Abstract
The pharmacodynamic measurement of in vivo skin penetration of lidocaine was explored with an instrument used in dentistry to determine tooth pulp vitality. The instrument delivers a low-current, pulsatile electrical waveform of increasing intensity with time. The readings, which are reproducible, are in arbitrary units on a scale of 0–80. Testing of naive sites showed variation as a function of location, even over relatively small distances. The response at a marked site over a 12-hr period generally was consistent in five subjects. Following intradermal administration of 1 or 2% lidocaine hydrochloride injection in one subject, the instrument reached its maximum value within 2 min. This was followed by a sustained plateau and then a gradual falloff of the effect. Topical formulations containing 5% lidocaine base and corresponding blank formulations were applied under occlusion within Hilltop chambers to intact skin on the forearms of human volunteers for 3 hr. While the response to a 40% propylene glycol formulation was not significantly different from the corresponding control, a cream exhibited slow development of profound anesthesia that lasted for several hours following chamber removal.
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Kushla, G.P., Zatz, J.L. Evaluation of a Noninvasive Method for Monitoring Percutaneous Absorption of Lidocaine in Vivo . Pharm Res 7, 1033–1037 (1990). https://doi.org/10.1023/A:1015939100073
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DOI: https://doi.org/10.1023/A:1015939100073