乙醇摄入对盐酸苯环壬酯控释片释放行为的影响  

The influence of ethanol intake on the release behaviors of phencynonate hydrochloride extended release tablets

作　　者：赵静[1,2] 曾媛 刘辉 陈志龙[1] 廖诗琴[1,3] 王彦辰 ZHAO Jing;ZENG Yuan;LIU Hui;CHEN Zhi-long;LIAO Shi-qin;WANG Yan-chen(Depart- ment of Pharmacy, Wuhan General Hospital of Guangzhou Military, Hubei Wuhan 430070, China;College of Pharmacy, Hu- bei University of TCM, Hubei Wuhan 430065 ,China;Clinical Medicine College of Southern Medical University, Hubei Wu- han 430070, China)

机构地区：[1]中国人民解放军武汉总医院药剂科,湖北武汉430070 [2]湖北中医药大学药学院,湖北武汉430065 [3]南方医科大学武汉临床医学院,湖北武汉430070

出　　处：《中国医院药学杂志》2018年第10期1035-1039,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家"十二五"重大新药创制科技重大专项经费资助课题(编号:2013ZX09J13109-05C)

摘　　要：目的:考察乙醇摄入对盐酸苯环壬酯控释片释放行为的影响。方法:测定盐酸苯环壬酯控释片中盐酸苯环壬酯原料在不同浓度乙醇磷酸盐缓冲液(pH3.0)中溶解度;关键辅料WSR-HM、WSR-LM在不同浓度乙醇磷酸盐缓冲液(pH3.0)中的黏度;以0%、5%、20%、30%、40%乙醇磷酸盐缓冲液(pH3.0)为释放介质,考察并比较盐酸苯环壬酯控释片的体外累积释放度,并采用扫描电镜观察释放介质中不同浓度的乙醇对盐酸苯环壬酯控释片薄膜衣的表面结构和释药孔的影响。据此分析乙醇影响盐酸苯环壬酯控释片体外释放的原因。结果:盐酸苯环壬酯在pH3.0磷酸盐缓冲液和5%、20%、30%、40%乙醇磷酸盐缓冲液(pH3.0)中的溶解度分别为39.6,47.3,84.7,171.4,235.4 mg·mL^(-1);WSR-HM、WSR-LM的黏度随释放介质中乙醇浓度的增加而下降;盐酸苯环壬酯控释片在pH3.0磷酸盐缓冲液和5%乙醇磷酸盐缓冲液释放介质中的释放曲线相似(相似因子f_2=74),但在20%、30%、40%乙醇磷酸盐缓冲液(pH3.0)释放介质中的释放度有显著变化;盐酸苯环壬酯控释片完全释放后,残留释药孔的直径分别为552,600,630,718,815μm。结论:5%乙醇对盐酸苯环壬酯控释片的释放影响最小,而随着乙醇浓度的增加,乙醇通过改变盐酸苯环壬酯溶解度、WSR-HM及WSR-LM黏度和溶胀程度从而对盐酸苯环壬酯控释片的释放产生影响,并且乙醇浓度越大,体外释放越快。OBJECTIVE To investigating the effect of ethanol intake on the release behaviors of phencynonate hydrochloride extended release tablets.METHODS The solubility of phencynonate hydrochloride,the viscosity of the key materials WSR-HM and WSR-LM were measured in different concentrations of ethanol phosphate buffer solution（pH3.0）.The 0%,5%,20%,30%,40% ethanol phosphate buffer（pH3.0）were taken as release media to investigate and compare the cumulative release of phencynonate hydrochloride extended release tablets in vitro.Then scanning electron microscopy was used to observe the surface structure of coated film and the release hole on the tablets when taking 0%,5%,20%,30%,40% ethanol phosphate buffer（pH3.0）as release media.And causes were analyzed for release in vitro influenced by different concentrations of ethanol.RESULTS In pH3.0 phosphate buffer and 5%,20%,30%,40% ethanol phosphate buffer media,the solubility values of phencynonate hydrochloride were 39.6,47.3,84.7,171.4,235.4 mg·mL-1.The viscosity of WSR-HM WSR-LM decreased with increasing of ethanol concentration in release media.In pH3.0 phosphate buffer and 5% ethanol phosphate buffer medium,the release curves of phencynonate hydrochloride extended release tablets were similar（f2=74）,but there was a significant change in 20%,30%,40% ethanol phosphate buffer release medium.After full release,the release hole diameters were respectively 552,600,630,718,815μm.CONCLUSION 5% ethanol has the minimal impact on phencynonate hydrochloride extended release tablets.With increasing ethanol concentrations,the ethanol effcts the release of phencynonate hydrochloride extended release tablets by changing the solubility of phencynonate hydrochloride and the swelling of WSR-HM and WSR-LM.Higher concentrations of ethanol produce the greater effect and faster release behaviors in vitro.

关 键 词：盐酸苯环壬酯控释片 乙醇 累积释放度 扫描电镜 

分 类 号：R944[医药卫生—药剂学]