Preparation and Evaluation of Vardenafil Cross-linked Hydrogel Patch
ZHANG Yu-jia1, TAN Hua-jin1,2, JIANG Dong1, SONG Hui1, TAN Xiao-chuan1, WANG Kai-kang1, ZHENG Wen-sheng1*
1. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing City Key Laboratory of Drug Delivery Technology and Novel Formulation, Beijing 100050, China; 2. Anhui University of Chinese Medicine, Hefei 230012, China
Abstract��OBJECTIVE To prepare a vardenafil cross-linked hydrogel patch and evaluate its quality characteristics. METHODS The vardenafil cross-linked hydrogel patch was prepared by using sodium polyacrylate as the basic matrix material and aluminum hydroxide as the crosslinking agent, which was compared on transdermal permeation properties in vitro with vardenafil hydrochloride cross-linked patch and vardenafil hydrochloride gel. Transdermal permeation properties and drug content were determined by transdermal diffusion cell and HPLC. Then adhesive force was evaluated by initial adhesion tester, adhesion tester and peel tester. Besides, deformation resistance with moisture, heat and cold resistance, formability and skin irritation were also investigated. RESULTS The vardenafil cross-linked hydrogel patch was a transparent and gelatinous solid with suitable viscidity. The method of content determination was validated in accordance with the requirements. The in vitro permeation rate of vardenafil cross-linked hydrogel patch fitted the zero-order release realation, and its permeation rate was higher than rates of vardenafil hydrochloride cross-linked patch and vardenafil hydrochloride gel in 24 h. And the cross-linked patch has better deformation resistance with moisture, heat and cold resistance, formability and no skin irritation. CONCLUSION The vardenafil cross-linked hydrogel patch has good transdermal permeation properties and vardenafil is more suitable for transdermal delivery system than vardenafil hydrochloride, which provides theoretical and practical references for further research.
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2019, Vol. 54 
