Abstract：
:Plasma stability plays an important role in drug discovery and development. Unstable compounds tend to have rapid clearance and short half-life, resulting in poor in vivo performance. This paper examines the variables that affect the plasma stability assay results, including substrate concentration, %DMSO, plasma concentration, enzyme activity upon incubation and batch variation. The results show that plasma stability can accommodate a wide range of experimental conditions. Relatively minor differences in results are produced with major differences in conditions. Significant batch-to-batch variations were observed for rat plasma. We selected the following conditions: 1 microM substrate concentration, 2.5% DMSO, and 50% dilution of plasma in pH 7.4 buffer. Plasma stability can be used as a diagnostic assay when compounds are unexpectedly rapidly cleared, as a special assay when structural classes contain groups that may be susceptible to plasma enzyme hydrolysis, or as general screen for compounds if resources are available. Plasma stability assay has many applications in drug discovery: to alert teams to labile structural motifs, to prioritize compounds for in vivo studies and to screen prodrugs and antedrugs.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Di L,Kerns EH,Hong Y,Chen Hdoi
10.1016/j.ijpharm.2005.03.022keywords:
subject
Has Abstractpub_date
2005-06-13 00:00:00pages
110-9issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(05)00188-2journal_volume
297pub_type
杂志文章abstract：:The objective of this study was to gain insights into the structural integrity of PLGA during an ammonolysis-based microencapsulation process. PLGA (lactide:glycolide ratio=75:25; M(w)=25,925 g/mol) was dissolved in ethyl acetate or isopropyl formate (3-6 ml), which was emulsified in an aqueous phase. Ammonia, being a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.07.022
更新日期：2011-10-31 00:00:00
abstract：:Phenotyping of cytochrome P450 isoenzymes is used for metabolic profiling. Phenotyping cocktails are usually administered as individual marketed products, which are not designed for diagnostic applications. Therefore, a formulation strategy was developed, which can be applied to any phenotyping cocktail. The formulati...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.08.043
更新日期：2016-10-15 00:00:00
abstract：:Antibiotics are well-known disruptive elements of the intestinal microbiota and antibiotic-associated diarrhea appeared as the most common complication related with post-antibiotic dysbiosis. Lactobacillus rhamnosus GG (LGG) strain is very effective in preventing antibiotic-associated diarrhea in children and adults. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119414
更新日期：2020-06-30 00:00:00
abstract：:Albumin microparticles have found many applications in diagnosis and treatment in recent years and more than 100 diagnostic agents and drugs have been incorporated into albumin microparticles. In the present study, bovine serum albumin (BSA) based microparticles bearing captopril were prepared by an emulsification-hea...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.10.025
更新日期：2006-01-03 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：UNLABELLED:The aim of this study is to validate the ability of the disappearance model to predict absorption rates of insulin aspart in pigs. The disappearance model is used as a screening tool to estimate absorption rates after subcutaneous injections in humans or pigs especially of insulin and insulin analogues. The ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.004
更新日期：2007-02-07 00:00:00
abstract：:11-Keto-β-boswellic acid (KBA) is an important and potent boswellic acids responsible for anti-inflammatory action of Boswellia extract. However, its pharmaceutical development has been severely limited by its poor oral bioavailability. The present work aims to investigate the permeability related hurdles in oral deli...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.01.019
更新日期：2014-04-10 00:00:00
abstract：:Intracranial injection of the rodent adapted CAM/RB strain of measles virus (MV) induces encephalitis in CBA/ca mice. It has already been shown that cyclodextrins can be used as carriers to increase the antiviral activity of ribavirin (RBV) against MV in cellular model. In this study, the antiviral activity of a RBV/a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.043
更新日期：2008-06-05 00:00:00
abstract：:Glutathione (GSH) grafted onto nanoliposomes (GSH-liposomes) have the potential to enhance drug delivery into the brain. GSH is known to be an unstable tripeptide, however, despite widespread use to promote active transport its stability has been largely ignored to date. Therefore this study focuses on the optimisatio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118451
更新日期：2019-08-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.07.021
更新日期：2014-10-01 00:00:00
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
更新日期：2011-02-14 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
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.01.003
更新日期：2007-06-07 00:00:00
abstract：:Polysaccharides are suitable for application as hydrophilic matrices because of their ability to hydrate and swell upon contact with fluids, forming a gel layer which controls drug release. When extracted from plants, polysaccharides often contain significant quantities of starch that impacts upon their functional pro...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.10.071
更新日期：2015-12-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.12.026
更新日期：2012-02-28 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.07.048
更新日期：2015-09-30 00:00:00
abstract：:The combination of a highly soluble salt form of a drug with a polymeric precipitation inhibitor has the potential to prolong drug supersaturation even following salt disproportionation. In this study, dissolution profiles of ibuprofen sodium in the presence of various cellulosic polymers, including hydroxypropyl meth...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.09.015
更新日期：2014-11-20 00:00:00
abstract：:Low-frequency Raman (LFR) spectroscopy probes vibrational modes related to long-range order (i.e., crystallinity) that can provide unique information on the solid-state/structural characteristics among other properties. Furthermore, the recent advancements in instrumentation (most notably, narrow wavelength band filte...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.120034
更新日期：2021-01-05 00:00:00
abstract：:A general and simple method was presented for preparing supramolecular hydrogels to deliver anticancer drugs. In this system, hydrophobic anticancer drug doxorubicin (Dox) was loaded into poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL) amphiphilic block copolymer micelles by hydrophobic interaction. The drug ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.08.007
更新日期：2012-11-01 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
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.02.037
更新日期：2016-04-11 00:00:00
abstract：:The aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the glycopeptide antibiotic vancomycin (VAN) with improved intestinal mucosa permeating properties in order to increase oral drug absorption. VAN was effectively incorporated into SEDDS increasing the lipophilicity of the d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2019-01-10 00:00:00
abstract：:Methyl methacrylate (MMA) copolymers have recently been proposed as an alternative in controlled-release matrix tablets. The aims of this study were to assess the potential value of these copolymers as direct compression excipients and to investigate relationships between the physical and structural properties of the ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00432-5
更新日期：2002-11-06 00:00:00
abstract：:The aim of this study was to develop a novel drug delivery system using two biocompatible copolymers of Solutol(®)HS15 and Soluplus(®) to improve solubility, oral bioavailability and anticancer activity of paclitaxel (PTX). The PTX-loaded mixed micelles (PTX-M) were prepared by ethanol thin-film hydration method. The ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.08.045
更新日期：2016-10-15 00:00:00
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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：:Superdisintegrants are a key excipient used in immediate release formulations to promote fast tablet disintegration, therefore understanding the impact of superdisintegrant variability on product performance is important. The current study examined the impact of superdisintegrant critical material attributes (viscosit...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2020-03-15 00:00:00
abstract：:Honokiol (HK) shows potential application in cancer treatment, but its poor water solubility restricts clinical application greatly. In this paper, monomethoxy poly(ethylene glycol)-poly(lactic acid) (MPEG-PLA) was synthesized by ring-opening polymerization and processed into nanoparticle for honokiol delivery. Chemic...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.11.014
更新日期：2010-02-15 00:00:00
abstract：:The effect of the GlycoPEGylation process used for prolonging the half-life of recombinant factor IX (rFIX) has no impact on the primary and higher order structure of activated factor IX. Characterisation work performed on recombinant factor IX and on the GlycoPEGylated form of rFIX (N9-GP), confirm that the primary s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2020-10-15 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：: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
