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 collected throughout a 96-h period after administration of reference product (R) and test product (T) to 28 fasting volunteers. A simple, accurate, precise and sensitive high-performance liquid chromatographic (HPLC) method with ultraviolet detection was developed and validated for quantification of fluconazole in plasma samples after liquid-liquid extraction. Bioequivalence between the products was determined by calculating 90% confidence intervals (90% C.I.) for the ratio of C(max), AUC(0-t) and AUC(0-infinity) values for the test and reference products, using logarithmic transformed data. The 90% confidence intervals for the ratio of C(max) (101.06-105.45%), AUC(0-t) (97.11-104.69%) and AUC(0-infinity) (97.96-103.36%) values for the test and reference products are within the 80-125% interval, proposed by FDA and EMEA. It was concluded that the two fluconazole formulations are bioequivalent in their rate and extent of absorption.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Porta V,Chang KH,Storpirtis Sdoi
10.1016/j.ijpharm.2004.09.013keywords:
subject
Has Abstractpub_date
2005-01-06 00:00:00pages
81-6issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(04)00549-6journal_volume
288pub_type
临床试验,杂志文章,随机对照试验abstract：:Different types of Carbopols are frequently applied excipients of various dosage forms. Depending on the supramolecular structure, their water sorption behaviour could significantly differ. The purpose of the present study was to track the supramolecular changes of two types of Carbopol polymers (Carbopol 71G and Ultr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.06.028
更新日期：2011-09-15 00:00:00
abstract：:A co-polymer of poly(N-isopropylacrylamide) (85%) co-butyl acrylate (10%) co-methacrylic acid (5%) (NIPAM/BA/MAA) (85/10/5) microgel was synthesised and investigated as a potential pH and temperature sensitive transdermal delivery device. Three compounds having different octanol/water partition coefficients and solubi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.11.040
更新日期：2005-03-23 00:00:00
abstract：:The objective of the present study was to establish several methods for the introduction of thiol groups onto the surface of human serum albumin (HSA) nanoparticles. Besides the epsilon-amino groups of lysine, the carboxyl groups of asparaginic and glutaminic acid, and the carbonyl groups of the cross-linker glutarald...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00590-1
更新日期：2000-12-15 00:00:00
abstract：:Because of their properties, ionic liquids (ILs) (Ranke et al.) offer many advantages in topical drug delivery systems. For example, ionic liquids can be used to increase the solubility of sparingly soluble drugs and to enhance their topical and transdermal delivery. Furthermore, ILs can be used either to synthesize a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.10.035
更新日期：2013-01-30 00:00:00
abstract：:During the pharmaceutical development of pregabalin extended-release tablets, an unknown degradant at a relative retention time (RRT) of 11.7 was observed and its nominal amount exceeded the ICH identification threshold in an accelerated stability study. The aim of this study is to identify the structure and investiga...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118910
更新日期：2020-02-15 00:00:00
abstract：:The absorption mechanism of several penicillins was characterized using in situ single-pass intestinal perfusion in the rat. The intrinsic membrane parameters were determined using a modified boundary layer model (fitted value +/- S.E.): Jmax* = 11.78 +/- 1.88 mM, Km = 15.80 +/- 2.92 mM, Pm* = 0, Pc* = 0.75 +/- 0.04...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/0378-5173(92)90147-t
更新日期：1992-09-20 00:00:00
abstract：:Nanoprecipitation is a simple and increasingly trending method for nanoparticles preparation. The self-assembly feature of poly (ethylene glycol)-poly (lactide-co-glycolic acid) (PEG-PLGA) amphiphilic copolymer into a nanoparticle and its versatile structure makes nanoprecipitation one of the best methods for its prep...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2017.09.054
更新日期：2017-11-25 00:00:00
abstract：:Here we explore the opportunity to design and then produce tailored release of therapeutic drugs from microcapsules. By use of "building blocks," formed from well characterized microcapsule populations, an inverse design algorithm has been developed that provides an optimal (in a least squares sense) combination of bu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.09.010
更新日期：2010-01-04 00:00:00
abstract：:The objective of this study is to evaluate the biodistribution characteristics of liposomes surface-modified with the mixture of polyethylene glycol (PEG) and polyvinyl alcohol (PVA) as a drug carrier for passive targeting of drugs. The liposomes (egg phosphatidylcholine:cholesterol=55:40, molar ratio) modified with b...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.04.004
更新日期：2008-07-09 00:00:00
abstract：:Mechanical treatments such as grinding, milling or micronization applied to crystalline drug substances may induce changes such as the occurrence of crystal defects and/or amorphous regions. These changes are likely to affect the chemical and physical properties of the material as well as the corresponding drug produc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00273-2
更新日期：1999-12-01 00:00:00
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
更新日期：2020-08-30 00:00:00
abstract：:Cancer is a malignancy engendering enormous global mortality, steering extensive research for early diagnosis and efficacious prognosis leading to emergence of cancer sensing technologies for multitudinous biomarkers. In this context, nanofibers, imparting high surface area, facile production, morphology control, and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2020.119364
更新日期：2020-06-15 00:00:00
abstract：:The aim of the present work was to find a suitable method for the introduction of thiol functions on the surface of poly(DL-lactic acid) (PLA) nanoparticles. Three different approaches were investigated. The modification of the surface involves the activation of PLA carboxylic acid groups followed by the attack of a n...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00542-2
更新日期：2003-01-16 00:00:00
abstract：:The aim of the present work was the synthesis and study the kinetics and profiles of camptothecin (CPT) release form block co- and ter-polymer conjugates comprising polylactide (PLA) segments and CPT moieties, structurally diverse by degrees of branching, content of d-PLA units and poly(ethylene glycol) methyl ether m...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.01.022
更新日期：2018-03-01 00:00:00
abstract：:The knowledge of the solubility of PEG 1500 as well as the swelling and melting point variation in supercritical CO(2) in a relatively high-pressure range is a necessary prerequisite to set-up pharmaceutical processes dealing with the polymer in the molten state. Experiments carried out in a pressurized view cell indi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.12.048
更新日期：2008-05-22 00:00:00
abstract：:In order to protect protein and peptide drugs against inactivation by different barriers in the gastro-intestinal tract and to improve their absorption, alginate microparticles as a carrier of L-lactate dehydrogenase, were developed by spray-drying technique. However, alginate complexation and spray-drying conditions ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00171-0
更新日期：2002-08-21 00:00:00
abstract：:Matrix metalloproteinases (MMPs) overexpression plays a critical role in cancer invasion and metastasis. We utilized this key feature of tumor microenvironment to develop a disease-stimuli triggered drug delivery system. Poly(acrylic acid) hydrogels were synthesized by UV polymerization and pendant MMP-2 sensitive pep...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.03.012
更新日期：2012-06-15 00:00:00
abstract：:This opinion piece gives reasons for high dose DPI applications, points out challenges and shows opportunities and possible solutions for high dose DPI. This piece of work shall set the stage for more in-depth reviews of state of the art and research papers addressing the challenges of high dose DPI which shall be inc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.06.038
更新日期：2018-09-05 00:00:00
abstract：:In this short note we report on the shelf-life stability of pDERMATT (plasmid DNA encoding recombinant MART-1 and tetanus toxin fragment-c) 2mg lyophilized powder for reconstitution for intradermal administration, used in an in-house, investigator-initiated clinical phase I study. pDERMATT was stored at 25°C/60% relat...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.06.010
更新日期：2013-09-10 00:00:00
abstract：:To evaluate the potency of hydrolyzed polyvinyl alcohols (PVAs) as matrices for solid dispersion (SD) formulations, we examined their inhibitory effects on precipitation of a poorly water-soluble drug, indomethacin (IND). Additionally, to clarify their mechanism, we investigated the intermolecular interaction of IND w...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.08.018
更新日期：2018-10-05 00:00:00
abstract：:Despite the presence of a variety of modern anticancer drugs at the market, doxorubicin (Dox) is still widely used in antineoplastic therapy, although its administration causes severe side effects. To enhance specific activity of such molecules, various approaches have been exploited: targeted moieties like monoclonal...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.12.073
更新日期：2019-03-25 00:00:00
abstract：:The fluid dynamics in the flow-through cell (USP apparatus 4) has been predicted using the mathematical modeling approach of computational fluid dynamics (CFD). The degree to which flow structures in this apparatus can be qualified as 'ideal' both spatially and temporally has been assessed. The simulations predict the...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.04.012
更新日期：2009-07-06 00:00:00
abstract：:NLC topical formulation as an alternative to oral and parenteral (IM) delivery of artemether (ART), a poorly water-soluble drug was designed. A Phospholipon 85G-modified Gelucire 43/01 based NLC formulation containing 75% Transcutol was chosen from DSC studies and loaded with gradient concentration of ART (100-750 mg)...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.10.004
更新日期：2014-12-30 00:00:00
abstract：:pH-sensitive microgels were prepared by crosslinking carboxymethylcellulose (CMC) and polymeric beta-cyclodextrin (PbetaCD) using (2-hydroxyethyl)trimethylammonium chloride benzoate (TMACB) as a crosslinker. PbetaCD was prepared by reacting epichlorohydrin and beta-CD in an aqueous phase (NaOH solution, 30% (w/w)). TM...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.12.035
更新日期：2010-03-30 00:00:00
abstract：:The aim of this study was to elucidate the importance of potential limited solubility effects for the control of drug release from hydrophilic matrix tablets loaded with a freely water-soluble drug. It is often assumed that the considerable amounts of water penetrating into this type of advanced drug delivery systems ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.05.001
更新日期：2017-06-30 00:00:00
abstract：:For use in chronic oral chemotherapeutic regimens, the potent anticancer drug docetaxel needs a solid oral dosage form. Because docetaxel has a very low permeability and a very low aqueous solubility (biopharmaceutical classification system class IV), a pharmacokinetic booster was combined with a newly developed solid...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ijpharm.2011.08.041
更新日期：2011-11-28 00:00:00
abstract：:Macromolecular crowding and the presence of organelles in the cytosol present barriers to particle mobility, such that it is unclear how nano-carriers can deliver their active agents to the nucleus. In this work a sixth generation amino terminated polyamide polylysine dendrimer (Gly-Lys(63) (NH(2))(64)) (MW 8149, diam...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.12.012
更新日期：2007-03-01 00:00:00
abstract：:Polymeric micelles (PM) based on poly(ethylene glycol)-b-poly(N-2-benzoyloxypropyl methacrylamide) (mPEG-b-p(HPMA-Bz)) loaded with paclitaxel (PTX-PM) have shown promising results in overcoming the suboptimal efficacy/toxicity profile of paclitaxel. To get insight into the stability of PTX-PM formulations upon storage...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119409
更新日期：2020-06-30 00:00:00
abstract：:The purpose of the present study was to design an optimal ketoprofen gel with appropriate penetration rate, shortened lag time and acceptable skin irritation. The combination of different mechanism enhancers including nonivamide, menthol and ethanol were used as multi-enhancers for producing a synergistic enhancement ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.02.020
更新日期：2007-07-18 00:00:00
abstract：:A series of biodegradable P(L)LA-PEG1.5 kDa-P(L)LA copolymers have been synthesized and compared as processing aid versus Poloxamer 407 (PEO-PPO-PEO), in the formulation of protein encapsulated microparticles, using supercritical carbon dioxide (scCO2). Bovine serum albumin (BSA) loaded microcarriers were prepared app...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.04.031
更新日期：2014-07-01 00:00:00
