Fluconazole Represses Cytochrome P450 1B1 and Its Associated Arachidonic Acid Metabolites in the Heart and Protects Against Angiotensin II-Induced Cardiac Hypertrophy.

abstract：:Dabrafenib is a small-molecule inhibitor of BRAF kinase activity that is currently being developed for the treatment of BRAF V600 mutation-positive melanoma. This clinical, open-label, two-cohort (n = 14 per cohort), randomized study was designed to evaluate the effect of drug substance particle size, and food on the ...

journal_title：Journal of pharmaceutical sciences

authors： Ouellet D,Grossmann KF,Limentani G,Nebot N,Lan K,Knowles L,Gordon MS,Sharma S,Infante JR,Lorusso PM,Pande G,Krachey EC,Blackman SC,Carson SW

更新日期：2013-09-01 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：:Homologous series of L-methionine alkyl ester hydrochlorides and tosylates were synthesized and evaluated for in vitro growth inhibitory activity in Meth A sarcoma. Cytotoxicity, as determined by [3H]thymidine incorporation, was found to be directly proportional to alkyl chain length and surface tension lowering activ...

journal_title：Journal of pharmaceutical sciences

authors： Clement MA,Chapman JM,Roberts J

更新日期：1989-06-01 00:00:00

abstract：:An electron-capture GLC method was developed for measuring pindolol in human plasma and urine. The unchanged drug was extracted with benzene from alkalinized plasma or urine using propranolol as the internal standard. Both compounds subsequently were back-extracted into 0.1 M HCl and then into benzene. After evaporati...

journal_title：Journal of pharmaceutical sciences

authors： Guerret M,Lavene D,Kiechel JR

更新日期：1980-10-01 00:00:00

abstract：:The degradation kinetics of phentolamine hydrochloride in aqueous solution over a pH range of 1.2 to 7.2 and its stability in propylene glycol- or polyethylene glycol 400-based solutions were investigated. The observed rate constants were shown to follow apparent first-order kinetics in all cases. The pKa determinatio...

journal_title：Journal of pharmaceutical sciences

authors： Wang DP,Tu YH,Allen LV Jr

更新日期：1988-11-01 00:00:00

abstract：:A crude chloroform-soluble fraction of the ethanol extract of the leaves of Bursera klugii showed activity against two test systems, the P-388 lymphocytic leukemia (3PS) and the human epidermoid carcinoma of the nasopharynx (9KB). The PS activity was due to two constituents, sapelins A and B. ...

journal_title：Journal of pharmaceutical sciences

authors： Jolad SD,Wiedhopf RM,Cole JR

更新日期：1977-06-01 00:00:00

abstract：:This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...

journal_title：Journal of pharmaceutical sciences

authors： Connolly BD,Le L,Patapoff TW,Cromwell MEM,Moore JMR,Lam P

更新日期：2015-12-01 00:00:00

abstract：:Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

journal_title：Journal of pharmaceutical sciences

authors： Borodkin S,Tucker FE

更新日期：1975-08-01 00:00:00

abstract：:Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to powders in a mixer. It is essential to understand the effect of powder substrate on foam drainage and half-life, which are relevant to nucleation and agglomeration during foam granulation. Hydroxypropyl methylce...

journal_title：Journal of pharmaceutical sciences

authors： Koo OM,Ji J,Li J

更新日期：2012-04-01 00:00:00

abstract：:The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...

journal_title：Journal of pharmaceutical sciences

authors： Brewster ME,Anderson WR,Estes KS,Bodor N

更新日期：1991-04-01 00:00:00

abstract：:The purpose of this paper was to investigate the relaxation behavior of amorphous hesperetin (HRN), using dielectric spectroscopy, and assessment of its crystallization kinetics above glass transition temperature (Tg ). Amorphous HRN exhibited both local (β-) and global (α-) relaxations. β-Relaxation was observed belo...

journal_title：Journal of pharmaceutical sciences

authors： Shete G,Khomane KS,Bansal AK

更新日期：2014-01-01 00:00:00

abstract：:Although inaccurate true density affects analysis of powder compaction data, such effects have not been systematically evaluated in the literature. This work is aimed at quantitatively evaluating effects of inaccurate true density on tableting data analysis using the Ryshkewitch equation, sigma = sigma0 e - bepsilon, ...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC

更新日期：2005-09-01 00:00:00

abstract：:A method is presented for encapsulating high molecular weight biological materials such as viral antigen, concanavalin A, and other proteins with cellulose acetate phthalate. The method is simple, inexpensive, and rapid; the process takes approximately 15 min. Capsules generated by this method are produced as microsph...

journal_title：Journal of pharmaceutical sciences

authors： Maharaj I,Nairn JG,Campbell JB

更新日期：1984-01-01 00:00:00

abstract：:We investigate the presence of a surface species for the active pharmaceutical ingredient (API) AZD9496 with dynamic nuclear polarization surface enhanced nuclear spectroscopy (DNP SENS). We show that using DNP we can elucidate the presence of an amorphous form of the API at the surface of crystalline particles of the...

journal_title：Journal of pharmaceutical sciences

authors： Viger-Gravel J,Pinon AC,Björgvinsdóttir S,Skantze U,Svensk Ankarberg A,Von Corswant C,Schantz S,Emsley L

更新日期：2021-01-05 00:00:00

abstract：:The pharmacokinetics of sulfisoxazole and sulfanilamide were studied in control rats and in rats treated for 5 days with a daily 100 mg/kg ip dose of phenobarbital. These drugs represent the organic anionic and nonionized drugs, respectively, whose nonmicrosomal enzymatic metabolisms were unstimulated by phenobarbital...

journal_title：Journal of pharmaceutical sciences

authors： Nagwekar JB,Kundu S

更新日期：1982-04-01 00:00:00

abstract：:Dogs were used to examine the effect of elevated gastric pH on the absorption of controlled-released theophylline dosage forms with pH-dependent dissolution. In vitro studies showed that a controlled-release theophylline tablet dissolved more rapidly if it was initially exposed to an acidic media. In contrast, a contr...

journal_title：Journal of pharmaceutical sciences

authors： Vashi VI,Meyer MC

更新日期：1988-09-01 00:00:00

abstract：:Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...

journal_title：Journal of pharmaceutical sciences

authors： Sethi ML

更新日期：1985-08-01 00:00:00

abstract：:The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

journal_title：Journal of pharmaceutical sciences

authors： Clausen AE,Bernkop-Schnürch A

更新日期：2000-10-01 00:00:00

abstract：:The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volu...

journal_title：Journal of pharmaceutical sciences

authors： Yap PS,Fung HL

更新日期：1978-04-01 00:00:00

abstract：:The purpose of the present study was to clarify the expression levels of transporter proteins in human lung tissue and to analyze regional and interindividual differences in primary cultured epithelial cells. Organic cation/carnitine tranporter 1 (OCTN1) protein expression was highest (2.08 ± 1.19 fmol/μg protein) in ...

journal_title：Journal of pharmaceutical sciences

authors： Sakamoto A,Matsumaru T,Yamamura N,Uchida Y,Tachikawa M,Ohtsuki S,Terasaki T

更新日期：2013-09-01 00:00:00

abstract：:The P-glycoprotein (Pgp), a drug efflux pump, is expressed in intestinal epithelial cells, where it constitutes a barrier against xenobiotics. In inflammatory bowel disease, a dysregulation in the production of tumor necrosis factor (TNF)alpha and interferon (IFN)gamma, and an alteration of Pgp expression and activity...

journal_title：Journal of pharmaceutical sciences

authors： Belliard AM,Lacour B,Farinotti R,Leroy C

更新日期：2004-06-01 00:00:00

abstract：:Specifically tailored amino acid-based formulations were previously shown to have a high potential to avoid stress-mediated degradation of complex molecules such as monoclonal antibodies and viral vectors. By using adenovirus 5 (Ad5) as a model, we studied whether such formulations may also efficiently protect viral v...

journal_title：Journal of pharmaceutical sciences

authors： Reinauer EB,Grosso SS,Henz SR,Rabas JA,Rodenstein C,Altrichter J,Scholz M,Kemter KF

更新日期：2020-01-01 00:00:00

abstract：:Over the past few decades alternate routes of administration have gained significant momentum and attention, to complement approved drug products, or enable those that cannot be delivered by the oral or parenteral route. Intranasal, buccal/sublingual, pulmonary, and transdermal routes being the most promising non-inva...

journal_title：Journal of pharmaceutical sciences

authors： Mathias NR,Hussain MA

更新日期：2010-01-01 00:00:00

abstract：:Microparticles are of considerable interest for drug delivery, vaccination and diagnostic imaging. In order to obtain microparticles with long circulation times, or to provide the prerequisite for tissue specific targeting through decoration with suitable ligands, their surfaces need to be modified such that they beco...

journal_title：Journal of pharmaceutical sciences

authors： Wattendorf U,Merkle HP

更新日期：2008-11-01 00:00:00

abstract：:Near-infrared spectroscopy was used to monitor the phase conversion for two solvatomorphs of caffeine, an anhydrous form and a nonstoichiometric hydrate, as a function of time, temperature, and relative humidity. The transformation kinetics between these caffeine forms was determined to increase with temperature. The ...

journal_title：Journal of pharmaceutical sciences

authors： Krzyzaniak JF,Williams GR,Ni N

更新日期：2007-05-01 00:00:00

abstract：:The goal was to evaluate the effects of acidity, expressed as the Hammett acidity function, on chemical reactivity in freeze-dried materials (lyophiles). Dextran-sucrose-citrate and polyvinyl pyrrolidone (PVP)-sucrose-citrate aqueous solutions, adjusted to pH values of 2.6, 2.8, and 3.0 were freeze dried, and characte...

journal_title：Journal of pharmaceutical sciences

authors： Chatterjee K,Shalaev EY,Suryanarayanan R,Govindarajan R

更新日期：2008-01-01 00:00:00

abstract：:An HPLC methodology is described which enables the quantitation of thiothixene (N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthe ne-2- sulfonamide) in bulk drug, finished product, and dissolution samples using a single analytical column (SiAl: a mixture of silica and alumina). The Z (cis) and the less...

journal_title：Journal of pharmaceutical sciences

authors： Severin G

更新日期：1987-03-01 00:00:00

abstract：:A highly sensitive and specific electron-capture GLC assay capable of detecting picogram quantities of metoclopramide, a procaine derivative, in biological fluids was developed. This assay consisted of extracting metoclopramide from an alkalinized aqueous layer into benzene. A portion of the organic phase was derivati...

journal_title：Journal of pharmaceutical sciences

authors： Tam YK,Axelson JE

更新日期：1978-08-01 00:00:00

abstract：:1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal ...

journal_title：Journal of pharmaceutical sciences

authors： Amlaiky N,Leclerc G

更新日期：1985-10-01 00:00:00

abstract：:The pharmacokinetics of atropine in three healthy male volunteers after intravenous administration of 1.35 and 2.15 mg of the drug was determined. Pharmacodynamic effects of atropine were measured simultaneously. All the data were fitted to a novel integrated kinetic-dynamic model. Plasma concentrations of atropine an...

journal_title：Journal of pharmaceutical sciences

authors： Hinderling PH,Gundert-Remy U,Schmidlin O

更新日期：1985-07-01 00:00:00