当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF PHARMACEUTICS期刊下所有文献 > Enhanced solid-state stability of amorphous ibrutinib formulations prepared by hot-melt extrusion.

Enhanced solid-state stability of amorphous ibrutinib formulations prepared by hot-melt extrusion.

Abstract：

:One of the applications of Hot-Melt Extrusion (HME) is the stabilization of amorphous drugs through its incorporation into polymeric blends in the form of Amorphous Solid Dispersions (ASDs). In this study, HME was applied to solve a real problem in the development of an ibrutinib product, stabilizing the amorphous form. A systematic approach was followed by combining theoretical calculations, high-throughput screening (HTS) focused on physical stability and Principal Components Analysis (PCA). The HTS enabled the evaluation of 33 formulations for physical stability and the PCA was key to select four promising systems. The low relevance of drug loading on the drug crystallization supported the HME tests with a very high drug load of 50%. Milled extrudates were characterized and demonstrated to be fully amorphous. The thermal analysis detected a glass transition temperature much higher than the predicted values. Along with several weak intermolecular interactions detected in Raman spectroscopy, a dipolar interaction involving the α, β unsaturated ketone function of ibrutinib was also noticed. The additive effect of these intermolecular interactions changed markedly the performance of the ASDs. The physical strength of the prepared systems was corroborated by stability studies until 6 months at long-term and accelerated conditions.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Simões MF,Nogueira BA,Tabanez AM,Fausto R,Pinto RMA,Simões S

doi

10.1016/j.ijpharm.2020.119156

subject

Has Abstract

pub_date

2020-04-15 00:00:00

pages

119156

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(20)30140-X

journal_volume

579

pub_type

杂志文章

相关文献

INTERNATIONAL JOURNAL OF PHARMACEUTICS文献大全
  • Transdermal iontophoretic delivery of terbinafine hydrochloride: quantitation of drug levels in stratum corneum and underlying skin.

    abstract：:The objective of this study was to determine the effect of iontophoresis on the delivery of terbinafine hydrochloride (4%, w/w) into and across hairless rat skin. In vitro skin uptake and permeation studies were performed using Franz diffusion cells. Anodal iontophoresis was applied for 1h at current densities of 0.2,...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2009.12.029

    authors： Sachdeva V,Siddoju S,Yu YY,Kim HD,Friden PM,Banga AK

    更新日期：2010-03-30 00:00:00

  • In vivo study of an instantly formed lipid-water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate.

    abstract：:We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1 min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2013.05.047

    authors： Evenbratt H,Jonsson C,Faergemann J,Engström S,Ericson MB

    更新日期：2013-08-16 00:00:00

  • Amino acid based amphiphilic copolymer micelles as carriers of non-steroidal anti-inflammatory drugs: solubilization, in vitro release and biological evaluation.

    abstract：:Three novel amino acid based anionic amphiphilic copolymers poly(sodium N-acryloyl-l-valinate-co-alkylacrylamide) (where, alkyl=octyl and dodecyl) with either 9 or 16 mol% hydrophobic substitution were synthesized. These hydrophobically modified polyelectrolytes (HMPs), above a critical concentration, self-assemble in...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.01.041

    authors： Dutta P,Dey J,Perumal V,Mandal M

    更新日期：2011-04-04 00:00:00

  • Pediatric oral formulation of dendrimer-N-acetyl-l-cysteine conjugates for the treatment of neuroinflammation.

    abstract：:N-Acetyl-l-cysteine (NAC) commonly used as an antidote in acetaminophen poisoning has shown promise in the treatment of neurological disorders such as cerebral palsy (CP). However, NAC suffers from drawbacks such as poor oral bioavailability and suboptimal blood-brain-barrier (BBB) permeability limiting its clinical s...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2018.04.040

    authors： Yellepeddi VK,Mohammadpour R,Kambhampati SP,Sayre C,Mishra MK,Kannan RM,Ghandehari H

    更新日期：2018-07-10 00:00:00

  • Development of enteric polymer-based microspheres by spray-drying for colonic delivery of Lactobacillus rhamnosus GG.

    abstract：:Antibiotics are well-known disruptive elements of the intestinal microbiota and antibiotic-associated diarrhea appeared as the most common complication related with post-antibiotic dysbiosis. Lactobacillus rhamnosus GG (LGG) strain is very effective in preventing antibiotic-associated diarrhea in children and adults. ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119414

    authors： Akanny E,Bourgeois S,Bonhommé A,Commun C,Doleans-Jordheim A,Bessueille F,Bordes C

    更新日期：2020-06-30 00:00:00

  • Effect of the surface free energy of materials on the lamination tendency of bilayer tablets.

    abstract：:Dosage forms with fixed dose combinations of drugs is a frequent and advantageous mode of administration, but their production involves a number of technological problems. Numerous interactions in a homogeneous vehicle may be avoided through the use of layered tablets. The mechanical properties of these dosage forms d...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2015.10.061

    authors： Papós K,Kása P Jr,Ilič I,Blatnik-Urek S,Regdon G Jr,Srčič S,Pintye-Hódi K,Sovány T

    更新日期：2015-12-30 00:00:00

  • Enhancing bioavailability through thermal processing.

    abstract：:Formulation intervention, through the application of processing technologies, is a requirement for enabling therapy for the vast majority of drugs. Without these enabling technologies, poorly soluble drugs may not achieve therapeutic concentrations in the blood or tissue of interest. Conversely, freely soluble and/or ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2013.04.042

    authors： Keen JM,McGinity JW,Williams RO 3rd

    更新日期：2013-06-25 00:00:00

  • Encapsulation of NSAIDs for inflammation management: Overview, progress, challenges and prospects.

    abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely prescribed drugs. Debilitating diseases such as rheumatoid arthritis and osteoarthritis are commonly managed by NSAIDs. However, NSAIDs pharmacological mechanism is often associated with the presence of gastrointestinal side effects. NSAIDs encap...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2016.11.002

    authors： Badri W,Miladi K,Nazari QA,Greige-Gerges H,Fessi H,Elaissari A

    更新日期：2016-12-30 00:00:00

  • Development and in vitro evaluation of a self-emulsifying drug delivery system (SEDDS) for oral vancomycin administration.

    abstract：:The aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the glycopeptide antibiotic vancomycin (VAN) with improved intestinal mucosa permeating properties in order to increase oral drug absorption. VAN was effectively incorporated into SEDDS increasing the lipophilicity of the d...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2018.11.010

    authors： Zaichik S,Steinbring C,Caliskan C,Bernkop-Schnürch A

    更新日期：2019-01-10 00:00:00

  • Improved oral bioavailability and anticancer efficacy on breast cancer of paclitaxel via Novel Soluplus(®)-Solutol(®) HS15 binary mixed micelles system.

    abstract：:The aim of this study was to develop a novel drug delivery system using two biocompatible copolymers of Solutol(®)HS15 and Soluplus(®) to improve solubility, oral bioavailability and anticancer activity of paclitaxel (PTX). The PTX-loaded mixed micelles (PTX-M) were prepared by ethanol thin-film hydration method. The ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2016.08.045

    authors： Hou J,Sun E,Sun C,Wang J,Yang L,Jia XB,Zhang ZH

    更新日期：2016-10-15 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

  • In vitro and in vivo degradation behavior and the long-term performance of biodegradable PLCL balloon implants.

    abstract：:Biodegradable poly(l-lactide-co-ε-caprolactone) (PLCL) are used to prepare inflatable balloon implants in treating rotator-cuff injuries and tissue separation. These balloon implants act as a temporary spacer for tissues, while reducing pain and allowing rehabilitation after surgery. It is essential to ensure that eac...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2019.118870

    authors： Haim Zada M,Kumar A,Elmalak O,Markovitz E,Icekson R,Domb AJ

    更新日期：2020-01-25 00:00:00

  • In vivo antiviral activity of ribavirin/alpha-cyclodextrin complex: evaluation on experimental measles virus encephalitis in mice.

    abstract：:Intracranial injection of the rodent adapted CAM/RB strain of measles virus (MV) induces encephalitis in CBA/ca mice. It has already been shown that cyclodextrins can be used as carriers to increase the antiviral activity of ribavirin (RBV) against MV in cellular model. In this study, the antiviral activity of a RBV/a...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2008.01.043

    authors： Jeulin H,Grancher N,Kedzierewicz F,Finance C,Le Faou AE,Venard V

    更新日期：2008-06-05 00:00:00

  • Induction of apoptosis of human lung carcinoma cells by hybrid liposomes containing polyoxyethylenedodecyl ether.

    abstract：:Hybrid liposomes can be prepared by simply ultrasonicating a mixture of vesicular and micellar molecules in aqueous solution. A clear solution of hybrid liposomes composed of 90 mol% dimyristoylphosphatidylcholine (DMPC) and 10 mol% polyoxyethylene(23)dodecyl ether (C12(EO)23) having a hydrodynamic diameter of 100-120...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2004.11.034

    authors： Iwamoto Y,Matsumoto Y,Ueoka R

    更新日期：2005-03-23 00:00:00

  • Public engagement workshop: how to improve medicines for older people?

    abstract：:Public engagement in medication management has become more and more important in promoting population health. A public engagement workshop attended by 78 members of the geriatric community, family carers as well as professionals from academic research, industry and regulatory agencies entitled 'How to improve medicine...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2013.11.024

    authors： Orlu-Gul M,Raimi-Abraham B,Jamieson E,Wei L,Murray M,Stawarz K,Stegemann S,Tuleu C,Smith FJ

    更新日期：2014-01-01 00:00:00

  • Development and evaluation of a tampering resistant transdermal fentanyl patch.

    abstract：:With the increasing number of misuse and abuse of opioids, the resistance to tampering becomes an important attribute for transdermal opioid patches. In this study, drug-containing geopolymer granules were integrated into an adhesive matrix to improve the resistance of fast drug release against some common abuse techn...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2015.04.061

    authors： Cai B,Engqvist H,Bredenberg S

    更新日期：2015-07-05 00:00:00

  • Toward predicting tensile strength of pharmaceutical tablets by ultrasound measurement in continuous manufacturing.

    abstract：:An ultrasound measurement system was employed as a non-destructive method to evaluate its reliability in predicting the tensile strength of tablets and investigate the benefits of incorporating it in a continuous line, manufacturing solid dosage forms. Tablets containing lactose, acetaminophen, and magnesium stearate ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2016.04.064

    authors： Razavi SM,Callegari G,Drazer G,Cuitiño AM

    更新日期：2016-06-30 00:00:00

  • Characterisation of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids.

    abstract：:A drug carrier of colloidal lipid particles with improved payloads and enhanced storage stability was investigated. Based on the experiences with hard fats nanoparticles, a new type of solid lipid nanoparticles (SLN) has been developed by incorporating triglyceride containing oils in the solid core of said particle. T...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(00)00378-1

    authors： Jenning V,Thünemann AF,Gohla SH

    更新日期：2000-04-20 00:00:00

  • Risperidone solid dispersion for orally disintegrating tablet: its formulation design and non-destructive methods of evaluation.

    abstract：:The focus of present investigation was to assess the utility of non-destructive techniques in the evaluation of risperidone solid dispersions (SD) with methyl-β-cyclodextrin (MBCD) and subsequent incorporation of the SD into orally disintegrating tablets (ODT) for a faster release of risperidone. The SD was prepared b...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2010.08.025

    authors： Rahman Z,Zidan AS,Khan MA

    更新日期：2010-11-15 00:00:00

  • Mesoporous silica nanoparticles as a promising skin delivery system for methotrexate.

    abstract：:The systemic administration of methotrexate (MTX), a commonly used, antineoplastic drug which is also used in cutaneous disorders, is primarily associated with prolonged retention in the body and consequently with side effects. Innovative drug delivery techniques and alternative administration routes would therefore c...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2017.07.058

    authors： Sapino S,Oliaro-Bosso S,Zonari D,Zattoni A,Ugazio E

    更新日期：2017-09-15 00:00:00

  • Critical factors in manufacturing multi-layer tablets--assessing material attributes, in-process controls, manufacturing process and product performance.

    abstract：:Advancement in the fields of material science, analytical methodologies, instrumentation, automation, continuous monitoring, feed forward/feed back control and comprehensive data collection have led to continual improvement of pharmaceutical tablet manufacturing technology, notably the multi-layer tablets. This review...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2010.07.025

    authors： Vaithiyalingam SR,Sayeed VA

    更新日期：2010-10-15 00:00:00

  • Nanoparticles based on natural, engineered or synthetic proteins and polypeptides for drug delivery applications.

    abstract：:Medicine formulations at the nanoscale, referred to as nanomedicines, have managed to overcome key challenges encountered during the development of new medical treatments and entered clinical practice, but considerable improvement in terms of local efficacy and reduced toxicity still need to be achieved. Currently, th...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119537

    authors： Georgilis E,Abdelghani M,Pille J,Aydinlioglu E,van Hest JCM,Lecommandoux S,Garanger E

    更新日期：2020-08-30 00:00:00

  • Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs.

    abstract：:The objective of this study was to develop a novel fenofibric acid-loaded controlled release pellet showing enhanced, or equivalent to, bioavailability compared with two commercially available products containing fenofibrate or choline fenofibrate. The effect of solubilizing agents on drug solubility and the impact of...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2015.05.059

    authors： Kim KS,Jin SG,Mustapha O,Yousaf AM,Kim DW,Kim YH,Kim JO,Yong CS,Woo JS,Choi HG

    更新日期：2015-07-25 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

  • Targeted killing of cancer cells in vivo and in vitro with IGF-IR antibody-directed carbon nanohorns based drug delivery.

    abstract：:Oxidized single-wall carbon nanohorns (oxSWNHs) have shown great potential in drug delivery. The purpose of this study was to design an effective targeted drug delivery system (DDS) based on oxSWNHs, which could carry high dose of drug to tumor sites and improve the therapeutic efficacy with less adverse effects. OxSW...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2014.12.015

    authors： Li N,Zhao Q,Shu C,Ma X,Li R,Shen H,Zhong W

    更新日期：2015-01-30 00:00:00

  • Evaluation of the bioequivalence of capsules containing 150 mg of fluconazole.

    abstract：:Fluconazole is an antifungal agent. The purpose of this study was to evaluate bioequivalence of two commercial 150 mg capsule formulations of fluconazole available in the Brazilian market. The study was an open, randomized, two-period, two-group crossover trial with a 2-week washout interval. Blood samples were collec...

    journal_title：International journal of pharmaceutics

    pub_type： 临床试验,杂志文章,随机对照试验

    doi：10.1016/j.ijpharm.2004.09.013

    authors： Porta V,Chang KH,Storpirtis S

    更新日期：2005-01-06 00:00:00

  • Taste sensing systems (electronic tongues) for pharmaceutical applications.

    abstract：:Electronic tongues are sensor array systems able to detect single substances as well as complex mixtures by means of particular sensor membranes and electrochemical techniques. Two systems are already commercially available, the Insent taste sensing system and the αAstree electronic tongue. In addition, various labora...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2010.11.028

    authors： Woertz K,Tissen C,Kleinebudde P,Breitkreutz J

    更新日期：2011-09-30 00:00:00

  • Evaluation of novel lipid based formulation of β-Artemether and Lumefantrine in murine malaria model.

    abstract：:The present investigation aims at formulating lipid based drug delivery system of β-Artemether and Lumefantrine and comparative pharmacological evaluation with innovator formulation. Commercial modified oil and indigenous natural fatty acids comprised the oily phase in developing lipidic formulation of β-Artemether an...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2013.07.033

    authors： Patil S,Suryavanshi S,Pathak S,Sharma S,Patravale V

    更新日期：2013-10-15 00:00:00

  • Polyhydroxy surfactants for the formulation of lipid nanoparticles (SLN and NLC): effects on size, physical stability and particle matrix structure.

    abstract：:The two polyhydroxy surfactants polyglycerol 6-distearate (Plurol(®)Stearique WL1009 - (PS)) and caprylyl/capryl glucoside (Plantacare(®) 810 - (PL)) are a class of PEG-free stabilizers, made from renewable resources. They were investigated for stabilization of aqueous solid lipid nanoparticle (SLN) and nanostructured...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2010.12.036

    authors： Kovacevic A,Savic S,Vuleta G,Müller RH,Keck CM

    更新日期：2011-03-15 00:00:00

  • A multifunctional ternary Cu(II)-carboxylate coordination polymeric nanocomplex for cancer thermochemotherapy.

    abstract：:Metal-based photothermal therapy has been widely used in the biomedicine field and includes gold nanoparticles, silver nanoparticles and copper sulfide nanoparticles. Furthermore, the coordination bonding-based metal nanocomplex is a new generation of photothermal agents for cancer therapy due to its high photothermal...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2018.06.048

    authors： Zhang C,Li J,Qian C,Luo X,Wang K,Zhao P,Sun M

    更新日期：2018-10-05 00:00:00