Abstract:
PURPOSE:The pharmacokinetics, analgesic efficacy, and irritancy potential of Buprederm, a new transdermal delivery system of buprenorphine, was evaluated. METHODS:Single and multiple dose pharmacokinetic studies were conducted in mice and rabbits. The analgesic efficacy and skin irritation potential were determined by tail flick and writhing tests in mice and by the Draize dermal scoring system in rabbits. RESULTS:Fast absorption of buprenorphine into the bloodstream was observed in mice and rabbits after Buprederm application. The peak buprenorphine level in plasma was achieved between 1 and 24 h, and the effective therapeutic drug concentration was maintained for 72 h. No significant accumulation of buprenorphine was seen after multiple consecutive applications of patches to rabbits with a 4-day dosing interval. Buprederm induced prolongation of tail-flick latency in a dose- and time-dependent manner. Maximum analgesic effect was attained between 3 and 6 h and was maintained for 24 h after patch application. No skin irritation was demonstrated in rabbits after repeated Buprederm application. CONCLUSIONS:Buprederm was shown to be efficacious by achieving the effective buprenorphine concentration in the blood and brain sufficient to maintain an analgesic effect for 72 h, and was also shown to be safe following multiple applications.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Park I,Kim D,Song J,In CH,Jeong SW,Lee SH,Min B,Lee D,Kim SOdoi
10.1007/s11095-007-9470-6subject
Has Abstractpub_date
2008-05-01 00:00:00pages
1052-62issue
5eissn
0724-8741issn
1573-904Xjournal_volume
25pub_type
杂志文章abstract:PURPOSE:Stable transformants expressing human multidrug resistance 1 (MDR1), monkey MDR1, canine MDR1, rat MDR1a, rat MDR1b, mouse mdr1a, and mouse mdr1b in LLC-PK1 were established to investigate species differences in P-glycoprotein (P-gp, ABCB1) mediated efflux activity. METHODS:The seven cDNAs of MDR1 from five an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0285-7
更新日期:2006-07-01 00:00:00
abstract:PURPOSE:We investigated the characteristics of transport of an organic anion, p-aminohippurate (PAH), at the apical membrane in a kidney epithelial cell line OK. METHODS:Efflux and uptake of [14C]PAH across the apical membrane were measured using OK cell monolayers grown on microporous membrane filters. RESULTS:PAH e...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1021437306990
更新日期:2002-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1014212630566
更新日期:2002-02-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9783-0
更新日期:2009-04-01 00:00:00
abstract:PURPOSE:This study was designed to investigate the stability of recombinant FVIII (rFVIII) in solution at different pHs and to probe the cause(s) of rFVIII inactivation under accelerated storage conditions. METHODS:Aqueous stability samples of full-length rFVIII at different pHs were incubated at 40 degrees C for seve...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023271405005
更新日期:2003-04-01 00:00:00
abstract:PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9295-3
更新日期:2007-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000008053.69903.c1
更新日期:2003-12-01 00:00:00
abstract:PURPOSE:Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1660-z
更新日期:2015-08-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2005-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023250900462
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2013-01-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9110-6
更新日期:2006-10-01 00:00:00
abstract:PURPOSE:A rapid immune response is required to prevent death from Anthrax, caused by Bacillus anthracis. METHOD:We formulated a vaccine carrier comprised of acetalated dextran microparticles encapsulating recombinant protective antigen (rPA) and resiquimod (a toll-like receptor 7/8 agonist). RESULTS:We were able to p...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-0975-x
更新日期:2013-05-01 00:00:00
abstract::The synthesis of an homologous series of new water-soluble derivatives of pilocarpine is described. The new compounds, referred to as soft quaternary salts, are water soluble by virtue of a cationic ammonium head and their lipophilicity can be modulated by manipulating the size and the nature of the substituent in the...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015847103862
更新日期:1992-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018921306200
更新日期:1994-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1298-2
更新日期:2014-08-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018907825281
更新日期:1994-05-01 00:00:00
abstract::A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016346018962
更新日期:1984-11-01 00:00:00
abstract::Micelle-associated epoetin is still a possible explanation for the upsurge of pure red blood cell aplasia associated with subcutaneous use of epoetin alpha in patients with chronic renal failure. ...
journal_title:Pharmaceutical research
pub_type: 评论,信件
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更新日期:2006-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9891-5
更新日期:2009-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0790-9
更新日期:2012-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9499-6
更新日期:2008-05-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-021-02991-4
更新日期:2021-01-26 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018919811227
更新日期:1994-02-01 00:00:00
abstract:PURPOSE:Understanding the critical factors governing the crystallization tendency of organic compounds is vital when assessing the feasibility of an amorphous formulation to improve oral bioavailability. The objective of this study was to investigate potential links between viscosity and crystallization tendency for or...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0540-4
更新日期:2012-01-01 00:00:00
abstract:PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011913723928
更新日期:1998-07-01 00:00:00
abstract::The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016381017357
更新日期:1986-02-01 00:00:00
abstract::During the past two decades the nanomedicine field has experienced significant progress. To date, over sixty nanoparticle (NP) formulations have been approved in the US and EU while many others are in clinical or preclinical development, indicating a concerted effort to translate promising bench research to commercial...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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更新日期:2019-12-11 00:00:00
abstract::This study utilized different statistical techniques to evaluate the reliability (internal consistency) and the discriminant validity of the most widely used measures of organizational commitment and intention to quit (the employing organization). Data were obtained from a national mail survey of members of the Americ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018930718979
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2249-5
更新日期:2017-12-01 00:00:00