Mechanism of the Inhibitory Effect of Polysorbate 80 on Intramuscular Absorption of Drugs. (1)

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The mechanism of the inhibition caused by polysorbate 80 on the intramuscular absorption of water-soluble drugs was studied. It was found that the absorption pattern of isonicotinamide was different from that of polysorbate 80. The inhibition of the absorption requires the existence of polysorbate 80 at the site of injection. Histological studies showed that there is no correlation between the inhibition in absorption and the local effect of polysorbate 80 which was found to cause some inflammation at the site of injection. The influence of polysorbate 80 on the capillary permeability was investigated. This was done by intravenous pre-administration of polysorbate 80,sympatholytic agent or conjugated estrogen. No difference in the intramuscular absorption of the tested drugs in the presence or absence of polysorbate 80,whether the animals were pretreated or not, could be demonstrated. Therefore, the inhibition in the intramuscular absorption of these drugs could not be attributed to a direct nor indirect effect of polysorbate 80 on the capillary walls. It was suggested that the permeation of drug through the intercellular spaces of muscle fibers and connective tissues is the more dominant process.
公益社団法人日本薬学会の論文
1976-10-25