Pharmacokinetic studies of pentylenetetrazol in dogs.

abstract：:Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with eth...

journal_title：Journal of pharmaceutical sciences

authors： Varin F,Cubeddu LX,Powell JR

更新日期：1986-12-01 00:00:00

abstract：:The insidious nature of Zika virus (ZIKV) infections can have a devastating consequence for fetal development. Recent reports have highlighted that chloroquine (CQ) is capable of inhibiting ZIKV endocytosis in brain cells. We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an...

journal_title：Journal of pharmaceutical sciences

authors： Olafuyi O,Badhan RKS

更新日期：2019-01-01 00:00:00

abstract：:Alpha-Hydroxyaryl ketones such as 2-hydroxypropiophenone and 1-(2,4-difluorophenyl)-2-hydroxy-1-propanone, the key intermediates in the preparation of antifungal agents, decompose into oxidized, rearranged, and condensed products. These products were isolated and characterized. The possible mechanisms for the formatio...

journal_title：Journal of pharmaceutical sciences

authors： Gala D,Puar MS,Das PR,Kugelman M,DiBenedetto DJ

更新日期：1992-12-01 00:00:00

abstract：:Aqueous wet massing of stable anhydrous theophylline (A) with polyvinylpyrrolidone (PVP) resulted in its complete transformation to theophylline monohydrate (M). Drying at 45 degrees C, resulted in the formation of metastable anhydrous theophylline (A*) which then transformed to A. PVP, a known crystallization inhibit...

journal_title：Journal of pharmaceutical sciences

authors： Tantry JS,Tank J,Suryanarayanan R

更新日期：2007-05-01 00:00:00

abstract：:The dependency of metformin in vivo disposition on the rate and extent of dissolution was studied. The analysis includes the use of fundamental principles of drug input, permeability, and intestinal transit time within the framework of a compartmental absorption transit model to predict key pharmacokinetic (PK) parame...

journal_title：Journal of pharmaceutical sciences

authors： Crison JR,Timmins P,Keung A,Upreti VV,Boulton DW,Scheer BJ

更新日期：2012-05-01 00:00:00

abstract：:Contraceptive natural steroids, such as progesterone and estradiol, are ineffective when administered orally because of extensive metabolism in the gastrointestinal (GI) tract during absorption and first-pass metabolism. Consequently, highly potent and potentially harmful synthetic steroids are now being used in oral...

journal_title：Journal of pharmaceutical sciences

authors： Hussain AA,Hirai S,Bawarshi R

更新日期：1981-04-01 00:00:00

abstract：:Poly(methyl [1-14C]methacrylate) nanoparticles were injected subcutaneously into rats. Almost all of the radioactivity stayed at the injection site. After an initial urinary and fecal excretion of approximately 1% of the administered dose per day, the rate of elimination dropped to a low level (approximately 0.005%/da...

journal_title：Journal of pharmaceutical sciences

authors： Kreuter J,Nefzger M,Liehl E,Czok R,Voges R

更新日期：1983-10-01 00:00:00

abstract：:The pharmacokinetics of fluorouracil were examined after single 250-mg iv doses and 500-mg oral doses to female patients with breast cancer. In five patients who received intravenous fluorouracil, the mean peak plasma level of unchanged drug was 13.4 microgram/ml, the elimination half-life was 6.3 min, and the plasma ...

journal_title：Journal of pharmaceutical sciences

authors： Phillips TA,Howell A,Grieve RJ,Welling PG

更新日期：1980-12-01 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...

journal_title：Journal of pharmaceutical sciences

authors： Salmona M,Lakszner K,Fanelli R,Saronio C,Bianchi R,Mussini E

更新日期：1975-09-01 00:00:00

abstract：:The purpose of the present study was to develop a physiologically based pharmacokinetic model for dextromethorphan (DEX) and its metabolites in extensive and poor metabolizers. The model was used to study the influence of dissolution rates on the sensitivity of maximum plasma concentration and area under the concentra...

journal_title：Journal of pharmaceutical sciences

authors： Bolger MB,Macwan JS,Sarfraz M,Almukainzi M,Löbenberg R

更新日期：2019-01-01 00:00:00

abstract：:Racemic and homochiral sodium ibuprofen were characterized by thermal analysis and powder X-ray diffractometry. The melting point phase diagram was constructed and thermodynamic calculation was performed. In contrast to racemic ibuprofen, which is a racemic compound, racemic sodium ibuprofen forms both a racemic congl...

journal_title：Journal of pharmaceutical sciences

authors： Zhang GG,Paspal SY,Suryanarayanan R,Grant DJ

更新日期：2003-07-01 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：: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：:The reaction kinetics of blue tetrazolium with selected arylhydrazines were investigated under pseudo-first-order conditions. The reaction rate constants were obtained at various temperatures, and the enthalpy (8.4-11.2 kcal/mole) and entropy (-38--45 eu) of activations were calculated. A Hammett plot yielded a straig...

journal_title：Journal of pharmaceutical sciences

authors： Biehl ER,Wooten R,Kenner CT,Graham RE

更新日期：1978-07-01 00:00:00

abstract：:A method of depicting dimensional illustrations of molecules in vacuo that are sensitive to small electronic perturbations was attempted. This method would be useful in determining the effects of either perturbing groups from other molecules or changes produced by the addition or modification of an existing atom or ch...

journal_title：Journal of pharmaceutical sciences

authors： Breon TL,Petersen H Jr,Paruta AN

更新日期：1978-01-01 00:00:00

abstract：:Porcine gelatins have been widely used as stabilizers of macromolecular based pharmaceuticals but the mechanism by which they stabilize has not been precisely established. Their variability and immunogenicity, however, make them less than ideal excipients. In this work, we take advantage of the availability of recombi...

journal_title：Journal of pharmaceutical sciences

authors： Thyagarajapuram N,Olsen D,Middaugh CR

更新日期：2007-12-01 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：:A confocal Raman microscopic technique was optimized to more efficiently detect amorphous-amorphous phase separation in freeze-dried protein formulations. A Renishaw Raman inVia confocal microscope was used to collect 100-200 μm line maps (2 μm step size) of freeze-dried protein-excipient formulations. At each point a...

journal_title：Journal of pharmaceutical sciences

authors： Forney-Stevens KM,Pelletier MJ,Shalaev EY,Pikal MJ,Bogner RH

更新日期：2014-09-01 00:00:00

abstract：:The relationship between the concentration of a drug and its pharmacologic effect is of central interest in pharmacodynamics. Various compartmental and noncompartmental methods have been proposed for elucidating this relationship when the plasma drug concentration and effects are both measured. Although the relationsh...

journal_title：Journal of pharmaceutical sciences

authors： Modi NB,Veng-Pedersen P

更新日期：1994-03-01 00:00:00

abstract：:Three series of 3,4,5-trisubstituted pyrazolesulfonylurea derivatives were prepared and evaluated as hypoglycemic agents. Preliminary biological testing revealed that the new compounds possess moderate hypoglycemic activity. ...

journal_title：Journal of pharmaceutical sciences

authors： Soliman R,Mokhtar H,Mohamed HF

更新日期：1983-09-01 00:00:00

abstract：:Hyperthermia (HT)-dependent cisplatin (CDDP) release and tumor CDDP level increase after the administration of thermosensitive, large unilamellar vesicles (LUVs: LUV-1 and LUV-2) and a thermosensitive, small unilamellar vesicle (SUV: SUV-1) were examined in comparison with those following administration of a non-therm...

journal_title：Journal of pharmaceutical sciences

authors： Iga K,Hamaguchi N,Igari Y,Ogawa Y,Toguchi H,Shimamoto T

更新日期：1991-06-01 00:00:00

abstract：:The mechanism of organic solvent evaporation during microencapsulation and its role during microsphere hardening has been investigated. Evaporation and encapsulation studies were carried out in a jacketed beaker, filled with aqueous hardening solution, which was maintained at constant temperature and constant stirring...

journal_title：Journal of pharmaceutical sciences

authors： Wang J,Schwendeman SP

更新日期：1999-10-01 00:00:00

abstract：:This whitepaper highlights current challenges and opportunities associated with continuous synthesis, workup, and crystallization of active pharmaceutical ingredients (drug substances). We describe the technologies and requirements at each stage and emphasize the different considerations for developing continuous proc...

journal_title：Journal of pharmaceutical sciences

authors： Baxendale IR,Braatz RD,Hodnett BK,Jensen KF,Johnson MD,Sharratt P,Sherlock JP,Florence AJ

更新日期：2015-03-01 00:00:00

abstract：:Platinum-based anticancer agents such as cisplatin and carboplatin are in widespread clinical use but associated with many side effects. Improving the delivery of cytotoxic platinum compounds may lead to reduced side effects and achieve greater efficacy at lower doses. Polymer-based therapeutics have been investigated...

journal_title：Journal of pharmaceutical sciences

authors： Haxton KJ,Burt HM

更新日期：2009-07-01 00:00:00

abstract：:The stereospecificity of the metabolic reduction of arylalkylketones was investigated. The ketones, propiophenone (I), phenyl-acetone (III), and 1-phenyl-1,2-propanedione (V) were reduced in vitro and in vivo in rats and rabbits to the corresponding alcohols, 1-phenyl-1-propanol (II), 1-phenyl-2-propanol (IV), and 1-p...

journal_title：Journal of pharmaceutical sciences

authors： Prelusky DB,Coutts RT,Pasutto FM

更新日期：1982-12-01 00:00:00

abstract：:A solution of selegiline hydrochloride reference standard, which contained no detectable impurities at the time of its preparation, was found by HPLC to contain a trace of a compound at the locus of methamphetamine when analyzed after 1 year. Heating selegiline solutions at pH 7 and 105 degrees C produced methamphetam...

journal_title：Journal of pharmaceutical sciences

authors： Chafetz L,Desai MP,Sukonik L

更新日期：1994-09-01 00:00:00

abstract：:The morphology of spray-dried particles composed of psicose and hydroxypropyl methylcellulose was modified by adding ammonium bicarbonate (ABC) to the solution. The surface structure of the particles was altered by immediate transformation of ABC to gaseous components during the spray drying. As a result, low-density ...

journal_title：Journal of pharmaceutical sciences

authors： Kawakami K,Hasegawa Y,Zhang S,Yoshihashi Y,Yonemochi E,Terada K

更新日期：2014-04-01 00:00:00

abstract：:Phenytoin (DPH) was delivered to the brain by a dihydropyridine in equilibrium pyridinium salt redox system, which was evaluated for anticonvulsant activity. Following iv injection of the lipophilic delivery system of DPH (2) to rats, concentrations of DPH were lower but sustained and, after 30 min, essentially the sa...

journal_title：Journal of pharmaceutical sciences

authors： Shek E,Murakami T,Nath C,Pop E,Bodor NS

更新日期：1989-10-01 00:00:00

abstract：:Evaluation of a multiplexed capillary electrophoresis (CE) method for pK(a) measurements of organic compounds, including low solubility compounds, is presented. The method is validated on a set of 105 diverse compounds, mostly drugs, and results are compared to literature values obtained from multiple references. Two ...

journal_title：Journal of pharmaceutical sciences

authors： Shalaeva M,Kenseth J,Lombardo F,Bastin A

更新日期：2008-07-01 00:00:00