The use of N,N-diethyl-m-toluamide to enhance dermal and transdermal delivery of drugs.


:A dermal penetration enhancer has been found which improves the dermal delivery of a wide variety of drugs and at the same time has a history of low toxicity for human dermal application. N,N-Diethyl-m-toluamide (I) has been shown to improve the delivery of many drugs through hairless mouse skin in an in vitro diffusion cell model. A topically applied steroid, hydrocortisone, has been used to demonstrate the in vivo effectiveness of I on human skin. The degree of pallor produced on human skin by the corticosteroids was used as a measure of the relative delivery of hydrocortisone from formulations with and without I.


J Pharm Sci


Windheuser JJ,Haslam JL,Caldwell L,Shaffer RD




Has Abstract


1982-11-01 00:00:00














  • Indolizines II: search for potential oral hypoglycemic agents.

    abstract::A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provide...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: De AU,Saha BP

    更新日期:1975-02-01 00:00:00

  • Effect of bile salts on nasal permeability in vitro.

    abstract::Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hersey SJ,Jackson RT

    更新日期:1987-12-01 00:00:00

  • Phosphodiesterase inhibition by succinic and related acid biphenylalkyl monoesters.

    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

    pub_type: 杂志文章


    authors: Rogers ME,Boots SG,Boots MR

    更新日期:1979-07-01 00:00:00

  • Meropenem exists in equilibrium with a carbon dioxide adduct in bicarbonate solution.

    abstract::Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Almarsson O,Kaufman MJ,Stong JD,Wu Y,Mayr SM,Petrich MA,Williams JM

    更新日期:1998-05-01 00:00:00

  • N-hydroxymethyl derivatives of nitrogen heterocycles as possible prodrugs II: possible prodrugs of allopurinol, glutethimide, and phenobarbital.

    abstract::Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bansal PC,Pitman IH,Higuchi T

    更新日期:1981-08-01 00:00:00

  • 2-(methylamino)-5-chlorobenzophenone imine: a novel product formed in base-catalyzed hydrolysis of diazepam.

    abstract::Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yang SK,Tang R,Yang TJ,Pu QL,Bao Z

    更新日期:1996-07-01 00:00:00

  • Microstructure of calcium stearate matrix pellets: a function of the drying process.

    abstract::Drying is a common pharmaceutical process, whose potential to modify the final drug and/or dosage form properties is often underestimated. In the present study, pellets consisting of the matrix former calcium stearate (CaSt) incorporating the active pharmaceutical ingredient ibuprofen were prepared via wet extrusion a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schrank S,Kann B,Windbergs M,Glasser BJ,Zimmer A,Khinast J,Roblegg E

    更新日期:2013-11-01 00:00:00

  • Enhanced cytotoxicity of core modified chitosan based polymeric micelles for doxorubicin delivery.

    abstract::In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) mediu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ye YQ,Chen FY,Wu QA,Hu FQ,Du YZ,Yuan H,Yu HY

    更新日期:2009-02-01 00:00:00

  • Liquid membrane phenomenon in diuretics.

    abstract::Surface activity and critical micelle concentrations are reported for two diuretic drugs, furosemide and triamterene. The drugs generate a liquid membrane on a supporting membrane. Transport of chloride, sodium, and potassium ions through the liquid membranes generated by the drugs was studied. The data suggest that t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bhise SB,Bhattacharjee D,Srivastava RC

    更新日期:1984-11-01 00:00:00

  • Protein effects on surfactant adsorption suggest the dominant mode of surfactant-mediated stabilization of protein.

    abstract::Surfactants stabilize proteins through two major mechanisms: (1) their preferential location at nearby interfaces, in this way precluding protein adsorption; and/or (2) their association with protein into "complexes" that prevent proteins from interacting with surfaces as well as each other. However, selection of surf...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kim HL,McAuley A,McGuire J

    更新日期:2014-05-01 00:00:00

  • Concomitant adsorption and stability of some anthracycline antibiotics.

    abstract::Using liquid scintillation counting and liquid chromatographic techniques, it has been demonstrated that the anthracycline antibiotics, doxorubicin hydrochloride, N-trifluoroacetyladriamycin-14-valerate, and N-trifluoroacetyladriamycin-14-octanoate, can be strongly absorbed to the walls of containers, depending on the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tomlinson E,Malspeis L

    更新日期:1982-10-01 00:00:00

  • Tocainide conjugation in humans: novel biotransformation pathway for a primary amine.

    abstract::The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

    更新日期:1980-01-01 00:00:00

  • Antiradiation compounds XV: condensations of carbon disulfide with amino, chloro, cyanomethyl, and sulfonamido heterocycles.

    abstract::Condensations of carbon disulfide were carried out with amino, chloro, and diamino heterocycles to give condensed ring thiazoline-2-thiones and imidazoline-2-thiones, with cyanomethyl heterocycles to give dithio acid derivatives, and with heterocyclic sulfonamides to give sulfonyldithiocarbamates. Of several examples ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Foye WO,Kauffman JM,Lanzillo JJ,LaSala EF

    更新日期:1975-08-01 00:00:00

  • Absorption, distribution, and excretion of 14C-meglumine in rats and dogs after administration of 14C-meglumine salicylate.

    abstract::Meglumine labeled with carbon-14 was administered orally as 14C-meglumine salicylate to rats and dogs to study its distribution and excretion. The compound was incompletely absorbed; that which was absorbed was rapidly excreted in the urine. Peak blood levels were about 5-10 mug/ml in rats and 2-8 mug/ml in dogs. Tiss...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Heeg JF,Born GS,Kessler WV,Shaw SM,Lange WE

    更新日期:1977-01-01 00:00:00

  • Relationship of in vitro hydrolysis of 17-chloroacetylajmaline and 17-acetylajmaline in different animal species.

    abstract::17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Salmona M,Lakszner K,Fanelli R,Saronio C,Bianchi R,Mussini E

    更新日期:1975-09-01 00:00:00

  • In the search for new anticancer drugs. 28. Synthesis and evaluation of highly active aminoxyl labeled amino acid derivatives containing the [N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl group.

    abstract::The aminoxyl (nitroxyl) labeled (2-chloroethyl)nitrosocarbamoyl (CNC) derivatives of amino acids, i.e., N-[[N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl]-A-(1-oxy-2,2,6,6- tetramethylpiperidin-4-yl)amides, A = glycyl (10a), A = L-alanyl (10b), A = L-valyl (10c), A = L-phenylalanyl (10d), were synthesized and evaluated ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sosnovsky G,Baysal M,Erciyas E

    更新日期:1994-07-01 00:00:00

  • Reversible adsorption of nicotinic acid onto charcoal in vitro.

    abstract::The effects of various factors on the adsorption of nicotinic acid onto and desorption from activated charcoal were investigated in vitro. The affinity of nicotinic acid for charcoal was poor both in acidic and neutral media. Adsorption increased with increasing charcoal:drug ratios and decreasing incubation volume:ch...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Roivas L,Neuvonen PJ

    更新日期:1992-09-01 00:00:00

  • Correlation of in vivo bioavailability of erythromycin stearate tablets with in vitro tests.

    abstract::Correlations between the bioavailability parameters for erythromycin stearate tablets from five manufacturers and in vitro tests of these tablets were examined using forward (stepwise), multiple linear regression analysis. Bioavailability parameters were determined in clinical studies employing a balanced, incomplete ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Stavchansky S,Doluisio JT,Martin A,Martin C,Cabana B,Dighe S,Loper A

    更新日期:1980-11-01 00:00:00

  • Enhancing the Pharmaceutical Behavior of Nateglinide by Cocrystallization: Physicochemical Assessment of Cocrystal Formation and Informed Use of Differential Scanning Calorimetry for Its Quantitative Characterization.

    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

    pub_type: 杂志文章


    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

  • Insight From Molecular Dynamics Simulations on the Crystallization Tendency of Indomethacin Polymorphs in the Undercooled Liquid State.

    abstract::The crystallization tendency of 2 crystalline polymorphs of indomethacin (Iα, Iγ) in the undercooled melt has been investigated using molecular dynamics simulations. The main thermodynamical and dynamical physical parameters involved in the nucleation and growth processes have been determined. A careful attention has ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Gerges J,Affouard F

    更新日期:2020-02-01 00:00:00

  • Methionine, tryptophan, and histidine oxidation in a model protein, PTH: mechanisms and stabilization.

    abstract::Recent oxidation events on monoclonal antibody candidates prompted us to investigate the mechanism of oxidation of Met, Trp, and His residues and to search for suitable stabilizers. By using parathyroid hormone (1-34), PTH, as a model protein and various oxidants, aided by liquid chromatography, peptide mapping, and m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ji JA,Zhang B,Cheng W,Wang YJ

    更新日期:2009-12-01 00:00:00

  • General linearized biexponential model for QSAR data showing bilinear-type distribution.

    abstract::A major impediment of many QSAR-type analyses is that the data show a maximum or minimum and can no longer be adequately described by linear functions that provide unrivaled simplicity and usually give good description over more restricted ranges. Here, a general linearized biexponential (LinBiExp) model is proposed t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Buchwald P

    更新日期:2005-11-01 00:00:00

  • Phase behavior of carbamyloxyphosphatidylcholine, a sphingolipid analogue.

    abstract::The phase behavior of two series of phosphatidylcholines (PC) possessing carbamyloxy-linked fatty acids has been studied by differential scanning calorimetry. These non-natural phosphatidylcholines are of interest because they possess the capability of forming interlipid hydrogen bonds via the carbamyloxy function and...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Curatolo W,Bali A,Gupta CM

    更新日期:1985-12-01 00:00:00

  • Effect of lipophilicity on the bioavailability of drugs after percutaneous administration by dissolving microneedles.

    abstract::To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ito Y,Yoshimura M,Tanaka T,Takada K

    更新日期:2012-03-01 00:00:00

  • Kinetics of drug action in disease states. XXXVI: Effect of cyclosporine on the pharmacodynamics and pharmacokinetics of a barbiturate (heptabarbital) in rats.

    abstract::Pretreatment with cyclosporine reportedly prolongs the effect of certain general anesthetics in humans and the sleeping time of mice after pentobarbital administration. This investigation was designed to determine the mechanism(s) of the cyclosporine-barbiturate interaction. Adult female Wistar rats received cyclospor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hoffman A,Levy G

    更新日期:1990-01-01 00:00:00

  • A physiologically relevant pharmacokinetic model of xenobiotic percutaneous absorption utilizing the isolated perfused porcine skin flap.

    abstract::A physiologic pharmacokinetic model describing percutaneous absorption of topically applied compounds in the isolated perfused porcine skin flap (IPPSF) is presented. As an extension of a previously reported hybrid physiologically relevant compartmental model of uptake of intra-arterially administered drug in the IPPS...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Williams PL,Carver MP,Riviere JE

    更新日期:1990-04-01 00:00:00

  • Delivery of theophylline into excised human skin from alkanoic acid solutions: a "push-pull" mechanism.

    abstract::Human skin samples are permeable to theophylline delivered from 1.5% solutions in various alkanecarboxylic acids and their mixtures. The respective permeability coefficients of theophylline, calculated from steady-state flux, correlate negatively with the permeability coefficients of the donor carboxylic acids and pos...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kadir R,Stempler D,Liron Z,Cohen S

    更新日期:1987-10-01 00:00:00

  • Inactivation of gamma-glutamylcysteine synthetase by SAPH-3 disulfide: role of the histaminyl moiety.

    abstract::Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schor NF,Cheng B,Siuda JF

    更新日期:1991-04-01 00:00:00

  • Pharmacokinetics of oral and intravenous fluorouracil in humans.

    abstract::The pharmacokinetics of fluorouracil were examined after single 250-mg iv doses and 500-mg oral doses to female patients with breast cancer. In five patients who received intravenous fluorouracil, the mean peak plasma level of unchanged drug was 13.4 microgram/ml, the elimination half-life was 6.3 min, and the plasma ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Phillips TA,Howell A,Grieve RJ,Welling PG

    更新日期:1980-12-01 00:00:00

  • Optical crystallographic characteristics of some USP drugs.

    abstract::Optical crystallographic data were determined on a variety of newer USP drugs for which data had not been previously obtained. The ingredients in an unknown sample can be identified by polarized light microscopy by mounting small amounts of the material in successive specific refractive index liquids and determining r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Jordan DD

    更新日期:1993-12-01 00:00:00