乙醇摄入对盐酸苯环壬酯控释片释放行为的影响

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pH 3.0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f₂=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552,600,630,718,815 μm。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。

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

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 (pH 3.0) 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 pH 3.0 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 pH 3.0 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 552,600,630,718,815 μm.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.