吐温-80对尼莫地平HPMC骨架片的溶胀、溶蚀和药物释放的影响  

Influence of Tween-80 on swelling,erosion and drug release behavior of HPMC matrix tablets contained Nimodipine

作　　者：刘波 姜燕燕 杨晓玲 

机构地区：[1]武警宁夏总队医院药械科,宁夏银川750004

出　　处：《武警后勤学院学报（医学版）》2014年第3期202-205,F0002,共5页Journal of Logistics University of PAP（Medical Sciences）

摘　　要：【目的】探讨溶出介质中吐温-80对难溶性药物羟丙基甲基纤维素(hydroxy propyl methyl cellulose,HPMC)骨架片的溶胀、溶蚀和药物释放的影响。【方法】以尼莫地平为模型药物制备HPMC骨架片,采用改良的桨法,以不同浓度的吐温-80溶液为溶出介质,测定不同时间尼莫地平HPMC骨架片的湿重和干重,并考察尼莫地平的释放度;采用摇瓶法测定尼莫地平在不同浓度吐温-80溶液中的溶解度。【结果】尼莫地平HPMC骨架片在不同浓度吐温-80溶出介质中的吸水速率常数(k1)均在9.00h0.5左右,溶蚀速度常数(k2)均在0.022/h左右,均无显著性差异;尼莫地平在蒸馏水中32 h内累计释放百分率低于15%,而在吐温-80水溶液中,32 h内累计释放百分率均接近100%;尼莫地平的溶解度随吐温-80的浓度增加而增加。【结论】溶出介质中的吐温-80对HPMC骨架片的溶胀和溶蚀无明显影响,但可加快尼莫地平的释放;释放介质中的吐温-80主要通过增加尼莫地平在释放介质中的溶解度而加快药物的释放。[Objective] To investigate the effect of Tween-80 on the swelling, erosion and release behavior of HPMC matrix tablets containing a poorly water-soluble drug. [ Methods ] HPMC matrix tablets containing nimodipine were prepared, CP 2010 apparatus II （paddle） was employed with a slight medication, and swelling and erosion of HPMC matrix tablets were determined by measuring the wet and subsequent dry weights of matrices, and the release of nimodipine from HPMC matrix tablets was also investigated; the solubility of nimodipine was determined in Tween-80 solutions at various concentrations using a standardized shake flask method. [ Results ] The rate constants for the penetration rate of the medium into the HPMC matrix tablet were about 9.00 h0.5, the erosion rate constants were about 0.022/h, and there were no significant difference in the different medium. The dissolution of nimodipine HPMC tablets in water without Tween-80 was less than 15% within 32 h, however, this increased up to 100% when Tween-80 was added to the dissolution medium.The solubility of nimodipine increased with the concentration of Tween-80. [Conclusion] Tween-80 does not affect the swelling and erosion of HPMC matrix tablets, but can accelerate the release of nimodipine from HPMC matrix tablets. The reason that Tween-80 accelerates the release of nimodipine from PMC matrix tablets is due to the increasing nimodipine solubility in the dissolution medium.

关 键 词：吐温-80 尼莫地平 羟丙基甲基纤维素 骨架片 难溶性药物 释放 

分 类 号：R944.4[医药卫生—药剂学]