Expression of human polyspecific renal organic cation transport activity in Xenopus laevis oocytes.

abstract：:The purpose of this work was to study the permeability of two relatively lipophilic sulfenamide prodrugs of linezolid (clogP 0.85), N-(phenylthio)linezolid (1, clogP 2.77) and N-[(2-ethoxycarbonyl)ethylthio]linezolid (2, clogP 1.43), across Caco-2 cell monolayers. Both prodrugs were found to convert to linezolid in th...

journal_title：Journal of pharmaceutical sciences

authors： Nti-Addae KW,Guarino VR,Dalwadi G,Stella VJ

更新日期：2012-09-01 00:00:00

abstract：:This study evaluates the effect of variation in the ambient moisture on the compaction behavior of microcrystalline cellulose (MCC) powder. The study was conducted by comparing the physico-mechanical properties of, and the near infrared (NIR) spectra collected on, compacts prepared by roller compaction with those coll...

journal_title：Journal of pharmaceutical sciences

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

更新日期：2005-10-01 00:00:00

abstract：:Detection and quantification of the amorphous phase of etoricoxib bulk drug substances, a selective cycloogenase-2 inhibitor used for the treatment of osteoarthritis, rheumatoid arthritis, and dental pain, was carried out using modulated differential scanning calorimetry (MDSC), dynamic mechanical analysis (DMA), and ...

journal_title：Journal of pharmaceutical sciences

authors： Clas SD,Lalonde K,Khougaz K,Dalton CR,Bilbeisi R

更新日期：2012-02-01 00:00:00

abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Hoffman L,Bongers J,Tao L,Huang Y,Slaney T,Das TK,Leone A,Kar SR

更新日期：2019-06-01 00:00:00

abstract：:The equilibrium constants, kinetics, and mechanism of promazine and promethazine oxidation by ferric perchlorate were investigated at different temperatures and acidities using a stopped-flow spectrophotometric technique. The overall reaction can be represented as follows: (formula: see text) where P+ represents the r...

journal_title：Journal of pharmaceutical sciences

authors： Gasco MR,Carlotti ME

更新日期：1978-02-01 00:00:00

abstract：:A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

journal_title：Journal of pharmaceutical sciences

authors： Won CM,Zalipsky JJ,Patel DM,Grim WM

更新日期：1982-03-01 00:00:00

abstract：:An electron-capture GLC method to measure nofedone in human serum was developed. A homolog of nofedone was added to the serum as an internal standard before the sample was alkalinized with pH 9.5 phosphate buffer and extracted with ethylene dichloride containing 0.5% isopentyl alcohol. This organic phase was extracted...

journal_title：Journal of pharmaceutical sciences

authors： Heusse D,Populaire P,Renard A,Pasquier P,Gregoire J

更新日期：1980-05-01 00:00:00

abstract：:Herein, curcumin amorphous solid dispersions (Cur ASDs) were prepared using binary polymers (Eudragit EPO with polyvinylpyrrolidone K30 [EuD-PVP], Eudragit EPO with hydroxypropyl methylcellulose E50 [EuD-HPMC]) as excipient, and surface tracking of Cur ASDs was mainly addressed. Infrared spectroscopy, in situ Raman im...

journal_title：Journal of pharmaceutical sciences

authors： Fan N,Lu T,Li J

更新日期：2020-02-01 00:00:00

abstract：:Chlortetracycline was successfully separated from its degradation products and from other tetracyclines on a paper chromatogram previously impregnated with a mixture of edetate disodium and urea solution in pH 5.0 McIlvaine buffer. Chlortetracycline separation from its degradation products and from both tetracycline a...

journal_title：Journal of pharmaceutical sciences

authors： Youssef MK,Attia IA,Safwat S

更新日期：1978-04-01 00:00:00

abstract：:Human insulin exists in different association states, from monomer to hexamer, depending on the conditions. In the presence of zinc the "normal" state is a hexamer. The structural properties of 20 variants of human insulin were studied by near-UV circular dichroism, fluorescence spectroscopy, and small-angle X-ray sca...

journal_title：Journal of pharmaceutical sciences

authors： Uversky VN,Garriques LN,Millett IS,Frokjaer S,Brange J,Doniach S,Fink AL

更新日期：2003-04-01 00:00:00

abstract：:The micellar properties of Poloxamer 213 (1), a Pluronic copolymer shown to affect lipid absorption and serum cholesterol level in experimental animals, are investigated by surface tension measurements, photon correlation spectroscopy (PCS), Reichardt's dye solubilization technique, differential scanning calorimetry (...

journal_title：Journal of pharmaceutical sciences

authors： Cheng HY,Holl WW

更新日期：1990-10-01 00:00:00

abstract：:Product temperature (Tb) and drying time constitute critical material attributes and process parameters in the lyophilization process and especially during the primary drying stage. In the study, we performed a temperature measurement by the sublimation rate (TMbySR) to monitor the Tb value and determine the end point...

journal_title：Journal of pharmaceutical sciences

authors： Kawasaki H,Shimanouchi T,Sawada H,Hosomi H,Hamabe Y,Kimura Y

更新日期：2019-07-01 00:00:00

abstract：:Low-density lipoproteins (LDLs), the physiological vehicles for lipids, are potentially useful drug delivery devices for (hydrophobic) drugs. The physicochemical characteristics of LDL loaded with the adriamycin derivative AD 32 or the N-mustard derivative WB 4291 were compared to that of native and reconstituted LDL ...

journal_title：Journal of pharmaceutical sciences

authors： Westesen K,Gerke A,Koch MH

更新日期：1995-02-01 00:00:00

abstract：:Colonic drug delivery is intended for local or systemic therapies. The lack of predictive in vitro or animal model leads to considerable time delays in colonic product development. The objective of this scintigraphic study was to provide "proof of concept" for a novel capsule-type colonic delivery system (Colon-Target...

journal_title：Journal of pharmaceutical sciences

authors： Ishibashi T,Pitcairn GR,Yoshino H,Mizobe M,Wilding IR

更新日期：1998-05-01 00:00:00

abstract：:Griseofulvin/cyclodextrin interactions were investigated in aqueous environment and in solid state. Two cyclodextrin derivatives (beta-cyclodextrin and 2-hydroxypropyl beta-cyclodextrin) were used to prepare different physical mixtures and kneaded systems, and the drug/cyclodextrin ratios were 1:1 and 1:2 mol/mol. Sca...

journal_title：Journal of pharmaceutical sciences

authors： Veiga MD,Díaz PJ,Ahsan F

更新日期：1998-07-01 00:00:00

abstract：:The biological activity of a series of 10 silver sulfanilamides is studied in relation to the physical parameters pK alpha, log K, and the aqueous solubility. None of the parameters demonstrate a simple relationship with the activity. A discussion of the significance of log K and the solubility in relation to the acti...

journal_title：Journal of pharmaceutical sciences

authors： Bult A,Bajema BL,Boelema GJ,Saene JJ,Doornbos DA

更新日期：1984-01-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

journal_title：Journal of pharmaceutical sciences

authors： Buchan B,Kay G,Matthews KH,Cairns D

更新日期：2012-10-01 00:00:00

abstract：:In this paper, we demonstrate that by employing a combination of sedimentation field-flow fractionation (sedFFF) and other characterization techniques, such as photon correlation spectroscopy (PCS) and freeze-fracture electron microscopy (EM), it is possible to show that commercial fat emulsions of similar overall che...

journal_title：Journal of pharmaceutical sciences

authors： Li J,Caldwell KD

更新日期：1994-11-01 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：:In previous studies (Yoneto et al., 1995. J Pharm Sci 84:312-317; Kim et al., 1992. Int J Pharm 80:17-31; and Warner et al., 2001. J Pharm Sci 90:1143-53), the transport enhancing effects of four homologous series of enhancers-the n-alkanols, 1-alkyl-2-pyrrolidones, 1,2-alkanediols, and N,N-dimethylalkanamides - on th...

journal_title：Journal of pharmaceutical sciences

authors： He N,Li SK,Suhonen TM,Warner KS,Higuchi WI

更新日期：2003-02-01 00:00:00

abstract：:Live attenuated influenza vaccine (LAIV) is considered one of the most effective vaccines and can be manufactured quickly and inexpensively to counter seasonal or pandemic influenza. Lyophilization is widely used in vaccine production. However, it requires a longer production cycle and large-scale equipment, thus posi...

journal_title：Journal of pharmaceutical sciences

authors： Sun Y,Shen Z,Zhang C,Yi Y,Zhu K,Xu F,Kong W

更新日期：2019-07-01 00:00:00

abstract：:A stability-indicating analytical method is described for the simultaneous determination of nitrate, and if present, its reductive degradation product, nitrite, in toothpastes. Nitrate and nitrite were extracted from the toothpaste using distilled water and separated from other water-soluble excipients by two RP-8 col...

journal_title：Journal of pharmaceutical sciences

authors： Lulla H,Chen SS,Sena FJ

更新日期：1984-07-01 00:00:00

abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

journal_title：Journal of pharmaceutical sciences

authors： Hudgins PM,Stubbins JF

更新日期：1975-08-01 00:00:00

abstract：:Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...

journal_title：Journal of pharmaceutical sciences

authors： Trapa PE,Belova E,Liras JL,Scott DO,Steyn SJ

更新日期：2016-02-01 00:00:00

abstract：:2',7'-Bis(2-carboxyethyl)-5(6)-carboxyfluorescein (BCECF) is a fluorescent probe used to examine multidrug resistance-associated protein (MRP) transporter activity in cells. BCECF is introduced into the cell as the nonfluorescent membrane permeable acetoxymethyl ester, BCECF-AM, where it is hydrolyzed to the membrane ...

journal_title：Journal of pharmaceutical sciences

authors： Bachmeier CJ,Trickler WJ,Miller DW

更新日期：2004-04-01 00:00:00

abstract：:A simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...

journal_title：Journal of pharmaceutical sciences

authors： El-Tahtawy A,Harrison F,Zirkelbach JF,Jackson AJ

更新日期：2012-11-01 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：:The purpose of the study was to characterize mucosal attachment of a cationized model protein, bovine serum albumin (BSA), onto the various fractions of colonic crypts epithelium in the rat. BSA was labeled with fluorescein isothiocyanate (FITC) and its surface net electric charge was modified from negative to positiv...

journal_title：Journal of pharmaceutical sciences

authors： Blau S,Levin N,Schwartz B,Rubinstein A

更新日期：2001-10-01 00:00:00

abstract：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00