| 引用本文: | 徐兵勇,潘迎锋,平丽.氟伐他汀钠缓释片的制备及其Beagle犬体内药动学研究[J].中国现代应用药学,2019,36(4):421-425. |
| XU Bingyong,PAN Yingfeng,PING Li.Study on Preparation of Fluvastatin Sodium Extended-release Tablet and Its Pharmacokinetics in Beagle Dogs[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(4):421-425. |
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| 摘要: |
| 目的 制备氟伐他汀钠缓释片，进行体外释放特性以及Beagle犬体内药动学研究。方法 以羟丙甲纤维素为缓释材料制备氟伐他汀钠缓释片，测定其体外释放度和Beagle犬口服单剂量及多剂量后的血药浓度，推算药动学参数。结果 制备的氟伐他汀钠缓释片体外释放行为相似，口服单剂量和多剂量药动学参数Cmax分别为（3 304.23±1 043.30）μg·L-1和（3 760.86±754.77）μg·L-1，T1/2分别为（7.37±4.09）h和（6.04±2.63）h，AUC（0-t）分别为（15 052.91±3 878.01）μg·L-1和（15 374.91±2 712.20）μg·h·L-1。结论 制备的氟伐他汀钠缓释片具有较明显的缓释效果，多次给药未出现明显的蓄积现象，表现出良好的安全性。 |
| 关键词: 氟伐他汀钠 缓释片 药动学研究 体外释放度 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.04.008 |
| 分类号:R943 |
| 基金项目: |
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| Study on Preparation of Fluvastatin Sodium Extended-release Tablet and Its Pharmacokinetics in Beagle Dogs |
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XU Bingyong1,2, PAN Yingfeng1, PING Li3
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1.Zhejiang Center for Drug and Cosmetics Evaluation, Hangzhou 310012, China;2.Chiatai Qingchunbao Pharmaceutical Co. Ltd, Hangzhou 310023, China;3.Center for Drug Safety Evaluation, Zhejiang University, Hangzhou 310058, China
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| Abstract: |
| OBJECTIVE To prepare the fluvastatin extended-release tablet and investigate its pharmacokinetics in Beagle dogs and in vitro release. METHODS Hydroxypropyl methyl cellulose was used as a sustained release material to prepare fluvastatin sodium extended release tablet. The release degree in vitro and the concentration of blood drug after single and multi dose oral administration of Beagle dogs were measured. The pharmacokinetic parameters were calculated. RESULTS The release behavior of fluvastatin extended-release tablets were similar in vitro, Cmax in Beagle dogs after single dose and multi dose oral administration were (3 304.23±1 043.30)μg·L-1 and (3 760.86±754.77)μg·L-1, T1/2 were (7.37±4.09)h and (6.04±2.63)h, AUC(0-t) were (15 052.91±3 878.01)μg·L-1 and (15 374.91±2 712.20)μg·h·L-1. CONCLUSION The fluvastatin extended-release tablet shows a significant sustained release effect, and good security but not obvious accumulation phenomenon during repeated administration. |
| Key words: fluvastatin extended-release tablet pharmacokinetics release degree in vitro |
