Self-microemulsifying drug delivery systems (SMEDDS) for improving in vitro dissolution and oral absorption of Pueraria lobata isoflavone.
The aim of our investigation was to develop and characterize self-microemulsifying drug delivery systems (SMEDDS) of Pueraria lobata isoflavone to improve its in vitro dissolution and oral absorption in beagle dogs. SMEDDS consisted of oil (ethyl oleate), a surfactant (Tween 80), and a cosurfactant (Transcutol P). In all the SMEDDS, the level of Pueraria lobata isoflavone was fixed at 20% w/w of the vehicle. The in vitro self-microemulsification properties and droplet size analysis of SMEDDS were studied following their addition to water under mild agitation. A pseudoternary phase diagram was constructed identifying the efficient self-microemulsification region. From these investigations, an optimized formulation was selected and its dissolution and bioavailability were compared with a tablet formulation in beagle dogs. The in vitro dissolution rate of puerarin from SMEDDS was more than threefold faster than that from Yufengningxin tablets (Pueraria lobata isoflavone tablets). A 2.5-fold increase in the relative bioavailability was observed for the SMEDDS compared with Yufengningxin tablets. The absolute bioavailability of the SMEDDS was 82.32 +/- 15.51%, which was significantly improved compared with that of Yufengningxin tablets. These results demonstrate the potential of SMEDDS as an efficient way of improving the oral absorption of Pueraria lobata isoflavone.
Cui
Shengmiao
S
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
Zhao
Chunshun
C
Chen
Dawei
D
He
Zhonggui
Z
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D004285:Dogs; D016503:Drug Delivery Systems / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D004655:Emulsions / Q000737:chemistry / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D007529:Isoflavones / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D010316:Particle Size; D029908:Pueraria / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods
D004365:Drugs, Chinese Herbal; D045703:Emulsifying Agents; D004655:Emulsions; D007529:Isoflavones; D013607:Tablets; C511199:yufengningxin; C033607:puerarin