Adsorption of Local Anesthetics from Aqueous Solution. Analysis of Factors Affecting the Nerve Blocking

概要

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Evaluating the extent of the hydrophobicity of 8 local anesthetics by the adsorbability on carbon black, discussions were made what kind of role the hydrophobicity plays in the nerve blocking. Additionally, the relationship between the partition coefficient in n-octanol/buffer solution and the blocking potency was investigated. The adsorbed amount (represented by a) increased with pH, while the reported data of minimum blocking concentration (MBC) decreased. There was no comparison between the increases of a and 1/(MBC) with pH, because the latter increase was so remarkable. The blocking potency (represented by -log (MBC)) increased with the adsorbability (represented by log b), where all the data were included between log b=2.8,and log b=4.1. The most available local anesthetics had the adsorbability around log b=4. The blocking potency increased with the decrease in the occupied area by one molecule. The increasing tendency of partition coefficient with pH was closer to that of 1/(MBC) than that of a or b. All the results suggested that a minimum adsorbability of drug is necessary in the nerve blocking and the behavior of drug under the surface of nerve membrane which may be related with the penetration forms a necessary factor affecting the activity.
公益社団法人日本薬学会の論文
1971-01-25