| 水飞蓟素磷脂复合物微孔渗透泵控释片比格犬体内药动学及体内外相关性研究 |
| 投稿时间：2022-06-13 修订日期：2022-08-31 点此下载全文 |
| 引用本文：曾棋平,杨丽娜,刘建清,宋洪涛.水飞蓟素磷脂复合物微孔渗透泵控释片比格犬体内药动学及体内外相关性研究[J].药学实践杂志,2023,41(12):741~746 |
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| 基金项目:国家自然科学基金面上项目（81073064）；福建省自然科学基金（2015J01491） |
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| 中文摘要:目的 评价水飞蓟素磷脂复合物微孔渗透泵（SM-PC MPOP）控释片的体外释药特性、比格犬体内药动学及其体内外相关性。方法 释放介质为pH7.5的磷酸盐缓冲液（添加0.5%十二烷基硫酸钠），以高效液相色谱法（HPLC）检测SM-PC MPOP的体外释放特征。用6只比格犬进行双周期交叉对照实验，按照30 mg/kg的剂量给药。HPLC法测定比格犬血浆内水飞蓟素的主要成分水飞蓟宾的质量浓度，应用药动学软件进行数据分析。结果 SM-PC MPOP在12 h累积释放度超过85%。药动学研究情况表明，受试制剂（SM-PC MPOP）和参比制剂（市售水飞蓟素胶囊）在比格犬体内的主要药动学参数：Tmax分别为（3.2±0.4）、（0.9±0.1）h，Cmax分别为（0.298 6±0.068 9）、（0.629 9±0.076 5） μg/ml，AUC0→24分别为（2.996 8±0.583 3）、（2.268 9±0.432 8） h·μg /ml，SM-PC-MPOP对市售水飞蓟素胶囊的相对生物利用度为（162.21±30.82）%。结论 自制的SM-PC MPOP实现了缓慢释药且增加生物利用度的目标，其体内吸收与体外释药具备相对较好的关联性（r＝0.839 0）。 |
| 中文关键词:水飞蓟素 磷脂复合物 微孔渗透泵控释片 药动学 体内外相关性 高效液相色谱法 生物利用度 |
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| In vivo pharmacokinetics and in vitro-in vivo correlation of silymarin phospholipid complex microporous osmotic pump controlled-release tablets in beagle dogs |
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| Abstract:Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of silymarin phospholipid complex microporous osmotic pump controlled release tablets（SM-PC MPOP）.Methods The release characteristics of SM-PC MPOP in vitro were detected by HPLC in the artificial gastric fluid. Six beagle dogs were subjected to double cycle cross control, which were given SM-PC MPOP and Legalon（30 mg/kg）. The concentration of silybin in plasma was determined by HPLC and the data were processed by software. Results The cumulative release rate of SM-PC MPOP in vitro was over 85% in 12 h. The pharmacokinetics in beagle dogs showed that SM-PC MPOP and legalon conformed to double compartment first-order absorption model and the pharmacokinetic parameters were obtained: tmax:（3.2±0.4）and（0.9±0.1）h, Cmax:（0.298 6±0.068 9）and（0.629 9±0.076 5）μg/ml, AUC0→24:（2.996 8±0.583 3）and（2.268 9±0.432 8）h·μg /ml. The relative bioavailability of SM-PC MPOP was（162.21 ±30.82）%. Conclusion SM-PC MPOP could release slowly, which could increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro was fine（r = 0.839 0）. |
| keywords:silymarin phospholipid complex microporous osmotic pump controlled release tablets pharmacokinetics in vivo-in vitro correlation HPLC bioavailability |
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