Consideration of Mechanism for Gargle Remedy of Cevimeline Hydrochloride Hydrate

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  • 塩酸セビメリン含嗽療法の作用機序に関する1考察

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In spite of excellent effectiveness, cevimeline hydrochloride als induced gastrointestinal complications, which led in some cases to the discontinuation of administration of the agent. In order to solve the problem, a therapy has been tried using cevimeline hydrochloride as a gargle, which has been reported to increases in salivation and decreases in occurrence of complications. The mechanism of the action remains to be unclear. In order to elucidate the mechanism, concentrations of cevimeline hydrochloride in plasma and labial glands were measured after the therapy was performed. The gargle solution was prepared by adding 1g of sodium bicarbonate to 30mg of cevimeline hydrochloride dissolved in 50cc of drinking water. Oral cevimeline hydrochloride (30mg) was used as control. In the gargle group, the mean concentration of cevimeline hydrochloride in the labial gland peaked 30min later at 2, 571.3ng/g and decreased gradually thereafter. In the control group, the concentration was below the measuring limit at 30min later, 413.5ng/g at 60min later and 4, 640ng/g at 90min later. As for the mean plasma concentration of the agent, it was approximately 20ng/mL at all measurements in the gargle group and less than 20ng/mL at 30 and 60min later and 138.7ng/mL at 90min later in the control group. The above results suggested that the agent was absorbed directly by the labial glands in the gargle therapy, and the increase in salivation was due to local absorption by the salivary glands.

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