Tablet disintegration and drug dissolution in viscous media: paracetamol IR tablets.

Abstract:

:An investigation into the influence of viscous media on tablet disintegration and drug dissolution was performed with the aim to simulate the potential formulation-specific food effect for a selected highly soluble model drug. Literature data on the in vivo drug absorption in fasted and fed state have been evaluated for in vitro-in vivo correlation (IVIVC) purposes. In vitro studies were conducted in simple buffer media with or without addition of HPMC K4M as a viscosity enhancing agent. Good IVIVC correlation (r>0.95) was obtained for paracetamol dissolution in viscous media at 50rpm and fed state absorption profiles, while in vitro dissolution in simple media at lower stirring speed was predictable of drug products in vivo behaviour in the fasted state. The data obtained support the existing idea that relatively simple dissolution media and/or set of experimental conditions may be used to differentiate formulation-specific food-drug interactions. Such tests would be a useful tool in the development of formulations that would not be susceptible to the influence of co-administered meal and, furthermore, facilitate regulatory decision on the necessity to conduct food effect studies in vivo.

journal_name

Int J Pharm

authors

Parojcić J,Vasiljević D,Ibrić S,Djurić Z

doi

10.1016/j.ijpharm.2007.11.058

subject

Has Abstract

pub_date

2008-05-01 00:00:00

pages

93-9

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(07)00998-2

journal_volume

355

pub_type

杂志文章
  • Nanostructure of liquid crystalline matrix determines in vitro sustained release and in vivo oral absorption kinetics for hydrophilic model drugs.

    abstract::Nanostructured lipid-based liquid crystalline systems have been proposed as sustained oral drug delivery systems, but the interplay between their intrinsic release rates, susceptibility to digestive processes, and the manner in which these effects impact on their application in vivo, are not well understood. In this s...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.08.022

    authors: Lee KW,Nguyen TH,Hanley T,Boyd BJ

    更新日期:2009-01-05 00:00:00

  • Prolongation of residence time of liposome by surface-modification with mixture of hydrophilic polymers.

    abstract::The objective of this study is to evaluate the biodistribution characteristics of liposomes surface-modified with the mixture of polyethylene glycol (PEG) and polyvinyl alcohol (PVA) as a drug carrier for passive targeting of drugs. The liposomes (egg phosphatidylcholine:cholesterol=55:40, molar ratio) modified with b...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.04.004

    authors: Shehata T,Ogawara K,Higaki K,Kimura T

    更新日期:2008-07-09 00:00:00

  • A review of factors affecting electrostatic charging of pharmaceuticals and adhesive mixtures for inhalation.

    abstract::Pharmaceutical powders are typically insulators consisting of relatively small particles and thus they usually exhibit significant electrostatic charging behaviours. In the inhalation field, the measurement of electrostatic charge is an imperative stage during pharmaceutical formulation development. The electrostatic ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2016.01.076

    authors: Kaialy W

    更新日期:2016-04-30 00:00:00

  • Liposomes as cytokine-supplement in tumor cell-based vaccines.

    abstract::Subcutaneous vaccination of C57bl/6 mice with irradiated B16 melanoma cells supplemented with liposomal interleukin-2 (IL2) or murine interferon-gamma (mIFNgamma), resulted in systemic protection in 50% of the animals, against a subsequent tumor cell challenge in a dose dependent manner. The protective efficacy was co...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00039-3

    authors: van Slooten ML,Kircheis R,Koppenhagen FJ,Wagner E,Storm G

    更新日期:1999-06-10 00:00:00

  • Amino Acid-functionalized hollow mesoporous silica nanospheres as efficient biocompatible drug carriers for anticancer applications.

    abstract::Herein, a series of new amino acid-functionalized hollow mesoporous silica nanospheres (HMSNs) by post-grafting methods were prepared. These new materials were characterized by different techniques and were studied as matrices for the antineoplastic drug (cisplatin) transport and delivery. The results demonstrate that...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118709

    authors: Ezzati N,Mahjoub AR,Abolhosseini Shahrnoy A,Syrgiannis Z

    更新日期:2019-12-15 00:00:00

  • Novel semisolid SNEDDS based on PEG-30-dipolyhydroxystearate: development and characterization.

    abstract::The aim of the current study is to explore the potential of PEG-30-dipolyhydroxystearate (Cithrol(®) DPHS) and Soluplus(®) as ingredients in novel semisolid self-nanoemulsifying drug delivery systems (SNEDDS). Semisolid SNEDDS consisting of Cithrol(®) DPHS, Capmul(®) MCM and Kolliphor(®) HS 15 were successfully prepar...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.10.063

    authors: Hassan TH,Metz H,Mäder K

    更新日期:2014-12-30 00:00:00

  • Effective melanoma cancer suppression by iontophoretic co-delivery of STAT3 siRNA and imatinib using gold nanoparticles.

    abstract::Co-delivery of chemotherapeutic agents improve anti-tumor efficacy and reduce cancer resistance. Here, we report development of layer-by-layer assembled gold nanoparticles (LbL-AuNP) containing anti-STAT3 siRNA and imatinib mesylate (IM) to treat melanoma. The combination treatment with STAT3 siRNA and IM in B16F10 me...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.03.087

    authors: Labala S,Jose A,Chawla SR,Khan MS,Bhatnagar S,Kulkarni OP,Venuganti VVK

    更新日期:2017-06-20 00:00:00

  • Thermosensitivity and release from poly N-isopropylacrylamide-polylactide copolymers.

    abstract::A series of thermoresponsive-co-biodegradable polymers, containing varying molar ratios of N-isopropylacrylamide (NIPA) and poly-lactic acid diacrylate macromer (PLAM) were prepared and characterised. Chemical structures were confirmed by nuclear magnetic resonance (NMR) and Fourier transform infrared (FTIR). The hydr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.08.036

    authors: Chearúil FN,Corrigan OI

    更新日期:2009-01-21 00:00:00

  • Dextran-methylprednisolone succinate as a prodrug of methylprednisolone: dose-dependent pharmacokinetics in rats.

    abstract::The dose-dependency in the pharmacokinetics of a macromolecular prodrug of methylprednisolone (MP), dextran-methylprednisolone succinate (DMP), was investigated in rats. Single doses (MP equivalent) of 2.5, 5.0, 10, 20, and 30 mg/kg of DMP were administered intravenously to rats (n=5/group), and serial blood samples (...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00854-7

    authors: Zhang X,Mehvar R

    更新日期:2001-10-23 00:00:00

  • Evaluation of the effect of rifampicin on the biophysical properties of the membranes: significance for therapeutic and side effects.

    abstract::This work aims to study the biophysical interactions of rifampicin (RIF) with three-dimensional macrophage membrane models, under environments with physiological and pathological relevance. The interaction of RIF with liposomes formed by 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) in different pH values (i.e., ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.03.005

    authors: Pinheiro M,Pisco S,Silva AS,Nunes C,Reis S

    更新日期:2014-05-15 00:00:00

  • Evaluation of the vibratory feeder method for assessment of powder flow properties.

    abstract::The flow properties of pharmaceutical powders and blends used in solid oral dosage forms are an important consideration during dosage form development. The vibratory feeder method, a flow measurement technique that quantifies avalanche flow, has been adapted for measurement of the flow properties of common pharmaceuti...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2003.09.024

    authors: Bhattachar SN,Hedden DB,Olsofsky AM,Qu X,Hsieh WY,Canter KG

    更新日期:2004-01-28 00:00:00

  • Lipid nanovehicles with adjustable surface properties for overcoming multiple barriers simultaneously in oral administration.

    abstract::Lipid nanoparticles (LNs) are widely investigated for oral drug delivery, and for achieving significant advantages in colloidal stability, biocompatibility and scaled-up possibility. However, researchers face challenge of developing methods to improve the ability of LNs in overcoming multiple barriers (i.e., mucus and...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.02.015

    authors: Wu L,Liu M,Shan W,Cui Y,Zhang Z,Huang Y

    更新日期:2017-03-30 00:00:00

  • Preparation and characterization of mucoadhesive polymer-coated nanoparticles.

    abstract::The transmucosal routes such as pulmonary, nasal and oral routes are most important and common routes for drug delivering to the body. However, peptide and protein drugs are degraded before they reach the blood stream and cannot cross the mucosal barriers. The mucoadhesive polymer-coated nanoparticles colloidal carrie...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.02.031

    authors: Cui F,Qian F,Yin C

    更新日期:2006-06-19 00:00:00

  • Development of novel topical tranexamic acid liposome formulations.

    abstract::The aims of this study were to develop novel liposome formulations for tranexamic acid (TA) from various lipid compositions [neutral (hydrogenated soya phosphatidylcholine and cholesterol), positive (stearylamine) or negative (dicetyl phosphate) charged lipid], and to investigate the effects of concentrations of TA (5...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00980-2

    authors: Manosroi A,Podjanasoonthon K,Manosroi J

    更新日期:2002-03-20 00:00:00

  • In vitro skin penetration enhancement techniques: A combined approach of ethosomes and microneedles.

    abstract::Dermal administration of different macromolecules, such as nucleic acids, remains a real challenge because of the difficulty of crossing the main skin barrier, the stratum corneum (SC). To overcome this barrier, the use of deformable lipid-based nanovectors were developed to increase topical penetration through the SC...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118793

    authors: Bellefroid C,Lechanteur A,Evrard B,Mottet D,Debacq-Chainiaux F,Piel G

    更新日期:2019-12-15 00:00:00

  • Reformulation of etoposide with solubility-enhancing rubusoside.

    abstract::Etoposide (ETO), a widely used anti-cancer drug, is constrained by its low aqueous solubility and by side effects from both the drug and its solubilizing excipients. In this study, a recently discovered natural solubilizer rubusoside (RUB) was used to achieve the solubilization of ETO. Dynamic light scattering and fre...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.06.013

    authors: Zhang F,Koh GY,Hollingsworth J,Russo PS,Stout RW,Liu Z

    更新日期:2012-09-15 00:00:00

  • Thermal insight of mechanically activated bile acid powders.

    abstract::Mechanical activation of pharmaceutical materials presents an important but poorly understood phenomenon of milled molecular crystals. In this work, a strategy was followed in an effort to understand this phenomenon, cryo-milled of both crystalline and amorphous counterpart of bile acids materials were characterized b...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.08.022

    authors: Ito T,Byrn S,Chen X,Carvajal MT

    更新日期:2011-11-25 00:00:00

  • Development of biodegradable porous starch foam for improving oral delivery of poorly water soluble drugs.

    abstract::A biodegradable porous starch foam (BPSF) was developed for the first time as a carrier in order to improve the dissolution and enhance the oral bioavailability of lovastatin - defined as a model poorly water soluble BCS type II drug. In this paper, BPSF was prepared by the solvent exchange method and characterized by...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.09.040

    authors: Wu C,Wang Z,Zhi Z,Jiang T,Zhang J,Wang S

    更新日期:2011-01-17 00:00:00

  • Physico-chemical characterisation and transfection efficiency of lipid-based gene delivery complexes.

    abstract::Cationic liposomes spontaneously interact with negatively charged plasmid DNA to form a transfection competent complex capable of promoting the expression of a therapeutic gene. This work aims to improve the understanding of the poorly defined mechanisms and structural rearrangements associated with the lipid-DNA inte...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00117-9

    authors: Birchall JC,Kellaway IW,Mills SN

    更新日期:1999-06-25 00:00:00

  • Selection of high efficient transdermal lipid vesicle for curcumin skin delivery.

    abstract::Curcumin shows effective anti-inflammatory activities but is seldom used in clinic because of its poor solubility in water and vulnerablity to sunshine ultraviolet effect. Novel lipid vesicles have been developed as carriers for skin delivery. In this paper, lipid vesicles-propylene glycol liposomes (PGL), Ethosomes a...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.06.052

    authors: Zhao YZ,Lu CT,Zhang Y,Xiao J,Zhao YP,Tian JL,Xu YY,Feng ZG,Xu CY

    更新日期:2013-09-15 00:00:00

  • Nanoparticles of glycol chitosan and its thiolated derivative significantly improved the pulmonary delivery of calcitonin.

    abstract::A novel thiomer derivative of glycol chitosan (GCS) was synthesized by coupling with thioglycolic acid (TGA) and evaluated for the pulmonary delivery of peptides. Nanoparticles (NPs) based on GCS and GCS-TGA were obtained by the ionic gelation method and demonstrated a particle size in the range of 0.23-0.33 microm wi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.07.001

    authors: Makhlof A,Werle M,Tozuka Y,Takeuchi H

    更新日期:2010-09-15 00:00:00

  • Effect of preparation technique on the properties of liposomes encapsulating ketoprofen-cyclodextrin complexes aimed for transdermal delivery.

    abstract::The combined approach of cyclodextrin complexation and entrapment in liposomes was investigated in order to develop an effective topical formulation of ketoprofen. Equimolar complex of drug and hydroxypropyl-beta-cyclodextrin (HPbetaCyd) was added at different concentrations to the aqueous phase of liposomes consistin...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.12.047

    authors: Maestrelli F,González-Rodríguez ML,Rabasco AM,Mura P

    更新日期:2006-04-07 00:00:00

  • Solubility-physicochemical-thermodynamic theory of penetration enhancer mechanism of action.

    abstract::The hypothesis for the investigation was that the overall mechanism of action of skin penetration enhancers is best explained by the Solubility-Physicochemical-Thermodynamic (SPT) theory. To our knowledge, this is the first report of the application of SPT theory in transdermal/topical/enhancer research. The SPT theor...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118920

    authors: Haq A,Chandler M,Michniak-Kohn B

    更新日期:2020-02-15 00:00:00

  • Interplay of stimuli-responsiveness, drug loading and release for a surface-engineered dendrimer delivery system.

    abstract::The objectives of this study were to generate novel thermo and pH dual responsive poly(amidoamine) (PAMAM) via precise surface engineering, and investigate the interplay of dendrimer stimuli-responsiveness and the loading and release properties of a model agent, vitamin E acetate (VEAc). A higher dendrimer generation ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.12.031

    authors: Liu R,Sun M,Liu X,Fan A,Wang Z,Zhao Y

    更新日期:2014-02-28 00:00:00

  • Design and characterization of submicron formulation for a poorly soluble drug: the effect of Vitamin E TPGS and other solubilizers on skin permeability enhancement.

    abstract::In transdermal drug delivery systems (TDDS), it is a challenge to achieve stable and prolonged high permeation rates across the skin since the concentrations of the drug dissolved in the matrix have to be high in order to maintain zero order release kinetics. Several attempts have been reported to improve the permeabi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.05.031

    authors: Ghosh I,Michniak-Kohn B

    更新日期:2012-09-15 00:00:00

  • Powder, capsule and device: An imperative ménage à trois for respirable dry powders.

    abstract:OBJECTIVES:The development of inhaled products to treat or to prevent lung infection is a very active research field in drug delivery. The pulmonary route is extremely attractive but very challenging. This paper reports the study of excipient, capsule brand and device influence on the aerodynamic behavior of dry powder...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.08.012

    authors: Schoubben A,Blasi P,Giontella A,Giovagnoli S,Ricci M

    更新日期:2015-10-15 00:00:00

  • A novel formulation of solubilised amphotericin B designed for ophthalmic use.

    abstract::Amphotericin B (AmB) is a wide spectrum antifungal with low incidence of clinical resistance. However, there are no licensed topical formulations with AmB in most developed countries. Extemporaneous preparations of AmB are frequently prepared from available marketed parenteral formulations. Herein, a solution of AmB w...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.07.065

    authors: Serrano DR,Ruiz-Saldaña HK,Molero G,Ballesteros MP,Torrado JJ

    更新日期:2012-11-01 00:00:00

  • Physicochemical characterisation of liposomes with encapsulated local anaesthetics.

    abstract::Local anaesthetics may be added to intravenous o/w emulsions of propofol to reduce the initial pain of injection. Due to incompatibility problems of the emulsion on the addition of a local anaesthetic solution, prior encapsulation of the drug within liposomes is suggested. The liposomes were prepared with the sonicati...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.01.015

    authors: Müller M,Mackeben S,Müller-Goymann CC

    更新日期:2004-04-15 00:00:00

  • General procedure to aid the development of continuous pharmaceutical processes using multivariate statistical modeling - an industrial case study.

    abstract::Streamlining the manufacturing process has been recognized as a key issue to reduce production costs and improve safety in pharmaceutical manufacturing. Although data available from earlier developmental stages are often sparse and unstructured, they can be very useful to improve the understanding about the process un...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.01.018

    authors: Tomba E,De Martin M,Facco P,Robertson J,Zomer S,Bezzo F,Barolo M

    更新日期:2013-02-28 00:00:00

  • Multifunctional TK-VLPs nanocarrier for tumor-targeted delivery.

    abstract::Virus-like particles (VLPs) have been exploited for various biomedical applications, such as the monitoring, prevention, diagnosis and therapy of disease. In this study, a novel multifunctional VLPs nanocarrier (TK-VLPs) was prepared and used for tumor-targeted delivery. The SPR and cell uptake results indicated that ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.02.037

    authors: Ren Y,Mu Y,Jiang L,Yu H,Yang S,Zhang Y,Wang J,Zhang H,Sun H,Xiao C,Peng H,Zhou Y,Lu W

    更新日期:2016-04-11 00:00:00