Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation.

Abstract:

:Conventional manufacturing of pharmaceutical tablets often involves single processes such as blending, granulation, milling and direct compression. A process that minimizes and incorporates all these in a single continuous step is desirable. The concept of omitting milling step followed by direct-molding of tablets utilizing a twin-screw extruder in a melt granulation process using thermoplastic binders was explored. The objective of this study was to investigate the effect of combining hydrophilic binder (HPMC K4M, PEO 1M), and hydrophobic binder (Compritol® ATO 888, Precirol® ATO 5) on the release profiles of direct-molded tablets and direct-compressed tablets from milled extrudates using a quality-by-design approach. It was identified that hydrophilic binder type and process significantly affects (p=0.005) the release profiles of verapamil. Moreover, two-way interaction analysis demonstrated that the combination of process with type of hydrophilic polymer (p=0.028) and the type of hydrophilic polymer with polymer ratio (p=0.033) significantly affected the release profiles. The formulation release kinetics correlated to Higuchi release model and the mechanism correlated to a non-Fickian release mechanism. The results of the present study indicated that direct-molded tablets with different release profiles can be manufactured without milling process and through a continuous melt granulation using twin-screw extruder with appropriate thermoplastic binder ratio.

journal_name

Int J Pharm

authors

Tan DC,Chin WW,Tan EH,Hong S,Gu W,Gokhale R

doi

10.1016/j.ijpharm.2013.12.053

subject

Has Abstract

pub_date

2014-03-10 00:00:00

pages

89-97

issue

1

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(13)01129-0

journal_volume

463

pub_type

杂志文章
  • Application of a colorimetric technique in quality control for printed pediatric orodispersible drug delivery systems containing propranolol hydrochloride.

    abstract::The feasibility of a colorimetric technique was investigated in CIELAB color space as an analytical quality control method for content uniformity of printed orodispersible pediatric delivery systems. Inkjet printing was utilized to fabricate orodispersibe film formulations containing propranolol hydrochloride in a col...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.07.032

    authors: Vakili H,Nyman JO,Genina N,Preis M,Sandler N

    更新日期:2016-09-10 00:00:00

  • Chitosomes as drug delivery systems for C-phycocyanin: preparation and characterization.

    abstract::The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH-XG-microcomplexes were prepared in aqueous lactic acid at diffe...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.03.038

    authors: Manconi M,Mura S,Manca ML,Fadda AM,Dolz M,Hernandez MJ,Casanovas A,Díez-Sales O

    更新日期:2010-06-15 00:00:00

  • Does ciprofloxacin interact with neutral bilayers? An aspect related to its antimicrobial activity.

    abstract::Ciprofloxacin (CPX) physicochemical properties, mainly hydrophobicity and microspeciation, appear to be related with the ability of this drug to adsorb and diffuse through lipid environments. We have combined the information from fluorescence anisotropy, quenching and epifluorescence of phospholipid monolayers, to exp...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00633-6

    authors: Hernández-Borrell J,Montero MT

    更新日期:2003-02-18 00:00:00

  • Design, synthesis and evaluation of N-acetyl glucosamine (NAG)-PEG-doxorubicin targeted conjugates for anticancer delivery.

    abstract::Efficacy of anticancer drug is limited by the severe adverse effects induced by drug; therefore the crux is in designing delivery systems targeted only to cancer cells. Toward this objectives, we propose, synthesis of poly(ethylene glycol) (PEG)-doxorubicin (DOX) prodrug conjugates consisting N-acetyl glucosamine (NAG...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.05.078

    authors: Pawar SK,Badhwar AJ,Kharas F,Khandare JJ,Vavia PR

    更新日期:2012-10-15 00:00:00

  • Self-double-emulsifying drug delivery system (SDEDDS): a new way for oral delivery of drugs with high solubility and low permeability.

    abstract::Water-in-oil-in-water (w/o/w) double emulsions are potential for enhancing oral bioavailability of drugs with high solubility and low permeability, but their industrial application is limited due to the instability. Herein, we developed a novel formulation, self-double-emulsifying drug delivery systems (SDEDDS) by for...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.02.047

    authors: Qi X,Wang L,Zhu J,Hu Z,Zhang J

    更新日期:2011-05-16 00:00:00

  • Influence of surface charge and inner composition of porous nanoparticles to cross blood-brain barrier in vitro.

    abstract::The aim of these studies was to evaluate the binding, uptake and transcytosis of 60 nm porous nanoparticles (NPs) that differed in their surface charge and inner composition on the blood-brain barrier (BBB). They were prepared from maltodextrins derived with or without a cationic ligand. In the cationic NPs an anionic...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.06.023

    authors: Jallouli Y,Paillard A,Chang J,Sevin E,Betbeder D

    更新日期:2007-11-01 00:00:00

  • Dissolution from solid lipid extrudates containing release modifiers.

    abstract::The influence of different types of release modifiers on the dissolution from solid lipid extrudates was investigated. Diprophylline was extruded together with 45% tristearin and 5% (w/w) of a release modifier to suitable extrudates. Three groups of release modifiers were defined: Hydrocolloids, disintegrants and pore...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.04.010

    authors: Güres S,Kleinebudde P

    更新日期:2011-06-30 00:00:00

  • Aerosolized semifluorinated alkanes as excipients are suitable for inhalative drug delivery--a pilot study.

    abstract::Semifluorinated alkanes (SFAs) have been described as potential excipients for pulmonary drug delivery, but proof of their efficacy is still lacking. We tested whether SFA formulations with the test drug ibuprofen can be nebulised and evaluated their pharmacokinetics. Physico-chemical properties of five different ibup...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.10.051

    authors: Tsagogiorgas C,Jung T,Krebs J,Theisinger B,Beck G,Yard BA,Quintel M

    更新日期:2012-01-17 00:00:00

  • Search for technological reasons to develop a capsule or a tablet formulation with respect to wettability and dissolution.

    abstract::Proquazone, a poorly wettable compound, was used as a model drug in the search for reasons to develop a capsule or tablet formulation. The capsules were filled with proquazone as active ingredient, with lactose monohydrate (200 mesh) as filler and with magnesium stearate as lubricant. The tablet was made out of a gran...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.09.006

    authors: von Orelli J,Leuenberger H

    更新日期:2004-12-09 00:00:00

  • Chitosan-graft-polyethylenimine for Akt1 siRNA delivery to lung cancer cells.

    abstract::Efficient delivery of small interfering RNA (siRNA) remains a challenging task in RNA interference (RNAi) studies. In this study, we used chitosan-graft-polyethylenimine (CHI-g-PEI) copolymer composed of chitosan and low molecular weight polyethylenimine (PEI) for the delivery of siRNA. The CHI-g-PEI carrier formed st...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.05.046

    authors: Jere D,Jiang HL,Kim YK,Arote R,Choi YJ,Yun CH,Cho MH,Cho CS

    更新日期:2009-08-13 00:00:00

  • Strategies for bringing drug delivery tools into discovery.

    abstract::The past decade has yielded a significant body of literature discussing approaches for development and discovery collaboration in the pharmaceutical industry. As a result, collaborations between discovery groups and development scientists have increased considerably. The productivity of pharma companies to deliver new...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2011.03.024

    authors: Kwong E,Higgins J,Templeton AC

    更新日期:2011-06-30 00:00:00

  • Squalene-based nanoparticles for the targeting of atherosclerotic lesions.

    abstract::Native low-density lipoproteins (LDL) naturally accumulate at atherosclerotic lesions and are thought to be among the main drivers of atherosclerosis progression. Numerous nanoparticular systems making use of recombinant lipoproteins have been developed for targeting atherosclerotic plaque. These innovative formulatio...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119282

    authors: Brusini R,Dormont F,Cailleau C,Nicolas V,Peramo A,Varna M,Couvreur P

    更新日期:2020-05-15 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

  • The dispersion behaviour of dry powder inhalation formulations cannot be assessed at a single inhalation flow rate.

    abstract::The dispersion performances of inhalation powders are often tested at only one inhalation flow rate in mechanistic formulation studies. This limited approach is challenged by studies showing that interactions exist between inhalation flow rate and the effects on dispersion performance of several formulation variables....

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.02.024

    authors: Grasmeijer F,de Boer AH

    更新日期:2014-04-25 00:00:00

  • Preparation of poly(DL-lactide-co-glycolide) nanoparticles by modified spontaneous emulsification solvent diffusion method.

    abstract:PURPOSE:The objectives of this study were to establish a new preparation method for poly(DL-lactide-co-glycolide) (PLGA) nanoparticles by modifying the spontaneous emulsification solvent diffusion (SESD) method and to elucidate the mechanism of nanoparticle formation on the basis of the phase separation principle of PL...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00187-8

    authors: Murakami H,Kobayashi M,Takeuchi H,Kawashima Y

    更新日期:1999-10-05 00:00:00

  • Chitosan-magnesium aluminum silicate composite dispersions: characterization of rheology, flocculate size and zeta potential.

    abstract::Composite dispersions of chitosan (CS), a positively charged polymer, and magnesium aluminum silicate (MAS), a negatively charged clay, were prepared and rheology, flocculate size and zeta potential of the CS-MAS dispersions were investigated. High and low molecular weights of CS (HCS and LCS, respectively) were used ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.09.038

    authors: Khunawattanakul W,Puttipipatkhachorn S,Rades T,Pongjanyakul T

    更新日期:2008-03-03 00:00:00

  • Gastro-floating tablets of cephalexin: preparation and in vitro/in vivo evaluation.

    abstract::Gastro-floating tablets of cephalexin were developed to prolong the residence time in major absorption sites. Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in terms of floating ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.05.011

    authors: Yin L,Qin C,Chen K,Zhu C,Cao H,Zhou J,He W,Zhang Q

    更新日期:2013-08-16 00:00:00

  • Suppression of agglomeration in fluidized bed coating. II. Measurement of mist size in a fluidized bed chamber and effect of sodium chloride addition on mist size.

    abstract::It has been reported that the degree of particle agglomeration in fluidized bed coating is greatly affected by the spray mist size of coating solution. However, the mist size has generally been measured in open air, and few reports have described the measurement of the mist size in a chamber of the fluidized bed, in w...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(98)00370-6

    authors: Yuasa H,Nakano T,Kanaya Y

    更新日期:1999-02-01 00:00:00

  • Quaternization enhances the transgene expression efficacy of aminoglycoside-derived polymers.

    abstract::The objective of the present study was to synthesize and investigate the transgene expression efficacy of quaternized derivatives of aminoglycoside polymers in different cancer cell lines. A series of glycidyltrimethylammonium chloride (GTMAC) derivatives of aminoglycoside polymers (GTMAC-AM polymers), containing vary...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.04.026

    authors: Miryala B,Feng Y,Omer A,Potta T,Rege K

    更新日期:2015-07-15 00:00:00

  • Solid lipid nanoparticles suspension versus commercial solutions for dermal delivery of minoxidil.

    abstract::Solid lipid nanoparticles have been reported as possible carrier for skin drug delivery. Solid lipid nanoparticles are produced from biocompatible and biodegradable lipids. Solid lipid nanoparticles made of semi-synthetic triglycerides stabilized with a mixture of polysorbate and sorbitan oleate were loaded with 5% of...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.06.014

    authors: Padois K,Cantiéni C,Bertholle V,Bardel C,Pirot F,Falson F

    更新日期:2011-09-15 00:00:00

  • Enhanced brain accumulation of pazopanib by modulating P-gp and Bcrp1 mediated efflux with canertinib or erlotinib.

    abstract::Primary objective of this investigation was to delineate the differential impact of efflux transporters P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp1/Abcg2) on brain disposition and plasma pharmacokinetics of pazopanib. In addition, this research investigated whether inhibition of these efflu...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.05.038

    authors: Minocha M,Khurana V,Qin B,Pal D,Mitra AK

    更新日期:2012-10-15 00:00:00

  • Pluronic gels for nasal delivery of Vitamin B12. Part I: preformulation study.

    abstract::Thermoreversible nasal gels of Vitamin B(12) using pluronic PF 127 were aimed to improve absorption and patient compliance. In the present research work, effects of Vitamin B(12) and gel additives, viz. PF concentration, osmolarity, polyethylene glycol (PEG 15000) on thermodynamic properties of phase transitions at ge...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2003.10.005

    authors: Pisal SS,Paradkar AR,Mahadik KR,Kadam SS

    更新日期:2004-02-11 00:00:00

  • A substrate pharmacophore for the human sodium taurocholate co-transporting polypeptide.

    abstract::Human sodium taurocholate co-transporting polypeptide (NTCP) is the main bile acid uptake transporter in the liver with the capability to translocate xenobiotics. While its inhibitor requirements have been recently characterized, its substrate requirements have not. The objectives of this study were (a) to elucidate N...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.11.022

    authors: Dong Z,Ekins S,Polli JE

    更新日期:2015-01-15 00:00:00

  • Formulation of sustained release nanoparticles loaded with a tripentone, a new anticancer agent.

    abstract::The purpose of the present work is to develop nanoparticles of a new antitubulin agent of the family of tripentones by means of a phase inversion process. Dynamic light scattering, transmission electron microscopy and zeta-potential measurements were used to characterize tripentone loaded nanoparticles. From interfaci...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.04.007

    authors: Malzert-Fréon A,Vrignaud S,Saulnier P,Lisowski V,Benoît JP,Rault S

    更新日期:2006-08-31 00:00:00

  • Influence of methyl-beta-cyclodextrin and liposomes on rheological properties of Carbopol 974P NF gels.

    abstract::The influence of positively-charged and sterically stabilized liposomes and/or methyl-beta-cyclodextrin on rheological properties of Carbopol 974P NF hydrogels was investigated. All formulations have displayed a shear-thinning behavior of Carbopol gels, and the rate stress as a function of the shear rate was fitted us...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00683-x

    authors: Boulmedarat L,Grossiord JL,Fattal E,Bochot A

    更新日期:2003-03-18 00:00:00

  • A novel particle engineering technology: spray-freezing into liquid.

    abstract::Spray-freezing into liquid (SFL) is a novel particle engineering technology where a feed solution containing an active pharmaceutical ingredient (API) and pharmaceutical excipient(s) is atomized beneath the surface of a cryogenic liquid, such as liquid nitrogen. Intense atomization results from the impingement that oc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00154-0

    authors: Rogers TL,Hu J,Yu Z,Johnston KP,Williams RO 3rd

    更新日期:2002-08-21 00:00:00

  • Polymeric micelles for the solubilization and delivery of STAT3 inhibitor cucurbitacins in solid tumors.

    abstract::Poly(ethylene oxide)-block-poly(epsilon-caprolactone) (PEO-b-PCL) and newly developed poly(ethylene oxide)-block-poly(alpha-benzyl carboxylate epsilon-caprolactone) (PEO-b-PBCL) micelles were evaluated for the solubilization and delivery of cucurbitacin I and B, poorly water soluble inhibitors of signal transducer and...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.06.032

    authors: Molavi O,Ma Z,Mahmud A,Alshamsan A,Samuel J,Lai R,Kwon GS,Lavasanifar A

    更新日期:2008-01-22 00:00:00

  • The solubility, permeability and the dose as key factors in formulation development for oral lipophilic drugs: Maximizing the bioavailability of carbamazepine with a cosolvent-based formulation.

    abstract::The purpose of this research was to investigate drug dose, solubility, permeability, and their interplay, as key factors in oral formulation development for lipophilic drugs. A PEG400-based formulation was studied for five doses of the lipophilic drug carbamazepine, accounting for biorelevant dissolution of the dose i...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119307

    authors: Fine-Shamir N,Beig A,Miller JM,Dahan A

    更新日期:2020-05-30 00:00:00

  • Transdermal iontophoresis of ranitidine: an opportunity in paediatric drug therapy.

    abstract::The objective of this study was to examine the use of transdermal iontophoresis for the delivery of ranitidine hydrochloride in children. Constant, direct current, anodal iontophoresis of ranitidine was performed in vitro across dermatomed pig skin. The effect of donor vehicle, current intensity, and drug concentratio...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.03.006

    authors: Djabri A,Guy RH,Delgado-Charro MB

    更新日期:2012-10-01 00:00:00

  • Evaluation of the transdermal permeation of different paraben combinations through a pig ear skin model.

    abstract::Although parabens have several features of ideal preservatives, different studies have shown that they may affect human health due to their estrogenic activity. Therefore, various strategies have been applied to reduce their skin penetration. However, the effect of paraben combinations on transdermal permeation has no...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.02.006

    authors: Caon T,Costa AC,de Oliveira MA,Micke GA,Simões CM

    更新日期:2010-05-31 00:00:00