Du Qing, Ping Qi-neng, Liu Guo-jie
Hebei Medical University, Shijiazhuang 050017, China.
Yao Xue Xue Bao. 2002 Aug;37(8):653-6.
To prepare buspirone hydrochloride buccal adhesive tablet and investigate factors that influence drug release behavior and the drug release mechanism.
Buspirone hydrochloride buccal adhesive tablet was prepared with double layers structure composed of drug core and adhesive layer. The materials of the drug core were carbopol 974 and lactose, the adhesive layers were carbopol 974 and HPMC K4M. The influence of drug release factors such as adhesive layer component, adhesive layer weight and adhesive tablet hardness was investigated. The relationship between adhesive layer weight and drug release mechanism in vitro was studied.
The results showed that the weight of the adhesive layer and the hardness of adhesive tablet showed significant effects on drug release, but the adhesive layer component showed no significant effect. The optimum prescription of buspirone hydrochloride buccal adhesive tablet was carbopol: HPMC = 1:1, adhesive layer weight = 50%, and adhesive tablet hardness = 4 kg. The study of drug release mechanism from adhesive tablet showed that it was double directions when adhesive layer weight was 20%, and single direction first then double directions when 33.33%, and single direction all along when 50%.
The speed and direction of drug release from adhesive tablet can be controlled by regulating adhesive layer weight.
制备盐酸丁螺环酮口腔黏附片，并考察影响其药物释放行为的因素及药物释放机制。
采用双层结构制备盐酸丁螺环酮口腔黏附片，内层为含药层，外层为黏附层。含药层材料为卡波姆974和乳糖，黏附层材料为卡波姆974和羟丙甲纤维素K4M。考察黏附层组成、黏附层重量及黏附片硬度等药物释放因素的影响。研究黏附层重量与体外药物释放机制之间的关系。
结果表明，黏附层重量和黏附片硬度对药物释放有显著影响，但黏附层组成无显著影响。盐酸丁螺环酮口腔黏附片的最佳处方为卡波姆∶羟丙甲纤维素=1∶1，黏附层重量=50%，黏附片硬度=4 kg。黏附片药物释放机制研究表明，黏附层重量为20%时呈双向释放，33.33%时先单向释放后双向释放，50%时一直呈单向释放。
通过调节黏附层重量可控制黏附片药物释放的速度和方向。
