[Cutaneous permeation kinetics and pharmacodynamics of topical lidocaine gel in rat].
OBJECTIVE
To study the cutaneous permeation kinetics and pharmacodynamics of lidocaine gel.


METHODS
The concentration of lidocaine in dermis following topical application in rats was determined by the cutaneous microdialysis technique and related parameters were calculated; the pharmacodynamics of the gel was evaluated by electric stimulation method with EMLA (eutectic mixture of local anesthetics) cream as a control.


RESULTS
The peak of percutaneous absorption kinetic profile of lidocaine gel across rat skin occurred at 1.25 h; the onset time of local anesthetic action of lidociane gel was similar to that of EMLA, but both the duration and depth of anesthetic effect were superior to EMLA cream.


CONCLUSIONS
Lidocaine gel showed good anesthetic effect. The minimum effective concentration of lidocaine in dermis is 12 mg.L-1.
Jia
Shi-cong
SC
School of Pharmacy, Shenyang Pharmacetical University, Shenyang 110016, China.
Ding
Ping-tian
PT
Chen
Duo
D
Zheng
Jun-min
JM
D000772:Anesthesia, Local; D000779:Anesthetics, Local / Q000493:pharmacokinetics* / Q000494:pharmacology; D000818:Animals; D005782:Gels; D008012:Lidocaine / Q000493:pharmacokinetics* / Q000494:pharmacology; D000077442:Lidocaine, Prilocaine Drug Combination; D008297:Male; D017288:Pain Threshold / Q000187:drug effects; D011318:Prilocaine / Q000493:pharmacokinetics* / Q000494:pharmacology; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption
D000779:Anesthetics, Local; D005782:Gels; D000077442:Lidocaine, Prilocaine Drug Combination; D011318:Prilocaine; D008012:Lidocaine