[Self-microemulsifying drug delivery system of patchoulic alcohol to improve oral bioavailability in rats].
OBJECTIVE
To improve the oral bioavailability of patchoulic alcohol in rats by using self-microemulsifying drug delivery systems (SMEDDS).


METHODS
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.


RESULTS
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).


CONCLUSIONS
SMEDDS can effectively improve the oral bioavailability of patchoulic alcohol in rats.
You
Xiuhua
X
Research and Development Center of Pharmaceutics, School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510006, China.
Wang
Rongchang
R
Tang
Wenxing
W
Li
Ying
Y
He
Zhijian
Z
Hu
Haiyan
H
Wu
Chuanbin
C
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D045703:Emulsifying Agents / Q000737:chemistry*; D000431:Ethanol / Q000737:chemistry; D005260:Female; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012646:Self Administration; D012717:Sesquiterpenes / Q000737:chemistry*; D012995:Solubility
D045703:Emulsifying Agents; D012717:Sesquiterpenes; D000431:Ethanol; C052983:patchouli alcohol