摘要
目的制备释药稳定的时间依赖型结肠定位释药系统。方法以蜡质材料合并羧甲基淀粉钠、氯化钠为片芯骨架,Eudragit?NE 30D为内层控释层,ACRYL-EZE为外层肠溶层制备时间依赖型结肠定位释药系统。考察蜡质材料和片芯的膨胀性及影响制剂释药时滞和释放度的主要因素,并比较含蜡质材料控释片与不含蜡质材料控释片的释放行为。结果影响制剂释药时滞及释放度的主要因素有蜡质材料、CMS-Na的用量及控释层的包衣增质量及致孔剂用量。蜡质材料熔融后体积增加(9.4±0.7)%;片芯吸水膨胀后含蜡质材料片芯厚度增加为不含蜡质片芯的1.1倍,且释放过程中也可见控释片破裂释药均在厚度方向上;含蜡质材料控释片的释药时滞较为均一,其释放相似因子为62.83±5.86,较不含蜡质材料片剂相似因子38.07±7.12高,释药速率略有减慢,但在开始释药2 h后药物能够完全释放。结论制备的蜡质骨架包衣片在模拟肠液中时滞约为2 h且释药平稳,有结肠定位释药的特性。
Objective To develop a time-dependent colon-specific tablet of mesalazine based on wax-matrix. Methods The tablet core consisted of semi-synthetic glycerides, being the wax polymeric expanding agent, CMS-Na and NaCl. The core was coated with Eudragit?NE 30D as the inner coating materials and with ACRYL-EZE as the outer coating materials. The swelling properties of wax-matrix and tablet cores, the factors which influence the release behaviors of the tablets were investigated. The release profiles of coated tablets with wax-matrix and without wax-matrix were compared. Results Some factors had great effect on drug release, including the amount of CMS-Na, wax-matrix and pore former in controlling layer, and the weight gain of controlling layer. The volume of wax-matrix after melting increased by(9.4 ± 0.7)%. After absorbing water, tablet cores swelled, and the thickness of tablet cores with wax-matrix increased to be 1.1 times of that of tablets cores without wax-matrix. The rupture for burst release of coated tablets with wax-matrix occurred in the thickness direction. Meanwhile, tablets with wax-matrix demonstrated a relatively steady lag time, a higher f2 of 62.83 ± 5.86, a slight slower release rate, and a complete release of drug within 2 h. Conclusion The wax-matrix tablets have a steady lag time and release rate, together with colon specific properties.
出处
《中国药剂学杂志（网络版）》
2014年第3期88-96,共9页
Chinese Journal of Pharmaceutics：Online Edition
