Kim Min-Soo, Kim Jeong-Soo, Kang Sun-Ho, Yoo Yeon-Hee, Lee Sibeum, Park Jeong-Sook, Woo Jong-Soo, Hwang Sung-Joo
National Research Laboratory of Pharmaceutical Technology, College of Pharmacy, Chungnam National University, Daejeon, Korea.
Arch Pharm Res. 2007 Aug;30(8):1008-13. doi: 10.1007/BF02993970.
The objective of this study was to investigate the influence of various water-soluble additives and HPMCP as an enteric polymer into Surelease for the developement of oral controlled release system containg tamsulosin hydrochloride. The drug loaded pellets were coated with only Surelease or Surelease containing HPMC, PEG 4000, mannitol and HPMCP (20% w/w). In case of HPMC and PEG 4000 as additives into Surelease film, the rapid drug release was observed in pH 1.2 while the higher drug release was achieved by adding HPMCP into Surelease as well as by increasing the amount of HPMCP (10, 20, and 30% w/w) in pH 7.2. The incorporation of HPMCP into Surelease showed pH-denpendent drug release due to its pH-dependent nature. Therefore, the incorporation of HPMCP into Surelease based on aqueous coating formulation is an effective way to develop oral controlled release delivery systems containing tamsulosin hydrochloride.
本研究的目的是研究各种水溶性添加剂以及作为肠溶聚合物的羟丙甲纤维素邻苯二甲酸酯（HPMCP）加入到速释包衣材料（Surelease）中，对开发含盐酸坦索罗辛的口服控释系统的影响。载药微丸仅用Surelease包衣，或用含有羟丙基甲基纤维素（HPMC）、聚乙二醇4000（PEG 4000）、甘露醇和HPMCP（20% w/w）的Surelease包衣。当HPMC和PEG 4000作为添加剂加入到Surelease包衣膜中时，在pH 1.2条件下观察到药物快速释放，而在pH 7.2条件下，通过将HPMCP加入到Surelease中以及增加HPMCP的用量（10%、20%和30% w/w）可实现更高的药物释放。由于其pH依赖性，将HPMCP加入到Surelease中显示出pH依赖性药物释放。因此，基于水性包衣配方将HPMCP加入到Surelease中是开发含盐酸坦索罗辛的口服控释给药系统的有效方法。
