Delivery of a Calcium Channel Blocker Through Buccal Mucosa from Matrix Type Mucoadhesive Films for Improved Cardiac Drug Delivery
作者
Liu, DX;Ji, XF;Song, JT;Liu, ZQ;Hu, B
作者单位
[Liu, Dong-Xing; Ji, Xian-Fei; Song, Jian-Tao; Liu, Zun-Qi; Hu, Bo] Shandong Univ, Emergency Dept, Prov Hosp, Jinan 50021, Shandong, Peoples R China.
摘要
To improve the bioavailability of verapamil hydrochloride (calcium channel blocker used in several cardiac diseases like angina, arrhythmia, supraventricular tachycardias) by circumventing the hepatic first pass effect, the mucoadhesive buccal films were prepared. Mucoadhesive buccal films were prepared by solvent casting technique using hydroxy ethylcellulose, sodium carboxymethylcellulose, carbopol-972P and Eudragit RL-100. Films were evaluated for their weight, thickness, drug content uniformity, surface pH, swelling index, in vitro residence time, folding endurance, in vitro release and ex vivo permeation studies. All the films showed high drug content, good swelling and in vitro residence time. And controlled release over more than 6 h. After 6 h the in vitro release was found to be in the range of 70.24 to 94.56%. It was concluded that the films containing 50 mg verapamil in 5% w/v hydroxy ethylcellulose and 1.5% w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for cardiac diseases like arrythmia.
关键词
POLYMERS; RELEASE; HYDROCHLORIDE; MECHANISMS; SYSTEMS; VIVO