Novel methodology for predicting photogenotoxic risk of pharmaceutical substances based on reactive oxygen species (ROS) and DNA-binding assay.

abstract：:Stent implantation following angioplasty is the standard treatment of coronary artery disease necessitating interventional procedures. The use of stents as a platform for local drug delivery is a popular strategy to achieve local pharmacological treatment to the diseased artery. Drug eluting stents (DES) are now large...

journal_title：Journal of pharmaceutical sciences

authors： Sharkawi T,Cornhill F,Lafont A,Sabaria P,Vert M

更新日期：2007-11-01 00:00:00

abstract：:Baclofen immediate release mode of administration exhibit sharp plasma peaking that results in the emergence of side effects like hypotension. This research employs preformulation studies to design an optimum dosage form for baclofen to enhance therapeutic outcomes. These studies include partition coefficient and ex-v...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim M,Naguib YW,Sarhan HA,Abdelkader H

更新日期：2020-10-15 00:00:00

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：:Present study aims to improve efficiency and capacity of in vivo rat pharmacokinetic studies for rapid assessment of systemic exposure (AUC and C(max)) of new chemical entities. Plasma concentration-time profiles in rats from structurally diverse compounds were extracted from the Pfizer database. AUC(0-8) was calculat...

journal_title：Journal of pharmaceutical sciences

authors： Han HK,Sadagopan N,Reichard GA,Yapa U,Zhu T,Hubbel A,Johnson K,Brodfuehrer J

更新日期：2006-08-01 00:00:00

abstract：:Eleven quinazolinylformamidines and quinazolinediylbisformamidines were synthesized and investigated for antihypertensive activity in spontaneous hypertensive rats. Several compounds showed moderate antihypertensive activity at 100 mg/kg po. The same compounds were not hypotensive in the normotensive dog. ...

journal_title：Journal of pharmaceutical sciences

authors： Warren JD,Lang SA Jr,Chan PS,Marsico JW

更新日期：1978-10-01 00:00:00

abstract：:The quantitative analysis of a new pharmaceutically active amine hydrochloride is described. Samples are extracted with chloroform. A yellow amine-dye complex is formed by buffering a sample-bromthymol blue solution at pH 8.5 +/- 0.1 and subsequently extracted with chloroform. The complex is treated with 0.01 N NaOH t...

journal_title：Journal of pharmaceutical sciences

authors： Chang ZL,Papendick VE

更新日期：1976-10-01 00:00:00

abstract：:A sensitive high-performance liquid chromatographic (HPLC) assay for N-acetylcysteine in human plasma and urine has been developed. The method employs a prechromatographic stage to produce the dinitrophenyl derivative of N-acetylcysteine, which is chromatographed on a 5-microns C18 bonded reverse-phase column using an...

journal_title：Journal of pharmaceutical sciences

authors： Lewis PA,Woodward AJ,Maddock J

更新日期：1984-07-01 00:00:00

abstract：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...

journal_title：Journal of pharmaceutical sciences

authors： Sörgel F,Ettinger B,Benet LZ

更新日期：1986-02-01 00:00:00

abstract：:A tetrazole ring is often used in drug discovery as a replacement for the carboxylic acid group. Previous work indicates that compounds containing a tetrazole moiety show asymmetric permeability in Caco-2 cells characteristic of an efflux transporter substrate. The aim of this study is to determine which transporters ...

journal_title：Journal of pharmaceutical sciences

authors： Young AM,Audus KL,Proudfoot J,Yazdanian M

更新日期：2006-04-01 00:00:00

abstract：:In this contribution, we present an analysis of the main parameters influencing the efficiency of the (1)H → (13)C multiple-contact cross-polarization nuclear magnetic resonance (NMR) experiment in the context of solid pharmaceutical materials. Using the optimum experimental conditions, quantitative (13)C NMR spectra ...

journal_title：Journal of pharmaceutical sciences

authors： Saïdi F,Taulelle F,Martineau C

更新日期：2016-08-01 00:00:00

abstract：:The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

journal_title：Journal of pharmaceutical sciences

authors： Genina N,Hadi B,Löbmann K

更新日期：2018-01-01 00:00:00

abstract：:The molecular connectivity indexes of various aliphatic alcohols, ketones, ethers, and esters were used to describe structural features influencing chromatographic retention indexes. Good correlations were obtained within chemical classes for a particular stationary phase. ...

journal_title：Journal of pharmaceutical sciences

authors： Kier LB,Hall LH

更新日期：1979-01-01 00:00:00

abstract：:Solution pH and ionic strength (I) have complex effects on protein stability. We developed an experimental approach based on exploitation of the zwitterionic characteristic of amino acid molecules to probe the relative contribution from each. A variety of types of amino acid solutions were adopted to investigate the e...

journal_title：Journal of pharmaceutical sciences

authors： Zhou R,Nashine V,Palm T,Gandhi R,Adams M

更新日期：2014-10-01 00:00:00

abstract：:In this study, black phosphorus nanosheets (BPNSs) were incorporated into a hydrogel formed from dibenzaldehyde-functionalized polymer (DF-PEG) and polyaspartylhydrazide (PAHy) polymer to create an injectable and pH-sensitive DF-PEG-PAHy/BPNSs hydrogel, which can be used as a smart depot for synergistic chemo-photothe...

journal_title：Journal of pharmaceutical sciences

authors： Wu RS,Lin J,Xing YM,Dai ZL,Wang LW,Zhang XP

更新日期：2019-08-01 00:00:00

abstract：:Formulation pH has been reported to be responsible for the incidence of phlebitis. In this study, the effect of pH on injection phlebitis is investigated. Buffers of varying pHs were examined for their ability to produce phlebitis in rabbits. Thermal measurements as well as visual evaluations were used for phlebitis q...

journal_title：Journal of pharmaceutical sciences

authors： Simamora P,Pinsuwan S,Alvarez JM,Myrdal PB,Yalkowsky SH

更新日期：1995-04-01 00:00:00

abstract：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

journal_title：Journal of pharmaceutical sciences

authors： Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

更新日期：2014-05-01 00:00:00

abstract：:An HPLC method for the simultaneous determination of safrole (S), dihydrosafrole (DHS), and chloromethyldihydrosafrole (CM-DHS) in piperonyl butoxide, with fluorimetric detection and elution gradient, is described. Samples with internal standard (piperonyl isobutyrate) are adsorbed on silica cartridges, then eluted wi...

journal_title：Journal of pharmaceutical sciences

authors： Schreiber-Deturmeny EM,Pauli AM,Pastor JL

更新日期：1993-08-01 00:00:00

abstract：:The objectives of this work are to explore the pi-pi complexation of amitriptyline with pi electron-deficient aromatic rings and demonstrate the feasibility of pi-pi complexation for overdosed drug detoxification. Water-soluble oligochitosan was chemically modified with dinitrobenzenesulfonyl groups to induce selectiv...

journal_title：Journal of pharmaceutical sciences

authors： Lee DW,Flint J,Morey T,Dennis D,Partch R,Baney R

更新日期：2005-02-01 00:00:00

abstract：:The effects of the granule size and density on the drying rate kinetics of tablet granulations were studied using lactose and sulfathiazole granules prepared with acacia mucilage and providone solution. The drying rate kinetics consisted of three distinct phases of drying when the drying rate was platted against remai...

journal_title：Journal of pharmaceutical sciences

authors： Opankunle WO,Bhutani BR,Bhatia VN

更新日期：1975-06-01 00:00:00

abstract：:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of C...

journal_title：Journal of pharmaceutical sciences

authors： Adeleke OA,Choonara YE,Du Toit LC,Pillay V

更新日期：2014-04-01 00:00:00

abstract：:Although certain criteria have become recognized as being essential for a stable lyophilized formulation, the relative importance of different stability criteria has not been demonstrated quantitatively. This study uses multivariate statistical methods to determine the relative importance of certain formulation variab...

journal_title：Journal of pharmaceutical sciences

authors： Katayama DS,Kirchhoff CF,Elliott CM,Johnson RE,Borgmeyer J,Thiele BR,Zeng DL,Qi H,Ludwig JD,Manning MC

更新日期：2004-10-01 00:00:00

abstract：:A new synthesis is described for 10alpha-methoxy-delta8,9-lysergaldehyde involving the oxidation of elymoclavine with manganese dioxide in methanol. Lysergol and agroclavine provide no reaction under the same conditions. ...

journal_title：Journal of pharmaceutical sciences

authors： Choong TC,Thompson BL,Shough HR

更新日期：1977-09-01 00:00:00

abstract：:The effect of caffeine on the absorption of ergotamine from the rat small intestine was studied. The results of a series of experiments showed that caffeine significantly enhanced absorption of ergotamine from solutions of pH 5.0 when both substances were in solution and when an intact blood supply was either absent (...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Drehsen G,Pitman IH

更新日期：1981-06-01 00:00:00

abstract：:The application of raster image correlation spectroscopy (RICS) as a tool for the characterisation of protein diffusion was assessed using a model protein, bovine serum albumin (BSA), as a function of formulation and denaturing conditions. RICS results were also validated against dynamic light scattering and fluoresce...

journal_title：Journal of pharmaceutical sciences

authors： Hamrang Z,Pluen A,Zindy E,Clarke D

更新日期：2012-06-01 00:00:00

abstract：:Nicotine is absorbed from the lungs into the systemic circulation during cigarette smoking. However, there is little information concerning the transport mechanism of nicotine in alveolar epithelial cells. In this study, we characterized the uptake of nicotine in rat primary cultured type II (TII) and transdifferentia...

journal_title：Journal of pharmaceutical sciences

authors： Takano M,Nagahiro M,Yumoto R

更新日期：2016-02-01 00:00:00

abstract：:Drying is a common pharmaceutical process, whose potential to modify the final drug and/or dosage form properties is often underestimated. In the present study, pellets consisting of the matrix former calcium stearate (CaSt) incorporating the active pharmaceutical ingredient ibuprofen were prepared via wet extrusion a...

journal_title：Journal of pharmaceutical sciences

authors： Schrank S,Kann B,Windbergs M,Glasser BJ,Zimmer A,Khinast J,Roblegg E

更新日期：2013-11-01 00:00:00

abstract：:Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

journal_title：Journal of pharmaceutical sciences

authors： Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

更新日期：2010-09-01 00:00:00

abstract：:The wettability of the (001), (100), and (011) crystallographic facets of macroscopic aspirin crystals has been experimentally investigated using a sessile drop contact angle (theta) method. theta for a nonpolar liquid was very similar for all three facets, though significant theta differences were observed for three ...

journal_title：Journal of pharmaceutical sciences

authors： Heng JY,Bismarck A,Lee AF,Wilson K,Williams DR

更新日期：2007-08-01 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：: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