Thermodynamic Estimate of the Number of Solvent Molecules Displaced by a Solute Molecule for Enthalpy-Driven Adsorption: Phenobarbital and Activated Carbons as the Model System.

abstract：:The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

更新日期：1982-11-01 00:00:00

abstract：:A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...

journal_title：Journal of pharmaceutical sciences

authors： Rakestraw DC,Whitney CC Jr

更新日期：1984-12-01 00:00:00

abstract：:The nanosizing of poorly soluble drugs as a formulation strategy can eventually enhance their dissolution rate and bioavailability. Standard comminution techniques such as high-pressure homogenization (HPH) or wet bead milling have limitations in reaching the desired mean particle size. Combinative methods have been d...

journal_title：Journal of pharmaceutical sciences

authors： Salazar J,Müller RH,Möschwitzer JP

更新日期：2013-05-01 00:00:00

abstract：:A procedure was developed for the separation and selective quantitative determination of the (S)(+)- and (R)(-)-enantiomers of the racemic anti-inflammatory drug carprofen as their diastereomeric l-(-)-alpha-methylbenzylamides. These derivatives are obtained in equivalent yields by reacint purified 14C-carprofen from ...

journal_title：Journal of pharmaceutical sciences

authors： Kemmerer JM,Rubio FA,McClain RM,Koechlin BA

更新日期：1979-10-01 00:00:00

abstract：:Mycophenolate mofetil (MPM), a new immunosuppressant, is the morpholinoethyl ester of mycophenolic acid (MPA). The distribution in blood and pharmacokinetics of MPA after administration of MPM were examined. The plasma to erythrocyte concentration ratio was low (0.10-0.15). MPA existed in rat plasma as the highly boun...

journal_title：Journal of pharmaceutical sciences

authors： Sugioka N,Koyama H,Ohta T,Kishimoto H,Yasumura T,Takada K

更新日期：1996-03-01 00:00:00

abstract：:Gold nanoparticles through nucleation of Au clusters have been extensively studied. However, due to low potency, prolonged tissue retention, and irreversible accumulation, the safety considerations have limited their therapeutic and diagnostic applications. Novel gold nanostructures with retained physical properties a...

journal_title：Journal of pharmaceutical sciences

authors： Gao Y,Mu Q,Zhu L,Li Z,Ho RJY

更新日期：2020-05-01 00:00:00

abstract：:Pharmaceutical cocrystals have garnered significant interest as potential solids to address issues associated with formulation development of drug substances. However, studies concerning the understanding of formulation behavior of cocrystals are still at the nascent stage. We present results of our attempts to evalua...

journal_title：Journal of pharmaceutical sciences

authors： Aitipamula S,Wong ABH,Kanaujia P

更新日期：2018-02-01 00:00:00

abstract：:A method to determine the adherence of drugs to the esophagus was developed using isolated swine esophagi. A number of types of tablets and capsules (e.g., of doxycycline) were tested. The results showed that the tendency of products to adhere to the esophagus can be regulated by pharmaceutical properties. It was conc...

journal_title：Journal of pharmaceutical sciences

authors： Marvola M,Vahervuo K,Sothmann A,Marttila E,Rajaniemi M

更新日期：1982-09-01 00:00:00

abstract：:A high-pressure liquid chromatographic method suitable for determining plasma metoclopramide levels at normal (10-20 mg) doses is described. Eight metabolites as well as metclopramide were isolated and identified in rat, dog. and human urine. The only common metabolite in these species is 2-[(4-amino-5-chloro-2-metho...

journal_title：Journal of pharmaceutical sciences

authors： Teng L,Bruce RB,Dunning LK

更新日期：1977-11-01 00:00:00

abstract：:Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...

journal_title：Journal of pharmaceutical sciences

authors： Schantz S,Hoppu P,Juppo AM

更新日期：2009-05-01 00:00:00

abstract：:SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 receptor. Ivermectin has shown antiviral activity by inhibiting the formation of the importin-α (IMPα) and IMPβ1 subunits as well as dissociating the IMPα/β1 heterodimer and has in vitro efficacy agains...

journal_title：Journal of pharmaceutical sciences

authors： Jermain B,Hanafin PO,Cao Y,Lifschitz A,Lanusse C,Rao GG

更新日期：2020-12-01 00:00:00

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 00:00:00

abstract：:Nanoparticle tracking analysis (NTA) obtains particle size by analysis of particle diffusion through a time series of micrographs and particle count by a count of imaged particles. The number of observed particles imaged is controlled by the scattering cross-section of the particles and by camera settings such as sens...

journal_title：Journal of pharmaceutical sciences

authors： Defante AP,Vreeland WN,Benkstein KD,Ripple DC

更新日期：2018-05-01 00:00:00

abstract：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:Although significant progress had been made in developing general scale-up rules for an aqueous pan-coating process, there are often scenarios where small-scale experiments are not found to be truly reflective of what may be observed at the large scale. This article reviews some of the methods traditionally used for s...

journal_title：Journal of pharmaceutical sciences

authors： Pandey P,Bindra DS

更新日期：2014-11-01 00:00:00

abstract：:A series of N1-p-chlorophenyl-N5-alkylbiguanides were synthesized as potential inhibitors of dental plaque. Partition coefficients and pKa values were determined by standard methods. Biological activity was evaluated against Streptococcus mutans, a pure strain of plaque-forming bacteria. All compounds were compared to...

journal_title：Journal of pharmaceutical sciences

authors： Warner VD,Lynch DM,Ajemian RS

更新日期：1976-07-01 00:00:00

abstract：:The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

journal_title：Journal of pharmaceutical sciences

authors： Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

更新日期：1986-10-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 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：: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：: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：: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：:The molecular modeling program SYBYL was used to simulate the adsorption of various barbiturates by an activated charcoal surface. The compounds barbituric acid (BA), barbital (B), phenobarbital (PB), mephobarbital (M), and primidone (Pr) were modeled, and their structures were energetically minimized. These structure...

journal_title：Journal of pharmaceutical sciences

authors： Wurster DE,Kolling WM,Knosp BM

更新日期：1994-12-01 00:00:00

abstract：:Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...

journal_title：Journal of pharmaceutical sciences

authors： Teo SY,Yew MY,Lee SY,Rathbone MJ,Gan SN,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:A continuous nonisothermal-isothermal method for stability prediction was developed. The approach yields all necessary parameters for prediction, including reaction order. The experimental procedure involves changing the temperature of the samples being studied until degradation is rapid enough to proceed at a conveni...

journal_title：Journal of pharmaceutical sciences

authors： Zoglio MA,Maulding HV,Streng WH,Vincek WC

更新日期：1975-08-01 00:00:00

abstract：:The effects of permeant charge (z) on iontophoretic-enhanced transport were investigated with synthetic Nucleopore membranes and with human epidermal membranes using a four-electrode potentiostat with side-by-side diffusion cells. The modified Nernst-Planck model (Nernst-Planck theory with an additional transport term...

journal_title：Journal of pharmaceutical sciences

authors： Li SK,Ghanem AH,Peck KD,Higuchi WI

更新日期：1997-06-01 00:00:00

abstract：:Econazole is a feasible alternative treatment in the management of fungal keratitis. Nevertheless, its low water solubility is considered the main limitation to the incorporation into ophthalmic formulations. In this work, econazole nitrate is solubilized by using cyclodextrins to achieve an optimum therapeutic concen...

journal_title：Journal of pharmaceutical sciences

authors： Díaz-Tomé V,Luaces-Rodríguez A,Silva-Rodríguez J,Blanco-Dorado S,García-Quintanilla L,Llovo-Taboada J,Blanco-Méndez J,García-Otero X,Varela-Fernández R,Herranz M,Gil-Martínez M,Lamas MJ,González-Barcia M,Otero-Espinar FJ,Fern

更新日期：2018-05-01 00:00:00

abstract：:An equation was developed which enables blood level data to be utilized for determining whether or not the first-order absorption and elimination rate constants are equal in the one-compartment open model. This equation was tested using simulated data with excellent results. ...

journal_title：Journal of pharmaceutical sciences

authors： Macheras PE

更新日期：1985-05-01 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：:Successful development of stable solid protein formulations usually requires the addition of one or several excipients to achieve optimal stability. In these products, there is a potential risk of an inhomogeneous distribution of the various ingredients, specifically the ratio of protein and stabilizer may vary. Such ...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen KTT,Frijlink HW,Hinrichs WLJ

更新日期：2020-01-01 00:00:00