Tocainide conjugation in humans: novel biotransformation pathway for a primary amine.

abstract：:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...

journal_title：Journal of pharmaceutical sciences

authors： Ma YH,Wang Q,Gong J,Wu XY

更新日期：2016-03-01 00:00:00

abstract：:A rapid and simple high-performance liquid chromatographic (HPLC) method for the analysis of dichlorophen in raw material and in dichlorophen-toluene soft gelatin capsules for veterinary use was developed using a reverse-phase technique. This HPLC system was shown to isolate dichlorophen from its major impurity (the t...

journal_title：Journal of pharmaceutical sciences

authors： Shah KA,Samuels SA,Michaels MK,Warren JW

更新日期：1984-06-01 00:00:00

abstract：:An in vitro technique was developed to characterize the intermittent flume patterns associated with the short bursts of metered-dose aerosols. Two orthogonal video images are utilized to describe the complex shape and direction of the flume pattern. This technique facilitates the evaluation of components manufactured ...

journal_title：Journal of pharmaceutical sciences

authors： Miszuk S,Gupta BM,Chen FC,Clawans C,Knapp JZ

更新日期：1980-06-01 00:00:00

abstract：:To determine how structural changes in antibodies are connected with aggregation, the structural areas of an antibody prone to and/or impacted by aggregation must be identified. In this work, the higher-order structure and biophysical properties of two different monoclonal antibody (mAb) monomers were compared with th...

journal_title：Journal of pharmaceutical sciences

authors： Iacob RE,Bou-Assaf GM,Makowski L,Engen JR,Berkowitz SA,Houde D

更新日期：2013-12-01 00:00:00

abstract：:An aqueous solution of trimedoxime bromide, atropine, and benactyzine hydrochloride was formulated to have maximum stability as an antidote in organophosphorus poisoning. The stability of the mixture in glass and plastic cartridges was determined. Glass cartridges were more desirable than plastic; there was less vapor...

journal_title：Journal of pharmaceutical sciences

authors： Zvirblis P,Ellin RI

更新日期：1982-03-01 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：:Several controlled ice nucleation techniques have been developed to increase the efficiency of the freeze-drying process as well as to improve the quality of pharmaceutical products. Owing to the reduction in ice surface area, these techniques have the potential to reduce the degradation of proteins labile during free...

journal_title：Journal of pharmaceutical sciences

authors： Fang R,Tanaka K,Mudhivarthi V,Bogner RH,Pikal MJ

更新日期：2018-03-01 00:00:00

abstract：:A pharmacokinetic study of the dopamine D2 receptor agonist (S)-(-)-2-(N-propyl-N-(2-thienylethyl)amino)-5-hydroxytetralin+ ++-HCl (N-0923) infused in female cynomolgus monkeys over a 4-h period was carried out at International Research and Development Corporation. The purpose of this study was to estimate the elimina...

journal_title：Journal of pharmaceutical sciences

authors： Walters DR,McConnell WR,Cefali EA

更新日期：1994-05-01 00:00:00

abstract：:This work investigates the use of spray freeze-drying (SFD) to produce protein loaded particles suitable for epidermal delivery. In the first part of the study, the effects of formulation and process conditions on particle properties are examined. Aqueous solutions of trehalose produce SFD particles in the size range ...

journal_title：Journal of pharmaceutical sciences

authors： Sonner C,Maa YF,Lee G

更新日期：2002-10-01 00:00:00

abstract：:beta-Cyclodextrin was ethylated at the 2- and 6-hydroxyl positions. Diethyl sulfate was employed as an alkylating reagent. NMR spectra data indicate that heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (DCD) is the principal component of the product obtained. In addition, the FAB mass spectra obtained in nitrobenzyl alcoho...

journal_title：Journal of pharmaceutical sciences

authors： Vakily M,Pasutto FM,Daneshtalab M,Jamali F

更新日期：1995-08-01 00:00:00

abstract：:Investigation of the leaves of Montanoa tomentosa Cerv. ssp. microcephala (Sch.-Bip.) Funk (Compositae) resulted in the isolation of three novel guaianolide sesquiterpenes, montacephalin (1), tomencephalin (2), and 5-hydroxytomencephalin (3), which were shown to be cytotoxic (P-388). The structures of these sesquiterp...

journal_title：Journal of pharmaceutical sciences

authors： Topcu G,Cordell GA,Farnsworth NR,Fong HH

更新日期：1988-06-01 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：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...

journal_title：Journal of pharmaceutical sciences

authors： Stewart A,Yates I,Mudie D,Pivette P,Goodwin A,Sarmiento A,Winter M,Morgen M,Vodak D

更新日期：2019-01-01 00:00:00

abstract：:To study the effect of substituents on the antitumor activities of analogs of 1-phenyl-3-benzyl-3-methyltriazenes, a series of compounds was designed and synthesized in which the substituent on the 1-phenyl was an electron-withdrawing group and the substituent on the 3-benzyl had a broad range of physicochemical prope...

journal_title：Journal of pharmaceutical sciences

authors： Dunn WJ 3rd,Greenberg MJ

更新日期：1977-10-01 00:00:00

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：:Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...

journal_title：Journal of pharmaceutical sciences

authors： Grant J,Blicker M,Piquette-Miller M,Allen C

更新日期：2005-07-01 00:00:00

abstract：:Mechanical shock may cause cavitation in vials containing liquid formulations of therapeutic proteins and generate protein aggregates and other particulates. To test whether common formulation components such as protein molecules, air bubbles, or polysorbate 20 (PS20) micelles might nucleate cavitation, a high-speed v...

journal_title：Journal of pharmaceutical sciences

authors： Wu H,Chisholm CF,Puryear M,Movafaghi S,Smith SD,Pokhilchuk Y,Lengsfeld CS,Randolph TW

更新日期：2020-03-01 00:00:00

abstract：:An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble parti...

journal_title：Journal of pharmaceutical sciences

authors： Lassner P,Adler M,Lee G

更新日期：2014-04-01 00:00:00

abstract：:A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the alpha,beta-unsaturated ...

journal_title：Journal of pharmaceutical sciences

authors： Dimmock JR,Sidhu KK,Chen M,Li J,Quail JW,Allen TM,Kao GY

更新日期：1994-06-01 00:00:00

abstract：:The influence of various test meals and coadministered water volumes on erythromycin stearate bioavailability from orally dosed film-coated tablets was studied in healthy human subjects. Serum erythromycin levels were uniformly reduced by all test meals, with the reduction in mean peak serum levels varying from 47 to ...

journal_title：Journal of pharmaceutical sciences

authors： Welling PG,Huang H,Hewitt PF,Lyons LL

更新日期：1978-06-01 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：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 00:00:00

abstract：:The influences of 1-ethyl-, 1-butyl-, 1-hexyl-, and 1-octyl-2-pyrrolidone in their saline solutions on the transport of beta-estradiol, corticosterone, and hydrocortisone across hairless mouse skin under in vitro conditions have been investigated by the physical model approach. The experimental data were interpreted w...

journal_title：Journal of pharmaceutical sciences

authors： Yoneto K,Ghanem AH,Higuchi WI,Peck KD,Li SK

更新日期：1995-03-01 00:00:00

abstract：:Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absor...

journal_title：Journal of pharmaceutical sciences

authors： Wiseman EH,McIlhenny HM,Bettis JW

更新日期：1975-09-01 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：:To evaluate oral mucosal absorption of drugs in dogs, a newly designed in situ perfusion system with a circulating perfusion chamber was developed. The utility of the perfusion system was investigated by using three drugs: salicylic acid (SA), sulfadimethoxine (SM), and diltiazem (DIL). The oral mucosal absorption of ...

journal_title：Journal of pharmaceutical sciences

authors： Yamahara H,Suzuki T,Mizobe M,Noda K,Samejima M

更新日期：1990-11-01 00:00:00

abstract：:It is now becoming apparent that a common pathway of protein aggregation involves the unimolecular structural rearrangement from the native state to a slightly expanded aggregation-competent species. It is the goal of this study to understand the aggregation and the effects of buffer on the stability of IFN-tau. In th...

journal_title：Journal of pharmaceutical sciences

authors： Katayama DS,Nayar R,Chou DK,Valente JJ,Cooper J,Henry CS,Vander Velde DG,Villarete L,Liu CP,Manning MC

更新日期：2006-06-01 00:00:00

abstract：:A method for the determination of sematilide levels in human plasma is described. After the addition of an internal standard, plasma samples are adjusted to pH 8.5 and extracted with a solution of 7.5% isopropanol in methylene chloride. Separation from co-extracted matrix constituents is performed by reversed-phase HP...

journal_title：Journal of pharmaceutical sciences

authors： Dancik S,Koziol T,Nisperos E,Woolf E

更新日期：1991-02-01 00:00:00

abstract：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:Tissue-specific ultrasonic enhancement can be used for the detection and characterization of atherosclerosis. We have previously demonstrated the generation of inherently echogenic (acoustically reflective) liposomes solely by varying lipid composition and controlling the method of production. In this study, echogenic...

journal_title：Journal of pharmaceutical sciences

authors： Demos SM,Onyüksel H,Gilbert J,Roth SI,Kane B,Jungblut P,Pinto JV,McPherson DD,Klegerman ME

更新日期：1997-02-01 00:00:00