R

更新日期：1998-06-01 00:00:00

abstract：:4-Fluoroisoleucine was produced by ammonolysis of 2-bromo-4-fluoro-3-methylpentanoic acid, which resulted from the bromofluorination of 4-methyl-2-pentenoic acid. It did not inhibit Plasmodium berghei in mice at 640 mg/kg and was not toxic to the animals. The fluoroamino acid inhibited Aspergillus niger, Trichoderma v...

journal_title：Journal of pharmaceutical sciences

authors： Gershon H,Shanks L,Clarke DD

更新日期：1978-05-01 00:00:00

abstract：:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

journal_title：Journal of pharmaceutical sciences

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 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：:In this study, the influence of the preparation technique (ball milling, spray drying, and film casting) of a supersaturated amorphous dispersion on the quality of solubility determinations of indomethacin in polyvinylpyrrolidone was investigated by means of statistical analysis. After annealing of the amorphous dispe...

journal_title：Journal of pharmaceutical sciences

authors： Knopp MM,Olesen NE,Holm P,Löbmann K,Holm R,Langguth P,Rades T

更新日期：2015-01-01 00:00:00

abstract：:A new solid-state form of cyclosporine produced by spray-drying exhibited characteristics consistent with a liquid crystal. No sharp diffraction peaks were observed by powder X-ray diffraction; however, analysis by both small-angle X-ray diffraction (SAXR) and microscopic under polarized light (PLM) confirmed the exis...

journal_title：Journal of pharmaceutical sciences

authors： Lechuga-Ballesteros D,Abdul-Fattah A,Stevenson CL,Bennett DB

更新日期：2003-09-01 00:00:00

abstract：:Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

journal_title：Journal of pharmaceutical sciences

authors： Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

更新日期：2016-08-01 00:00:00

abstract：:Safety evaluation of self-assembled polymeric micelles is important for biomedical involvement in drug delivery systems in the future. In this study, biodegradable monomethyl poly (ethylene glycol)-poly (ε-caprolactone)-poly (trimethylene carbonate) [MPEG-P(CL-co-TMC)] copolymer was synthesized and characterized by Fo...

journal_title：Journal of pharmaceutical sciences

authors： Yang X,Cao D,Wang N,Sun L,Li L,Nie S,Wu Q,Liu X,Yi C,Gong C

更新日期：2014-01-01 00:00:00

abstract：:Tablets with a central hole and a water-impermeable coating were prepared. These perforated coated tablets (PCTs) dissolve and release drug through the central hole only. In vitro release of the model drugs sodium benzoate and benzamide from PCTs occurred at a constant rate up to 80% release. The zero-order release ra...

journal_title：Journal of pharmaceutical sciences

authors： Hansson AG,Giardino A,Cardinal JR,Curatolo W

更新日期：1988-04-01 00:00:00

abstract：:A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provide...

journal_title：Journal of pharmaceutical sciences

authors： De AU,Saha BP

更新日期：1975-02-01 00:00:00