Abstract：
:The aim of this work was to formulate a powder for inhalation with fusafungine, a drug substance initially highly cohesive. The classical approach based on micronization by jet milling to prepare respirable drug particles and then blending with a carrier was first applied. A fractional factorial experimental design was implemented to screen six formulation parameters. The effect of drug/lactose co-micronization on aerosolization was then evaluated. In vitro deposition studies were performed with the twin stage glass impinger and the inhaler Spinhaler. Micronization did not induce DSC-detectable amorphization and gave a highly cohesive, poor flowable powder with a theoretical aerodynamic diameter of 5 microm. The powder was then blended with coarse lactose and optionally fine lactose. Unfortunately, the respirable fraction could not be optimized and remained below 10%. On the other hand, a co-micronized powder drug/fine lactose 50:50 gave a respirable fraction of 16%. Following blending with a carrier, the respirable fraction and the emitted dose fraction reached 23% and 69%, respectively. The use of a fine lactose grade for co-micronization was essential. In conclusion, this study demonstrated that co-micronization with a fine lactose is an efficient and simple strategy to formulate a powder for inhalation with enhanced aerosolization properties, especially for highly cohesive drug substance.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Giry K,Péan JM,Giraud L,Marsas S,Rolland H,Wüthrich Pdoi
10.1016/j.ijpharm.2006.05.009subject
Has Abstractpub_date
2006-09-14 00:00:00pages
162-6issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(06)00374-7journal_volume
321pub_type
杂志文章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
更新日期：2006-08-17 00:00:00
abstract：:In this study, a temperature and ROS-responsive drug delivery system ROSP@MSN based on mesoporous silica nanoparticles has been designed and synthesized by taking advantage of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acrylate modified polymers (ROSP) as "nano-valve", which can respond selectively to cance...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.11.025
更新日期：2018-01-30 00:00:00
abstract：:The α-glucosyl hesperidin (Hsp-G)-induced improvement of both the dissolution and absorption properties of pranlukast hemihydrate (PLH) was achieved by means of a high-pressure homogenization (HPH) processing. The average particle size in the HPH-processed suspension was decreased significantly after 50 cycles of proc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.03.017
更新日期：2011-05-30 00:00:00
abstract：:Hydrogen-bonded interpolymer complexes can be used for development of novel dosage forms. In this study, two types of crosslinked hydrogels, copolymer networks of N-vinyl pyrrolidone and acrylamide (PVP-co-PAM) and interpenetrating polymer networks (IPN) composed of crosslinked PVP-co-PAM and poly(vinyl alcohol) (PVA)...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.04.037
更新日期：2012-07-15 00:00:00
abstract：:The aim of this study was to evaluate the transdermal permeation enhancement of N-trimethyl chitosan (TMC) with different degrees of quaternization (DQ). TMCs with DQ of 40 and 60% (TMC40 and TMC60) were synthesized and characterized by (1)H NMR. Testosterone (TS) used as an effective drug, four different gels were pr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.12.050
更新日期：2008-05-22 00:00:00
abstract：:Oxidative stress has been implicated in the progression of age-related macular degeneration (AMD). Treatment with antioxidants seems to delay progression of AMD. In this study, we suggested an antioxidant delivery system based on redox-sensitive liposome composed of phospholipids and a diselenide centered alkyl chain....
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.05.056
更新日期：2018-09-05 00:00:00
abstract：:The melting point of lidocaine was significantly lowered when mixed with thymol and/or aqueous ethanol. Mixtures of lidocaine and thymol at ratios within the range of 30:70-70:30 (w:w) became homogeneous oils at 25 degrees C. In a pH 9.2 carbonate buffer containing 25% ethanol, lidocaine (5%, w:w) also liquefied at 25...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00689-5
更新日期：2001-07-03 00:00:00
abstract：:Diabetic ulcers are prone to bacterial contamination and can severely affect patient's quality of life. This study is first report to explore copper-grafted graphene oxide-crosslinked zein scaffolds (Cu-GZS) for promoting cutaneous excision wounds healing as a promising therapeutic modality in diabetic male-rats. Cu-G...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119919
更新日期：2020-11-30 00:00:00
abstract：:Nutrient transporters expressed on cell membrane have been targeted for enhancing bioavailability of poorly permeable drugs. Sodium dependent multivitamin transporter (SMVT) is once such carrier system, utilized for improving drug targeting to specific tissues. Therefore, the main objective of this study is to charact...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.06.011
更新日期：2012-10-15 00:00:00
abstract：:The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow 600) or as mini-tablet...
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/s0378-5173(00)00549-4
更新日期：2000-11-04 00:00:00
abstract：:Polydimethylsiloxane (PDMS)-based levonorgestrel intrauterine systems (LNG-IUSs) contain a large amount of potent LNG, and therefore it is important to understand the impact of product design parameters on the in vitro and in vivo performance to ensure safety and efficacy, as well as to avoid serious side effects resu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119135
更新日期：2020-03-30 00:00:00
abstract：:The present study investigated the influence of in vitro dissolution conditions on the in vivo predictability of an amorphous solid dispersion of celecoxib (CCX) in the pH-sensitive polymer Eudragit® S 100. Different doses of a 25:75w/w% CCX:Eudragit® S 100 amorphous solid dispersion (CCX:EUD) were investigated. Durin...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.08.078
更新日期：2017-10-05 00:00:00
abstract：:The optimized formulation of N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N'-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug, was developed by utilizing the complexation between N-4472 and L-ascorbic acid (VC). It was found that the formulation with Gelucire((R)) 44/14, H...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00346-0
更新日期：2002-10-10 00:00:00
abstract：:Diabetic foot infections are the most common complications requiring hospitalisation of patients with diabetes. They often result in amputation to extremities and are associated with high morbi-mortality rates, especially when bone is infected. Treatment of these complications is based on surgical procedures, nursing ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119677
更新日期：2020-09-25 00:00:00
abstract：:This study describes the effect of coating temperature on the performance of mechanical particle coating using ethylcellulose, which was done to produce controlled-release particles (diameters less than 100 μm) with different release rates. First, theophylline crystals were spheronized using a mechanical powder proces...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.11.061
更新日期：2019-01-10 00:00:00
abstract：:Amorphous lactose will crystallise rapidly if its glass transition temperature is reduced below its storage temperature. This is readily achieved by storing samples at ambient temperature and a relative humidity (RH) of greater than 50%. If the sample is monitored in an isothermal microcalorimeter as it crystallises, ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.07.016
更新日期：2004-10-13 00:00:00
abstract：:As a new approach to analyzing the release behavior of lipophilic drugs from colloidal carriers, solid trimyristin nanoparticles were incorporated into differently sized (34-1363 μm) calcium alginate hydrogel microbeads to serve as acceptor in release studies. The microbeads were prepared by electrostatic droplet gene...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.03.082
更新日期：2015-07-15 00:00:00
abstract：:Experiments were conducted to illustrate some of the challenges associated with measuring dynamic MDI aerosols. Experimental HFA-134a solution MDIs containing 8 or 20% ethanol were measured using the Andersen cascade impactor using three different inlets. It was demonstrated that the size distribution of MDI aerosols ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.11.047
更新日期：2008-05-01 00:00:00
abstract：:Solid lipid nanoparticles (SLNs) conjugated with tamoxifen (TX) and lactoferrin (Lf) were applied to carry anticancer carmustine (BCNU) across the blood-brain barrier (BBB) for enhanced antiproliferation against glioblastoma multiforme (GBM). BCNU-loaded SLNs with modified TX and Lf (TX-Lf-BCNU-SLNs) were used to pene...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.12.054
更新日期：2016-02-29 00:00:00
abstract：:An increasing human population requires a secure food supply and a cost effective, oral vaccine delivery system for livestock would help facilitate this end. Recombinant antigen adsorbed onto silica beads and coated with myristic acid, was released (∼15% (w/v)) over 24 h at pH 8.8. At pH 2, the myristic acid acted as ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.03.046
更新日期：2014-07-01 00:00:00
abstract：:Docetaxel (DTX) is one of the important antitumor drugs, being used in several common chemotherapies to control leading cancer types. Severe toxicities of the DTX are prominent due to sudden parenteral exposure of desired loading dose to maintain the therapeutic concentration. Field of nanotechnology is leading to res...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2017.07.018
更新日期：2017-08-30 00:00:00
abstract：:In the present study, two indices of acute intestinal permeability changes were investigated as measurements of drug induced intestinal damage. The first method was based on 14C-polyethylene glycol (PEG) 4000 permeability assessment and the second was based on histological evaluation of the intestine. The test compoun...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.01.009
更新日期：2006-04-07 00:00:00
abstract：:In the present work, the Hot Air Coating (HAC) technique was used to prepare microparticulate systems containing nifedipine. Binary mixtures constituting of nifedipine and cetearyl alcohol (CA) in different proportions (30:70, 50:50, 70:30) were studied: they were homogenized by mixing or milling before spray treatmen...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.01.010
更新日期：2005-04-11 00:00:00
abstract：BACKGROUND:Pulmonary administration of the antimicrobial drugs colistin sulphomethate and tobramycin has been shown to be effective in slowing down pulmonary deterioration in cystic fibrosis (CF) patients. Both drugs are administered by liquid nebulisation, a technique known to have disadvantages. Dry powder inhalation...
journal_title：International journal of pharmaceutics
pub_type： 临床试验,杂志文章
doi：10.1016/j.ijpharm.2006.11.021
更新日期：2007-04-20 00:00:00
abstract：:The increasing realisation of the impact of size and surface properties on the bio-distribution of drug loaded colloidal particles has driven the application of micro fabrication technologies for the precise engineering of drug loaded microparticles. This paper demonstrates an alternative approach for producing size c...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.03.051
更新日期：2014-06-05 00:00:00
abstract：:Insulin, a key peptide hormone that conjointly with its receptor regulates blood glucose levels, is used as the major means to treat diabetes. This therapeutic hormone may undergo different chemical modifications during industrial processes, pharmaceutical formulation, and through its endogenous storage in the pancrea...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.06.023
更新日期：2018-08-25 00:00:00
abstract：:Oral administration of proteins and peptides still is a challenging task to overcome due to low permeability through absorptive epithelia, degradation and metabolism that lead to poor bioavailability. Attempting to overcome such limitations, an antihypertensive peptide derived from whey protein, with KGYGGVSLPEW seque...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.05.051
更新日期：2018-08-25 00:00:00
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
更新日期：2002-03-20 00:00:00
abstract：:Peptides and polypeptides have important pharmacological properties but only a limited number have been exploited as therapeutics because of problems related to their delivery. Most of these drugs require a parenteral delivery system which introduces the problems of pain, possible infection, and expertise required to ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.11.046
更新日期：2012-02-28 00:00:00
abstract：:Distribution of salicylic acid in human stratum corneum from treatment of six different formulations was assessed by quantitation of drug content in sequentially tape-stripped stratum corneum after a single 2-h dose was applied unoccluded to skin on the ventral forearm of four female subjects. The profile and total am...
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/s0378-5173(99)00217-3
更新日期：1999-10-25 00:00:00
