Polymorphism of rac-5,6-diisobutyryloxy-2-methylamino-1,2,3,4-tetrahydro-naphthalene hydrochloride (CHF 1035). I. Thermal, spectroscopic, and X-ray diffraction properties.

abstract：:Single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), and solid-state NMR (SSNMR) techniques are used to analyze the structures of two nonsolvated polymorphs of {4-(4-chloro-3-fluorophenyl)-2-[4-(methyloxy)phenyl]-1,3-thiazol-5-yl} acetic acid. These polymorphs are enantiotropically-related with a...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Katrincic LM,Long ST,Mueller RL,Carlton RA,Sun YT,Johnson MN,Copley RC,Light ME

更新日期：2008-11-01 00:00:00

abstract：:A sensitive, specific and reproducible high-performance liquid chromatographic procedure, using the normal phase and radial compression system, is described for the simultaneous determination of corticosterone, hydrocortisone, and dexamethasone in plasma, with prednisolone as the internal standard. Samples were extrac...

journal_title：Journal of pharmaceutical sciences

authors： Alvinerie M,Toutain PL

更新日期：1982-07-01 00:00:00

abstract：:Unlike most organic compounds, both digoxin and digitoxin melted over a wide temperature range, with the widest range being 88 and 33 degrees for both compounds, respectively. Furthermore, the melting ranges varied markedly among several untriturated powders obtained from commercial sources and after recrystallization...

journal_title：Journal of pharmaceutical sciences

authors： Chiou WL,Kyle LE

更新日期：1979-10-01 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

abstract：:A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...

journal_title：Journal of pharmaceutical sciences

authors： Scher M

更新日期：1980-03-01 00:00:00

abstract：:The location and conformation of fosinopril sodium (FS) in a lamellar liquid crystal of water, sodium dodecyl sulfate, and decanol was studied by low-angle X-ray diffraction. The result showed the FS molecule to be located within the amphiphilic part of the liquid crystalline structure with the polar parts anchored at...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Moaddel T,Morris KR,Abramowitz R,Amsberry KL

更新日期：1994-05-01 00:00:00

abstract：:The kinetics of irreversible aggregation of bovine Granulocyte-Colony Stimulating Factor (bG-CSF) in solution were investigated as a function of temperature (T), concentration, and pH, and analyzed in terms of an Extended Lumry-Eyring model of protein aggregation proceeding via a non-native conformational state. In th...

journal_title：Journal of pharmaceutical sciences

authors： Roberts CJ,Darrington RT,Whitley MB

更新日期：2003-05-01 00:00:00

abstract：:This review addresses a major question of importance to pharmaceutical scientists: how can novel drug delivery systems play a role in maximizing the UV protection of sunscreens? Because more and more people are being diagnosed with skin cancer each year than all other cancers combined, adequate sun protective measures...

journal_title：Journal of pharmaceutical sciences

authors： Damiani E,Puglia C

更新日期：2019-12-01 00:00:00

abstract：:The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

journal_title：Journal of pharmaceutical sciences

authors： Soliman FS,Shafik RM,Darwish M

更新日期：1982-02-01 00:00:00

abstract：:Intestinal transport of the type III phosphodiesterase inhibitor cilostazol was characterized to evaluate the influence of secretory transporter. Intestinal absorption of cilostazol measured by the in situ closed loop method, showed regional differences, with high permeability in the upper part of the small intestine....

journal_title：Journal of pharmaceutical sciences

authors： Toyobuku H,Tamai I,Ueno K,Tsuji A

更新日期：2003-11-01 00:00:00

abstract：:Mathematical relationships describing the delivery of drug to a target organ after intra-arterial, intravenous, and oral administration are presented. This discussion clearly demonstrates that administration into a blood vessel leading to the target organ often is superior to intravenous administration. However, this ...

journal_title：Journal of pharmaceutical sciences

authors： Oie S,Huang JD

更新日期：1981-12-01 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：:Recent studies have clearly demonstrated that Fourier transform IR spectroscopy can be a powerful tool for the study of protein stabilization during freeze-drying and for optimizing approaches to prevent lyophilization-induced protein aggregation. The purpose of the current review is to provide an overview of these to...

journal_title：Journal of pharmaceutical sciences

authors： Dong A,Prestrelski SJ,Allison SD,Carpenter JF

更新日期：1995-04-01 00:00:00

abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...

journal_title：Journal of pharmaceutical sciences

authors： Edwards DA,Langer R

更新日期：1994-09-01 00:00:00

abstract：:Bile acid (BA) retention within hepatocytes is an underlying mechanism of cholestatic drug-induced liver injury (DILI). We previously developed an assay using sandwich-cultured human hepatocytes (SCHHs) to evaluate drug-induced hepatocyte toxicity accompanying intracellular BA accumulation. However, due to shortcoming...

journal_title：Journal of pharmaceutical sciences

authors： Susukida T,Sekine S,Nozaki M,Tokizono M,Oizumi K,Horie T,Ito K

更新日期：2016-04-01 00:00:00

abstract：:The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Cerré C,Fini A,Sipahi AM,Baraldini M

更新日期：1995-05-01 00:00:00

abstract：:The increased incidence of human immunodeficiency virus infection in women has identified an urgent need to develop a female-controlled method to prevent acquisition of human immunodeficiency virus and other sexually transmitted diseases. Women would apply the product intravaginally before intercourse. Development of ...

journal_title：Journal of pharmaceutical sciences

authors： Sassi AB,McCullough KD,Cost MR,Hillier SL,Rohan LC

更新日期：2004-08-01 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：:The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...

journal_title：Journal of pharmaceutical sciences

authors： Shinohara Y,Magara H,Baba S

更新日期：1991-11-01 00:00:00

abstract：:The effect of pretreating callus membranes with dimethyl sulfoxide, dimethylacetamide, dimethylformamide, formamide, dioxane, or methyl orthoformate on sarin permeability was studied at three temperatures to determine the activation energy for transport. In addition, the effect of membrane pretreatment on permeability...

journal_title：Journal of pharmaceutical sciences

authors： Matheson LE,Wurster DE,Ostrenga JA

更新日期：1979-11-01 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：:Pepsin adsorbed on gibbsite or boehmite, non-acid-reactive forms of aluminum hydroxide, had a significantly lower activity than pepsin in solution. IR and desorbed pepsin activity studies showed that the reduced activity of adsorbed pepsin was not due to denaturation of pepsin on adsorption. Steric occlusion of the ac...

journal_title：Journal of pharmaceutical sciences

authors： Sepelyak RJ,Feldkamp JR,Regnier FE,White JL,Hem SL

更新日期：1984-11-01 00:00:00

abstract：:The effect of variable protein binding (taken as independent parameter) on pharmacological activity of drugs is considered in terms of the exposure or the steady state concentration of unbound drug at targeted tissue. Based on the application of the parallel tube or dispersion models it is shown that for the most comm...

journal_title：Journal of pharmaceutical sciences

authors： Berezhkovskiy LM

更新日期：2010-04-01 00:00:00

abstract：:A procedure is described for TLC detection and differentiation of the butyrophenone-diphenylbutylpiperidine group and phenothiazine derivatives at the microgram level. A two-dimensional TLC method to separate butyrophenone and diphenylbutylpiperidine compounds is reported. A variety of possible detection reagents were...

journal_title：Journal of pharmaceutical sciences

authors： Pluym A

更新日期：1979-08-01 00:00:00

abstract：:The hypothermic response following intraperitoneal doses (6.25, 12.5, and 25 mg/kg) of cobaltous chloride was investigated in Swiss albino mice. The magnitude and duration of rectal temperature depression were dose related. In each case, maximal hypothermia was evident within 30 min after injection. Body temperature d...

journal_title：Journal of pharmaceutical sciences

authors： Burke DH

更新日期：1978-06-01 00:00:00

abstract：:To reduce the inherent variability in serum uric acid levels of animals allowed ad libitum exposure to food containing potassium oxonate and uric acid, male Sprague-Dawley rats were trained to eat their daily food allotment in a 1.25-hr period each morning. After training the rats were fed a food mixture containing 5%...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Hsu TF,Combs AB

更新日期：1979-05-01 00:00:00

abstract：:Various novel diesters of pilocarpic acid were synthesized and evaluated as prodrug forms for pilocarpine with the aim of improving the ocular delivery characteristics of the drug. The pilocarpic acid monoesters previously studied cyclized spontaneously to pilocarpine in aqueous solution and although they showed enhan...

journal_title：Journal of pharmaceutical sciences

authors： Bundgaard H,Falch E,Larsen C,Mosher GL,Mikkelson TJ

更新日期：1986-08-01 00:00:00

abstract：:The permeability coefficient, Kp, of pure unbranched alkanoic acids (C2-C7) applied to isolated porcine skin, reached a maximum in the solubility parameter (delta 2) range of 9.7-10 cal1 /2/cm3/2. When these and other penetrants were delivered from a solvent vehicle, the following linear relationships could be demonst...

journal_title：Journal of pharmaceutical sciences

authors： Liron Z,Cohen S

更新日期：1984-04-01 00:00:00

abstract：:To study if electrostatic charge initially present in mannitol powder plays a role in the generation of aerosols, mannitol was unipolarly charged to varying magnitudes by tumbling the powder inside containers of different materials. The resulting charge in the powder was consistent with predictions from the triboelect...

journal_title：Journal of pharmaceutical sciences

authors： Adi H,Kwok PC,Crapper J,Young PM,Traini D,Chan HK

更新日期：2010-05-01 00:00:00

abstract：:Optical coherence tomography (OCT) is a recently developed optical technique that produces depth profiles of three-dimensional objects. It is a nondestructive interferometric method responding to refractive index variation in the sample under study and can reach a penetration depth of a few millimetres. OCT employs ne...

journal_title：Journal of pharmaceutical sciences

authors： Mauritz JM,Morrisby RS,Hutton RS,Legge CH,Kaminski CF

更新日期：2010-01-01 00:00:00