2种不同方法制备的紫杉醇壳聚糖缓释膜的药物缓释特性对比
Comparative Study on Releasing Characteristics of Paclitaxel Chitosan Membranes by Two Different Preparative Methods
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摘要: 目的 对比2种不同方法制备的紫杉醇壳聚糖缓释膜的药物缓释特性.方法 不同方法制备PTX-Suc-HECTS缓释膜和P-PTX-SRM缓释膜, 采用FTIR表征检测PTX载入壳聚糖缓释膜情况;多因素正交实验测量2种缓释膜平衡溶胀度最佳因素;测量出PTX的标准曲线;2种膜的不同交联度的体外PTX缓释率;根据PTX的标准曲线测量及比较2种缓释膜的药物体外释放率.结果PTX可以载入壳聚糖缓释膜中;PTX-Suc-HECTS缓释膜平衡溶胀度最佳因素是250 mg Suc-HECTS、1 mg/m L EDC·HCl与DMAP水溶液、交联时间为1 h、交联比例为1∶100, P-PTX-SRM缓释膜平衡溶胀度最佳因素是1%稀醋酸浓度、交联时间为1 h、交联比例为1∶100;2种膜片体外缓释中均有突释和缓释2部分, 其中PTX-Suc-HECTS突释率较P-PTX-SRM低 (P<0.05) , 两者缓释部分均平稳, 差异无统计学意义 (P>0.05) .交联比例越高, 48 h内突释阶段药物释放越少, 缓释阶段单位时间药物释放越多.结论 PTX-Suc-HECTS和P-PTX-SRM 2种缓释膜均有良好的缓释特性, P-PTX-SRM膜片制备过程简单, 制备时间大大缩短, 节省实验时间, 优先选择此方法制备壳聚糖缓释膜.Abstract: Objective To compare the sustained release characteristics of paclitaxel chitosan membranes prepared by two different methods.Methods We prepared PTX-Suc-HECTS sustained release film and P-PTX-SRM release film by different methods.Then we measured the PTX loaded in chitosan membrane with FTIR, measured the best of factors for equilibrium swelling degree in the two sustained release membranes with multifactors orthogonal experiment, measured the standard curve of PTX, measured the two sustained release membrane in vitro PTX release curve.According to the standard curve, we also measured and compared the drug rate between two kinds of sustained-release film release in vitro.Results PTX was loaded in the chitosan sustained release film.The best of equilibrium swelling factors for PTX-Suc-HECTS sustained-release membrane were 250 mg Suc-HECTS, 1 mg/m L EDC-HCl and DMAP aqueous solution, 1h the cross-linking time, 1∶100cross-linking ratio.The best of equilibrium swelling factors for P-PTX-SRM sustained release membrane were 1%dilute acetic acid, 1h crosslinking time, 1 ∶100 crosslinking ratio; the two sustained release membranes had bursting diaphragm part and sustained release part in vitro, but burst rate of PTX-Suc-HECTS was lower than P-PTX-SRM (P<0.05) , and there was no statistical difference between the release parts, (P>0.05) .The higher crosslinking ratio, the less drug release in burst release stage in 48 h, and more drug release in sustained release stage in unit time.Conclusion PTX-Suc-HECTS sustained release membrane and P-PTX-SRM sustained release membrane have good sustained-release characteristics, P-PTX-SRM has the advantages of simple preparation process, short preparation time and saving experiment time, so it can be a preferred method to prepare the chitosan membrane.
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Key words:
- Chitosan sustain film /
- PTX /
- Drug /
- Methods
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