[广藿香醇自微乳化给药系统改善大鼠口服生物利用度]
[Self-microemulsifying drug delivery system of patchoulic alcohol to improve oral bioavailability in rats].
作者信息
You Xiuhua, Wang Rongchang, Tang Wenxing, Li Ying, He Zhijian, Hu Haiyan, Wu Chuanbin
机构信息
Research and Development Center of Pharmaceutics, School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510006, China.
出版信息
Zhongguo Zhong Yao Za Zhi. 2010 Mar;35(6):694-8. doi: 10.4268/cjcmm20100607.
OBJECTIVE
To improve the oral bioavailability of patchoulic alcohol in rats by using self-microemulsifying drug delivery systems (SMEDDS).
METHOD
Patchoulic alcohol was separated and purified from patchoulic oil, and the SMEDDSs including patchoulic alcohol or patchoulic oil were optimized by pseudo-ternary phase diagrams via central composite design-response surface methodology. Pharmacokinetics of both SMEDDSs and patchoulic alcohol itself in rats were investigated.
RESULT
The patchoulic alcohol SMEDDS (Cremophor EL-Tween 80-PEG 400-isopropyl myristate-patchoulic alcohol, 2:2:0.8:1.95:0.65) was considered as the optimized formulation. The mean drop size of the system was 30. 1 nm after diluted 100 folds in water. The average self-microemulsifying time was 142 s. Patchoulic alcohol SMEDDS and patchoulic oil SMEDDS showed no signficant difference in Tmax compared with patchoulic alcohol with around 60 minutes, while the AUCs of both SMEDDSs (2001 745.6 +/- 329 663.6) and (1594 005.6 +/- 280 150.3) microg x min x L(-1) were significantly higher than that of patchoulic alcohol (1 163 153.3 +/- 232 324.3) microg x min x L(-1).
CONCLUSION
SMEDDS can effectively improve the oral bioavailability of patchoulic alcohol in rats.
目的
通过使用自微乳化药物传递系统（SMEDDS）提高广藿香醇在大鼠体内的口服生物利用度。
方法
从广藿香油中分离纯化出广藿香醇，采用中心复合设计-响应面法通过伪三元相图优化包含广藿香醇或广藿香油的SMEDDS。研究了两种SMEDDS以及广藿香醇本身在大鼠体内的药代动力学。
结果
广藿香醇SMEDDS（聚氧乙烯蓖麻油EL-吐温80-聚乙二醇400-肉豆蔻酸异丙酯-广藿香醇，2:2:0.8:1.95:0.65）被认为是优化后的制剂。该系统在水中稀释100倍后的平均液滴尺寸为30.1 nm。平均自微乳化时间为142 s。广藿香醇SMEDDS和广藿香油SMEDDS的达峰时间（Tmax）与广藿香醇相比无显著差异，约为60分钟，而两种SMEDDS的药时曲线下面积（AUC）（分别为2001 745.6±329 663.6和1594 005.6±280 150.3）μg·min·L⁻¹显著高于广藿香醇（1 163 153.3±232 324.3）μg·min·L⁻¹。
结论
SMEDDS可有效提高广藿香醇在大鼠体内的口服生物利用度。
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