当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF PHARMACEUTICS期刊下所有文献 > Development of enteric-coated fixed dose combinations of amorphous solid dispersions of ezetimibe and lovastatin: Investigation of formulation and process parameters.

Development of enteric-coated fixed dose combinations of amorphous solid dispersions of ezetimibe and lovastatin: Investigation of formulation and process parameters.

Abstract：

:Enteric-coated fixed-dose combinations of ezetimibe and lovastatin were prepared by fluid bed coating aiming to avoid the acidic conversion of lovastatin to its hydroxyacid derivative. In a two-step process, sucrose beads were layered with a glass solution of ezetimibe, lovastatin and Soluplus®, top-coated with an enteric layer. The impact of different bead size, enteric polymers (Eudragit L100® and Eudragit L100-55®) and coating time was investigated. Samples were evaluated by X-ray diffraction, scanning electron microscopy, laser diffraction and in vitro studies in 0.1M HCl and phosphate buffer pH 6.8. Results showed that smaller beads tend to agglomerate and release was jeopardized in acidic conditions, most likely due to irregular coating layer. Eudragit L100-55® required longer processing, but thinner coating layers provided lower drug release. Both polymers showed low drug release in acidic environment and fast release at pH 6.8. The off-line measurement of the coating thickness determined the ideal coating time as 15 and 30min for Eudragit L100-55® and Eudragit L100®-based samples, respectively. Both compounds were molecularly dispersed in Soluplus®, and Eudragit L100® formulations showed concave pores on the surface, presenting higher drug release in acidic conditions. Stability studies after 6 months showed unaltered physical properties and drug release.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Riekes MK,Dereymaker A,Berben P,Augustijns P,Stulzer HK,Van den Mooter G

doi

10.1016/j.ijpharm.2017.01.053

subject

Has Abstract

pub_date

2017-03-30 00:00:00

pages

49-58

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(17)30062-5

journal_volume

520

pub_type

杂志文章

相关文献

INTERNATIONAL JOURNAL OF PHARMACEUTICS文献大全
  • Cyclodextrin-containing poly(ethyleneoxide) tablets for the delivery of poorly soluble drugs: potential as buccal delivery system.

    abstract：:The aim of this work was to develop a tablet for the buccal delivery of the poorly soluble drug carvedilol (CAR), based on poly(ethyleneoxide) (PEO) as bioadhesive sustained-release platform and hydroxypropyl-beta-cyclodextrin (HPbetaCD) as modulator of drug release. As first, PEO tablets loaded with CAR/HPbetaCD bina...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2006.03.031

    authors： Cappello B,De Rosa G,Giannini L,La Rotonda MI,Mensitieri G,Miro A,Quaglia F,Russo R

    更新日期：2006-08-17 00:00:00

  • A combo-strategy to improve brain delivery of antiepileptic drugs: Focus on BCRP and intranasal administration.

    abstract：:The breast cancer resistance protein (BCRP) is an efflux transporter expressed at the apical surface of human brain endothelial cells of the blood-brain barrier (BBB). It was proposed as one of the transporters responsible for the development of drug resistance to several central nervous system (CNS) drugs, including ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.120161

    authors： Gonçalves J,Silva S,Gouveia F,Bicker J,Falcão A,Alves G,Fortuna A

    更新日期：2021-01-25 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

  • Poly(acrylic acid) microspheres containing beta-cyclodextrin: loading and in vitro release of two dyes.

    abstract：:Microspheres containing poly(acrylic acid) and beta-cyclodextrin or maltose were prepared by a w/o solvent evaporation technique. The dispersed aqueous phase contained poly(acrylic acid) (800 mg) and beta-cyclodextrin or maltose (0, 200 or 800 mg). Food-grade olive oil was the continuous phase. Microsphere particle si...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(99)00190-8

    authors： Bibby DC,Davies NM,Tucker IG

    更新日期：1999-10-05 00:00:00

  • Mixed backbone antisense glucosylceramide synthase oligonucleotide (MBO-asGCS) loaded solid lipid nanoparticles: in vitro characterization and reversal of multidrug resistance in NCI/ADR-RES cells.

    abstract：:In this study, solid lipid nanoparticles (SLN) loaded with MBO-asGCS oligonucleotide were prepared, characterized and evaluated for cytotoxicity against NCI/ADR-RES human ovary cancer cells. Two types of cetyltrimethyl ammonium bromide (CTAB) stabilized SLN, with or without ceramide VI, were prepared by mixed homogeni...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2010.08.044

    authors： Siddiqui A,Patwardhan GA,Liu YY,Nazzal S

    更新日期：2010-11-15 00:00:00

  • Synthesis, metabolism and cellular permeability of enzymatically stable dipeptide prodrugs of acyclovir.

    abstract：:The objective of this study was to synthesize and evaluate novel enzymatically stable dipeptide prodrugs for improved absorption of acyclovir. l-Valine-l-valine-acyclovir (LLACV), l-valine-d-valine-acyclovir (LDACV), d-valine-l-valine-acyclovir (DLACV) and d-valine-d-valine-acyclovir (DDACV) were successfully synthesi...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2008.05.024

    authors： Talluri RS,Samanta SK,Gaudana R,Mitra AK

    更新日期：2008-09-01 00:00:00

  • Encapsulation of azithromycin into polymeric microspheres by reduced pressure-solvent evaporation method.

    abstract：:Azithromycin loaded microspheres with blends of poly-l-lactide and ploy-D,L-lactide-co-glycolide as matrices were prepared by the atmosphere-solvent evaporation (ASE) and reduced pressure-solvent evaporation (RSE) method. Both the X-ray diffraction spectra and DSC thermographs demonstrated that poly-L-lactide existed ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2012.04.081

    authors： Li X,Chang S,Du G,Li Y,Gong J,Yang M,Wei Z

    更新日期：2012-08-20 00:00:00

  • Pulmonary drug delivery systems for tuberculosis treatment.

    abstract：:Tuberculosis (TB) remains a major global health problem as it is the second leading cause of death from an infectious disease worldwide, after the human immunodeficiency virus (HIV). Conventional treatments fail either because of poor patient compliance to the drug regimen or due to the emergence of multidrug-resistan...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2014.12.009

    authors： Pham DD,Fattal E,Tsapis N

    更新日期：2015-01-30 00:00:00

  • Pharmacokinetics and absolute bioavailability of oral cefuroxime axetil in the rat.

    abstract：:The objectives of this study were to determine the oral bioavailability of cefuroxime (C) and to evaluate the pharmacokinetic model that best describes the plasma concentration behaviour following single intravenous (IV), intraperitoneal (IP) and oral single doses. The same dose of C was administered by IV, IP and ora...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(00)00420-8

    authors： Ruiz-Carretero P,Nacher A,Merino-Sanjuan M,Casabo VG

    更新日期：2000-07-20 00:00:00

  • Ultrasonic real-time in-die monitoring of the tablet compaction process-a proof of concept study.

    abstract：:The mechanical properties of a drug tablet can affect its performance (e.g., dissolution profile and its physical robustness. An ultrasonic system for real-time in-die tablet mechanical property monitoring during compaction has been demonstrated. The reported set-up is a proof of concept compaction monitoring system w...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2012.09.014

    authors： Stephens JD,Kowalczyk BR,Hancock BC,Kaul G,Cetinkaya C

    更新日期：2013-02-14 00:00:00

  • Microencapsulation of amorphous solid dispersions of fenretinide enhances drug solubility and release from PLGA in vitro and in vivo.

    abstract：:The purpose of this study was to develop solid dispersions of fenretinide(4HPR), incorporate them into poly(lactic-co-glycolic)(PLGA) millicylindrical implants, and evaluate the resulting implants in vitro and in vivo for future applications in oral cancer chemoprevention. Due to the extreme hydrophobicity of 4HPR, 4H...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119475

    authors： Nieto K,Mallery SR,Schwendeman SP

    更新日期：2020-08-30 00:00:00

  • Tissue slice model of human lung cancer to investigate telomerase inhibition by nanoparticle delivery of antisense 2'-O-methyl-RNA.

    abstract：:Nanoparticles delivery of oligonucleotides represents a potential approach for cancer treatment. However, most of the experiments were based on established cancer cell lines and may not reflect the original solid tumor in vivo. Both, tumor microenvironment and tumor cell biological properties in the tumor can influenc...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.07.009

    authors： Dong M,Philippi C,Loretz B,Nafee N,Schaefer UF,Friedel G,Ammon-Treiber S,Griese EU,Lehr CM,Klotz U,Mürdter TE

    更新日期：2011-10-31 00:00:00

  • Comparative study of Pluronic(®) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats.

    abstract：:Liposomes modified using cationic and hydrophilic nonionic polymers are 2 popular carriers for improving oral drug absorption. Cationic polymer-modified liposomes can adhere to the intestinal wall mucus (mucoadhesive type), while liposomes modified using hydrophilic nonionic polymers can penetrate across the mucus bar...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2013.04.002

    authors： Chen D,Xia D,Li X,Zhu Q,Yu H,Zhu C,Gan Y

    更新日期：2013-06-05 00:00:00

  • Utilization of colorimetric and atomic absorption spectrometric determination of aztreonam through ion pair complex formation.

    abstract：:Three rapid and sensitive, colorimetric and atomic absorption spectrometric methods were developed for the determination of aztreonam. The proposed methods depend upon the reaction of cobaltthiocyanate (I) or reineckate (II) ions with the drug to form stable ion-pair complexes which extractable with chloroform. The gr...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(00)00467-1

    authors： Amin AS,Aly HM

    更新日期：2000-09-15 00:00:00

  • Chitosan/cyclodextrin nanoparticles as macromolecular drug delivery system.

    abstract：:The aim of this study was to generate a new type of nanoparticles made of chitosan (CS) and carboxymethyl-beta-cyclodextrin (CM-beta-CD) and to evaluate their potential for the association and delivery of macromolecular drugs. CS and CM-beta-CD or mixtures of CM-beta-CD/tripolyphosphate (TPP) were processed to nanopar...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.03.005

    authors： Krauland AH,Alonso MJ

    更新日期：2007-08-01 00:00:00

  • Characterisation and stability studies of a hydrophilic decapeptide in different adjuvant drug delivery systems: a comparative study of PLGA nanoparticles versus chitosan-dextran sulphate microparticles versus DOTAP-liposomes.

    abstract：:Poly[lactic-co-glycolide] (PLGA) nanoparticles, chitosan-dextran sulphate microparticles, and DOTAP-liposomes were prepared as vaccine adjuvants and drug carriers for a small hydrophilic model peptide, and their different physico-chemical properties (size, PDI, zeta-potential, pH-value and peptide loading) were invest...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.09.011

    authors： Wieber A,Selzer T,Kreuter J

    更新日期：2011-12-12 00:00:00

  • Effects of carriers on transgene expression from plasmids containing a DNA sequence with high histone affinity.

    abstract：:The intranuclear disposition of plasmid DNA is highly important for transgene expression. The effects of a left-handedly curved sequence with high histone affinity on transgene expression were examined in COS-7 cells with two kinds of carriers (Lipofectamine Plus and TransIT-LT1). Three plasmids containing the curved ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2009.04.032

    authors： Kamiya H,Fukunaga S,Ohyama T,Harashima H

    更新日期：2009-07-06 00:00:00

  • An apolipoprotein E modified liposomal nanoparticle: ligand dependent efficiency as a siRNA delivery carrier for mouse-derived brain endothelial cells.

    abstract：:A disorder in the brain endothelium is thought to be closely related to the pathophysiology of brain diseases. A method for delivering nucleic acids (i.e. short interference RNA; siRNA) to the brain endothelium should be an attractive strategy for curing brain disorders. A liposomal nanoparticle containing a proton-io...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2014.02.016

    authors： Tamaru M,Akita H,Kajimoto K,Sato Y,Hatakeyama H,Harashima H

    更新日期：2014-04-25 00:00:00

  • Discrete particle modeling and micromechanical characterization of bilayer tablet compaction.

    abstract：:A mechanistic particle scale model is proposed for bilayer tablet compaction. Making bilayer tablets involves the application of first layer compaction pressure on the first layer powder and a second layer compaction pressure on entire powder bed. The bonding formed between the first layer and the second layer particl...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2017.07.032

    authors： Yohannes B,Gonzalez M,Abebe A,Sprockel O,Nikfar F,Kiang S,Cuitiño AM

    更新日期：2017-08-30 00:00:00

  • Detection and characterization of protein aggregates by fluorescence microscopy.

    abstract：:Aggregation may compromise the stability as well as the biological activity of protein drugs. Detection of protein aggregates is needed in the process of protein characterization and during optimization of pharmaceutical formulations. This paper describes a technique, which consists of analysing protein aggregates by ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2006.08.024

    authors： Demeule B,Gurny R,Arvinte T

    更新日期：2007-02-01 00:00:00

  • Critical quality attributes, in vitro release and correlated in vitro skin permeation-in vivo tape stripping collective data for demonstrating therapeutic (non)equivalence of topical semisolids: A case study of "ready-to-use" vehicles.

    abstract：:This work aimed to prove the ability of "ready-to-use" topical vehicles based on alkyl polyglucoside-mixed emulsifier (with/without co-solvent modifications) to replace the conventionally used pharmacopoeial bases (e.g., non-ionic hydrophilic cream) in compounding practice. For this purpose, considering the regulatory...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2017.06.018

    authors： Ilić T,Pantelić I,Lunter D,Đorđević S,Marković B,Ranković D,Daniels R,Savić S

    更新日期：2017-08-07 00:00:00

  • Ex vivo skin permeation and retention studies on chitosan-ibuprofen-gellan ternary nanogel prepared by in situ ionic gelation technique--a tool for controlled transdermal delivery of ibuprofen.

    abstract：:The chemical potentials of drug-polymer electrostatic interaction have been utilized to develop a novel ternary chitosan-ibuprofen-gellan nanogel as controlled transdermal delivery tool for ibuprofen. The ternary nanogels were prepared by a combination of electrostatic nanoassembly and ionic gelation techniques. The e...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2015.05.030

    authors： Abioye AO,Issah S,Kola-Mustapha AT

    更新日期：2015-07-25 00:00:00

  • Design and characterization of a perivascular PLGA coated PET mesh sustaining the release of atorvastatin for the prevention of intimal hyperplasia.

    abstract：:Following vascular bypass interventions, autologous saphenous vein grafts are prone to fail due to intimal hyperplasia development. An atorvastatin (ATV)-eluting tubular mesh coated with poly(d,l-lactide-co-glycolisde) acid (PLGA) was designed for perivascular application, in order to prevent the development of this p...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2017.12.026

    authors： Mylonaki I,Trosi O,Allémann E,Durand M,Jordan O,Delie F

    更新日期：2018-02-15 00:00:00

  • Vascular targeting of doxorubicin using cationic liposomes.

    abstract：:Tumor vessel has been recognized as an important target for anticancer therapy. Cationic liposomes have been shown to selectively target tumor endothelial cells, thus can potentially be used as a carrier for chemotherapy agents. In this study, cationic liposomes containing 20 mol% cationic lipid dimethyl dioctadecyl a...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.01.003

    authors： Wu J,Lee A,Lu Y,Lee RJ

    更新日期：2007-06-07 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

  • Dual-responsive lidocaine in situ gel reduces pain of intrauterine device insertion.

    abstract：:The most effective and safe contraceptive method, intrauterine devices (IUDs), is still underutilized due to the pain barrier during IUD insertion. Lidocaine, a well-known local anesthetic, can be used to relieve IUD insertion pain. This study aimed at formulation, in vitro, in vivo and clinical evaluation of a novel ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,随机对照试验

    doi：10.1016/j.ijpharm.2018.01.033

    authors： Abd Ellah NH,Abouelmagd SA,Abbas AM,Shaaban OM,Hassanein KMA

    更新日期：2018-03-01 00:00:00

  • 125I used for labelling of proteins in an absorption model changes the absorption rate of insulin aspart.

    abstract：UNLABELLED:The aim of this study is to validate the ability of the disappearance model to predict absorption rates of insulin aspart in pigs. The disappearance model is used as a screening tool to estimate absorption rates after subcutaneous injections in humans or pigs especially of insulin and insulin analogues. The ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2006.09.004

    authors： Sohoel A,Plum A,Frokjaer S,Thygesen P

    更新日期：2007-02-07 00:00:00

  • Glucan particles as suitable carriers for the natural anti-inflammatory compounds curcumin and diplacone - Evaluation in an ex vivo model.

    abstract：:Natural compounds offer a wide spectrum of potential active substances, but often they have a poor bioavailability. To increase the bioavailability and bioactivity of the natural anti-inflammatory molecules curcumin and diplacone, we used glucan particles (GPs), hollow shells from Saccharomyces cerevisiae composed mai...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119318

    authors： Rotrekl D,Devriendt B,Cox E,Kavanová L,Faldyna M,Šalamúnová P,Baďo Z,Prokopec V,Štěpánek F,Hanuš J,Hošek J

    更新日期：2020-05-30 00:00:00

  • Design of a dissolution system for the evaluation of the release rate characteristics of artemether and dihydroartemisinin from tablets.

    abstract：:As none of the pharmacopoeial dissolution methods are suitable to evaluate the release rate of artemether and dihydroartemisinin from tablets, a 'two-phase partition-dissolution' method, based on the one of [J. Pharm. Sci. 85 (1996) 1060] was developed. It consists of an organic solvent in the upper part and the aqueo...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2004.01.022

    authors： Gabriëls M,Plaizier-Vercammen J

    更新日期：2004-04-15 00:00:00

  • Effect of nicotinamide on the properties of aqueous HPMC solutions.

    abstract：:The effect of nicotinamide on the properties of aqueous hydroxypropylmethylcellulose (HPMC) solutions was studied. Rheological studies showed that solutions of HPMC of concentration less than 3.0 w/v.% did not form gels and exhibited Newtonian flow patterns at 25 degrees C. The inclusion of nicotinamide increased the ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(01)00770-0

    authors： Hino T,Ford JL

    更新日期：2001-09-11 00:00:00