Abstract:
PURPOSE:Evaluate the ability of (-)-6-aminocarbovir ((-)-6AC) to improve the CNS exposure to (-)-carbovir ((-)-CBV). METHODS:Activation of (-)-6AC in vitro was assessed by incubations of rat brain tissue homogenates. The in vivo brain exposure to (-)-CBV was then examined in rats after iv infusions of either (-)-CBV (n = 4) or (-)-6AC (n = 5). The drugs were infused to steady-state via the jugular vein. At the end of the infusion, a bolus of [3H]inulin was injected via the femoral vein in order to obtain an estimate of the brain vascular space. RESULTS:(-)-6AC was converted to (-)-CBV by incubations of rat brain tissue homogenates. After iv infusion of (-)-CBV, the brain/blood concentration ratio of (-)-CBV was 0.032 +/- 0.009. The brain/blood concentration ratio of (-)-CBV after iv infusion of (-)-6AC was 0.080 +/- 0.020. CONCLUSIONS:(-)-6AC improved the brain delivery of (-)-CBV, although the absolute exposure of the brain tissue to (-)-CBV was still quite low.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Wen YD,Remmel RP,Pham PT,Vince R,Zimmerman CLdoi
10.1023/a:1016229624703subject
Has Abstractpub_date
1995-06-01 00:00:00pages
911-5issue
6eissn
0724-8741issn
1573-904Xjournal_volume
12pub_type
杂志文章abstract::The effect of freezing on formation of soluble and insoluble aggregates of human growth hormone (hGH) was studied. The amount of soluble aggregates was affected very little by freezing regardless of the cooling rate. In contrast, the formation of insoluble aggregates (particulates), as determined by light scattering i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015888704365
更新日期:1991-11-01 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:1998-09-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016239321494
更新日期:1995-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1385-4
更新日期:2014-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0812-7
更新日期:2012-11-01 00:00:00
abstract:PURPOSE:Exenatide, a potent insulinotropic agent, can be used for the treatment of non-insulin-dependent diabetes mellitus. However, the need for frequent injections seriously limits its therapeutic utility. The aim of present report was to develop an orally available exenatide formulation using goblet cell-targeting n...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2015-03-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016008102587
更新日期:1996-08-01 00:00:00
abstract:PURPOSE:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2744-y
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journal_title:Pharmaceutical research
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更新日期:2010-05-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1015809702296
更新日期:1991-01-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1992-01-01 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:1996-01-01 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:1998-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-7671-9
更新日期:2004-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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更新日期:2012-05-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2007-06-01 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:2006-01-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011973625803
更新日期:1998-04-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2752-y
更新日期:2020-01-06 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023230328687
更新日期:2003-04-01 00:00:00