Systematic study on the chemical stability of the prodrug antitumor agent carzelesin (U-80,244)

abstract：:Drug transporters expressed in liver and kidney play a critical role in the elimination of a wide range of drugs and xenobiotics and inhibition of these transporters may therefore cause clinically significant drug-drug interactions (DDIs). Currently, in vitro transporter inhibition data are used to assess the risk tha...

journal_title：Journal of pharmaceutical sciences

authors： Chu X,Chan GH,Evers R

更新日期：2017-09-01 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

abstract：:The metabolic disposition of 14C-labeled carprofen [(+/-)-6-chloro-alpha-methylcarbazole-2-acetic acid] was investigated in rats, dogs, and humans. Carprofen is eliminated predominantly by biotransformation in these three species. In dogs and rats, the direct conjugation of carprofen to form an ester glucuronide and o...

journal_title：Journal of pharmaceutical sciences

authors： Rubio F,Seawall S,Pocelinko R,DeBarbieri B,Benz W,Berger L,Morgan L,Pao J,Williams TH,Koechlin B

更新日期：1980-11-01 00:00:00

abstract：:In recent years, computational methods have garnered much attention in protein engineering. A large number of computational methods have been developed to analyze the sequences and structures of proteins and have been used to predict the various properties. Antibodies are one of the emergent protein therapeutics, and ...

journal_title：Journal of pharmaceutical sciences

authors： Kuroda D,Tsumoto K

更新日期：2020-05-01 00:00:00

abstract：:In this paper, we establish a mechanistic model for the prediction of amorphous solid dispersion (ASD) stability. The novel approach incorporates fundamental physical parameters, principally supersaturation, diffusivity, and interfacial energy, to model crystallization in ASDs accounting for both kinetic and thermodyn...

journal_title：Journal of pharmaceutical sciences

authors： Ojo AT,Lee PI

更新日期：2020-08-18 00:00:00

abstract：:Hard gelatin capsule (HGC) shells are widely used to encapsulate drugs for oral delivery but are vulnerable to gelatin cross-linking, which can lead to slower and more variable in vitro dissolution rates. Adding proteolytic enzymes to the dissolution medium can attenuate these problems, but this complicates dissolutio...

journal_title：Journal of pharmaceutical sciences

authors： Likar MD,Carroll SC,Colgan ST,Yeoh T,MacDonald BC,Johnson GM,Space JS

更新日期：2018-12-01 00:00:00

abstract：:Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mor...

journal_title：Journal of pharmaceutical sciences

authors： Gurgel Assis MS,Fernandes Pedrosa TC,de Moraes FS,Caldeira TG,Pereira GR,de Souza J,Ruela ALM

更新日期：2021-01-13 00:00:00

abstract：:Personalized medicine aims to determine the most adequate treatment and dose regimen to obtain the maximum efficacy and minimum side effect by taking into account patients' characteristics. For numerous reasons, one being ethical and methodological hurdles in including specific populations in clinical trials, innovati...

journal_title：Journal of pharmaceutical sciences

authors： Marsousi N,Desmeules JA,Rudaz S,Daali Y

更新日期：2017-09-01 00:00:00

abstract：:The bioavailability of single lots of 250-mg ampicillin capsules, available from 17 distributors and/or manufactures, was determined. Each product was evaluated in terms of the serum ampicillin levels achieved at 1, 2, 3, 4, 6, and 8 hr postadministration, the peak serum levels, the time of peak serum level, and the a...

journal_title：Journal of pharmaceutical sciences

authors： Whyatt PL,Slywka GW,Melikian AP,Meyer MC

更新日期：1976-05-01 00:00:00

abstract：:With the introduction of Quality by Design (QbD) to the pharmaceutical industry, there has been an increased focus on understanding the nature of particles and composites, with the aim of understanding and modeling how they interact in complex systems, leading to robust dosage forms. Particle characterization tools ha...

journal_title：Journal of pharmaceutical sciences

authors： Gamble JF,Tobyn M,Hamey R

更新日期：2015-05-01 00:00:00

abstract：:The crystallization tendency of 2 crystalline polymorphs of indomethacin (Iα, Iγ) in the undercooled melt has been investigated using molecular dynamics simulations. The main thermodynamical and dynamical physical parameters involved in the nucleation and growth processes have been determined. A careful attention has ...

journal_title：Journal of pharmaceutical sciences

authors： Gerges J,Affouard F

更新日期：2020-02-01 00:00:00

abstract：:The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...

journal_title：Journal of pharmaceutical sciences

authors： Kobuchi S,Kita Y,Hiramatsu Y,Sasaki K,Uno T,Ito Y,Sakaeda T

更新日期：2021-02-01 00:00:00

abstract：:The geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...

journal_title：Journal of pharmaceutical sciences

authors： Amato ME,Djedaïni F,Pappalardo GC,Perly B,Scarlata G

更新日期：1992-12-01 00:00:00

abstract：:The in vitro antifungal activity of a novel series of cis- and trans-5-([aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidines (13-24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloaddition reaction of 1-(2-t...

journal_title：Journal of pharmaceutical sciences

authors： Mullen GB,Mitchell JT,Allen SD,St Georgiev V

更新日期：1988-12-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 00:00:00

abstract：:Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens. However, in humans, an inhalable form of rifapentine may be necessary to considerably shorten treatment duration because of the physiological barr...

journal_title：Journal of pharmaceutical sciences

authors： Chan JG,Duke CC,Ong HX,Chan JC,Tyne AS,Chan HK,Britton WJ,Young PM,Traini D

更新日期：2014-05-01 00:00:00

abstract：:17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...

journal_title：Journal of pharmaceutical sciences

authors： Salmona M,Lakszner K,Fanelli R,Saronio C,Bianchi R,Mussini E

更新日期：1975-09-01 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：:A highly sensitive assay for the measurement of all-trans-retinoic acid (tretinoin) and 13-cis-retinoic acid (isotretinoin) has been developed. Collected plasma samples were protein precipitated with 2-propanol followed by solid phase extraction. The retinoic acids were subsequently derivatized to their pentafluoroben...

journal_title：Journal of pharmaceutical sciences

authors： Lehman PA,Franz TJ

更新日期：1996-03-01 00:00:00

abstract：:Anthralin and its decomposition products were separated by both column chromatographic and TLC techniques. Two decomposition products were characterized by TLC, melting-point data, and UV and IR spectroscopy. Pure anthralin and its decomposition products also were determined quantitatively. ...

journal_title：Journal of pharmaceutical sciences

authors： Elsabbagh HM,Whitworth CW,Schramm LC

更新日期：1979-03-01 00:00:00

abstract：:A rapid, sensitive, and specific determination of ketoprofen in human and animal deproteinized body fluids by reversed-phase high-pressure liquid chromatography is presented. The acid is detectable in amounts as low as 0.1 microgram/ml. Limits of error are in the range of +/- 5.1% of the sample mean. ...

journal_title：Journal of pharmaceutical sciences

authors： Ballerini R,Cambi A,Del Soldato P,Melani F,Meli A

更新日期：1979-03-01 00:00:00

abstract：:The human immunodeficiency virus has infected millions of people and the epidemic continues to grow rapidly in some parts of the world. Antiretroviral (ARV) therapy has provided improved treatment and prolonged the life expectancy of patients. Moreover, there is growing interest in using ARVs to protect against new in...

journal_title：Journal of pharmaceutical sciences

authors： Kirtane AR,Langer R,Traverso G

更新日期：2016-12-01 00:00:00

abstract：:A novel drug-deliver device based on a self-setting bioactive cement formed from tetracalcium phosphate and dicalcium phosphate has been developed and tested in vitro using bovine insulin and bovine albumin as model polypeptide drugs. Equimolar mixtures of the calcium phosphate powders containing bovine insulin and bo...

journal_title：Journal of pharmaceutical sciences

authors： Otsuka M,Matsuda Y,Suwa Y,Fox JL,Higuchi WI

更新日期：1994-02-01 00:00:00

abstract：:Development of high-throughput release and characterization assays is critical for the effective support of the rapidly growing biologics pipeline for biotherapeutics. Clipping of polypeptide chains is commonly monitored during process optimization, formulation development, and stability studies. A reduced capillary e...

journal_title：Journal of pharmaceutical sciences

authors： Stackhouse N,Miller AK,Gadgil HS

更新日期：2011-12-01 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：:A diffusion model for the percutaneous absorption of a solute through the skin is developed for the specific case of a constant donor concentration with a finite removal rate from the receptor due to either perfusion rate or sampling. The model has been developed to include a viable epidermal resistance and a donor-st...

journal_title：Journal of pharmaceutical sciences

authors： Anissimov YG,Roberts MS

更新日期：1999-11-01 00:00:00

abstract：:The previous paper in this series introduced an X-ray diffraction quantitation method for the polymorphic content in tablets made of pure components. Before the method could be transferred, further studies were required to explain the commonly observed X-ray intensity variation in analyzing compacts. The literature ty...

journal_title：Journal of pharmaceutical sciences

authors： Cao W,Mullarney MP,Hancock BC,Bates S,Morris KR

更新日期：2003-12-01 00:00:00

abstract：:The entropy of fusion of 84 disubstituted benzenes was essentially constant and independent of the participation of the compounds in intramolecular or intermolecular hydrogen bonding. It was also independent of the shapes, sizes, and dipole moments of the rigid molecules studied. While the entropy of fusion was indepe...

journal_title：Journal of pharmaceutical sciences

authors： Martin E,Yalkowsky SH,Wells JE

更新日期：1979-05-01 00:00:00

abstract：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:A fully automated system for dissolution rate analysis of potassium in slow release tablets is described. Aliquots are removed after 1, 2, and 4 hr from six samples, and potassium is analyzed in a flame photometer at 768 nm. A complete study of six samples takes 5.5 hr. The system may be run overnight. During the time...

journal_title：Journal of pharmaceutical sciences

authors： Engdahl A,Karlberg B,Thelander S

更新日期：1976-03-01 00:00:00