| 谭永刚 李海燕 杨茜 高立军 全东琴.氯雷他定固体自乳化制剂的体外溶出及体内药动学研究[J].,2015,15(14):2606-2609 |
| 氯雷他定固体自乳化制剂的体外溶出及体内药动学研究 |
| The Solid Self-emulsified Drug Delivery System(S-SEDDS) of Loratadine:Dissolution in Vitro and Pharmacokinetic Studies in Vivo |
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| DOI： |
| 中文关键词: 固体自乳化制剂 氯雷他定 生物利用度 溶出度 |
| 英文关键词: S-SEDDS Loratadine Bioavailability Dissolution |
| 基金项目:国家自然科学基金项目（81102390） |
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| 中文摘要: |
| 目的：研究氯雷他定固体自乳化制剂的体外溶出行为及其在比格犬体内的药物动力学。方法：采用HPLC 方法测定氯雷他
定固体自乳化制剂与市售片剂的体外溶出曲线；采用LC-MS/MS 测定市售片剂和氯雷他定固体自乳化制剂在比格犬体内的血药
浓度，考察氯雷他定固体自乳化制剂的相对生物利用度。结果：以0.1 mol·L-1盐酸溶液为溶出介质的体外溶出结果表明，氯雷他
定固体自乳化胶囊与市售片剂30 min 时均可以溶出80%以上；比格犬体内药物动力学研究结果表明，固体自乳化制剂比市售片
剂最高血药浓度显著性增加（P<0.05），Cmax=1.79 ug·L-1，而市售片剂Cmax=0.67 ug·L-1；AUC(0~t)提高了149%（P<0.05）。结论：固体自
乳化制剂可以显著提高氯雷他定的体内吸收。 |
| 英文摘要: |
| Objective:To evaluate the dissolution behavior in vitro and the pharmacokinetic parameters of the solid self-emulsified
drug delivery system (S-SEDDS) containing loratadine in beagle dogs.Methods:The accumulated dissolution of loratadine from
tablets(Clarityne) and the S-SEDDS formulation in vitro were tested by HPLC method. The plasma concentrations were determined by
LC-MS/MS method, and the pharmacokinetic parameters of S-SEDDS in beagle dogs were also studied and compared with the tablets in
the market.Results:The results in vitro showed that the accumulated dissolution from S-SEDDS and Clarityne were more than 80%at
30 min. In vivo study, Cmax was 1.79ug·L-1 with S-SEDDS formulation, while Cmax was 0.67 ug·L-1 with Clarityne(P<0.05), the area
under the curve (AUC) was significantly higher than that in the commercial tablets, increased by 149%(P<0.05).Conclusion:S-SEDDS
can enhance the bioavailability of loratadine in vivo significantly. |
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