Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone.

摘要

Eperisone hydrochloride is widely used for the treatment of plasticity to relieve muscle stiffness and back pain. However, oral eperisone has a very low bioavailability and short muscle relaxant activity, because of the profound intestinal first-pass metabolism. To improve the efficacy and compliance of eperisone, we designed a new dosage form, a transdermal patch, and evaluated the efficacy of the eperisone patch with the muscle relaxant activity of rats. The muscle relaxant activity was assessed by the measurement of forelimb grip strength and hanging test in rats. The transdermal patch of eperisone showed significantly enhanced muscle relaxant activity at 0.5 1.5 and 3 cm2/200 g rat (1.39, 4.17 and 8.33 mg of eperisone hydrochloride/kg, respectively) in a dose-dependent manner and the effects lasted over 24 h. Even though oral eperisone hydrochloride showed significant muscle relaxant activity at 12.5, 25 and 50 mg/kg in a dose-dependent manner, the activity lasted only 1 or 2 h after administration. These results suggest that eperisone as transdermal patch form showed efficient absorption with more potent and longer-lasting muscle relaxant activity than oral solution. The transdermal patch form of eperisone will increase the efficacy and compliance in the clinical use of eperisone.