Degradation of trimethoprim.

abstract：:5-Methyl-2-[(4-methyl-2-nitrophenyl)amino]-3-thiophenecarbonitrile is an example of conformational and color polymorphism. The compound crystallizes in red (R), dark red (DR), light red (LR), and orange (O) modifications. There are two specific goals for this study. One is to characterize the complex thermodynamic rel...

journal_title：Journal of pharmaceutical sciences

authors： He X,Griesser UJ,Stowell JG,Borchardt TB,Byrn SR

更新日期：2001-03-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:Subcutaneous injection allows for self-administration of monoclonal antibodies using prefilled syringes, autoinjectors, and on-body injector devices. However, subcutaneous injections are typically limited to 1 mL due to concerns of injection pain from volume, viscosity, and formulation characteristics. Back pressure c...

journal_title：Journal of pharmaceutical sciences

authors： Doughty DV,Clawson CZ,Lambert W,Subramony JA

更新日期：2016-07-01 00:00:00

abstract：:Controlled-release delivery of 6-beta-naltrexol (NTXOL), the major active metabolite of naltrexone, via a transdermal patch is desirable for treatment of alcoholism. Unfortunately, NTXOL does not diffuse across skin at a therapeutic rate. Therefore, the focus of this study was to evaluate microneedle (MN) skin permeat...

journal_title：Journal of pharmaceutical sciences

authors： Banks SL,Pinninti RR,Gill HS,Paudel KS,Crooks PA,Brogden NK,Prausnitz MR,Stinchcomb AL

更新日期：2010-07-01 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：:As reported in the previous commentary (Ishii-Watabe et al., J Pharm Sci 2017), the Japanese biopharmaceutical research group is promoting collaborative multilaboratory studies to evaluate and standardize new methodologies for biopharmaceutical characterization and quality control. We have conducted the studies and he...

journal_title：Journal of pharmaceutical sciences

authors： Ishii-Watabe A,Shibata H,Suetomo H,Ikeda Y,Telikepalli S,Kiyoshi M,Hayashi Y,Muto T,Tanaka Y,Ueda S,Iwura T,Saitoh S,Aoyama M,Harazono A,Hyuga M,Goda Y,Torisu T,Uchiyama S

更新日期：2020-05-01 00:00:00

abstract：:The reaction of chlorthalidone with methanol to give the corresponding methyl ether was investigated. The kinetics are pseudo-first-order in chlorthalidone, but the observed pseudo-first-order rate constants show an unexpected dependence on the initial chlorthalidone concentration, attributable to the presence of trac...

journal_title：Journal of pharmaceutical sciences

authors： Pandit NK,Hinderliter JS

更新日期：1985-08-01 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：: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：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:Bacmecillinam is an amdinocillin prodrug designed to be easily hydrolyzed in biological materials, so special procedures were developed for the collection of blood specimens. Whole blood was collected in tubes containing bacampicillin as an adsorption inhibitor and kept at -70 degrees; the extracting solvent, hexane-m...

journal_title：Journal of pharmaceutical sciences

authors： Westerlund D,Pettersson B,Carlqvist J

更新日期：1982-10-01 00:00:00

abstract：:Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...

journal_title：Journal of pharmaceutical sciences

authors： Huang SL,Hamilton AJ,Nagaraj A,Tiukinhoy SD,Klegerman ME,McPherson DD,Macdonald RC

更新日期：2001-12-01 00:00:00

abstract：:The development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...

journal_title：Journal of pharmaceutical sciences

authors： Aboul-Enein N,Sam J

更新日期：1976-09-01 00:00:00

abstract：:Resveratrol trimethyl ether (trans-3,5,4'-trimethoxystilbene, RTE) is a naturally occurring and pharmacologically active resveratrol derivative. To evaluate its suitability as a drug candidate, a pharmacokinetic study was carried out in Sprague-Dawley rats with the emphasis to identify the impact of aqueous solubility...

journal_title：Journal of pharmaceutical sciences

authors： Lin HS,Ho PC

更新日期：2011-10-01 00:00:00

abstract：:A computational approach which concomitantly determines the capacity-limited rate constants of parent drug elimination and metabolite formation is presented. The approach applies both the presently derived total excretory recovery versus dose relationships of the metabolite and the AUC versus dose relationships of the...

journal_title：Journal of pharmaceutical sciences

authors： Chow AT,Jusko WJ

更新日期：1990-10-01 00:00:00

abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...

journal_title：Journal of pharmaceutical sciences

authors： Horikiri Y,Suzuki T,Mizobe M

更新日期：1998-03-01 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：:Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ. Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were...

journal_title：Journal of pharmaceutical sciences

authors： Tsuji A,Miyamoto E,Kubo O,Yamana T

更新日期：1979-07-01 00:00:00

abstract：:Although displacement from plasma protein binding (dPB) is usually of little clinical significance, it should be taken into account when interpreting changes in total plasma concentrations of drugs subject to metabolically based drug-drug interactions (mDDI). The aim of this study was to develop an approach to predict...

journal_title：Journal of pharmaceutical sciences

authors： Christensen H,Baker M,Tucker GT,Rostami-Hodjegan A

更新日期：2006-12-01 00:00:00

abstract：:The antimalarial endoperoxides, such as artemisinin, are postulated to exert their potent parasiticidal activity via the formation of reactive intermediates in the iron-rich infected erythrocyte. The in vitro chemical reaction profile of putative endoperoxide antimalarials and ferrous iron is often qualitatively used ...

journal_title：Journal of pharmaceutical sciences

authors： Creek DJ,Chiu FC,Prankerd RJ,Charman SA,Charman WN

更新日期：2005-08-01 00:00:00

abstract：:Levetiracetam therapy is often associated with high levels of individual variation in the recommended dose required to achieve preferential treatment. Thus, a reliable and dynamic regulation system to accurately tailor dose is necessary. The main objective of this study is to explore and prepare a dose-flexible contro...

journal_title：Journal of pharmaceutical sciences

authors： Cui M,Li Y,Wang S,Chai Y,Lou J,Chen F,Li Q,Pan W,Ding P

更新日期：2019-02-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00

abstract：:A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the alpha,beta-unsaturated ...

journal_title：Journal of pharmaceutical sciences

authors： Dimmock JR,Sidhu KK,Chen M,Li J,Quail JW,Allen TM,Kao GY

更新日期：1994-06-01 00:00:00

abstract：:Experimental sulfadiazine tablets prepared by direct compression, using a commercially available direct compression tablet mass, were compared with experimental sulfadiazine tablets prepared by fluidized-bed granulation and commercially available sulfadiazine tablets USP. The values for friability and the time require...

journal_title：Journal of pharmaceutical sciences

authors： Ritschel WA,Erni W

更新日期：1977-10-01 00:00:00

abstract：:Virtually all biological variables, including those affected by drugs, are subject to adaptive self regulation. In the description of the pharmacodynamics (PD) of drugs, it may be necessary to consider the endogenous control system (ECS) as an integral part of the PD. A PDECS model based on system analysis principles ...

journal_title：Journal of pharmaceutical sciences

authors： Veng-Pedersen P,Modi NB

更新日期：1993-03-01 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：:At low protein concentrations (c2), non-native protein aggregation rates are known to be sensitive to changes in conformational stability and "weak" or "colloidal" protein-protein interactions. Protein-protein interactions are also known to be strong functions of c2. In the present work, protein-protein interactions a...

journal_title：Journal of pharmaceutical sciences

authors： Ghosh R,Calero-Rubio C,Saluja A,Roberts CJ

更新日期：2016-03-01 00:00:00

abstract：:The application of low-frequency ultrasound enhances drug transport through the skin, a phenomenon referred to as low-frequency sonophoresis. This enhancement is mediated through cavitation, the formation and collapse of gaseous bubbles. We hypothesized that the efficacy of low-frequency sonophoresis can be significan...

journal_title：Journal of pharmaceutical sciences

authors： Terahara T,Mitragotri S,Langer R

更新日期：2002-03-01 00:00:00

abstract：:Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...

journal_title：Journal of pharmaceutical sciences

authors： Grant J,Blicker M,Piquette-Miller M,Allen C

更新日期：2005-07-01 00:00:00

abstract：:The degradation of batanopride hydrochloride, an investigational antiemetic drug, was studied in aqueous buffer solutions (pH 2-10; ionic strength, 0.5; 56 degrees C) in an attempt to improve drug stability for parenteral administration. Degradation occurs by two different mechanisms depending on the pH of the solutio...

journal_title：Journal of pharmaceutical sciences

authors： Nassar MN,House CA,Agharkar SN

更新日期：1992-11-01 00:00:00