Tolterodine, a nonselective muscarinic antagonist available only as immediate release (IR) or extended release (ER) oral formulations, is used for the treatment of overactive bladder (OAB). This study aimed to compare the efficacy and extent of dry mouth adverse effects of tolterodine transdermal patch to the oral formulation. The two formulations have been examined through the muscarinic receptor binding tests conducted in bladder and salivary gland tissues and the salivary secretion tests conducted in rats. Comparable average tolterodine blood concentration levels were obtained 3 h after oral administration of tolterodine 25 mg/kg and 12 h after transdermal application of tolterodine patch 6 mg/8 cm(2). While Kd in the bladder tissue increased to a similar degree in both formulations of tolterodine, Kd in the salivary gland increased to a greater degree in the oral formulation. These results indicate that similar degree of inhibitory effects were observed in the bladder for both formulations while less inhibitory effects were observed in the salivary gland with tolterodine transdermal formulation compared to the oral formulation. For assessment of salivary secretion, tolterodine transdermal patch 6 mg/8 cm(2) application resulted in significantly less inhibitory effects than oral tolterodine 25 mg/kg. Therefore, this study suggests that tolterodine transdermal patch could be a useful formulation that provides uniform and consistent inhibitory effects to effectively control OAB symptoms with reduced severity of dry mouth in comparison to the oral formulation.
Archives of pharmacal research. 2017 Nov 20 [Epub ahead of print]
Ji-Yeong Byeon, Young-Hoon Kim, Se-Hyung Kim, Choong-Min Lee, Chang-Ik Choi, Jung-Woo Bae, Choon-Gon Jang, Seok-Yong Lee, Yun Jeong Lee
School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea., College of Pharmacy, Dongguk University-Seoul, Goyang, 10326, Republic of Korea., College of Pharmacy, Keimyung University, Daegu, 42601, Republic of Korea., School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea. ., College of Pharmacy, Dankook University, Cheonan, 31116, Republic of Korea. .