氯雷他定固体自乳化制剂的体外溶出及体内药动学研究 |
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引用本文: | 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].现代生物医学进展,2015,15(14):2606-2609. |
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作者姓名: | 谭永刚 李海燕 杨茜 高立军 全东琴 |
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作者单位: | 军事医学科学院毒物药物研究所 |
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基金项目: | 国家自然科学基金项目(81102390) |
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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(P0.05),Cmax=1.79μg·L-1,而市售片剂Cmax=0.67μg·L-1;AUC(0~t)提高了149%(P0.05)。结论:固体自乳化制剂可以显著提高氯雷他定的体内吸收。
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关 键 词: | 固体自乳化制剂 氯雷他定 生物利用度 溶出度 |
The Solid Self-emulsified Drug Delivery System(S-SEDDS) of Loratadine:
Dissolution in Vitro and Pharmacokinetic Studies in Vivo |
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Abstract: | 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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Keywords: | S-SEDDS Loratadine Bioavailability Dissolution |
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