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 intravenous administration of DA-8159 at 22:00 h, the AUC of DA-8159 was significantly greater (528 versus 368 microg min/ml) due to significantly slower CL (56.1 versus 79.5 ml/min/kg) in the rats. After intravenous administration of DA-8159 at 22:00 h, the AUC of DA-8164 was also significantly greater (108 versus 66.8 microg min/ml) possibly due to significantly greater exposure of the parent drug (AUC of DA-8159). After intravenous administration of DA-8164 at 22:00 h, the CL of DA-8164 was significantly slower; hence, this factor could also contribute to the greater AUC of DA-8164 after intravenous administration of DA-8159. However, after oral administration of DA-8159, the AUC values of both DA-8159 and DA-8164 were not significantly different between 10:00 h and 22:00 h. This was not due to decrease in gastrointestinal absorption of DA-8159 at 22:00 h and may be due to changes in intestinal first-pass effect at 22:00 h. The above data suggested that modification of dosage regimen of oral DA-8159 is not necessary in humans between 10:00 h and 22:00 h. Further studies are needed in humans.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Lee JH,Kim YC,Kwon JW,Kim WB,Lee MGdoi
10.1016/j.ijpharm.2005.03.006keywords:
subject
Has Abstractpub_date
2005-05-30 00:00:00pages
94-102issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(05)00161-4journal_volume
296pub_type
杂志文章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 purpose of this study is designing non-viral gene delivery vectors for transfection of the primary human retinal pigment epithelial cells (RPE). In the design process of gene delivery vectors, considering physicochemical properties of vectors alone does not seem to be enough since they interact with constituents o...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.12.048
更新日期：2017-02-25 00:00:00
abstract：:Twenty diclofenac sodium buccoadhesive discs containing Cp974p, polycarbophil, PEO, SCMC-medium viscosity (SCMC-MV), SCMC-ultrahigh viscosity (SCMC-UHV) or their combinations were prepared. These buccoadhesive discs were evaluated for release pattern, swelling capacity, surface pH, mucoadhesion performance, and in vit...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.07.033
更新日期：2004-11-22 00:00:00
abstract：:The purpose of the study is to screen the interactions of fourth generation fluoroquinolone-gatifloxacin with efflux pumps, i.e., P-gp, MRP2 and BCRP. Mechanism of gatifloxacin interaction with efflux transporters may explain its acquired resistance. Such clarification may lead to the development of strategies to over...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.05.027
更新日期：2010-08-16 00:00:00
abstract：:New therapeutic strategies against inflammatory bowel disease (IBD) consider the usage of probiotics, prebiotics and synbiotics as beneficial for the intestinal microbial balance. Limitations of such an approach are addressed into difference in survival, persistence, colonization and variable effects among different p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.05.049
更新日期：2017-07-15 00:00:00
abstract：:Drug interactions with diosmectite, a gastric-protective drug, were studied in vitro using an artificial stomach-duodenum model. The behavior of neutral and ionisable drugs with pKa values ranging between 2 and 8 was monitored to determine the physicochemical characteristics of the interactions. The main neutral (digo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00073-3
更新日期：1999-05-10 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：:We examined the effects of metabolic inhibitors on skin permeation of edaravone. SKF-525A, diclofenac sodium (DIC) and indomethacin (IND) were added to supernatant fluid (SF) of hairless rat (HR) skin homogenate. L-Cysteine (L-Cys) and benzotriazole (BTA), as pharmaceutical additives, were added to HR skin homogenate ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.12.038
更新日期：2009-05-08 00:00:00
abstract：:Proteins generally will tend to aggregate under a variety of environmental conditions in comparison with small drug molecules. The extent of aggregation is dependent on many factors that can be broadly classified as intrinsic (primary, secondary, tertiary or quaternary structure) or extrinsic (environment in which pro...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2010.02.025
更新日期：2010-05-10 00:00:00
abstract：:Liquid dosage forms, generally based on aqueous solutions, take an important role in drug administration. The approaches to a theoretical description of solvent and solubility properties have not yet proved completely satisfying. In this work, the Debye equation, which describes well polar and nonpolar molecules in an...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00771-2
更新日期：2001-08-28 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：:Low-frequency ultrasound application is known to increase the skin's permeability to large molecules such as vaccines, and to enable transcutaneous immunisation. Sodium dodecyl sulphate (SDS) - a skin irritant - is often included in the coupling medium at 1% (w/v), as this has been found to enhance skin permeability. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.10.014
更新日期：2009-02-23 00:00:00
abstract：:Poor mechanical properties of crystalline drug particles require wet granulation technique for tablet production which is uneconomical, laborious, and tedious. The present investigation was aimed to improve flow and mechanical properties of racecadotril (RCD), a poorly water soluble antidiarrheal agent, by a crystallo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.04.073
更新日期：2013-08-16 00:00:00
abstract：:The principal component of aqueous extract of jelly fig (Ficus awkeotsang Makino) seeds is a pectin-type polysaccharide, gelling even at room temperature without adding any sugars, acids or ions. The objective of this study was to evaluate jelly fig extract (JF) as a matrix base for sustained release tablets. Drug rel...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.08.023
更新日期：2004-12-09 00:00:00
abstract：:The development of sunscreens containing reduced concentration of chemical UV filters, even though, possessing broad spectrum effectiveness with the use of natural raw materials that improve and infer UV absorption is of great interest. Due to the structural similarities between polyphenolic compounds and organic UV f...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.06.031
更新日期：2008-11-03 00:00:00
abstract：:Felodipine is a calcium channel blocker, which shows low oral bioavailability (<15%) owing to poor water solubility and high first pass metabolism. The aim of the present investigation was to study the surface science (dynamic surface tension) and characteristics of microemulsion (Capmul MCM, Tween 20 and polyethylene...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2021.120202
更新日期：2021-01-23 00:00:00
abstract：:Methotrexate (MTX) is one of the mainstays of treatment for rheumatoid arthritis (RA) and juvenile idiopathic arthritis (JIA) and it is mainly administered either orally or by subcutaneous (SC) injection, which are not so satisfactory. While orally administered MTX is associated with variable bioavailability and cause...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119580
更新日期：2020-08-30 00:00:00
abstract：:Despite their great potential, the nano-sized extracellular vesicles are yet to become effective delivery systems for poorly water-soluble drugs. Here, we present a novel platform of exosomes as a drug delivery system by engineering of a poorly water-soluble drug into a poloxamer-based molecular nanostructured dispers...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.06.028
更新日期：2019-07-20 00:00:00
abstract：:Previously, chemical enhancer-induced permeation enhancement on human stratum corneum (SC) lipoidal pathway at enhancer thermodynamic activities approaching unity in the absence of cosolvents (defined as Emax) was determined and hypothesized to be related to the enhancer solubilities in the SC lipid domain. The object...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.09.014
更新日期：2010-01-04 00:00:00
abstract：:Poly(methyl methacrylate) (PMMA) is used to fill the gap between the prosthesis and the surrounding bone in cemented arthroplasties. Biocompatibility problems related to bone cement application limit the clinical success of these cemented arthroplasties. Being the cement surface in close connection with the living bon...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.03.011
更新日期：2004-06-18 00:00:00
abstract：:Rebaudioside A (RA) self-assembled into ultrasmall nanomicelles can be utilized as ocular drug delivery system; nevertheless, the therapeutic efficacy of RA micelles has not evaluated thus far. In this manuscript, the RA micelles are thought to strengthen the therapeutic effects of pterostilbene (Pt). Results showed t...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119035
更新日期：2020-03-15 00:00:00
abstract：:The emulsions with various oils such as linseed oil, soybean oil and squalene were prepared to obtain the relationship between the stability and the transfection activity of the emulsions. 1,2-Dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) was used as a single cationic lipid emulsifier. The droplet sizes and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00676-2
更新日期：2003-02-18 00:00:00
abstract：:The Higuchi model for the rate of drug release from matrix devices where the drug loading exceeds the solubility in the matrix medium, whose 50-year anniversary is celebrated in this issue, has proven to be a robust framework and an invaluable tool in developing a significant part of the modern controlled drug deliver...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.10.037
更新日期：2011-10-10 00:00:00
abstract：:The infection of bone and bone marrow is called osteomyelitis. Treatment is difficult since antibiotics can not reach with enough concentration to the infected area. For the first time in this study, we have developed gentamicin-loaded magnetic gelatin nanoparticles (GMGNPs) for nanocarrier-mediated and magnetically t...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119999
更新日期：2021-01-05 00:00:00
abstract：:We report the synthesis, in vitro and in vivo investigation of folate-targeted, biocompatible, biodegradable self-assembled nanoparticles radiolabelled with (99m)Tc, as potential new SPECT or SPECT/CT imaging agent. Nanoparticles with hydrodynamic size in the range of 75-200 nm were prepared by self-assembly of chitos...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.03.049
更新日期：2013-06-05 00:00:00
abstract：:The present study aimed to develop an in situ gel formulation for intranasal delivery of tacrine (THA), an anti-Alzheimer's drug. Thermosensitive polymer Pluronic F-127 was used to prepare THA in situ gels. Sol-gel transition temperature (Tsol-gel), rheological properties, in vitro release, and in vivo nasal mucocilia...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.04.015
更新日期：2014-07-01 00:00:00
abstract：:We prepared an injectable depot system for the long-term delivery of alendronate using a solid/water/oil/water multiple emulsion technique with poly(lactic-co-glycolic acid) as a carrier. The microparticles were spherical with smooth surfaces, ranging from 20 to 70 μm in size. The microspheres (ALD-HA-RG504H-MC70) wer...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.01.020
更新日期：2015-03-01 00:00:00
abstract：:Hydrochlorothiazide (HCTZ) 60 mg strength tablets containing commonly used excipients and hydroxypropyl cellulose, marketed as either Klucel-EF (HPC, NF from Hercules, USA) or HPC-L (HPC, NF from Nippon Soda, Japan), as a binder were manufactured using identical aqueous wet granulation process. The tablets containing ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.10.011
更新日期：2006-02-03 00:00:00
abstract：:Oral drug delivery is the most preferred route for patients; however, the low solubility of drugs and the resultant poor absorption compromise the benefits of oral administration. On the other hand, for years, the overwhelmingly accepted mechanism for enhanced oral absorption using lipid nanocarriers was based on the ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.08.086
更新日期：2015-11-10 00:00:00
abstract：:Microspheres containing poly(acrylic acid) and beta-cyclodextrin or maltose were prepared by a w/o solvent evaporation technique. The dispersed aqueous phase contained poly(acrylic acid) (800 mg) and beta-cyclodextrin or maltose (0, 200 or 800 mg). Food-grade olive oil was the continuous phase. Microsphere particle si...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00190-8
更新日期：1999-10-05 00:00:00
