Quantification of the effect of excipients on bioavailability by means of response surfaces III: In vivo--in vitro correlations.

abstract：:Dissolving microneedle patches offer promise as a simple, minimally invasive method of drug and vaccine delivery to the skin that avoids the need for hypodermic needles. However, it can be difficult to control the amount and localization of drug within microneedles. In this study, we developed novel microneedle design...

journal_title：Journal of pharmaceutical sciences

authors： Chu LY,Choi SO,Prausnitz MR

更新日期：2010-10-01 00:00:00

abstract：:Pyrimethamine, an antimalarial drug, was found to be able to inhibit both enzymes (DHFR-TS and PTR1) of the leishmanial folate pathway, although this effect in vivo appears only in relatively high concentrations. To reach the parasites inside macrophage cells, where they are sheltered, targeted drugs of pyrimethamine,...

journal_title：Journal of pharmaceutical sciences

authors： De Carvalho PB,Ramos DC,Cotrim PC,Ferreira EI

更新日期：2003-10-01 00:00:00

abstract：:This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...

journal_title：Journal of pharmaceutical sciences

authors： Abshire C,Murad HY,Arora JS,Liu J,Mandava SH,John VT,Khismatullin DB,Lee BR

更新日期：2017-05-01 00:00:00

abstract：:Melanotan-II (1) is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH) which tans the skin and is currently being evaluated for the prevention of sunlight-induced skin cancers. The dissociation constants of 1 were determined using potentiometric titration and ultraviolet spectrophotomet...

journal_title：Journal of pharmaceutical sciences

authors： Lan EL,Ugwu SO,Blanchard J,Fang X,Hruby VJ,Sharma S

更新日期：1994-08-01 00:00:00

abstract：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...

journal_title：Journal of pharmaceutical sciences

authors： Sörgel F,Ettinger B,Benet LZ

更新日期：1986-02-01 00:00:00

abstract：:A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

journal_title：Journal of pharmaceutical sciences

authors： Won CM,Zalipsky JJ,Patel DM,Grim WM

更新日期：1982-03-01 00:00:00

abstract：:The location and conformation of fosinopril sodium (FS) in a lamellar liquid crystal of water, sodium dodecyl sulfate, and decanol was studied by low-angle X-ray diffraction. The result showed the FS molecule to be located within the amphiphilic part of the liquid crystalline structure with the polar parts anchored at...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Moaddel T,Morris KR,Abramowitz R,Amsberry KL

更新日期：1994-05-01 00:00:00

abstract：:A column-switching high-performance liquid chromatographic assay combined with a heart-cutting technique and UV detection (LC/LC/UV) was developed to determine ceftibuten, a new oral cephalosporin, in human plasma. Plasma samples were directly injected into the first chromatographic column for sample cleanup and extra...

journal_title：Journal of pharmaceutical sciences

authors： Pan HT,Kumari P,Lim J,Lin CC

更新日期：1992-07-01 00:00:00

abstract：:Uptake of the fluorescent probe, 1-anilino-8-naphthalene-sulfonate (I) into isolated rat liver cells was studied using both fluorescence and filtration methods. The time course of the fluorescence enhancement of I after addition to the isolated liver cells was analyzed in terms of rapid, medium, and slow phases. The s...

journal_title：Journal of pharmaceutical sciences

authors： Sugiyama Y,Kimura S,Lin JH,Izukura M,Awazu S,Hanano M

更新日期：1983-08-01 00:00:00

abstract：:A direct high-performance liquid chromatographic (HPLC) method was applied to monitor 2,5-diaziridinyl-3,6-bis(carboethoxyamino)-1,4-benzoquinone (I) and its degradation products in pharmaceutical vehicles at 25 +/- 0.1 degrees. At the optimal pH for stability of I, an increase in buffer concentration [phosphate and t...

journal_title：Journal of pharmaceutical sciences

authors： Poochikian GK,Kelley JA

更新日期：1981-02-01 00:00:00

abstract：:Solubility values of a selected group of nonsteroidal anti-inflammatory drugs have been determined in water and 1-octanol as a function of temperature. Thermodynamic functions of dissolution and partition have been calculated and discussed with respect to various physical parameters of each solute and the two solvents...

journal_title：Journal of pharmaceutical sciences

authors： Fini A,Laus M,Orienti I,Zecchi V

更新日期：1986-01-01 00:00:00

abstract：:The objectives of this work are to explore the pi-pi complexation of amitriptyline with pi electron-deficient aromatic rings and demonstrate the feasibility of pi-pi complexation for overdosed drug detoxification. Water-soluble oligochitosan was chemically modified with dinitrobenzenesulfonyl groups to induce selectiv...

journal_title：Journal of pharmaceutical sciences

authors： Lee DW,Flint J,Morey T,Dennis D,Partch R,Baney R

更新日期：2005-02-01 00:00:00

abstract：:The chemical stability of the novel anticancer agent carzelesin in aqueous buffer/acetonitrile (1:1, v/v) mixtures has been investigated utilizing a stability-indicating reversed-phase high-performance liquid chromatographic assay. The degradation kinetics of carzelesin has been studied as a function of pH, buffer com...

journal_title：Journal of pharmaceutical sciences

authors： Vries JD,Doppenberg WG,Henrar RE,Bult A,Beijnen JH

更新日期：1996-11-01 00:00:00

abstract：:Canrenone can be determined by high-speed liquid chromatography in pharmaceutical dosage forms without interference from common excipients or degradation products. This stability-indicating assay, using o-nitroaniline as the internal standard, is rapid and accurate. ...

journal_title：Journal of pharmaceutical sciences

authors： Williamson DE

更新日期：1976-01-01 00:00:00

abstract：:The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...

journal_title：Journal of pharmaceutical sciences

authors： Jain N,Yalkowsky SH

更新日期：2001-02-01 00:00:00

abstract：:As part of a study to examine cocaine disposition and interaction with ethanol, it was necessary to characterize various properties of cocaine in the blood of the experimental animal. All studies were conducted using blood from healthy adult male Sprague-Dawley rats. Cocaine was incubated in whole blood at 37 degrees ...

journal_title：Journal of pharmaceutical sciences

authors： Sukbuntherng J,Martin DK,Pak Y,Mayersohn M

更新日期：1996-06-01 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：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...

journal_title：Journal of pharmaceutical sciences

authors： Liebner R,Meyer M,Hey T,Winter G,Besheer A

更新日期：2015-02-01 00:00:00

abstract：:A sensitive and specific GLC method is described to determine therapeutic levels of tilidine and its two main metabolites, nortilidine and bisnortilidine, in plasma and urine. The method involves the extraction of the compounds and an internal standard with cyclohexane from alkalinized samples, followed by back-extrac...

journal_title：Journal of pharmaceutical sciences

authors： Hengy H,Vollmer KO,Gladigau V

更新日期：1978-12-01 00:00:00

abstract：:Site I of human serum albumin is an important and complex region for high-affinity binding of drugs. Equilibrium dialysis showed independent binding of dansyl-L-asparagine (DNSA) and n-alkyl p-aminobenzoates (p-ABEs) to regions Ib and Ic, respectively, in the pH range 6.0-9.0. However, individual binding of DNSA incre...

journal_title：Journal of pharmaceutical sciences

authors： Yamasaki K,Maruyama T,Takadate A,Suenaga A,Kragh-Hansen U,Otagiri M

更新日期：2004-12-01 00:00:00

abstract：:Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibio...

journal_title：Journal of pharmaceutical sciences

authors： Ceschan NE,Rosas MD,Olivera ME,Dugour AV,Figueroa JM,Bucalá V,Ramírez-Rigo MV

更新日期：2020-09-01 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 applicability of bioavailability assessment at quasi- and nonsteady state is illustrated with data from a study comparing two formulations of amitriptyline hydrochloride in humans. Relative bioavailability as a function of the observed mean plasma concentrations may be expressed in closed form, provided the affect...

journal_title：Journal of pharmaceutical sciences

authors： Bondi JV,Hucker HB,Yeh KC,Kwan KC

更新日期：1976-11-01 00:00:00

abstract：:In this work, a novel risk-based methodology for lot release is proposed. Its objective is to assess the risk that a lot declared to have passed truly meets product specifications. The methodology consists of 3 parts: adaptive sample size determination, estimation of the probability that the product was within specifi...

journal_title：Journal of pharmaceutical sciences

authors： Mockus L,Reklaitis G,Morris K,LeBlond D

更新日期：2020-02-01 00:00:00

abstract：:The goal of this research was to evaluate the effectiveness of cationic liposomes for intranasal administration of proteins to the brain. Cationic liposomes were loaded with a model protein, ovalbumin (OVAL), and a 50 microg dose was administered intranasally to rats. In qualitative studies, liposomes were loaded with...

journal_title：Journal of pharmaceutical sciences

authors： Migliore MM,Vyas TK,Campbell RB,Amiji MM,Waszczak BL

更新日期：2010-04-01 00:00:00

abstract：:The release kinetics of a polymeric-controlled release device are determined by its geometry and dimensions. A method to calculate the required size and shape of diffusion-controlled dosage forms to achieve a particular release profile is presented. The diffusion parameters are determined for various drugs (theophylli...

journal_title：Journal of pharmaceutical sciences

authors： Siepmann J,Ainaoui A,Vergnaud JM,Bodmeier R

更新日期：1998-07-01 00:00:00

abstract：:The granule strength (crushing load) of lactose granulated with 1-9% povidone was measured initially and at intervals during a 1-year period. The granule strengths of dibasic calcium phosphate dihydrate granulated with various concentrations of starch and povidone were measured. The axial and radial tensile strengths ...

journal_title：Journal of pharmaceutical sciences

authors： Jarosz PJ,Parrott EL

更新日期：1983-05-01 00:00:00

abstract：:A spectrophotofluorometric method is described for the quantitative analysis of coumarin, umbelliferone, and mixtures thereof in whole blood. The two drugs were selectively isolated from blood by solvent extraction. Analysis of the isolated coumarin was based on the measurement of the fluorophore at activation and emi...

journal_title：Journal of pharmaceutical sciences

authors： Tan HS,Ritschel WA,Sanders PR

更新日期：1976-01-01 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：:Chlorthalidone was analyzed in the concentration range of 0.1-3.0 microgram/ml with a precision of +/- 0.05 microgram/ml. Chlorthalidone inhibition of the enzymatic hydrolysis rate of p-nitrophenyl acetate by bovine erythrocyte carbonic anhydrase was used as a basis for the determination. The amount of p-nitrophenol f...

journal_title：Journal of pharmaceutical sciences

authors： Johnston MM,Li H,Mufson D

更新日期：1977-12-01 00:00:00