Membrane transport of drugs in different regions of the intestinal tract of the rat.


:Regional permeability coefficients of 19 drugs with different physicochemical properties were determined using excised segments from three regions of rat intestine: jejunum, ileum, and colon. The results are discussed in relation to the characteristics of the drug, i.e., MW (range 113-1071 Da), pKa, log D (octanol/water at pH 7.4) (range -3.1 to +2.4), and the regional change in the properties of the epithelial membrane. There was a significant decrease in permeability to hydrophilic drugs and a significant increase in permeability for hydrophobic drugs aborally to the small intestine (P < 0.0001). A good correlation could be obtained between MW and permeability coefficients of hydrophilic drugs. The correlation established between the apparent permeability coefficients and the partition coefficients of the drugs was sigmoidal in shape in all three regions and a log D between 0 and 2.5 predicts high permeability values. These permeability data are unique since they result from a diversity of chemical structures with different physicochemical characteristics and a variety of transport mechanisms and they are not influenced by interlaboratory differences. The large regional permeability database in the present study shows the utility of the Ussing chamber technique as a valuable predictive tool for human in vivo data. In addition, the regional permeability profiles obtained suggest a coupling between drug structure and the functional changes of the membrane, which might be useful for selecting a compound for an extended release formulation.


J Pharm Sci


Ungell AL,Nylander S,Bergstrand S,Sjöberg A,Lennernäs H




Has Abstract


1998-03-01 00:00:00














  • Transdermal delivery of naltrexol and skin permeability lifetime after microneedle treatment in hairless guinea pigs.

    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

    pub_type: 杂志文章


    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

  • Improvement in solubility and dissolution rate of 1, 2-dithiole-3-thiones upon complexation with beta-cyclodextrin and its hydroxypropyl and sulfobutyl ether-7 derivatives.

    abstract::Inclusion complexes between beta-cyclodextrin derivatives and 1, 2-dithione-3-thiones were studied in aqueous solution and in the solid state. Phase solubility study was used to evaluate the complexation in solution, at 37 degrees C, of three cyclodextrins, i. e., beta-cyclodextrin (betaCD), hydroxypropyl-beta-cyclode...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Dollo G,Le Corre P,Chollet M,Chevanne F,Bertault M,Burgot JL,Le Verge R

    更新日期:1999-09-01 00:00:00

  • Injectable polyanhydride granules provide controlled release of water-soluble drugs with a reduced initial burst.

    abstract::A method for preparing polyanhydride granules of an injectable size was developed. The resulting granules permitted a nearly constant release of low-molecular-weight, water-soluble drugs without an initial burst. The polyanhydrides used were poly(fatty acid dimer), poly(sebacic acid), and their copolymers. The dyes ac...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tabata Y,Domb A,Langer R

    更新日期:1994-01-01 00:00:00

  • In vitro and in vivo evaluation of a sulfenamide prodrug of basic metformin.

    abstract::In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Huttunen KM,Leppänen J,Vepsäläinen J,Sirviö J,Laine K,Rautio J

    更新日期:2012-08-01 00:00:00

  • Solubility and partitioning. VII: Solubility of barbiturates in water.

    abstract::The solubility equation of Yalkowsky was used to estimate the aqueous solubility of 33 barbiturates in the temperature range of 5 to 45 degrees C. The equation was extended by adding a term which accounts for the effect of pH on the solubility of the drug. The extended equation is successful in estimating the aqueous ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pinal R,Yalkowsky SH

    更新日期:1987-01-01 00:00:00

  • Isomerization of ceftibuten in aqueous solution.

    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

    pub_type: 杂志文章


    authors: Hashimoto N,Hirano K

    更新日期:1998-09-01 00:00:00

  • Verification and validation of computational models used in biopharmaceutical manufacturing: Potential application of the ASME Verification and Validation 40 standard and FDA proposed AI/ML model life cycle management framework.

    abstract::A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

    更新日期:2021-01-22 00:00:00

  • Modeling of transmitted X-ray intensity variation with sample thickness and solid fraction in glycine compacts.

    abstract::The previous paper in this series introduced an X-ray diffraction quantitation method for the polymorphic content in tablets made of pure components. Before the method could be transferred, further studies were required to explain the commonly observed X-ray intensity variation in analyzing compacts. The literature ty...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cao W,Mullarney MP,Hancock BC,Bates S,Morris KR

    更新日期:2003-12-01 00:00:00

  • Mechanism of Drug Release From Temperature-Sensitive Formulations Composed of Low-Melting-Point Microcrystalline Wax.

    abstract::It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled man...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Matsumoto K,Kimura SI,Noguchi S,Itai S,Kondo H,Iwao Y

    更新日期:2019-06-01 00:00:00

  • Enrichment of Relevant Oxidative Degradation Products in Pharmaceuticals With Targeted Chemoselective Oxidation.

    abstract::The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

    更新日期:2019-04-01 00:00:00

  • Apparent absorption kinetics of micronized griseofulvin after its oral administration on single- and multiple-dose regimens to rats as a corn oil-in-water emulsion and aqueous suspension.

    abstract::This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bates TR,Carrigan PJ

    更新日期:1975-09-01 00:00:00

  • On the hydrolytic behavior of tinidazole, metronidazole, and ornidazole.

    abstract::Using two UV-spectrophotometric methods, the hydrolysis of tinidazole was studied at pH 1.00-8.45 at 80 degrees C. The reaction followed apparent first-order kinetics throughout the studied range. No kinetic salt effect was detected, indicating that at least one of the reacting partners forming the transition state ha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Salo JP,Yli-Kauhaluoma J,Salomies H

    更新日期:2003-04-01 00:00:00

  • Phase transformation in thiamine hydrochloride tablets: Influence on tablet microstructure, physical properties, and performance.

    abstract::The objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chakravarty P,Suryanarayanan R,Govindarajan R

    更新日期:2012-04-01 00:00:00

  • pH-Sensitive cationic copolymers of different macromolecular architecture as potential dexamethasone sodium phosphate delivery systems.

    abstract::This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Georgieva D,Kostova B,Ivanova S,Rachev D,Tzankova V,Kondeva-Burdina M,Christova D

    更新日期:2014-08-01 00:00:00

  • Interleukin-1 receptor antagonist: a new therapy for type 2 diabetes mellitus.

    abstract::Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Akash MS,Shen Q,Rehman K,Chen S

    更新日期:2012-05-01 00:00:00

  • Expected particle size distributions of crystals produced from nonisothermal recrystallization.

    abstract::It is shown, using oxalic acid dihydrate as a model, that nonisothermal recrystallization of powders gives rise to particle size distributions which approach log-normality in many cases. The number of particles formed is, primarily, a function of the nucleation rate constants and the particle size distribution, i.e., ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Carstensen JT,Rodriguez-Hornedo N

    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

  • X-ray microtomography analysis of intragranular drug migration during fluidized bed and oven tray drying.

    abstract::During the drying process of a wet granulate, water-soluble compounds can migrate to the outer layers of the granule with the evaporating solvent. This migration can affect structural and mechanical characteristics of the granules as the solute accumulates on the granule's outer crust. The objective of this study was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Poutiainen S,Honkanen M,Becker J,Nachtweide D,Järvinen K,Ketolainen J

    更新日期:2012-04-01 00:00:00

  • Utilising Magnetically Isolated Lysosomes for Direct Quantification of Intralysosomal Drug Concentrations by LC-MS/MS Analysis: An Investigatory Study With Imipramine.

    abstract::Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Francis L,Harrell A,Hallifax D,Galetin A

    更新日期:2020-09-01 00:00:00

  • Hypolipidemic activity of 3-N-(1',8'-Naphthalimido)propionic acid in rodents.

    abstract::3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GH

    更新日期:1984-07-01 00:00:00

  • Physicochemical and pharmacokinetic characteristics of plasmid DNA/cationic liposome complexes.

    abstract::The objectives of this study were (i) to characterize the plasmid DNA encoding the chloramphenicol acetyltransferase reporter gene (pCAT) complexed with cationic liposomes (Lipofectin and LipofectACE) in terms of particle size and zeta potential, (ii) to compare pharmacokinetic characteristics, and (iii) to study the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mahato RI,Kawabata K,Nomura T,Takakura Y,Hashida M

    更新日期:1995-11-01 00:00:00

  • Prediction of solubility in nonideal multicomponent systems using the UNIFAC group contribution model.

    abstract::There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ochsner AB,Sokoloski TD

    更新日期:1985-06-01 00:00:00

  • A novel inhalable form of rifapentine.

    abstract::Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens. However, in humans, an inhalable form of rifapentine may be necessary to considerably shorten treatment duration because of the physiological barr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chan JG,Duke CC,Ong HX,Chan JC,Tyne AS,Chan HK,Britton WJ,Young PM,Traini D

    更新日期:2014-05-01 00:00:00

  • Quantitative microradiographic study of simultaneous demineralization/remineralization of dental enamel in weak acid buffers.

    abstract::The remineralization behavior of weak acid-treated bovine tooth enamel has been investigated using a recently developed quantitative microradiographic method. Acetate buffer solutions at pH 4.5 containing calcium, phosphate, and 10 ppm fluoride were used in this study. When the solution ion activity product ( KFAP = a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bergstrom DH,Fox JL,Higuchi WI

    更新日期:1984-05-01 00:00:00

  • Fusion of disubstituted benzenes.

    abstract::The entropy of fusion of 84 disubstituted benzenes was essentially constant and independent of the participation of the compounds in intramolecular or intermolecular hydrogen bonding. It was also independent of the shapes, sizes, and dipole moments of the rigid molecules studied. While the entropy of fusion was indepe...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Martin E,Yalkowsky SH,Wells JE

    更新日期:1979-05-01 00:00:00

  • Determination of phenylpropanolamine salts in dosage forms through fluroescent derivative formation.

    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

    pub_type: 杂志文章


    authors: Shankle LL

    更新日期:1978-11-01 00:00:00

  • Infrared spectroscopic studies of lyophilization- and temperature-induced protein aggregation.

    abstract::Recent studies have clearly demonstrated that Fourier transform IR spectroscopy can be a powerful tool for the study of protein stabilization during freeze-drying and for optimizing approaches to prevent lyophilization-induced protein aggregation. The purpose of the current review is to provide an overview of these to...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Dong A,Prestrelski SJ,Allison SD,Carpenter JF

    更新日期:1995-04-01 00:00:00

  • Studies on the structure of the complex of the boron neutron capture therapy drug, L-p-boronophenylalanine, with fructose and related carbohydrates: chemical and 13C NMR evidence for the beta-D-fructofuranose 2,3,6-(p-phenylalanylorthoboronate) structure.

    abstract::The complex of L-L-boronophenylalanine (L-p-BPA) with fructose has been used for the past 5 years in clinical trials of boron neutron capture therapy to treat both melanoma and glioblastoma multiforme. However, the structure of this complex in water buffered at physiologic pH has not been established. In the (1)H NMR ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shull BK,Spielvogel DE,Head G,Gopalaswamy R,Sankar S,Devito K

    更新日期:2000-02-01 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

  • In situ perfusion system for oral mucosal absorption in dogs.

    abstract::To evaluate oral mucosal absorption of drugs in dogs, a newly designed in situ perfusion system with a circulating perfusion chamber was developed. The utility of the perfusion system was investigated by using three drugs: salicylic acid (SA), sulfadimethoxine (SM), and diltiazem (DIL). The oral mucosal absorption of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yamahara H,Suzuki T,Mizobe M,Noda K,Samejima M

    更新日期:1990-11-01 00:00:00