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汪宇星, 孙敏捷, 平其能, 张灿. 琥珀酸美托洛尔缓释微丸的制备及大鼠体内药代动力学[J]. 中国药科大学学报, 2013, 44(4): 334-338. DOI: 10.11665/j.issn.1000-5048.20130409
引用本文: 汪宇星, 孙敏捷, 平其能, 张灿. 琥珀酸美托洛尔缓释微丸的制备及大鼠体内药代动力学[J]. 中国药科大学学报, 2013, 44(4): 334-338. DOI: 10.11665/j.issn.1000-5048.20130409
WANG Yuxing, SUN Mingjie, PING Qineng, ZHANG Can. Praparation of metoprolol succinate sustained-release pellets and its pharmacokinetics in rats[J]. Journal of China Pharmaceutical University, 2013, 44(4): 334-338. DOI: 10.11665/j.issn.1000-5048.20130409
Citation: WANG Yuxing, SUN Mingjie, PING Qineng, ZHANG Can. Praparation of metoprolol succinate sustained-release pellets and its pharmacokinetics in rats[J]. Journal of China Pharmaceutical University, 2013, 44(4): 334-338. DOI: 10.11665/j.issn.1000-5048.20130409

琥珀酸美托洛尔缓释微丸的制备及大鼠体内药代动力学

Praparation of metoprolol succinate sustained-release pellets and its pharmacokinetics in rats

  • 摘要: 采用空白丸芯上药制备含药丸芯,以乙基纤维素为缓释材料,采用流化床包衣法制备了琥珀酸美托洛尔缓释微丸。以美国药典为标准对比,分析了自制品和市售品在pH 6.8 PBS、0.1 mol/L盐酸(pH 1.0)和水3种介质中的释放曲线,计算出相似因子(f2),并进一步对比分析了自制品和市售品在大鼠体内药代动力学行为差异。结果显示,采用60~88目空白丸芯,上药增重为100%,缓释层增重为22.7%~25.46%的缓释微丸与市售品在3种介质中的释放曲线的f2均大于50,相似性良好,同时方差分析显示两种制剂在大鼠体内的主要药代动力学参数没有显著性差异。

     

    Abstract: The sustained-release pellets of metoprolol succinate which comprise a drug-layered sugar core and a ethyl cellulose layer were prepared by a fluid bed dryer. The release of the domestic products and the commercial ones were tested in pH 6. 8 PBS, 0. 1 mol/L HCl and water based on the USP standard. And f2 value was calculated. In vivo pharmacokinetic parameters of self and domestic products were also compared. The results showed that the formula could reach the USP standard and the optimal ratio of sugar core(200-300 μm in diameter), drug layer and EC layer based on the sugar core weight was 100: 100: 45. 4-50. 92. The f2 value of the release curves in pH 6. 8 PBS, water and 0. 1 mol/l HCl was 79. 34, 65. 04, 54. 43, respectively. Analysis of variance indicated no significant deviation between the two products.

     

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