Abstract:
:Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentrations of free CQ greatly exceeding toxic plasma levels. Cell structural integrity is not essential for uptake, indicating that CQ is bound to tissue constituents and not trapped inside cells by an active process. At pH 7.4, binding of ionized CQ at anionic sites on tissue predominates over lipid partitioning of the un-ionized species. Binding to phospholipids is a major component of total muscle binding.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
MacIntyre AC,Cutler DJdoi
10.1002/jps.2600751109subject
Has Abstractpub_date
1986-11-01 00:00:00pages
1068-70issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47264-8journal_volume
75pub_type
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