Clickhaler dry powder inhaler: focussed in vitro proof of principle evaluation of a new chemical entity for asthma.

Abstract:

:A new chemical entity (NCE) was evaluated in the Clickhaler (Innovata Biomed Ltd.) dry powder inhaler, a reservoir-based multidose delivery system. The standard device metering system was modified to handle higher doses (nominally 20 mm(3) of lactose based blend). The micronized drug was formulated at 12.5% w/w in lactose monohydrate (Pharmatose 325M, DMV) equivalent to a nominal dose of approximately 1 mg. Delivered shot weight (mg of blend) and emitted dose (microg drug) averaged 7.4 mg and 905 microg, respectively, and were consistent (within +/-20 to 25% of mean) through the life of the inhaler. The fine particle fraction (FPF) (Andersen cascade impactor) was typically 60%. A short stability study (i.e. 3 months at room temperature, 53 or 75% RH, unpacked) showed that the in vitro performance was maintained. The results of these studies provide in vitro proof of principle for this novel drug/device combination.

journal_name

Int J Pharm

authors

Thibert R,Parry-Billings M,Shott M

doi

10.1016/s0378-5173(02)00106-0

keywords:

subject

Has Abstract

pub_date

2002-06-04 00:00:00

pages

149-56

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378517302001060

journal_volume

239

pub_type

杂志文章
  • Induction of immunogenic cell death of cancer cells through nanoparticle-mediated dual chemotherapy and photothermal therapy.

    abstract::The use of nanomedicines to induce immunogenic cell death is a new strategy that aims to increase tumor immunogenicity and thereby prime tumors for further immunotherapies. In this study, we developed a nanoparticle formulation for combinatory chemotherapy and photothermal therapy based only on materials previously us...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119787

    authors: Heshmati Aghda N,Abdulsahib SM,Severson C,Lara EJ,Torres Hurtado S,Yildiz T,Castillo JA,Tunnell JW,Betancourt T

    更新日期:2020-09-06 00:00:00

  • Controlled release from hydrogel-based solid matrices. A model accounting for water up-take, swelling and erosion.

    abstract::Design and realization of drug delivery systems based on polymer matrices could be greatly improved by modeling the phenomena which take place after the systems administration. Availability of a reliable mathematical model, able to predict the release kinetic from drug delivery systems, could actually replace the reso...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.01.023

    authors: Lamberti G,Galdi I,Barba AA

    更新日期:2011-04-04 00:00:00

  • Correlation of solid dosage porosity and tensile strength with acoustically extracted mechanical properties.

    abstract::Currently, the compressed tablet and its oral administration is the most popular drug delivery modality in medicine. The accurate porosity and tensile strength characterization of a tablet design is vital for predicting its performance such as disintegration, dissolution, and drug-release efficiency upon administratio...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.03.018

    authors: Xu X,Mack C,Cleland ZJ,Vallabh CKP,Dave VS,Cetinkaya C

    更新日期:2018-05-05 00:00:00

  • Kinetic analysis of in vitro and in vivo release of prednisolone from the conjugate of glycol-chitosan and succinyl-prednisolone.

    abstract::Recently, many people have developed rheumatoid arthritis (RA), and prednisolone (PD) is often used for treatment; however, long use and a large dose of PD can cause toxic side effects. In this study, in order to enhance the therapeutic effects and to suppress the toxic side effects, the conjugate (GC-SP) was prepared...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.03.004

    authors: Onishi H,Saito Y,Sasatsu M,Machida Y

    更新日期:2011-05-30 00:00:00

  • Effect of drug lipophilicity on in vitro release rate from oil vehicles using nicotinic acid esters as model prodrug derivatives.

    abstract::The rate constants for transfer of a homologous series of nicotinic acid esters from oil vehicles to aqueous buffer phases were determined using a rotating dialysis cell. The chemical stability of butyl nicotinate has been investigated at 60 degrees C over pH range 0.5--10. Maximum stability occurs at pH 4--5 and an i...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00568-3

    authors: Weng Larsen S,Engelbrecht Thomsen AE,Rinvar E,Friis GJ,Larsen C

    更新日期:2001-03-23 00:00:00

  • An in vitro kinetic method for detection of precipitation of poorly soluble drugs.

    abstract::A simple in vitro method for the detection of precipitation using 96-well microplates and a SpectraMax Plus microtiter plate reader has been developed and described. The method requires only small amount of drug and is, therefore, potentially applicable in early pre-formulation. The method is based on opacity changes ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.08.012

    authors: Wu Z,Tucker IG,Razzak M,Medlicott NJ

    更新日期:2005-11-04 00:00:00

  • Preactivated hyaluronic acid: A potential mucoadhesive polymer for vaginal delivery.

    abstract::The objective of this study was to develop mucoadhesive polymeric excipients for vaginal drug delivery systems. Hyaluronic acid was thiolated and subsequently preactivated with 6-mercaptonicotinamide (HA-CYS-MNA) to enhance stability and mucoadhesive properties on vaginal mucosa. After determination of the thiol group...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.11.048

    authors: Nowak J,Laffleur F,Bernkop-Schnürch A

    更新日期:2015-01-15 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

  • Quantification of surface composition and surface structure of inhalation powders using TOF-SIMS.

    abstract::A multivariate TOF-SIMS methodology has been developed and applied to quantify surface composition and chemical distribution for dry powder blends. Surface properties are often critical to the behavior of powder formulations, especially in the case of dry powders for inhalation, as surface properties directly affect i...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119666

    authors: Nicholas M,Josefson M,Fransson M,Wilbs J,Roos C,Boissier C,Thalberg K

    更新日期:2020-09-25 00:00:00

  • PLGA microparticles with zero-order release of the labile anti-Parkinson drug apomorphine.

    abstract::The treatment of patients suffering from advanced Parkinson's disease is highly challenging, because the efficacy of the "gold standard" levodopa declines with time. Co-administration of the dopamine receptor agonist apomorphine is beneficial, but difficult due to the poor oral bioavailability and short half-life of t...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.01.008

    authors: Regnier-Delplace C,Thillaye du Boullay O,Siepmann F,Martin-Vaca B,Degrave N,Demonchaux P,Jentzer O,Bourissou D,Siepmann J

    更新日期:2013-02-25 00:00:00

  • Rapid and soft formulation of folate-functionalized nanoparticles for the targeted delivery of tripentone in ovarian carcinoma.

    abstract::We report the development of folate-functionalized nanoparticles able to target folate receptors, and to deliver a poorly water soluble cytotoxic agent, a tripentone, in ovarian carcinoma. The stability under incubation of lipid nanoparticles formulated by a low-energy phase inversion temperature method was investigat...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.09.025

    authors: Tomasina J,Poulain L,Abeilard E,Giffard F,Brotin E,Carduner L,Carreiras F,Gauduchon P,Rault S,Malzert-Fréon A

    更新日期:2013-12-15 00:00:00

  • Evaluation of collagen and methylated collagen as gene carriers.

    abstract::This study explores the potential of DNA complexes prepared with methylated collagen (MC) and unmodified native collagen (NC) to deliver genes into cells. The physicochemical properties and transfection abilities of these two types of complexes are studied in parallel. MC was prepared by methylation of the carboxyl gr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.04.014

    authors: Wang J,Lee IL,Lim WS,Chia SM,Yu H,Leong KW,Mao HQ

    更新日期:2004-07-26 00:00:00

  • Spray-freeze-drying production of thermally sensitive polymeric nanoparticle aggregates for inhaled drug delivery: effect of freeze-drying adjuvants.

    abstract::Inhalable dry-powder aggregates of drug-loaded thermally sensitive poly(caprolactone) (PCL) nanoparticles are produced using spray-freeze-drying (SFD) as the low melting point of PCL prohibits the use of high-temperature spray-drying. The effects of freeze-drying adjuvant formulation on the particle morphology, aerody...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.11.021

    authors: Cheow WS,Ng ML,Kho K,Hadinoto K

    更新日期:2011-02-14 00:00:00

  • Preparation of enteric coated timed-release press-coated tablets and evaluation of their function by in vitro and in vivo tests for colon targeting.

    abstract::As a new oral drug delivery system for colon targeting, enteric coated timed-release press-coated tablets (ETP tablets) were developed by coating enteric polymer on timed-release press-coated tablets composed of an outer shell of hydroxypropylcellulose and core tablet containing diltiazem hydrochloride (DIL) as a mode...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(00)00454-3

    authors: Fukui E,Miyamura N,Uemura K,Kobayashi M

    更新日期:2000-08-25 00:00:00

  • Amphotericin B-incorporated polymeric micelles composed of poly(d,l-lactide-co-glycolide)/dextran graft copolymer.

    abstract::In this study, we prepared amphotericin B (AmpB)-encapsulated polymeric micelle of poly(d,l-lactide-co-glycolide) (PLGA) grafted-dextran (DexLG) copolymer and characterized its physicochemical properties in vitro. The average particle size of AmpB-encpasulated DexLG polymeric micelles was around 30-150nm while particl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.12.011

    authors: Choi KC,Bang JY,Kim PI,Kim C,Song CE

    更新日期:2008-05-01 00:00:00

  • In vivo efficacy of paclitaxel-loaded injectable in situ-forming gel against subcutaneous tumor growth.

    abstract::Injectable in situ-forming gels have received considerable attention as localized drug delivery systems. Here, we examined a poly(ethylene glycol)-b-polycaprolactone (MPEG-PCL) diblock copolymer gel as an injectable drug depot for paclitaxel (Ptx). The copolymer solution remained liquid at room temperature and rapidly...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.03.033

    authors: Lee JY,Kim KS,Kang YM,Kim ES,Hwang SJ,Lee HB,Min BH,Kim JH,Kim MS

    更新日期:2010-06-15 00:00:00

  • Interfacial elastic relaxation during the ejection of bi-layered tablets.

    abstract::The predilection of a bi-layered tablet to fail in the interface region after its initial formation in the compaction process reduces its practicality as a choice for controlled release solid drug delivery system. Hence, a fundamental appreciation of the governing mechanism that causes the weakening of the interfacial...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.11.031

    authors: Anuar MS,Briscoe BJ

    更新日期:2010-03-15 00:00:00

  • Protein assembled nano-vehicle entrapping photosensitizer molecules for efficient lung carcinoma therapy.

    abstract::The efficiency of drug depends not only on its potency but also on its ability to reach the target sites in preference to non-target sites. In this regard, protein assembled nanocarrier is the most promising strategy for intracellular anti-cancer drug delivery. The key motive of this study is to fabricate biocompatibl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119192

    authors: Nag S,Bagchi D,Chattopadhyay D,Bhattacharyya M,Pal SK

    更新日期:2020-04-30 00:00:00

  • Superparamagnetic iron oxide nanoparticles stabilized by alginate: pharmacokinetics, tissue distribution, and applications in detecting liver cancers.

    abstract::The objectives of this study were to describe the pharmacokinetics and tissue distribution of superparamagnetic iron oxide nanoparticle (SPIO) stabilized with alginate (SPIO-alginate), and investigate its potential in detecting liver cancers as a newly developed magnetic resonance (MR) contrast agent. Pharmacokinetics...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.11.036

    authors: Ma HL,Xu YF,Qi XR,Maitani Y,Nagai T

    更新日期:2008-04-16 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

  • Development of machine learning models of β-cyclodextrin and sulfobutylether-β-cyclodextrin complexation free energies.

    abstract::A new set of 142 experimentally determined complexation constants between sulfobutylether-β-cyclodextrin and diverse organic guest molecules, and 78 observations reported in literature, were used for the development of the QSPR models by the two machine learning regression methods - Cubist and Random Forest. Similar m...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.03.065

    authors: Merzlikine A,Abramov YA,Kowsz SJ,Thomas VH,Mano T

    更新日期:2011-10-14 00:00:00

  • High loading fragrance encapsulation based on a polymer-blend: preparation and release behavior.

    abstract::The six fragrances, camphor, citronellal, eucalyptol, limonene, menthol and 4-tert-butylcyclohexyl acetate, which represent different chemical functionalities, were encapsulated with a polymer-blend of ethylcellulose (EC), hydroxypropyl methylcellulose (HPMC) and poly(vinyl alcohol) (PV(OH)) using solvent displacement...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.02.020

    authors: Sansukcharearnpon A,Wanichwecharungruang S,Leepipatpaiboon N,Kerdcharoen T,Arayachukeat S

    更新日期:2010-05-31 00:00:00

  • Triclosan loaded electrospun nanofibers based on a cyclodextrin polymer and chitosan polyelectrolyte complex.

    abstract::This work focuses on the relevance of antibacterial nanofibers based on a polyelectrolyte complex formed between positively charged chitosan (CHT) and an anionic hydroxypropyl betacyclodextrin (CD)-citric acid polymer (PCD) complexing triclosan (TCL). The study of PCD/TCL inclusion complex and its release in dynamic c...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.09.060

    authors: Ouerghemmi S,Degoutin S,Tabary N,Cazaux F,Maton M,Gaucher V,Janus L,Neut C,Chai F,Blanchemain N,Martel B

    更新日期:2016-11-20 00:00:00

  • Water solubilization capacity of pharmaceutical microemulsions based on Peceol®, lecithin and ethanol.

    abstract::Biocompatible microemulsions composed of Peceol(®), lecithin, ethanol and water developed for encapsulation of hydrophilic drugs were investigated. The binary mixture Peceol(®)/ethanol was studied first. It was shown that the addition of ethanol to pure Peceol(®) has a significant fluidifying and disordering effect on...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.07.018

    authors: Mouri A,Diat O,Lerner DA,El Ghzaoui A,Ajovalasit A,Dorandeu C,Maurel JC,Devoisselle JM,Legrand P

    更新日期:2014-11-20 00:00:00

  • The consideration of indolicidin modification to balance its hemocompatibility and delivery efficiency.

    abstract::Indolicidin (IL) is an antimicrobial peptide (AMP), which has been utilized as a cell penetrating peptide (CPP) for drug delivery. However, the hemolysis restricts its clinical application. Therefore, we investigated the delivery efficiency and hemocompatibility of IL and its derivatives. The transportation of fluorop...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.08.037

    authors: Tsai CW,Hu WW,Liu CI,Ruaan RC,Tsai BC,Jin SL,Chang Y,Chen WY

    更新日期:2015-10-15 00:00:00

  • Comparative evaluation of cytotoxicity of a glucosamine-TBA conjugate and a chitosan-TBA conjugate.

    abstract::D-glucosamine and chitosan were modified by the immobilization of thiol groups utilizing 2-iminothiolane. The toxicity profile of the resulting D-glucosamine-TBA (4-thiobutylamidine) conjugate, of chitosan-TBA conjugate and of the corresponding unmodified controls was evaluated in vitro. On the one hand, the cell memb...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.03.016

    authors: Guggi D,Langoth N,Hoffer MH,Wirth M,Bernkop-Schnürch A

    更新日期:2004-07-08 00:00:00

  • Stability study of amorphous valdecoxib.

    abstract::Formulation of poorly water-soluble drugs in the most stable dosage form for oral delivery perhaps presents the greatest challenge to pharmaceutical industry. Physical transformation of drug substance into its more soluble but metastable amorphous form is one of the approaches for improving dissolution rate of such dr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.06.009

    authors: Ambike AA,Mahadik KR,Paradkar A

    更新日期:2004-09-10 00:00:00

  • Physico-chemical properties of co-formulated fast-acting insulin with pramlintide.

    abstract::Since the discovery of amylin its use has been discouraged by the inadequacy of the protocol involving multiple injections in addition to insulin. We aimed here to develop a combined fixed-dose formulation of pramlintide with fast-acting insulin. We have investigated the compatibility of regular and fast-acting insuli...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.06.039

    authors: da Silva DC,Lima LMTR

    更新日期:2018-08-25 00:00:00

  • Development and characterization of layer-by-layer coated liposomes with poly(L-lysine) and poly(L-glutamic acid) to increase their resistance in biological media.

    abstract::Multilayered coated liposomes were prepared using the layer-by-layer (LbL) technique in an effort to improve their stability in biological media. The formulation strategy was based on the alternate deposition of two biocompatible and biodegradable polyelectrolytes - poly(L-lysine) (PLL) and poly(L-glutamic acid) (PGA)...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119568

    authors: Hermal F,Frisch B,Specht A,Bourel-Bonnet L,Heurtault B

    更新日期:2020-08-30 00:00:00

  • Raman mapping of pharmaceuticals.

    abstract::Raman spectroscopy may be implemented through a microscope to provide fine scale axial and lateral chemical maps. The molecular structure of many drugs makes Raman spectroscopy particularly well suited to the investigation of pharmaceutical systems. Chemometric methods currently used to assess bulk Raman spectroscopic...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2010.12.030

    authors: Gordon KC,McGoverin CM

    更新日期:2011-09-30 00:00:00