Bioavailability Control Laboratory, College of Pharmacy, Kangwon National University, Chuncheon, Korea.
AAPS PharmSciTech. 2010 Jun;11(2):630-6. doi: 10.1208/s12249-010-9377-0. Epub 2010 Apr 7.
Polymeric coating materials have been widely used to modify release rate of drug. We compared physical properties and release-controlling efficiency of polymeric coating materials using matrix-type casted film and diffusion-controlled coated tablet. Hydroxypropylmethyl cellulose (HPMC) with low or high viscosity grade, ethylcellulose (EC) and Eudragit(R) RS100 as pH-independent polymers and Eudragit S100 for enteric coatings were chosen to prepare the casted film and coated tablet. Tensile strength and contact angle of matrix-type casted film were invariably in the decreasing order: EC> Eudragit S100> HPMC 100000> Eudragit RS100>HPMC 4000. There was a strong linear correlation between tensile strength and contact angle of the casted films. In contrast, weight loss (film solubility) of the matrix-type casted films in three release media (gastric, intestinal fluid and water) was invariably in the increasing order: EC < HPMC 100000 < Eudragit RS100 < HPMC 4000 with an exception of Eudragit S100. The order of release rate of matrix-type casted films was EC > HPMC 100000 > Eudragit RS100 > HPMC 4000 > Eudragit S100. Interestingly, diffusion-controlled coated tablet also followed this rank order except Eudragit S100 although release profiles and lag time were highly dependent on the coating levels and type of polymeric coating materials. EC and Eudragit RS100 produced sustained release while HPMC and Eudragit S100 produced pulsed release. No molecular interactions occurred between drug and coating materials using (1)H-NMR analysis. The current information on release-controlling power of five different coating materials as matrix carrier or diffusion-controlled film could be applicable in designing oral sustained drug delivery.
高分子包衣材料被广泛应用于控制药物释放速率。我们比较了基质型铸膜和扩散控制包衣片两种方法所用高分子包衣材料的物理性质和控释效率。选择低、高粘度羟丙甲纤维素(HPMC)、乙基纤维素(EC)、Eudragit® RS100(pH 非依赖性聚合物)和 Eudragit S100(肠溶包衣材料)制备铸膜和包衣片。铸膜的拉伸强度和接触角依次减小:EC>Eudragit S100>HPMC 100000>Eudragit RS100>HPMC 4000。铸膜的拉伸强度和接触角之间存在强线性相关性。相反,三种释放介质(胃液、肠液和水)中基质型铸膜的失重(膜溶性)依次增大:EC<HPMC 100000<Eudragit RS100<HPMC 4000,Eudragit S100 除外。铸膜的释放速率顺序为:EC>HPMC 100000>Eudragit RS100>HPMC 4000>Eudragit S100。有趣的是,除了 Eudragit S100 之外,扩散控制包衣片也遵循这一顺序,尽管释放曲线和滞后时间高度依赖于包衣层的厚度和类型。EC 和 Eudragit RS100 产生持续释放,而 HPMC 和 Eudragit S100 则产生脉冲释放。(1)H-NMR 分析表明药物与包衣材料之间未发生分子相互作用。目前关于五种不同包衣材料作为基质载体或扩散控制膜的控释能力的信息可用于设计口服缓控释药物。