Abstract：
:Intravenously administered (i.v.) drug-cyclodextrin (CD) inclusion complexes are generally expected to dissociate rapidly and completely, such that the i.v. pharmacokinetic profile of a drug is unchanged in the presence of CD. The altered pharmacokinetics of a synthetic ozonide in rats has been attributed to an unusually high-binding affinity (2.3 × 10(6) M(-1) ) between the drug and sulfobutylether7 -β-cyclodextrin (SBE7 -β-CD) with further studies suggesting a significant binding contribution from the adamantane ring. This work investigated the binding affinity of three adamantane derivatives [amantadine (AMA), memantine (MEM) and rimantadine (RIM)] to SBE7 -β-CD and the impact of complexation on their i.v. pharmacokinetics. In vitro studies defined the plasma protein binding, as well as the impact of SBE7 -β-CD on erythrocyte partitioning of each compound. SBE7 -β-CD binding constants for the compounds were within the typical range for drug-like molecules (10(2) -10(4) M(-1) ). The pharmacokinetics of AMA and MEM were unchanged; however, significant alteration of RIM plasma and urinary pharmacokinetics was observed when formulated with CD. In vitro studies suggested two factors contributing to the altered pharmacokinetics: (1) low plasma protein binding of RIM, and (2) decreased erythrocyte partitioning in the presence of high SBE7 -β-CD concentrations. This work demonstrated the potential for typical drug-cyclodextrin interactions to alter drug plasma pharmacokinetics.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Leong NJ,Prankerd RJ,Shackleford DM,Mcintosh MPdoi
10.1002/jps.24331subject
Has Abstractpub_date
2015-04-01 00:00:00pages
1492-8issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)30172-6journal_volume
104pub_type
杂志文章abstract：:The dissolution behavior and absorption of mefenamic acid following oral and rectal administration from drug:egg albumin solid dispersions have been studied in comparison with those of the drug alone. The interaction of drug with egg albumin in aqueous solution and solid state were examined by solubility analysis, dia...
journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600720908
更新日期：1983-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
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journal_title：Journal of pharmaceutical sciences
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更新日期：2010-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600640536
更新日期：1975-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650221
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更新日期：2005-09-01 00:00:00
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doi：10.1002/jps.2600790107
更新日期：1990-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/jps.2600750416
更新日期：1986-04-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740408
更新日期：1985-04-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670212
更新日期：1978-02-01 00:00:00
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pub_type： 杂志文章
doi：10.1002/jps.21777
更新日期：2009-12-01 00:00:00
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pub_type： 杂志文章
doi：10.1002/jps.2600650908
更新日期：1976-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600790308
更新日期：1990-03-01 00:00:00
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doi：10.1016/j.xphs.2017.03.020
更新日期：2017-10-01 00:00:00
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pub_type： 杂志文章
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doi：10.1002/jps.2600640807
更新日期：1975-08-01 00:00:00
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更新日期：2012-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731137
更新日期：1984-11-01 00:00:00
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doi：10.1016/j.xphs.2017.03.032
更新日期：2017-09-01 00:00:00
abstract：:Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600681034
更新日期：1979-10-01 00:00:00
abstract：:A radioimmunoassay procedure was developed for the antihistamine terfenadine (alpha[4-(1,2-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol). The keto analog of terfenadine was converted to its O-carboxymethyloxime derivative, which was conjugated to bovine thyroglobulin by a mixed anhydride techniq...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600691218
更新日期：1980-12-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790203
更新日期：1990-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.06.021
更新日期：2016-10-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600641213
更新日期：1975-12-01 00:00:00
abstract：:Porcine gelatins have been widely used as stabilizers of macromolecular based pharmaceuticals but the mechanism by which they stabilize has not been precisely established. Their variability and immunogenicity, however, make them less than ideal excipients. In this work, we take advantage of the availability of recombi...
journal_title：Journal of pharmaceutical sciences
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更新日期：2007-12-01 00:00:00
