Abstract:
:The required replacement of chlorofluorocarbon (CFC) with hydrofluoroalkane (HFA) propellants has challenged formulators of pressurized metered dose inhalers in several major respects. Conventional (CFC soluble) surfactants are effectively insoluble in the major CFC replacement candidates, HFA 134 and HFA 227ea, in the absence of co-solvents. While these ethane and propane derivatives have comparable boiling points and vapor pressures to dichlorodifluoromethane (CFC 12), their increased polarity demands that formulators use either alternative (soluble) surfactants, or co-solvents along with traditional surfactants, in order to stabilize pressurized suspension products. The use of either approach is complicated by the existence of many competing patents and the fact that the science in the area is empirical; predictive theoretical approaches are frustrated by the lack of an adequate database. Technical developments in this area must also take into account the need to avoid crystal growth and/or adhesion of micronized, suspended drugs to internal container surfaces, problems which may be catalyzed by some combinations of surfactant type/concentration, vehicle(s) and physical form/type(s) of drug substance. For some drugs, it appears simpler to use co-solvents with HFA propellants to dissolve the drug, avoiding the need for suspension stabilization. This article presents an overview of the present state of the art with respect to the formulation of MDIs.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Vervaet C,Byron PRdoi
10.1016/s0378-5173(99)00134-9keywords:
subject
Has Abstractpub_date
1999-09-10 00:00:00pages
13-30issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(99)00134-9journal_volume
186pub_type
杂志文章,评审abstract::To facilitate targeting drug delivery and combined therapy, we develop titanium dioxide-encapsulated Fe3O4 nanoparticles (Fe3O4@TiO2 NPs). Titanium dioxide (TiO2), which is employed as a sonosensitizer for sonodynamic therapy (SDT), can also be used for the loading of doxorubicin (DOX). The fabricated Fe3O4@TiO2 NPs e...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.03.070
更新日期:2015-01-01 00:00:00
abstract::Lipid emulsions can be used as a vehicle for the production of low-volume injectable preparations with minimally water-soluble active ingredients. First, we focus on the galenic and technological conditions established by ultrasound techniques. A 2(5) factorial design was used to optimize the carrier emulsion. The stu...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00664-5
更新日期:2001-03-23 00:00:00
abstract::Niosomes are vesicles formed by self-assembly of non-ionic surfactants. In this investigation, the effects of processing variables, particularly temperature and sonication, on the physical characteristics and phase transitional behaviour of two niosomal systems based on a hexadecyl diglycerol ether (C(16)G(2)) have be...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00362-8
更新日期:2000-05-15 00:00:00
abstract::Charged drug delivery systems are interesting candidates for the delivery of drugs through skin. In the present study, it was possible to create negatively and positively charged oil/water nanoemulsions by using sucrose laureate and polysorbate 80 as non-ionic surfactants. The positively charged nanoemulsions were gen...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2008.11.014
更新日期:2009-03-31 00:00:00
abstract::The present study evaluates the effect of several pharmaceutical plasticizers on the thermo-physical and physicochemical properties of partially hydrolyzed poly(vinyl alcohol) (PVA) used in fusion-based pharmaceutical formulation processes. Specifically, the effect of mannitol (MAN), sorbitol (SOR), sucrose (SUC), anh...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119121
更新日期:2020-03-30 00:00:00
abstract::A biodegradable porous starch foam (BPSF) was developed for the first time as a carrier in order to improve the dissolution and enhance the oral bioavailability of lovastatin - defined as a model poorly water soluble BCS type II drug. In this paper, BPSF was prepared by the solvent exchange method and characterized by...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.09.040
更新日期:2011-01-17 00:00:00
abstract::Hydrotalcite (HT), also known as a layered double hydroxide (LDH) compound, has been widely used in past years in the formulation of drugs due to its specific properties including good biocompatibility, null toxicity, high chemical stability and pH-dependent solubility which aid in drug controlled release. In this wor...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.04.048
更新日期:2016-06-15 00:00:00
abstract::Developments in the field of molecular oncology have revealed that resistance to chemotherapeutics is acqured through several mechanisms including overexpression of common oncogenic proteins. Signal Transducer and Activator of Transcription 3 (STAT3) is one of these oncogenes that is overexpressed in many cancer types...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.04.034
更新日期:2017-06-15 00:00:00
abstract::Alzheimer's disease (AD) is a common and severe brain disease with a high mortality among the elders, but no highly efficient medications are currently available. For example, timosaponin BII, an efficient anti-AD agent, has low oral bioavailability. Here, timosaponin BII was formulated in a temperature/ion-sensitive ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119115
更新日期:2020-03-30 00:00:00
abstract::Maedi Visna virus (MVV) is an ovine lentivirus with high prevalence all over the world. Since conventional vaccines had failed in protecting animals against the infection, the development of a DNA vaccine can be an alternative. The candidate vaccine was constructed by cloning the sequence encoding MVV p25 protein and ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.05.005
更新日期:2009-07-30 00:00:00
abstract::Electrospun nanofibers are being utilized for a wide range of healthcare applications. A plethora of natural and synthetic polymers are exploited for their ability to be electrospun and replace the complex habitat provided by the extracellular matrix for the cells. The fabrication of nanofibers can be tuned to act as ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2017.03.013
更新日期:2017-05-15 00:00:00
abstract::Ciclopirox olamine (CPO) metal complexes have been prepared and characterized using elemental analysis, infra red (IR), melting point and differential scanning calorimetry (DSC). Spectroscopic titration using molar ratio method indicated the occurrence of 1:1 complexes for CPO with almost all the examined metals. Phys...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.11.009
更新日期:2005-01-31 00:00:00
abstract::Most pH-sensitive polymer coating studies for potential colonic delivery systems apply multiple layers to protect the active agent from degradation and early release in the stomach and small intestine. This study designed a single-coat pH-sensitive layer for colon-specific delivery with a potential biopolymer, namely,...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.01.066
更新日期:2019-03-25 00:00:00
abstract::The objective of the present study was to determine the optimum composition for sustained-release of tamsulosin hydrochloride from microparticles intended for orally disintegrating tablets. Microparticles were prepared from an aqueous ethylcellulose dispersion (Aquacoa®), and an aqueous copolymer based on ethyl acryla...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.01.053
更新日期:2011-04-15 00:00:00
abstract::Cystic fibrosis (CF), an atypical genetic disorder, develops due to mutations in cystic fibrosis transmembrane conductance regulator gene, which consequently leads to infection and inflammation. CF infections are commonly characterized by the presence of an extracellular polymeric substance (EPS) matrix or the 'biofil...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119696
更新日期:2020-09-25 00:00:00
abstract::In this paper, we report a new method based on supercritical carbon dioxide (scCO(2)) to fill and distribute the porous magnetic nanoparticles with n-octanol in a homogeneous manner. The high solubility of n-octanol in scCO(2) and high diffusivity and permeability of the fluid allow efficient delivery of n-octanol int...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.07.031
更新日期:2006-12-11 00:00:00
abstract::In this study, topical minoxidil solutions supplemented with TPGS in cosolvent systems of various compositions consisting of water, alcohol, and polyethylene glycol 400 were designed to evaluate the efficacy of promoting hair growth after topical application and the safety in terms of the amount of minoxidil absorbed ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.09.005
更新日期:2005-12-08 00:00:00
abstract::Pharmaceutical containers for parenterals have been predominantly manufactured using glass as a packaging material of choice, especially Type-I glass, since it has been regarded as a chemically inert and an effective container closure system (CCS). Nevertheless, there have been reports and recalls related to glass qua...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118510
更新日期:2019-09-10 00:00:00
abstract::Exosomes are lipid bilayer-enclosed vesicles of endosomal origin, which initially considered as garbage bins to dispose unwanted cellular components, but they are now emerged as an intercellular communication system involved in several physiological and pathological conditions. With the increasing understanding that t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2020.119333
更新日期:2020-06-15 00:00:00
abstract::In a recent paper published in this journal, authors were perplexed by their results seemingly conflicting with our earlier findings [Sun, C.C., Himmelspach, M.W., 2006. Reduced tabletability of roller compacted granules as a result of granule size enlargement. J. Pharm. Sci. 95, 200-206]. After carefully reviewing th...
journal_title:International journal of pharmaceutics
pub_type: 评论,信件
doi:10.1016/j.ijpharm.2007.10.002
更新日期:2008-01-22 00:00:00
abstract::Various biomacromolecules (BMs) such as proteins, DNA, and carbohydrates are extremely difficult to be dissolved in a single organic solvent phase for sustained release or targeted delivery formulation. In this study, three different BMs could be solubilized in selected organic solvents by forming poly(ethylene glycol...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2008.01.033
更新日期:2008-05-22 00:00:00
abstract::Niacinamide-containing moisturisers are known be efficacious in alleviating dry skin conditions and improving stratum corneum (SC) barrier function. However, the mechanisms of action of niacinamide at the molecular level in the SC are still not well understood. Previously, we have reported the development of novel met...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.ijpharm.2012.11.043
更新日期:2013-01-30 00:00:00
abstract::The aim of this work was to investigate the anti-tumor effect of paclitaxel (PTX)-loaded methoxy poly(ethylene glycol)-poly(ɛ-caprolactone) nanoparticles (MPEG-NP/PTX) against glioblastoma multiforme (GBM). MPEG-NP/PTX was prepared by the emulsion and evaporation technique with particle size of 72.5±2.2nm and did not ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.10.005
更新日期:2010-12-15 00:00:00
abstract::Sodium salts are often used in drug formulation but their partial solubility parameters are not available. Sodium alters the physical properties of the drug and the knowledge of these parameters would help to predict adhesion properties that cannot be estimated using the solubility parameters of the parent acid. This ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00374-9
更新日期:2000-01-20 00:00:00
abstract::The aim of this research was to study the gastrointestinal transit and gastric emptying of non-disintegrating solid dosage forms in rats using X-ray imaging. Commercial gelatin minicapsules were filled with barium sulfate and enterically coated using Eudragit S100. The capsules were administered orally to rats followe...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.01.001
更新日期:2010-03-30 00:00:00
abstract::The aim of this study was to investigate the importance of liposome structure in oestradiol skin delivery as a tool for understanding the delivery mechanism from lipid vesicles. Liposomes of phosphatidylcholine (PC) (1), PC, sodium cholate; 86:14 w/w (II), PC, Span 80; 86.7:13.3 w/w (III) and PC, oleic acid: 84:16 w/w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00493-2
更新日期:2000-08-25 00:00:00
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
更新日期:2010-06-15 00:00:00
abstract::The content of latanoprost, a therapeutic drug for glaucoma, is likely to decrease in solution. In a previous study, we confirmed that this was associated with latanoprost adsorption to the container and hydrolysis of latanoprost, and established a formulation of latanoprost eye drop solution that can be stored at roo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.07.027
更新日期:2012-10-15 00:00:00
abstract::The low bioavailability of poorly water-soluble drugs is currently one of the major focuses of pharmaceutical research. One strategy currently being investigated to overcome this limitation is to decrease the particle size of the active pharmaceutical ingredients (API). An innovative process for this is spray drying w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.06.069
更新日期:2018-09-05 00:00:00
abstract::Solid dosage forms are the pharmaceutical drug delivery systems of choice for oral drug delivery. These solid dosage forms are often coated to modify the physico-chemical properties of the active pharmaceutical ingredients (APIs), in particular to alter release kinetics. Since the product performance of coated dosage ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2013.03.053
更新日期:2013-12-05 00:00:00