Abstract：
:The purpose of this study was to determine the plasma concentrations of selected NSAIDs after topical gel administration and to determine the influence of the physicochemical characteristics of these drugs on transdermal absorption. Plasma concentrations of the drugs were determined using high performance liquid chromatography. The logP values obtained from literature for piroxicam, ketoprofen, naproxen, ibuprofen and indomethacin, (1.8, 0.97, 3.22, 3.6 and 3.8, respectively) correlated with the area under the plasma-time curve (AUC) values. The AUC values determined were 527.00 (piroxicam) 269. 45 (ketoprofen) 258.65 (naproxen) 243.22 (indomethacin) and 88.09 (ibuprofen) microg/ml per h. It was concluded that the most reliable parameter for transdermal absorption was the lipophilic character of a drug (logP value). The molecular mass, solubility constraint and percentage unionized moiety can only be used in combination with other properties in the prediction of possible transdermal drug delivery.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Beetge E,du Plessis J,Müller DG,Goosen C,van Rensburg FJdoi
10.1016/s0378-5173(99)00340-3keywords:
subject
Has Abstractpub_date
2000-01-05 00:00:00pages
261-4issue
2eissn
0378-5173issn
1873-3476pii
S0378-5173(99)00340-3journal_volume
193pub_type
杂志文章abstract：:The purpose of this work was to investigate distribution, transition, bioadhesion and release behaviors of insulin loaded pH-sensitive nanoparticles in the gut of rats, as well as the effects of viscosity agent on them. Insulin was labeled with fluorescein isothiocyanate (FITC). The FITC-insulin solution and FITC-insu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.08.040
更新日期：2007-02-01 00:00:00
abstract：:Little is known about chronopharmacokinetics of PDE V inhibitors in rats as well as in humans. Hence, the pharmacokinetics of DA-8159 and one of its metabolites, DA-8164, were investigated after intravenous and oral administration of DA-8159 at a dose of 30 mg/kg administered at 10:00 h versus 22:00 h in rats. After i...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.03.006
更新日期：2005-05-30 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：: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 wa...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.05.009
更新日期：2006-09-14 00:00:00
abstract：:Many fabrication methods for microneedle (MN) involve harsh conditions and long drying time. This study aims to fabricate a dissolving MN patch in a simple and efficient manner under mild conditions, using a combination of thermal and photo polymerisation. The MN patch was fabricated by pre-polymerisation of vinylpyrr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118992
更新日期：2020-02-15 00:00:00
abstract：:The USP tablet dissolution test is an analytical tool used for the verification of drug release processes and formulation selection within the pharmaceutical industry. Given the strong impact of this test, it is surprising that operating conditions and testing devices have been selected empirically. In fact, the flow ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.08.003
更新日期：2005-03-23 00:00:00
abstract：:Antimicrobial resistance (AMR) has become a global health problem. Bacteria are able to adapt to different environments, with the presence or absence of a host, forming colonies and biofilms. In fact, biofilm formation confers chemical protection to the microbial cells, thus making most of the conventional antibiotics...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2020.119478
更新日期：2020-07-30 00:00:00
abstract：:The objective of the present study was to evaluate three formulation parameters for the application of polymethacrylic films from aqueous dispersions in order to obtain multiparticulate sustained release of diclofenac sodium. Film coating of pellet cores was performed in a laboratory fluid bed apparatus. The chosen in...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00061-9
更新日期：2003-04-30 00:00:00
abstract：:The aim of this work was to prepare and characterize inclusion complexes between a synthetic curcumin analog (dibenzalacetone, DBA) and beta-cyclodextrin (β-CD); and to evaluate their in vitro antileishmanial activity. DBA was synthetized and characterized by spectroscopic methods and the inclusion complexes were obta...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119764
更新日期：2020-08-25 00:00:00
abstract：:Topical aciclovir cream (ACV, Zovirax Cream) containing 40% propylene glycol (PG), the optimum found for skin penetration, is clinically effective in the treatment of recurrent herpes labialis. One hundred and thirty-nine ACV generic creams were analysed and 80% of these contained less than 20% PG. From this, we hypot...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.07.020
更新日期：2005-11-04 00:00:00
abstract：:The understanding of tablet disintegration is still incomplete as not all involved factors and processes are known or accounted for. E.g., the negative influence of soluble fillers, on disintegration is usually attributed to increased viscosity due to dissolved filler. When the most common filler, lactose, dissolves, ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.07.025
更新日期：2018-09-05 00:00:00
abstract：:The effect of different preparation parameters were analyzed with respect to the rheological and pharmaceutical characteristics of hydrogel blend patches, as transdermal delivery formulation. Mixtures of pectin and gelatin were employed for the production of patches, with adjustable properties, following a two-step ge...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.06.081
更新日期：2013-09-15 00:00:00
abstract：:Econazole is a commonly used azole antifungal in clinical treatment of superficial fungal infections. It is generally used as conventional cream and gel preparations under the brand names of Spectazole (United States), Ecostatin (Canada), Pevaryl (Western Europe). Treatment efficiency of antifungal drugs depends on th...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2015.09.015
更新日期：2015-11-10 00:00:00
abstract：:PLGA-microparticles with 4.7 μm in diameter were prepared by the double emulsion technique and loaded with 1.7 μg fluorescein/mg PLGA mimicking a hydrophilic API. In an effort to further elucidate the release and bioadhesive characteristics of lectin-grafted formulations in vitro, the particles were coated with wheat ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.07.025
更新日期：2012-10-15 00:00:00
abstract：:The study of controlled release and drug release devices has been dominated by considerations of the bulk or average properties of material or devices. Yet the outermost surface atoms play a central role in their performance. The objective of this article has been to characterize the surface of hydrophilic matrix tabl...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.11.054
更新日期：2015-01-15 00:00:00
abstract：:In order to develop a mucosal delivery system based on biocompatible polymers, a new methodology for production of protein-loaded microparticles is developed. Chitosan anionic precipitation/coacervation is accomplished by the addition of sodium deoxycholate (DCA). These microparticles were prepared under mild conditio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.01.006
更新日期：2006-04-07 00:00:00
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
更新日期：2010-05-31 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：:This work presents a simple and fast method for the simultaneous determination of amiloride and furosemide by digital derivative spectrophotometry. HCl 1 x 10(-2) mol/l dissolved in ethanol was used as solvent and to extract drugs from formulations. Subsequently the samples were evaluated directly by first digital der...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00482-9
更新日期：2002-12-05 00:00:00
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
更新日期：2010-05-31 00:00:00
abstract：:To develop a low-dose therapeutic system for amphotericin B (AmB), the efficacy and toxicity of lipid nano-sphere (LNS) incorporating AmB (LNS-AmB) were evaluated and compared with those of Fungizone, the conventional dosage form of AmB with sodium deoxycholate. LNS-AmB and Fungizone showed nearly equal activity again...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00342-9
更新日期：2003-09-16 00:00:00
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
更新日期：2015-12-30 00:00:00
abstract：:In this paper, we present a kinetic investigation of the polymorphic transformation γ → α of sorbitol under milling in the objective to identify the microscopic mechanisms that govern this type of solid-state transformation. The milling was performed with a high energy planetary mill and the milled material was analys...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119902
更新日期：2020-11-30 00:00:00
abstract：:Cutaneous delivery of combinations of antioxidants offers the possibility of enhanced protection against UV-radiation. In this study, we investigated the potential of sugar-based microemulsions containing monoglycerides to promote simultaneous cutaneous delivery of lycopene and ascorbic acid, and increase tissue antio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.06.016
更新日期：2012-09-15 00:00:00
abstract：:In a previous study, it was shown that the incorporation of poorly soluble drugs (BCS class II) in sugar glasses could largely increase the drug's dissolution rate [van Drooge, D.J., Hinrichs, W.L.J., Frijlink, H.W., 2004 b. Anomalous dissolution behaviour of tablets prepared from sugar glass-based solid dispersions. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.07.023
更新日期：2008-02-12 00:00:00
abstract：:The aim of the present work was to study the influence of surface hydrophilicity of biodegradable polymeric nanoparticles on cellular uptake by Caco-2 cells. Poly(D,L-lactide-co-glycolide acid) particles loaded with a fluorescent dye, 3,3'-dioctadecyloxacarbo-cyanine perchlorate (DiO), were prepared by the emulsion-ev...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.10.008
更新日期：2010-05-05 00:00:00
abstract：:The pharmaceutical industry is strictly regulated, where precise and accurate control of the end product quality is necessary to ensure the effectiveness of the drug products. For such control, the process and raw materials variability ideally need to be fed-forward in real time into an automatic control system so tha...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.09.029
更新日期：2015-11-10 00:00:00
abstract：:The purpose of this study was to engineer nanoparticles with various sustained profiles of drug release and prolonged circulation by blending poly(D,L-lactic acid)/poly(D,L-lactic/glycolic acid) (PLA/PLGA) homopolymers and poly(ethylene glycol) (PEG)-block-PLA/PLGA copolymers encapsulating betamethasone disodium 21-ph...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.04.001
更新日期：2009-06-22 00:00:00
abstract：:This study was conducted to evaluate the feasibility of developing inhalable dry powders of liposomal encapsulated ciprofloxacin nanocrystals (LECN) for controlled drug release. Dry powders of LECN were produced by freeze-thaw followed by spray drying. The formulations contained sucrose as a lyoprotectant in different...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.05.068
更新日期：2019-07-20 00:00:00
abstract：:The present study evaluates the effect of L-leucine concentration and operating parameters of a laboratory spray dryer on characteristics of trehalose dry powders, with the goal of optimizing production of these powders for inhaled drug delivery. Trehalose/L-leucine mixtures were spray dried from aqueous solution usin...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.03.004
更新日期：2019-05-01 00:00:00
