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Transdermal Bioavailability in Rats of Lidocaine inthe Forms of Ionic Liquids Salts and Deep Eutectic

机译:利多卡因大鼠体内的透皮生物利用度。离子液体盐和深共晶的形式

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摘要

Tuning the bioavailability of lidocaine was explored by its incorporation into the ionic liquid lidocainium docusate ([Lid][Doc]) and the deep eutectic Lidocaine·Ibuprofen (Lid·Ibu) and comparing the transdermal absorption of these with the crystalline salt lidocainium chloride ([Lid]Cl). Each form of lidocaine was dissolved in a vehicle cream and topically applied to Sprague–Dawley rats. The concentrations of the active pharmaceutical ingredients (APIs) in blood plasma were monitored over time as an indication of systemic absorption. The concentration of lidocaine in plasma varied between applied API-based creams, with faster and higher systemic absorption of the hydrogen bonded deep eutectic Lid·Ibu than the absorption of the salts [Lid]Cl or [Lid][Doc]. Interestingly, a differential transdermal absorption was observed between lidocaine and ibuprofen when Lid·Ibu was applied, possibly indicating different interactions with the tissue components.
机译:通过将利多卡因掺入离子液体利多卡因多库酯([Lid] [Doc])和深共晶利多卡因·布洛芬(Lid·Ibu)中,并通过将其与结晶盐利多卡因氯化物(透皮吸收)进行比较,探索了利多卡因的生物利用度的调整方法。 [Lid] Cl)。每种形式的利多卡因均溶解在载体乳膏中,并局部施用于Sprague-Dawley大鼠。随时间监测血浆中活性药物成分(API)的浓度,以指示全身吸收。血浆中利多卡因的浓度在使用的基于API的乳膏之间有所不同,氢键结合的深共晶Lid·Ibu的系统吸收比盐[Lid] Cl或[Lid] [Doc]的吸收更快和更高。有趣的是,当使用Lid·Ibu时,在利多卡因和布洛芬之间观察到了不同的透皮吸收,这可能表明与组织成分的相互作用不同。

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