A physiologically based pharmacokinetic model of zidovudine (AZT) in the mouse: model development and scale-up to humans.

abstract：:The aim of this work is to determine if a stability testing protocol based on the correlations between crystallization onset and relaxation time above the glass transition temperature (T(g)) can be used to predict the crystallization onsets in amorphous pharmaceutical systems well below their T(g). This procedure assu...

journal_title：Journal of pharmaceutical sciences

authors： Caron V,Bhugra C,Pikal MJ

更新日期：2010-09-01 00:00:00

abstract：:In pharmaceutical development alternative drug delivery modalities are being increasingly employed. One example is an implant, which achieves gradual drug release in patients over a period of many months or years. Due to the complexity of these long-acting formulations, advanced physical characterization methods are d...

journal_title：Journal of pharmaceutical sciences

authors： Skomski D,Liu Z,Su Y,John CT,Doty A,Forster SP,Teller R,Barrett SE,Xu W

更新日期：2020-09-01 00:00:00

abstract：:Despite being a major breakthrough in multiple myeloma therapy, carfilzomib (CFZ, a second-generation proteasome inhibitor drug) has been largely ineffective against solid cancer, possibly due to its pharmacokinetic drawbacks including metabolic instability. Recently, quinic acid (QA, a low-affinity ligand of selectin...

journal_title：Journal of pharmaceutical sciences

authors： Jun Y,Xu J,Kim H,Park JE,Jeong YS,Min JS,Yoon N,Choi JY,Yoo J,Bae SK,Chung SJ,Yeo Y,Lee W

更新日期：2020-04-01 00:00:00

abstract：:The relationship between the lone tryptophan residue at position 214 and drug binding sites (Sites I and II) in human serum albumin (HSA) was studied by fluorescence energy transfer. The distance between the lone tryptophan residue and ligands bound to HSA was estimated by Förster's equation, taking into consideration...

journal_title：Journal of pharmaceutical sciences

authors： Kasai S,Horie T,Mizuma T,Awazu S

更新日期：1987-05-01 00:00:00

abstract：:3,6-Diformyl- and 3,6-dipropanoylmorphine and 6-formyl- and 6-propanoylmorphine were prepared to obtain longer acting, heroin-like compounds. The 6-acylated compounds were more potent than heroin subcutaneously and were orally effective, and their duration of action was at least two to three times greater than that of...

journal_title：Journal of pharmaceutical sciences

authors： May EL,Jacobson AE

更新日期：1977-02-01 00:00:00

abstract：:The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...

journal_title：Journal of pharmaceutical sciences

authors： Nagy ZK,Balogh A,Drávavölgyi G,Ferguson J,Pataki H,Vajna B,Marosi G

更新日期：2013-02-01 00:00:00

abstract：:A multichannel continuous-flow apparatus for dissolution rate measurements is described. Typical data are presented to demonstrate its utility for studies with bulk drug powders as well as with tablets and capsules without any change of setup. Procedures are given for the preparation of powder samples for dissolution ...

journal_title：Journal of pharmaceutical sciences

authors： Cakiryildiz C,Mehta PJ,Rahmen W,Schoenleber D

更新日期：1975-10-01 00:00:00

abstract：:The purpose of this study was to examine the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on P-glycoprotein (P-gp)-mediated transport in LLC-GA5-COL150, a transfectant cell line of a porcine kidney epithelial cell line LLC-PK1 with human MDR1 cDNA. Ethanol extract obtained from...

journal_title：Journal of pharmaceutical sciences

authors： Patanasethanont D,Nagai J,Yumoto R,Murakami T,Sutthanut K,Sripanidkulchai BO,Yenjai C,Takano M

更新日期：2007-01-01 00:00:00

abstract：:The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

更新日期：1992-02-01 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：:P,P-Bis(1-aziridinyl)-N-1-adamantylphosphinic amide displayed oncolytic activity against intracerebral and intraperitoneal L-1210 leukemia. Administration of the isotope-labeled compound to rats shows 32P distribution to the brain. ...

journal_title：Journal of pharmaceutical sciences

authors： Cates LA,Cramer MB

更新日期：1976-03-01 00:00:00

abstract：:Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

journal_title：Journal of pharmaceutical sciences

authors： Loftsson T,Bodor N

更新日期：1981-07-01 00:00:00

abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

journal_title：Journal of pharmaceutical sciences

authors： Tu YH,Allen LV Jr

更新日期：1989-03-01 00:00:00

abstract：:Recently, our laboratory reported that intravenous immunoglobulin (IVIG) treatment increased antiplatelet antibody (7E3) clearance in a rat model of immune thrombocytopenic purpura (ITP). However, due to the multifaceted nature of IVIG therapy, the contribution of this increase in antiplatelet antibody clearance to th...

journal_title：Journal of pharmaceutical sciences

authors： Hansen RJ,Balthasar JP

更新日期：2003-06-01 00:00:00

abstract：:Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

journal_title：Journal of pharmaceutical sciences

authors： Segarra I,Movshin DA,Zarif L

更新日期：2002-08-01 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：:Taxanes such as paclitaxel (Taxol) and docetaxel (Taxotere) are promising agents for use against ovarian cancer and other malignancies. Recently, SB-T-1011, a semisynthetic taxane, has been prepared from 14-hydroxy-10-deacetylbaccatin III. SB-T-1011 shows similar or greater in vitro cytostatic activity than paclitaxel...

journal_title：Journal of pharmaceutical sciences

authors： Sharma A,Straubinger RM,Ojima I,Bernacki RJ

更新日期：1995-12-01 00:00:00

abstract：:A simple and sensitive method is reported for the quantitative determination of the bronchodilator tulobuterol in human serum. Tulobuterol and an internal standard were extracted from alkalinized serum with ether and then back-extracted into dilute hydrochloric acid. After alkalinization and extraction of the aqueous ...

journal_title：Journal of pharmaceutical sciences

authors： Matsumura K,Kubo O,Sakashita T,Kato H,Watanabe K,Hirobe M

更新日期：1983-05-01 00:00:00

abstract：:Reactive high gravity controlled precipitation (HGCP) was carried out to produce salbutamol sulphate (SS) particles suitable for inhalation. Aqueous solutions of free salbutamol base and sulphuric acid were mixed intensely inside a HGCP reactor to form the particles. Spray drying was employed to obtain dry powders. Ph...

journal_title：Journal of pharmaceutical sciences

authors： Hu T,Chiou H,Chan HK,Chen JF,Yun J

更新日期：2008-02-01 00:00:00

abstract：:A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B

更新日期：1985-10-01 00:00:00

abstract：:The aim of this study was to synthetize cocrystals of nateglinide, an antidiabetic agent of biopharmaceutics classification system Class IIa, as a strategy to improve both the solubility and the dissolution rate of the drug. Benzamide was selected by a screening procedure as a suitable coformer, and binary mixtures wi...

journal_title：Journal of pharmaceutical sciences

authors： Bruni G,Maggi L,Mustarelli P,Sakaj M,Friuli V,Ferrara C,Berbenni V,Girella A,Milanese C,Marini A

更新日期：2019-04-01 00:00:00

abstract：:The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

journal_title：Journal of pharmaceutical sciences

authors： Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

更新日期：2019-04-01 00:00:00

abstract：:The crystal structure of zolpidem hemitartrate hemihydrate (I, Form E) has been solved from high-resolution laboratory powder diffraction data. It crystallizes in the orthorhombic P2(1)2(1)2(1) space group with a = 22.4664(6) A, b = 26.0420(7) A, and c = 7.4391(1) A. Protonation of zolpidem molecules could not be unam...

journal_title：Journal of pharmaceutical sciences

authors： Halasz I,Dinnebier RE

更新日期：2010-02-01 00:00:00

abstract：:The viscosity and surface tension of systems containing small amounts of salicylic acid in aqueous solutions of cetrimide were determined. An abrupt increase in viscosity was observed, and the molar ratio of salicylic acid to certrimide at which this viscosity increase occurred was 1:2. The surface tension of these sy...

journal_title：Journal of pharmaceutical sciences

authors： Wan LS

更新日期：1977-12-01 00:00:00

abstract：:The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

journal_title：Journal of pharmaceutical sciences

authors： Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

更新日期：2004-06-01 00:00:00

abstract：:The kinetic profile for the decomposition of ditiocarb sodium salt in aqueous solution was achieved with UV-visible absorption spectrometry. The kinetic profile indicates that the decomposition reaction is hydrogen ion-catalyzed over the entire 4-10 pH range and enables the determination of the value of the acid-base ...

journal_title：Journal of pharmaceutical sciences

authors： Martens T,Langevin-Bermond D,Fleury MB

更新日期：1993-04-01 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

abstract：:Solution preparation is the first unit operation of the manufacturing process for spray-dried solid dispersions. Visual inspection and offline high-performance liquid chromatography analysis are routinely used to assess the solution preparation end point as well as the final solution composition. However, the accuracy...

journal_title：Journal of pharmaceutical sciences

authors： Lee YC,Zhou G,Ikeda C,Chouzouri G,Howell L

更新日期：2019-03-01 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：:The possibility tht metronidazole exerts several of its biological actions via interaction with important metal ions was investigated. NMR spectroscopy and polarography (ac) were used to test for any interaction, to locate the probable sites for complexation, and to determine the molecular stoichiometry of any complex...

journal_title：Journal of pharmaceutical sciences

authors： Chien YW,Lambert HJ,Sanvordeker DR

更新日期：1975-06-01 00:00:00