Synthesis and binding to beta-adrenergic receptors of p-aminobenzyl analogues of practolol and atenolol.

abstract：:Polymethyl [1-14C]methacrylate nanoparticles were administered orally to bile cannulated rats. Ten to fifteen percent of the administered radioactivity was absorbed and found in the bile and urine. Within 48 h, 94-97% of the absorbed radioactivity had been eliminated from the body. After 8 d, the highest residual radi...

journal_title：Journal of pharmaceutical sciences

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

更新日期：1984-09-01 00:00:00

abstract：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...

journal_title：Journal of pharmaceutical sciences

authors： Maniar ML,Kalonia DS,Simonelli AP

更新日期：1991-08-01 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：:Biphenylalkyl monoesters of succinic and related acids represent a potent new class of cyclic AMP phosphodiesterase inhibitors. The biphenyl group is necessary for potent inhibition. The spatial relationship of the carboxyl and ester groups and alkyl chain length are important to inhibitory potency. ...

journal_title：Journal of pharmaceutical sciences

authors： Rogers ME,Boots SG,Boots MR

更新日期：1979-07-01 00:00:00

abstract：:The kinetic barrier against the transport of methyl and ethyl nicotinates across the water-isopropyl myristate interface has been studied as a function of temperature using a rotating diffusion cell. The temperature dependence of the interfacial transfer kinetics has enabled calculation of the thermodynamic parameters...

journal_title：Journal of pharmaceutical sciences

authors： Fleming R,Guy RH,Hadgraft J

更新日期：1983-02-01 00:00:00

abstract：:Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2016-09-01 00:00:00

abstract：:A procedure is described for TLC detection and differentiation of the butyrophenone-diphenylbutylpiperidine group and phenothiazine derivatives at the microgram level. A two-dimensional TLC method to separate butyrophenone and diphenylbutylpiperidine compounds is reported. A variety of possible detection reagents were...

journal_title：Journal of pharmaceutical sciences

authors： Pluym A

更新日期：1979-08-01 00:00:00

abstract：:A three-way crossover bioavailability study was performed using nine adult male volunteers with three different commercial prednisone tablets. Plasma samples were assayed for prednisolone, the active metabolite of prednisone, by a radioimmunoassay method. Statistical analysis showed significant differences in the rate...

journal_title：Journal of pharmaceutical sciences

authors： Sullivan TJ,Sakmar E,Albert KS,Blair DC,Wagner JG

更新日期：1975-10-01 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：:Acitretin, a retinoid for the treatment of severe psoriasis, exhibits extremely low aqueous solubility and high photosensitivity. This study investigated the effects of the complexation of acitretin with the respective hydroxypropyl-beta-cyclodextrin (HPBCD) and randomly substituted methyl-beta-cyclodextrin (RMBCD) on...

journal_title：Journal of pharmaceutical sciences

authors： Liu X,Lin HS,Thenmozhiyal JC,Chan SY,Ho PC

更新日期：2003-12-01 00:00:00

abstract：:We present a systematic evaluation of the Wajima superpositioning method to estimate the human intravenous (i.v.) pharmacokinetic (PK) profile based on a set of 54 marketed drugs with diverse structure and range of physicochemical properties. We illustrate the use of average of "best methods" for the prediction of cle...

journal_title：Journal of pharmaceutical sciences

authors： Lombardo F,Berellini G,Labonte LR,Liang G,Kim S

更新日期：2016-03-01 00:00:00

abstract：:We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...

journal_title：Journal of pharmaceutical sciences

authors： Brown LR,Edelman ER,Fischel-Ghodsian F,Langer R

更新日期：1996-12-01 00:00:00

abstract：:A model is presented for transdermal drug delivery from single-layered silicone matrix systems. The work is based on our previous results that, in particular, extend the well-known Higuchi model. Recently, we have introduced a numerical transient model describing matrix systems where the drug dissolution can be non-in...

journal_title：Journal of pharmaceutical sciences

authors： Snorradóttir BS,Jónsdóttir F,Sigurdsson ST,Másson M

更新日期：2014-08-01 00:00:00

abstract：:The purpose of the present study was to develop guidance toward rational choice of blenders and processing conditions to make robust and high performing adhesive mixtures for dry-powder inhalers and to develop quantitative experimental approaches for optimizing the process. Mixing behavior of carrier (LH100) and Astra...

journal_title：Journal of pharmaceutical sciences

authors： Sarkar S,Minatovicz B,Thalberg K,Chaudhuri B

更新日期：2017-01-01 00:00:00

abstract：:There has been a growing interest in predicting in vivo metabolic drug-drug interactions from in vitro systems. High-throughput screening methods aimed at assessing the potential of drug candidates for drug interactions are widely used in industry. However, at present, there is no consensus on methodologies that would...

journal_title：Journal of pharmaceutical sciences

authors： Yao C,Levy RH

更新日期：2002-09-01 00:00:00

abstract：:The deamidation of asparagine into aspartate and isoaspartate moieties is a major pathway for the chemical degradation of monoclonal antibodies (mAbs). It can affect the shelf life of a therapeutic antibody that is not formulated or stored appropriately. A new approach to detect deamidation using ion exchange chromato...

journal_title：Journal of pharmaceutical sciences

authors： Pace AL,Wong RL,Zhang YT,Kao YH,Wang YJ

更新日期：2013-06-01 00:00:00

abstract：:Some coated aspirin tablet formulations were evaluated by relating their properties to disintegrating force development patterns. The treatment of disintegrating force-time curves was effected using the Weibull distribution as proposed for dissolution. Such parameters as the maximum disintegrating force developed, the...

journal_title：Journal of pharmaceutical sciences

authors： Colombo P,Conte U,Caramella C,Geddo M,La Manna A

更新日期：1984-05-01 00:00:00

abstract：:The correlation of log P (in octanol--water) with the nonempirical, topologically dependent, calculated molecular connectivity index (1chiv) delineates substituted hydroxyureas into two families of linearly related groups of compounds. The first group, composed of the 3-substituted ethyl, n-propyl, and n-butyl analogs...

journal_title：Journal of pharmaceutical sciences

authors： Parker GR

更新日期：1978-04-01 00:00:00

abstract：:Polysorbate 80, a surfactant often assumed to be inert, was found to bind a number of biochemically important ions (K+, Na+, NH4+, Ca2+) and transport them through a model membrane (CH2Cl2). The rates and fluxes of potassium ions were found to depend on the initial concentration of potassium ion, the polysorbate 80 co...

journal_title：Journal of pharmaceutical sciences

authors： Thoman CJ

更新日期：1986-10-01 00:00:00

abstract：:Dose individualization is essential in epilepsy treatment, especially in antiepileptic drugs that present high interindividual variability such as lamotrigine. We aimed an observational study to develop a population pharmacokinetic model for quantitative evaluation of the factors that influence lamotrigine pharmacokin...

journal_title：Journal of pharmaceutical sciences

authors： Chávez-Castillo CE,Medellín-Garibay SE,Milán-Segovia RDC,Rodríguez-Leyva I,Romano-Moreno S

更新日期：2020-09-01 00:00:00

abstract：:The sensitivity of pharmacokinetic deconvolution algorithms with respect to simulated experimental error has been studied. Approximations of cumulative absorption profiles reconstructed from simulated data sets with normally distributed random error were compared with corresponding known input functions. The coinciden...

journal_title：Journal of pharmaceutical sciences

authors： Süverkrüp R,Bonnacker I,Raubach HJ

更新日期：1989-11-01 00:00:00

abstract：:A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...

journal_title：Journal of pharmaceutical sciences

authors： Ghanekar AG,Das Gupta V

更新日期：1978-06-01 00:00:00

abstract：:A hydraulic calcium phosphate cement made of beta-tricalcium phosphate [beta-Ca3(PO4)2], monocalcium phosphate monohydrate [Ca(H2PO4)2-H2O], and water was used as a delivery system for the antibiotic gentamicin sulfate (GS). GS, added as powder or as aqueous solution, was very beneficial to the physicochemical propert...

journal_title：Journal of pharmaceutical sciences

authors： Bohner M,Lemaître J,Van Landuyt P,Zambelli PY,Merkle HP,Gander B

更新日期：1997-05-01 00:00:00

abstract：:The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ce...

journal_title：Journal of pharmaceutical sciences

authors： Hashimoto N,Hirano K

更新日期：1998-09-01 00:00:00

abstract：:(-)-1-Cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo [a,d]cyclohepten-5-ylidene)piperidine (MK-160) was extracted from human plasma and urine with petroleum ether and quantitated by GLC using a nitrogen-sensitive detector. A homologue of the drug served as the internal standard. The method is specific for the d...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Hutt JE

更新日期：1983-07-01 00:00:00

abstract：:Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...

journal_title：Journal of pharmaceutical sciences

authors： Li GF,Yu G,Li Y,Zheng Y,Zheng QS,Derendorf H

更新日期：2018-07-01 00:00:00

abstract：:Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...

journal_title：Journal of pharmaceutical sciences

authors： Leopold CS,Lippold BC

更新日期：1995-02-01 00:00:00

abstract：:Two nonporous and three porous amorphous silicas were used as dispersion media to convert corticoid solutions into free-flowing powders. The corticoids (prednisone, prednisolone, and hydrocortisone) were dissolved in N,N-dimethylacetamide-polyethylene glycol 400 (7:3 v/v) and their 10% (w/v) solutions were mixed with ...

journal_title：Journal of pharmaceutical sciences

authors： Liao CC,Jarowski CI

更新日期：1984-03-01 00:00:00

abstract：:A colorimetric procedure for benzocaine and a number of its dosage forms was developed; it offers improvement in ease, speed, and sensitivity over the official method. The method is based on the formation of a red Schiff base between benzocaine and p-dimethylaminocinnamaldehyde in a nonaqueous acidic medium. At the ma...

journal_title：Journal of pharmaceutical sciences

authors： Tan HS,Bruemmer GA,Shelton D

更新日期：1977-07-01 00:00:00

abstract：:Cephalosporins are among the most frequently used broad-spectrum antimicrobial agents. Ceftazidime is a semisynthetic β-lactam antibiotic for parenteral administration widely used in the clinical practice, which has been categorized as a third-generation cephalosporin antibiotic. This drug crystallizes as a pentahydra...

journal_title：Journal of pharmaceutical sciences

authors： Alves de Santana MS,Santiago de Oliveira Y,de Castro Fonseca J,Ferreira WC,Neto VS,Ayala AP

更新日期：2020-03-01 00:00:00