Experimental evaluation of a model for predicting micellar composition and concentration of monomeric species in bile salt binary mixtures.


:The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on which the presumed validity of this model was based are discussed. The following binary mixtures were investigated: sodium chenodeoxycholate with cholate, ursocholate and ursodeoxycholate, either unconjugated or conjugated with taurine and glycine at different mole fractions (0, 0.25, 0.5, 0.75, 1) in 0.15 M NaCl. For these mixtures, experimentally determined data were in good agreement with values predicted by the theoretical model: both the cmc and the surface tension at this concentration of the mixtures were intermediate between those of the two pure bile salts; also, as the total bile salt concentration increased, the mixed micelles became enriched with the bile salt having the highest cmc, whereas the total monomer activity, determined by a potentiometric method employing a bile salt-selective electrode, increased only slightly. To test this model in an in vitro system, surface tension was also measured in ox bile samples that were enriched by 50% with sodium ursodeoxycholate, chenodeoxycholate, or their taurine amidates. The cmc and the surface tension at this concentration of the artificial bile increased when enriched with a bile salt with a cmc higher than that of endogenous salts (e.g. ursodeoxycholate versus taurocholate), whereas the reverse occurred for mixtures enriched with a bile salt with a lower cmc, such as chenodeoxycholate.(ABSTRACT TRUNCATED AT 250 WORDS)


J Pharm Sci


Roda A,Cerré C,Fini A,Sipahi AM,Baraldini M




Has Abstract


1995-05-01 00:00:00














  • Osmotic water transport through cellulose acetate membranes produced from a latex system.

    abstract::The advisability of a progressive curtailment of organic solvent film coating offers an incentive to develop latex systems. Here, the use of aqueous colloidal dispersions of cellulose acetate, plasticized with water-soluble additives, is proposed as an alternative way to obtain cellulose acetate membranes either by ca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bindschaedler C,Gurny R,Doelker E

    更新日期:1987-06-01 00:00:00

  • Surfactant Effects on Lipid-Based Vesicles Properties.

    abstract::Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokineti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Bnyan R,Khan I,Ehtezazi T,Saleem I,Gordon S,O'Neill F,Roberts M

    更新日期:2018-05-01 00:00:00

  • Improved delivery through biological membranes XIX: Novel redox carriers for brain-specific chemical delivery systems.

    abstract::New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bodor N,AbdelAlim AM

    更新日期:1985-03-01 00:00:00

  • Controlled delivery of basal insulin from phase-sensitive polymeric systems after subcutaneous administration: in vitro release, stability, biocompatibility, in vivo absorption, and bioactivity of insulin.

    abstract::The purpose of this study was to investigate the phase-sensitive delivery systems (D,L-polylactide in triacetin) for controlled delivery of insulin at basal level. The effect of varying concentration of zinc, polymer, and insulin on the in vitro release of insulin was evaluated. Stability of released insulin was inves...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Al-Tahami K,Oak M,Singh J

    更新日期:2011-06-01 00:00:00

  • Protein nanoparticles for intracellular delivery of therapeutic enzymes.

    abstract::The use of enzymes as therapeutics is very promising because of their catalytic activity and specificity. However, intracellular delivery of active enzymes is challenging due to their low stability and large size. The production of protein-enzyme nanoparticles was investigated with the goal of developing a protein car...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Estrada LH,Chu S,Champion JA

    更新日期:2014-06-01 00:00:00

  • Interactions of griseofulvin with cyclodextrins in solid binary systems.

    abstract::Griseofulvin/cyclodextrin interactions were investigated in aqueous environment and in solid state. Two cyclodextrin derivatives (beta-cyclodextrin and 2-hydroxypropyl beta-cyclodextrin) were used to prepare different physical mixtures and kneaded systems, and the drug/cyclodextrin ratios were 1:1 and 1:2 mol/mol. Sca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Veiga MD,Díaz PJ,Ahsan F

    更新日期:1998-07-01 00:00:00

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

    abstract::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 diffusi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Windheuser JJ,Haslam JL,Caldwell L,Shaffer RD

    更新日期:1982-11-01 00:00:00

  • Liquid chromatographic procedure for the quantitative analysis of carboplatin in beagle dog plasma ultrafiltrate.

    abstract::A specific and reproducible high-performance liquid chromatographic (HPLC) procedure was developed for the quantitative analysis of carboplatin (JM-8) in dog plasma ultrafiltrate. Plasma ultrafiltrate samples were generated using Amicon Centrifree micropartition systems or Amicon Centriflo cones, and injected onto a m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Duncan GF,Faulkner HC 3rd,Farmen RH,Pittman KA

    更新日期:1988-03-01 00:00:00

  • Study of morphology of reactive dissolution interface using fractal geometry.

    abstract::The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tromelin A,Gnanou JC,Andrès C,Pourcelot Y,Chaillot B

    更新日期:1996-09-01 00:00:00

  • Applications of circular dichroism (CD) for structural analysis of proteins: qualification of near- and far-UV CD for protein higher order structural analysis.

    abstract::Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

    更新日期:2011-11-01 00:00:00

  • Rationale for apparent differences in pharmacokinetic aspects of model compounds determined from blood level data and urinary excretion data in rats.

    abstract::Results of studies carried out in rats for model compounds, D-(-) mandelic acid, benzoylformic acid, and some of their para-alkylated homologs, showed that their biological half-lives determined from the elimination phase of urinary excretion data were longer than those determined from the elimination phase of blood l...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Amin YM,Nagwekar JB

    更新日期:1976-09-01 00:00:00

  • Nonadditive Effects of Repetitive Administration of Lipoplexes in Immunocompetent Mice.

    abstract::Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Betker JL,Anchordoquy TJ

    更新日期:2017-03-01 00:00:00

  • A site-directed mutagenesis study of drug-binding selectivity in genetic variants of human alpha(1)-acid glycoprotein.

    abstract::Human alpha(1)-acid glycoprotein (AGP), a major carrier of many basic drugs in circulation, consists of at least two genetic variants, namely A and F1*S variant. Interestingly, the variants of AGP have different drug-binding properties. The purpose of this study was to identify the amino acid residues that are respons...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Nishi K,Ueno M,Murakami Y,Fukunaga N,Akuta T,Kadowaki D,Watanabe H,Suenaga A,Maruyama T,Otagiri M

    更新日期:2009-11-01 00:00:00

  • Application of gas pycnometry for the density measurement of freeze-dried products.

    abstract::Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Stange U,Scherf-Clavel M,Gieseler H

    更新日期:2013-11-01 00:00:00

  • High-pressure liquid chromatographic determination of ibuprofen in plasma.

    abstract::A sensitive, simple, and rapid method for the quantitation of ibuprofen in plasma, using 1-(p-fluorobenzoyl)-5-methoxy-2-methylindole acetic acid as the internal standard, was developed. The method is based on reversed-phase high-pressure liquid chromatography with a mobile phase containing acetonitrile--0.1 M acetic ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ali A,Kazmi S,Plakogiannis FM

    更新日期:1981-08-01 00:00:00

  • Enzyme inhibition. VIII: Mode of inhibition of reverse transcriptase activity by analogues, isomers, and related alkaloids of coralyne.

    abstract::Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sethi ML

    更新日期:1985-08-01 00:00:00

  • Rapid determination of chlorpromazine hydrochloride and two oxidation products in various pharmaceutical samples using high-performance liquid chromatography and fluorescence detection.

    abstract::A rapid, simple, and accurate high-performance liquid chromatographic procedure using an amino-bonded microparticulate column is reported for the determination of chlorpromazine hydrochloride (I) and its two oxidation products, the sulfoxide (II) and the sulfone (III), in commercially available pharmaceutical dosage p...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Takahashi DM

    更新日期:1980-02-01 00:00:00

  • Predicting With Confidence: Using Conformal Prediction in Drug Discovery.

    abstract::One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Alvarsson J,Arvidsson McShane S,Norinder U,Spjuth O

    更新日期:2021-01-01 00:00:00

  • TOPS-MODE approach for the prediction of blood-brain barrier permeation.

    abstract::The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cabrera MA,Bermejo M,Pérez M,Ramos R

    更新日期:2004-07-01 00:00:00

  • Pharmacokinetics of transdermal drug delivery.

    abstract::The pharmacokinetics of drug delivery from transdermal controlled-release devices consisting of (a) a membrane plus a reservoir or (b) a monolithic slab are examined. For the period when the devices act as if the drug reservoir were infinite, simple relationships for the steady-state slope and time lag are derived and...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Berner B

    更新日期:1985-07-01 00:00:00

  • Cytotoxic effects of methionine alkyl esters and amides in normal and neoplastic cell lines.

    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

    pub_type: 杂志文章


    authors: Clement MA,Chapman JM,Roberts J

    更新日期:1989-06-01 00:00:00

  • Controlled and complete release of a model poorly water-soluble drug, prednisolone, from hydroxypropyl methylcellulose matrix tablets using (SBE)(7m)-beta-cyclodextrin as a solubilizing agent.

    abstract::Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Rao VM,Haslam JL,Stella VJ

    更新日期:2001-07-01 00:00:00

  • Capillary GLC assay for carbinoxamine and hydrocodone in human serum using nitrogen-sensitive detection.

    abstract::Capillary gas chromatography using an open tubular fused silica column and NP-FID was applied to the simultaneous analysis of the antihistamine, carbinoxamine, and the antitussive, hydrocodone, in human serum. Carbinoxamine and hydrocodone were extracted into methylene chloride-2-propanol (9:1) under alkaline conditio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hoffman DJ,Leveque MJ,Thomson T

    更新日期:1983-11-01 00:00:00

  • Effect of certain drugs in perfused human placenta XII: autacoid antagonism by phenothiazines.

    abstract::The effects of chlorpromazine, prochlorperazine, and trifluoperazine on the pressor actions of serotonin, angiotensin, and bradykinin in the perfused vessels of full-term human placentas were investigated. A significant inhibition of the effect of serotonin was observed with trifluoperazine and chlorpromazine but not ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wolstenholme WW,Gautieri RF

    更新日期:1976-10-01 00:00:00

  • Electron microscope study of effect of benzalkonium chloride and edetate disodium on cell envelope of Pseudomonas aeruginosa.

    abstract::Electron micrographs of Pseudomonas aeruginosa grown in nutrient broth or broth containing subinhibitory concentrations of benzalkonium chloride indicate that benzalkonium chloride at 50 and 100 mug/ml strips off the outer cell membrane. Cells grown in the presence of edetate disodium, 50-100 mug/ml had convoluted sur...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Richards RM,Cavill RH

    更新日期:1976-01-01 00:00:00

  • Secondary antithyroid action of drugs in relation to structure.

    abstract::Molecular interactions between iodine and disulfiram, clomethiazole, and tolnaftate were investigated by electron spectroscopy. Iodine forms charge transfer complexes with these molecules, with 1:1 stoichiometry and of the n-sigma type. The formation constants were compared with those obtained with antithyroid molecul...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Buxeraud J,Absil AC,Raby C

    更新日期:1984-12-01 00:00:00

  • Formulation and evaluation of quercetin polycaprolactone microspheres for the treatment of rheumatoid arthritis.

    abstract::Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthriti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Natarajan V,Krithica N,Madhan B,Sehgal PK

    更新日期:2011-01-01 00:00:00

  • Assessment of Bioequivalence of Weak Base Formulations Under Various Dosing Conditions Using Physiologically Based Pharmacokinetic Simulations in Virtual Populations. Case Examples: Ketoconazole and Posaconazole.

    abstract::Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cristofoletti R,Patel N,Dressman JB

    更新日期:2017-02-01 00:00:00

  • Solvent influences on metastable polymorph lifetimes: real-time interconversions using energy dispersive X-ray diffractometry.

    abstract::Solvent influences on the crystallization of polymorph and hydrate forms of the nootropic drug piracetam (2-oxo-pyrrolidineacetamide) were investigated from water, methanol, 2-propanol, isobutanol, and nitromethane. Crystal growth profiles of piracetam polymorphs were constructed using time-resolved diffraction snapsh...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: DeMatos LL,Williams AC,Booth SW,Petts CR,Taylor DJ,Blagden N

    更新日期:2007-05-01 00:00:00

  • Structure of polyvinylpyrrolidone-iodine (povidone-iodine).

    abstract::Hydrogen triiodide adducts were prepared from N,N-dimethylacetamide, N-alkylpyrrolidone derivatives, and polyvinylpyrrolidone, and their structures were investigated by IR spectra and X-ray structure analyses and compared with the structure of povidone-iodine USP. The results suggest that the iodine in povidone-iodine...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schenck HU,Simak P,Haedicke E

    更新日期:1979-12-01 00:00:00