On the identification of slip planes in organic crystals based on attachment energy calculation.

abstract：:The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS). Intranasal delivery is a noninvasive method that targets drugs to the brain and spinal cord along olfactory and trigeminal neural pathways, bypassing the BBB and minimizing systemic expo...

journal_title：Journal of pharmaceutical sciences

authors： Dhuria SV,Hanson LR,Frey WH 2nd

更新日期：2009-07-01 00:00:00

abstract：:The intracellular delivery of small interfering RNA (siRNA) is a therapeutic strategy to transiently block gene expression. Two silencing RNA strategies utilize either synthetic double stranded RNA or plasmid DNA encoding a short hairpin RNA (shRNA). In the present study, we have quantitatively compared the potency of...

journal_title：Journal of pharmaceutical sciences

authors： McAnuff MA,Rettig GR,Rice KG

更新日期：2007-11-01 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：:Although displacement from plasma protein binding (dPB) is usually of little clinical significance, it should be taken into account when interpreting changes in total plasma concentrations of drugs subject to metabolically based drug-drug interactions (mDDI). The aim of this study was to develop an approach to predict...

journal_title：Journal of pharmaceutical sciences

authors： Christensen H,Baker M,Tucker GT,Rostami-Hodjegan A

更新日期：2006-12-01 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 purpose of the present study was to examine whether the intestinal absorption of low-permeability drugs could be improved by utilization of the intestinal influx transporter PEPT1. We investigated whether peptide derivatives of poorly absorbable nonamino acid-like drugs might be substrates of PEPT1, using rebamipi...

journal_title：Journal of pharmaceutical sciences

authors： Kikuchi A,Tomoyasu T,Tanaka M,Kanamitsu K,Sasabe H,Maeda T,Odomi M,Tamai I

更新日期：2009-05-01 00:00:00

abstract：:Tissue damage caused by subcutaneous and intramuscular administration of three phenytoin prodrugs to rats was assessed. Since two of the prodrugs caused significant irritation, only 3-(hydroxymethyl)-5,5-diphenylhydantoin disodium phosphate ester might be useful as a nonirritant phenytoin prodrug suitable for parenter...

journal_title：Journal of pharmaceutical sciences

authors： Varia SA,Stella VJ

更新日期：1984-08-01 00:00:00

abstract：:Granules prepared by the high shear wet granulation (HSWG) process commonly exhibit the problem of overgranulation, a phenomenon characterized by a severe loss of the ability to form adequately strong tablet. We hypothesize that the incorporation of brittle excipients promotes brittle fracture of granules during compa...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Yeboah F,Zhang M,Feng Y,Sun CC

更新日期：2014-08-01 00:00:00

abstract：:The complex of L-L-boronophenylalanine (L-p-BPA) with fructose has been used for the past 5 years in clinical trials of boron neutron capture therapy to treat both melanoma and glioblastoma multiforme. However, the structure of this complex in water buffered at physiologic pH has not been established. In the (1)H NMR ...

journal_title：Journal of pharmaceutical sciences

authors： Shull BK,Spielvogel DE,Head G,Gopalaswamy R,Sankar S,Devito K

更新日期：2000-02-01 00:00:00

abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...

journal_title：Journal of pharmaceutical sciences

authors： Heiman AS,Taraporewala IB,McLean HM,Hong D,Lee HJ

更新日期：1990-07-01 00:00:00

abstract：:The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., o...

journal_title：Journal of pharmaceutical sciences

authors： Kawashima Y,Aoki S,Takenaka H,Miyake Y

更新日期：1984-10-01 00:00:00

abstract：:Ensuring the health of street-involved children is a growing public health challenge. These children are vulnerable, neglected, and rarely a priority for basic service providers and governments. Sizable populations of street-involved children are present in major urban areas worldwide and current trends in urbanizatio...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Twum JA,Wasan KM

更新日期：2012-10-01 00:00:00

abstract：:This article shows how milling can be used to explore the phase diagram of pharmaceuticals. This process has been applied to sulindac. A short milling has been found to trigger a polymorphic transformation between form II and form I upon heating which is not seen in the nonmilled material. This possibility was clearly...

journal_title：Journal of pharmaceutical sciences

authors： Latreche M,Willart JF,Guerain M,Hédoux A,Danède F

更新日期：2019-08-01 00:00:00

abstract：:The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). AO...

journal_title：Journal of pharmaceutical sciences

authors： Ouyang H,Chen W,Andersen TE,Steffansen B,Borchardt RT

更新日期：2009-01-01 00:00:00

abstract：:A simple and sensitive assay for quantitating 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (1; BMY 26517) in human plasma was developed using high-performance liquid chromatography with fluorescence detection. The method involves precipitation of protein and reversed-phase chromatography. The method i...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Pittman KA,Dandekar KA

更新日期：1987-12-01 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 method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...

journal_title：Journal of pharmaceutical sciences

authors： Bellantone RA,Patel P,Sandhu H,Choi DS,Singhal D,Chokshi H,Malick AW,Shah N

更新日期：2012-12-01 00:00:00

abstract：:After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...

journal_title：Journal of pharmaceutical sciences

authors： Wong BK,Bruhin PJ,Lin JH

更新日期：1999-02-01 00:00:00

abstract：:Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

journal_title：Journal of pharmaceutical sciences

authors： Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

更新日期：2010-09-01 00:00:00

abstract：:In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...

journal_title：Journal of pharmaceutical sciences

authors： Hamada Y,Ono M,Ohara M,Yonemochi E

更新日期：2017-04-01 00:00:00

abstract：:A three-way crossover bioavailability study was performed using nine adult male volunteers with three different commercial prednisone tablets. Plasma samples were assayed for prednisolone, the active metabolite of prednisone, by a radioimmunoassay method. Statistical analysis showed significant differences in the rate...

journal_title：Journal of pharmaceutical sciences

authors： Sullivan TJ,Sakmar E,Albert KS,Blair DC,Wagner JG

更新日期：1975-10-01 00:00:00

abstract：:In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Kita Y

更新日期：2000-05-01 00:00:00

abstract：:A reported fluorometric method to determine tetracycline in biological material was modified to determine low levels of the antibiotics when using only small amounts of starting material. The method is applicable to tissue distribution studies in small experimental animals and also can be used for serial determination...

journal_title：Journal of pharmaceutical sciences

authors： van den Bogert C,Kroon AM

更新日期：1981-02-01 00:00:00

abstract：:Blends of polymers with complementary properties hold promise for addressing the diverse, demanding polymer performance requirements in amorphous solid dispersions (ASDs), but we lack comprehensive property understanding for blends of important ASD polymers. Herein, we prepare pairwise blends of commercially available...

journal_title：Journal of pharmaceutical sciences

authors： Marks JA,Wegiel LA,Taylor LS,Edgar KJ

更新日期：2014-09-01 00:00:00

abstract：:Synthetic peptides corresponding to the variable tandem repeat domain of the cancer-associated antigen MUC1 mucin are candidates for cancer vaccines. In our investigation mice were immunized via subcutaneous injection with poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres containing a MUC1 mucin peptide. It was hy...

journal_title：Journal of pharmaceutical sciences

authors： Newman KD,Sosnowski DL,Kwon GS,Samuel J

更新日期：1998-11-01 00:00:00

abstract：:A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...

journal_title：Journal of pharmaceutical sciences

authors： Ellis KO,Schwan TJ,Wessels FL,Miles NJ

更新日期：1980-10-01 00:00:00

abstract：:While the number of clinical trials has continued to grow by about 20% in the past six months, no corresponding growth in product approval by the food and drug administration is seen or anticipated in the near future. Late-stage clinical failures due to lack of efficacy or toxicity continues to be a challenge. The opt...

journal_title：Journal of pharmaceutical sciences

authors： Ho RJ,Chien JY

更新日期：2009-06-01 00:00:00

abstract：:The heat of precipitation of dl-pseudoephedrine was determined by direct calorimetry using a Tronac isoperibolic calorimeter. The precipitation of dl-pseudoephedrine was induced by mixing aqueous solutions of the two enantiomers, namely, d- and l-pseudoephedrine, directly in the calorimeter. The molar heat of precipit...

journal_title：Journal of pharmaceutical sciences

authors： Pudipeddi M,Sokoloski TD,Duddu SP,Carstensen JT

更新日期：1995-10-01 00:00:00

abstract：:The significance of factors such as drug solubility, polymer molecular weight, drug loading dose, compression force, and hydrodynamic conditions on drug release from a swellable hydrophilic delivery system was investigated. Hydroxypropyl methylcellulose (HPMC) and pectin were major polymeric constituents of the delive...

journal_title：Journal of pharmaceutical sciences

authors： Kim H,Fassihi R

更新日期：1997-03-01 00:00:00

abstract：:Previous studies have shown that protein storage stability in freeze-dried l-arginine-based systems improved in the presence of chloride ions. However, chloride ions reduced the glass transition temperature of the freeze concentrate (Tg') and made freeze drying more challenging. In this study, l-arginine was freeze dr...

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：2016-10-01 00:00:00