The Introduction of a New Flexible In Vivo Predictive Dissolution Apparatus, GIS-Alpha (GIS-α), to Study Dissolution Profiles of BCS Class IIb Drugs, Dipyridamole and Ketoconazole.

Abstract:

:The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challenging using compendial methods. To overcome this limitation, in vivo predictive dissolution apparatuses, such as the transfer model, have been developed to predict bioperformance of oral formulation candidates and drug products. In this manuscript we utilize a new transfer-model dissolution apparatus, the gastrointestinal simulator-α (GIS-α), to characterize its behavior in terms of transfer kinetics and pH, assess its reproducibility and adaptability to mimic different transfer conditions, as well as study dissolution of ketoconazole and dipyridamole as model BCS class IIb compounds. Availability of commercially available dissolution transfer systems with similar configuration to compendial dissolution apparatus, may be helpful to simplify and standardize in vivo predictive dissolution methodologies for BCS class IIb compounds in the future.

journal_name

J Pharm Sci

authors

Tsume Y,Patel S,Wang M,Hermans A,Kesisoglou F

doi

10.1016/j.xphs.2020.08.020

subject

Has Abstract

pub_date

2020-11-01 00:00:00

pages

3471-3479

issue

11

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(20)30490-1

journal_volume

109

pub_type

杂志文章
  • GLC determination of procainamide in biological fluids.

    abstract::A GLC method for the determination of procainamide in biological fluids is presented. By using a dipropyl analog of procainamide as an internal standard, both compounds can be chromatographed directly, yielding linear calibration curves and a sensitivity that allows quantitative determination of concentrations as low ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600641213

    authors: Simons KJ,Levy RH

    更新日期:1975-12-01 00:00:00

  • Development of a Novel Lung Slice Methodology for Profiling of Inhaled Compounds.

    abstract::The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24575

    authors: Bäckström E,Lundqvist A,Boger E,Svanberg P,Ewing P,Hammarlund-Udenaes M,Fridén M

    更新日期:2016-02-01 00:00:00

  • Asparagine deamidation dependence on buffer type, pH, and temperature.

    abstract::The deamidation of asparagine into aspartate and isoaspartate moieties is a major pathway for the chemical degradation of monoclonal antibodies (mAbs). It can affect the shelf life of a therapeutic antibody that is not formulated or stored appropriately. A new approach to detect deamidation using ion exchange chromato...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23529

    authors: Pace AL,Wong RL,Zhang YT,Kao YH,Wang YJ

    更新日期:2013-06-01 00:00:00

  • Adsorption of cationized bovine serum albumin onto epithelial crypt fractions of the rat colon.

    abstract::The purpose of the study was to characterize mucosal attachment of a cationized model protein, bovine serum albumin (BSA), onto the various fractions of colonic crypts epithelium in the rat. BSA was labeled with fluorescein isothiocyanate (FITC) and its surface net electric charge was modified from negative to positiv...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1102

    authors: Blau S,Levin N,Schwartz B,Rubinstein A

    更新日期:2001-10-01 00:00:00

  • Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function.

    abstract::The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level Box-Behnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X(1)), Tween 20 (X(2)), and Transcutol HP (X(3)...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23333

    authors: Marasini N,Yan YD,Poudel BK,Choi HG,Yong CS,Kim JO

    更新日期:2012-12-01 00:00:00

  • Factors Influencing the Retention of Organic Solvents in Products Freeze-Dried From Co-Solvent Systems.

    abstract::Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2018.04.001

    authors: Kunz C,Gieseler H

    更新日期:2018-08-01 00:00:00

  • Sucrose esters increase drug penetration, but do not inhibit p-glycoprotein in caco-2 intestinal epithelial cells.

    abstract::Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24085

    authors: Kiss L,Hellinger É,Pilbat AM,Kittel Á,Török Z,Füredi A,Szakács G,Veszelka S,Sipos P,Ózsvári B,Puskás LG,Vastag M,Szabó-Révész P,Deli MA

    更新日期:2014-10-01 00:00:00

  • Application of salivary concentration data to pharmacokinetic studies with antipyrine.

    abstract::The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660140

    authors: Meffin PJ,Williams RL,Blaschke TF,Rowland M

    更新日期:1977-01-01 00:00:00

  • Toward Understanding Drug Release From Biodegradable Polymer Microspheres of Different Erosion Kinetics Modes.

    abstract::Two generalized modes of erosion kinetics, that is, the power law mode and root type mode, respectively, were found to be able to better describe the reported weight loss data compared to the existing linear mode, for commonly used surface-eroding polymer microspheres. Based on the newly identified modes, a set of dru...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.04.002

    authors: You S,Yang Z,Wang CH

    更新日期:2016-06-01 00:00:00

  • Onset of enzyme induction with pregnenolone-16alpha-carbonitrile in male and female rats.

    abstract::Male and female rats treated with a single 20-mg/kg ip dose of pregnenolone-16alpha-carbonitrile (PCN) produced parallel increases in hepatic cytochrome P-450 and aniline hydroxylase activity. However, the onset of increase in aniline hydroxylase activity and cytochrome P-450 content was slower in male than female ani...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650436

    authors: Stohs SJ,Rosenberg H

    更新日期:1976-04-01 00:00:00

  • Molecular Dynamics of Amorphous Sulfamethazine With Structurally Related Sulfonamide Impurities Evaluated Using Thermal Analysis.

    abstract::In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.12.008

    authors: Hamada Y,Ono M,Ohara M,Yonemochi E

    更新日期:2017-04-01 00:00:00

  • Colorimetric assay of benzocaine and some dosage forms.

    abstract::A colorimetric procedure for benzocaine and a number of its dosage forms was developed; it offers improvement in ease, speed, and sensitivity over the official method. The method is based on the formation of a red Schiff base between benzocaine and p-dimethylaminocinnamaldehyde in a nonaqueous acidic medium. At the ma...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660736

    authors: Tan HS,Bruemmer GA,Shelton D

    更新日期:1977-07-01 00:00:00

  • Rapid determination of gold in whole blood of arthritis patients using flameless atomic absorption spectrophotometry.

    abstract::An assay for gold in whole blood of arthritis patients was developed using the graphite furnace atomic absorption spectrophotometer. This method involves no pretreatment of the whole blood except for simple dilution, thereby eliminating some variables and saving laboratory time and expense. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670943

    authors: Barrett MJ,DeFries R,Henderson WM

    更新日期:1978-09-01 00:00:00

  • Swelling and polymer erosion for poly(ethylene oxide) tablets of different molecular weights polydispersities.

    abstract::The aim of the study was to determine and compare the degree of swelling and the swelling kinetics of poly(ethylene oxide) (PEO) hydrophilic matrix tablets without any additives for matrixes with different molecular weight polydispersities. A wide range of "mixed" polydisperse PEO tablets were obtained by mixing two P...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21892

    authors: Körner A,Larsson A,Andersson A,Piculell L

    更新日期:2010-03-01 00:00:00

  • Effect of thermodynamic activities of the unionized and ionized species on drug flux across buccal mucosa.

    abstract::The objective of this work was to delineate the contribution of thermodynamic activities of ionized and unionized species on buccal drug permeation. The flux and permeability of a model acidic (nimesulide) and basic (bupivacaine) drug were determined across porcine buccal mucosa at different pH conditions. Thermodynam...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21301

    authors: Kokate A,Li X,Singh P,Jasti BR

    更新日期:2008-10-01 00:00:00

  • STRITERFIT, a least-squares pharmacokinetic curve-fitting package using a programmable calculator.

    abstract::A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740510

    authors: Thornhill DP,Schwerzel E

    更新日期:1985-05-01 00:00:00

  • Stabilizing effect of fructose on aqueous solutions of hydrocortisone.

    abstract::Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720930

    authors: Bansal NP,Holleran EM,Jarowski CI

    更新日期:1983-09-01 00:00:00

  • Retrospective statistical analysis of lyophilized protein formulations of progenipoietin using PLS: determination of the critical parameters for long-term storage stability.

    abstract::Although certain criteria have become recognized as being essential for a stable lyophilized formulation, the relative importance of different stability criteria has not been demonstrated quantitatively. This study uses multivariate statistical methods to determine the relative importance of certain formulation variab...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20170

    authors: Katayama DS,Kirchhoff CF,Elliott CM,Johnson RE,Borgmeyer J,Thiele BR,Zeng DL,Qi H,Ludwig JD,Manning MC

    更新日期:2004-10-01 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

    doi:

    authors: De AU,Saha BP

    更新日期:1975-02-01 00:00:00

  • Chlorothiazide is a substrate for the human uptake transporters OAT1 and OAT3.

    abstract::The thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, beca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23491

    authors: Juhász V,Beéry E,Nagy Z,Bui A,Molnár E,Zolnerciks JK,Magnan R,Jani M,Krajcsi P

    更新日期:2013-05-01 00:00:00

  • Pharmacokinetics of Peptide-Fc fusion proteins.

    abstract::Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.23783

    authors: Wu B,Sun YN

    更新日期:2014-01-01 00:00:00

  • Studies on zoapatle. VIII: Novel cytotoxic sesquiterpene lactones from Montanoa tomentosa ssp. microcephala.

    abstract::Investigation of the leaves of Montanoa tomentosa Cerv. ssp. microcephala (Sch.-Bip.) Funk (Compositae) resulted in the isolation of three novel guaianolide sesquiterpenes, montacephalin (1), tomencephalin (2), and 5-hydroxytomencephalin (3), which were shown to be cytotoxic (P-388). The structures of these sesquiterp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770620

    authors: Topcu G,Cordell GA,Farnsworth NR,Fong HH

    更新日期:1988-06-01 00:00:00

  • Prediction of onset of crystallization in amorphous pharmaceutical systems: phenobarbital, nifedipine/PVP, and phenobarbital/PVP.

    abstract::The aim of this work is to determine if a stability testing protocol based on the correlations between crystallization onset and relaxation time above the glass transition temperature (T(g)) can be used to predict the crystallization onsets in amorphous pharmaceutical systems well below their T(g). This procedure assu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22232

    authors: Caron V,Bhugra C,Pikal MJ

    更新日期:2010-09-01 00:00:00

  • Aspirin--a national survey II: Determination of salicylic acid in bulk aspirin and aspirin formulations by high-pressure liquid chromatography using a fluorescence detector.

    abstract::A quantitative high-pressure liquid chromatographic method, using a reversed-phase column coupled to a fluorescence detector, was developed to determine salicylic acid in bulk aspirin and plain and buffered aspirin tablets. The aspirin was dissolved, filtered, and injected into the chromatograph; the fluorescence of t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690518

    authors: Kirchhoefer RD,Juhl WE

    更新日期:1980-05-01 00:00:00

  • Finding the Needle in the Haystack: High-Resolution Techniques for Characterization of Mixed Protein Particles Containing Shed Silicone Rubber Particles Generated During Pumping.

    abstract::During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.12.002

    authors: Deiringer N,Haase C,Wieland K,Zahler S,Haisch C,Friess W

    更新日期:2020-12-09 00:00:00

  • Secondary structure characterization of microparticulate insulin powders.

    abstract::The secondary structure content of microparticulate insulin powders produced by the supercritical antisolvent (SAS) precipitation technique was investigated via Raman spectroscopy. Precipitate samples were generated at 25 and 35 degrees C processing temperatures. Both precipitate samples gave amide I band spectra that...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600831203

    authors: Yeo SD,Debendetti PG,Patro SY,Przybycien TM

    更新日期:1994-12-01 00:00:00

  • Modeling of the Biological Activity of Monoclonal Antibodies Based on the Glycosylation Profile.

    abstract::The influence of the glycosylation profile of IgG on biological activity is known, but it is not clear which glycoforms have the highest impact on the main mechanism of action. The aim of this study was to design a mathematical model for predicting the antibody-dependent cellular cytotoxicity (ADCC) activity and the F...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2021.01.010

    authors: Bartusik-Czubek E,Toboła P,Czubek B,Bednarek M,Balcerek J,Pietrucha T,Jaros S

    更新日期:2021-01-20 00:00:00

  • Chemistry and pharmacology of homologs of 6-acetyl-and 3,6-diacetylmorphine.

    abstract::3,6-Diformyl- and 3,6-dipropanoylmorphine and 6-formyl- and 6-propanoylmorphine were prepared to obtain longer acting, heroin-like compounds. The 6-acylated compounds were more potent than heroin subcutaneously and were orally effective, and their duration of action was at least two to three times greater than that of...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660242

    authors: May EL,Jacobson AE

    更新日期:1977-02-01 00:00:00

  • Comparative pharmacokinetics of free muramyl tripeptide phosphatidyl ethanolamine (MTP-PE) and liposomal MTP-PE.

    abstract::The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600821005

    authors: Gay B,Cardot JM,Schnell C,van Hoogevest P,Gygax D

    更新日期:1993-10-01 00:00:00

  • A lamellar liquid crystal with fosinopril sodium.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.2600830517

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

    更新日期:1994-05-01 00:00:00