Effect of dosing volume on gastrointestinal absorption in rats: analysis of the gastrointestinal disposition of L-glucose and estimation of in vivo intestinal membrane permeability.


:The effect of the oral dosing volume (DV) on both gastric emptying and intestinal absorption was examined by analyzing the gastrointestinal disposition of a model solute, L-glucose, in rats. The amount of 14C-labeled L-glucose in the gastric and intestinal contents of sacrificed rats was measured at various times after administration, and the data were analyzed with a linear model, assuming first-order gastric emptying followed by first-order intestinal absorption. The gastric emptying rate constant (kg) rose from 0.025 to 0.072 min-1 by increasing DV from 0.1 to 3 mL/rat, whereas the intestinal absorption rate constant (ka) decreased from 0.031 to 0.015 min-1. This decrease in ka was attributed to an increase in the average intestinal lumen volume (Vav) from 24 to 39 microL/cm, assuming that the relationship ka = CLa,app/Vav holds (where CLa,app is the apparent intestinal membrane permeability clearance or the product of the apparent membrane permeability coefficient and surface area). The CLa,app (= kaVav), a measure of the in vivo intestinal membrane permeability, was 0.74 microL/cm/min for a DV value of 0.1 mL/rat and decreased only marginally by 20% for larger values of DV, suggesting an insignificant effect of DV on CLa,app. These results suggest that the accelerating effect of the increased kg, produced by the increased DV on the gastrointestinal absorption, may be canceled by the decrease in ka. A decrease in ka may lead to a decrease in the fraction absorbed. Finally, this study also provides a means for carrying out physiological modeling of drug absorption following oral administration.


J Pharm Sci


Yuasa H,Numata W,Ozeki S,Watanabe J




Has Abstract


1995-04-01 00:00:00














  • Combined Treatment of Tyrosine Kinase Inhibitor-Labeled Gold Nanorod Encapsulated Albumin With Laser Thermal Ablation in a Renal Cell Carcinoma Model.

    abstract::To characterize and evaluate human serum albumin-encapsulated nanoparticles for drug delivery of a tyrosine kinase inhibitor combined with induction of photothermal ablation combination therapy of renal cell carcinoma (RCC), nanoparticles of varying preparations and concentrations were characterized via zeta potential...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Callaghan C,Peralta D,Liu J,Mandava SH,Maddox M,Dash S,Tarr MA,Lee BR

    更新日期:2016-01-01 00:00:00

  • No clinically relevant pharmacokinetic and safety interactions of ambrisentan in combination with tadalafil in healthy volunteers.

    abstract::Ambrisentan is a nonsulfonamide, ET(A)-selective endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), and tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor under investigation for treatment of PAH. Due to the potential combination use, the pharmacokinetic (P...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,随机对照试验


    authors: Spence R,Mandagere A,Harrison B,Dufton C,Boinpally R

    更新日期:2009-12-01 00:00:00

  • Cocrystalline Solids of Telaprevir with Enhanced Oral Absorption.

    abstract::A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Stavropoulos K,Johnston SC,Zhang Y,Rao BG,Hurrey M,Hurter P,Topp EM,Kadiyala I

    更新日期:2015-10-01 00:00:00

  • Prediction of the adsorption of diazepam by activated carbon in aqueous media.

    abstract::Adsorption isotherms for the diazepam-activated carbon system in simulated intestinal fluid (SIF), without pancreatin, and in SIF with different percentages of ethanol were determined as were the solubilities of diazepam in SIF and in SIF with different percentages of ethanol. The surface area of the activated carbon ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wurster DE,Alkhamis KA,Matheson LE

    更新日期:2003-10-01 00:00:00

  • Fighting cancer: from the bench to bedside using second generation cationic liposomal therapeutics.

    abstract::The use of second generation cationic liposomes to deliver cytotoxic drugs to solid tumors is a rational and promising therapeutic approach, given the natural affinity of cationic carrier molecules for the tumor microvasculature. Cationic liposomal therapeutics are effective in the treatment of cancers that are resist...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Campbell RB,Ying B,Kuesters GM,Hemphill R

    更新日期:2009-02-01 00:00:00

  • Influence of race or ethnicity on pharmacokinetics of drugs.

    abstract::Review of the current literature on racial differences in pharmacokinetics of drugs supports the premise that only pharmacokinetic processes which are biologically or biochemically mediated have the potential to exhibit differences between racial or ethnic groups. Thus, the pharmacokinetic factors which can be expecte...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Johnson JA

    更新日期:1997-12-01 00:00:00

  • Isolation of cannabisativine, an alkaloid, from Cannabis sativa L. root.

    abstract::An ethanol extract of the root of a Mexican variant of Cannabis sativa L.(marijuana) afforded, after partitioning and chromatography, the new spermidine alkaloid cannabisativine. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Turner CE,Hsu MH,Knapp JE,Schiff PL Jr,Slatkin DJ

    更新日期:1976-07-01 00:00:00

  • Steroidal thiourea and thiazoline derivatives: synthesis and in vitro effects on bovine pancreatic ribonuclease activity.

    abstract::Two novel series of steroidal derivatives containing various thiourea and substituted thiazoline moieties attached to the 2- or 4-position of estrone were synthesized and examined for in vitro effect on bovine pancreatic ribonuclease activity. All compounds studied exhibited a catabolic activity. The steroidal thiazol...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ibrahim ES,Omar AM,Habib NS,Aboulwafa OM,El-Sewedy SM,Bourdais J

    更新日期:1983-10-01 00:00:00

  • Simple and rapid determination of a new pharmaceutically active amine hydrochloride.

    abstract::The quantitative analysis of a new pharmaceutically active amine hydrochloride is described. Samples are extracted with chloroform. A yellow amine-dye complex is formed by buffering a sample-bromthymol blue solution at pH 8.5 +/- 0.1 and subsequently extracted with chloroform. The complex is treated with 0.01 N NaOH t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chang ZL,Papendick VE

    更新日期:1976-10-01 00:00:00

  • Development of a CART Model to Predict the Synthesis of Cardiotoxic Daunorubicinol in Heart Tissue Samples From Donors With and Without Down Syndrome.

    abstract::Daunorubicin (DAUN) and doxorubicin (DOX) are used to treat a variety of cancers. The use of DAUN and DOX is hampered by the development of cardiotoxicity. Clinical evidence suggests that patients with leukemia and Down syndrome are at increased risk for anthracycline-related cardiotoxicity. Carbonyl reductases and al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hoefer CC,Blair RH,Blanco JG

    更新日期:2016-06-01 00:00:00

  • Effect of low molecular weight chitosans on drug permeation through mouse skin: 1. Transdermal delivery of baicalin.

    abstract::The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Impr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zhou X,Liu D,Liu H,Yang Q,Yao K,Wang X,Wang L,Yang X

    更新日期:2010-07-01 00:00:00

  • Excipients for Room Temperature Stable Freeze-Dried Monoclonal Antibody Formulations.

    abstract::Sucrose is a common cryoprotectant and lyoprotectant to stabilize labile biopharmaceuticals during freeze-drying and storage. Sucrose-based formulations require low primary drying temperatures to avoid collapse and monoclonal antibody (mAb) containing products need to be stored refrigerated. The objective of this stud...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Haeuser C,Goldbach P,Huwyler J,Friess W,Allmendinger A

    更新日期:2020-01-01 00:00:00

  • Oxidation of human insulin-like growth factor I in formulation studies. 3. Factorial experiments of the effects of ferric ions, EDTA, and visible light on methionine oxidation and covalent aggregation in aqueous solution.

    abstract::The influence of ferric ions, EDTA, and visible light on the oxidation of methionine and the covalent reducible and nonreducible dimerization in human Insulin-like Growth Factor I (hIGF-I) in aqueous (1 mM) phosphate buffer solution were studied. A reduced factorial experiment with two levels of each factor was used. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fransson JR

    更新日期:1997-09-01 00:00:00

  • Design of Hollow Hyaluronic Acid Cylinders for Sustained Intravitreal Protein Delivery.

    abstract::A hollow cylinder intravitreal implant was developed to achieve sustained release of protein to the retina for the treatment of retinal diseases. Hollow cylinders were fabricated by molding and cross-linking hyaluronic acid, the major component of the vitreous humor. Hollow cylinders were filled with a concentrated pr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Van Kampen E,Vandervelden C,Fakhari A,Qian J,Berkland C,Gehrke SH

    更新日期:2018-09-01 00:00:00

  • Molecular relaxation behavior and isothermal crystallization above glass transition temperature of amorphous hesperetin.

    abstract::The purpose of this paper was to investigate the relaxation behavior of amorphous hesperetin (HRN), using dielectric spectroscopy, and assessment of its crystallization kinetics above glass transition temperature (Tg ). Amorphous HRN exhibited both local (β-) and global (α-) relaxations. β-Relaxation was observed belo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shete G,Khomane KS,Bansal AK

    更新日期:2014-01-01 00:00:00

  • Development of a nanofiltration process to improve the stability of a novel anti-MRSA carbapenem drug candidate.

    abstract::The benzenesulfonate salt of an anti-methicillin-resistant Staphylococcus aureus carbapenem antibiotic studied is a crystalline, nonhygroscopic powder which is stable at room temperature, making it an ideal compound for long-term storage. However, the limited aqueous solubility of this salt prohibits parenteral admini...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Antonucci V,Yen D,Kelly J,Crocker L,Dienemann E,Miller R,Almarrsson O

    更新日期:2002-04-01 00:00:00

  • Tablet disintegration studied by high-resolution real-time magnetic resonance imaging.

    abstract::The present work employs recent advances in high-resolution real-time magnetic resonance imaging (MRI) to investigate the disintegration process of tablets containing disintegrants. A temporal resolution of 75 ms and a spatial resolution of 80 × 80 µm with a section thickness of only 600 µm were achieved. The histogra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Quodbach J,Moussavi A,Tammer R,Frahm J,Kleinebudde P

    更新日期:2014-01-01 00:00:00

  • Influence of pH, temperature, and buffers on the kinetics of ceftazidime degradation in aqueous solutions.

    abstract::First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zhou M,Notari RE

    更新日期:1995-05-01 00:00:00

  • Control of Globular Protein Thermal Stability in Aqueous Formulations by the Positively Charged Amino Acid Excipients.

    abstract::The positively charged amino acids are commonly used excipients in biopharmaceutical formulations for stabilization of therapeutic proteins, yet the mechanisms for their modulation of protein stability are poorly understood. In this study, both lysine and histidine are shown to affect the thermal stability of myoglobi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Platts L,Darby SJ,Falconer RJ

    更新日期:2016-12-01 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

  • Quantitative TLC determination of propranolol in human plasma.

    abstract::A spectrodensitometric assay was developed for propranolol based on measurement of the absorbance of the drug on silica gel plates irradiated at 822 nm. Quantities as low as 0.10 microgram can be detected, and a linear relationship was obtained between 0.010 and 0.400 microgram. The percent recovery from plasma spiked...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hadzija BW,Mattocks AM

    更新日期:1978-09-01 00:00:00

  • Evaluation of Systemic and Mucosal Immune Responses Induced by a Nasal Powder Delivery System in Conjunction with an OVA Antigen in Cynomolgus Monkeys.

    abstract::An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

    journal_title:Journal of pharmaceutical sciences

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    authors: Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

    更新日期:2020-12-03 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

  • Analysis of transcutaneous antigenic protein delivery by a hydrogel patch formulation.

    abstract::We have developed a hydrogel patch, which could promote antigen penetration through stratum corneum (SC), and have demonstrated its safety and efficacy in animals and humans. For the availability improvement of our system, it is important to develop a device, which enhances antigen penetration through SC more efficien...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Matsuo K,Ishii Y,Kawai Y,Saiba Y,Quan YS,Kamiyama F,Hirobe S,Okada N,Nakagawa S

    更新日期:2013-06-01 00:00:00

  • Stress Temperature Studies in Small Scale Hastelloy® Drug Substance Containers Lead to Increased Extent of and Increased Variability in Antibody-Drug Conjugate and Monoclonal Antibody Aggregation: Evidence for Novel Oxidation-Induced Crosslinking in Monoc

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Klair N,Kim MT,Lee A,Xiao NJ,Patel AR

    更新日期:2020-10-07 00:00:00

  • Investigation of the Changes in Aerosolization Behavior Between the Jet-Milled and Spray-Dried Colistin Powders Through Surface Energy Characterization.

    abstract::This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Jong T,Li J,Morton DA,Zhou QT,Larson I

    更新日期:2016-03-01 00:00:00

  • Improving Dissolution Properties by Polymers and Surfactants: A Case Study of Celastrol.

    abstract::Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zha J,Zhang Q,Li M,Wang JR,Mei X

    更新日期:2018-11-01 00:00:00

  • Design of Block Copolymer Costabilized Nonionic Microemulsions and Their In Vitro and In Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen via Topical Administration.

    abstract::Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Djekic L,Martinovic M,Stepanović-Petrović R,Tomić M,Micov A,Primorac M

    更新日期:2015-08-01 00:00:00

  • Effect of dispersion on the coloring properties of aluminum dye lakes.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wou LL,Mulley BA

    更新日期:1988-10-01 00:00:00

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

    abstract::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/wat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


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

    更新日期:1998-03-01 00:00:00