周 绚 傅超美 何 瑶 章津铭 刘红亚. 不同骨架材料控制三七总皂苷多成分体外均衡释放的特征J. 药学学报, 2010,45(4): 505-509.
引用本文: 周 绚 傅超美 何 瑶 章津铭 刘红亚. 不同骨架材料控制三七总皂苷多成分体外均衡释放的特征J. 药学学报, 2010,45(4): 505-509.
ZHOU Xuan, Fu-Chao-Mei, He- Yao, Zhang-Jin-Ming, Liu-Gong-E. In vitro balanced sustained-release of Panax notoginseng saponins controlled with various matrix materialsJ. 药学学报, 2010,45(4): 505-509.
Citation: ZHOU Xuan, Fu-Chao-Mei, He- Yao, Zhang-Jin-Ming, Liu-Gong-E. In vitro balanced sustained-release of Panax notoginseng saponins controlled with various matrix materialsJ. 药学学报, 2010,45(4): 505-509.

不同骨架材料控制三七总皂苷多成分体外均衡释放的特征

In vitro balanced sustained-release of Panax notoginseng saponins controlled with various matrix materials

  • 摘要:

    为了研究骨架材料对中药复杂成分释放的影响, 初步探讨基于体外多成分均衡释放的辅料筛选模式, 本文以三七总皂苷为模型药物, 考察骨架材料HPMC (K4MK15MK100M) 和卡波姆 (934P971P974P) 对三七总皂苷中主要成分——人参皂苷Rg1、人参皂苷Rb1和三七皂苷R1体外释放均衡性的影响, 优选适宜的骨架材料。通过制备含不同骨架材料的三七总皂苷缓释片, 分别测定其在水和人工肠液中的释放度, 采用Peppas方程对释放曲线进行拟合, 用相似因子 (f2) 法统计分析释放曲线。实验数据显示, 不同骨架材料组成的各缓释片中k值和n值大小均存在差异, 释放机制属于Non-Fickiansuper Case 的转运模式, 30%卡波姆971P的缓释片在水中释药的f2值为74.9153.4557.89, 在人工肠液中的f2值为79.3555.5151.89, 符合FDA对释药曲线差异性的规定。结果表明, Rg1Rb1R1在含30%卡波姆971P的缓释片中基本能够达到均衡释放。

     

    Abstract:

    To explore the influence of matrix materials in complicate ingredients on traditional Chinese medicine and investigate the excipients selection model based on balanced release characteristics of multi-  components, the influence of HPMC (K4M, K15M, K100M) and Carbomer (934P, 971P, 974P) was illustrated  by testing in vitro release of ginsenoside-Rg1, ginsenoside-Rb1 and notoginsenoside-R1 in Panax notoginseng saponins (model drug, PNS).  According to in vitro release results of PNS matrix tablets in water and artificial intestinal juice, the release curves were analyzed with Peppas equation and simulating factor (f2).  Significant differences in k value and n value among ginsenoside-Rg1, ginsenoside-Rb1 and notoginsenoside-R1 existed in various formulations.  The release behaviors from various excipients could be described with Non-Fickian transport or super Case transport pattern.  The f2 values for ginsenoside-Rg1, ginsenoside-Rb1 and notoginsenoside-R1 in 971P matrix tablet containing 30% Carbomer 971P were 74.91, 53.45, 57.89 in water and 79.35, 55.51, 51.89 in artificial intestinal juice, respectively.  The release profiles fit for the regulation of FDA.  The result revealed that the balanced release rates of Rg1, Rb1 and R1 in 971P matrix tablet were obtained.

     

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