[Assessment of Pueraria lobata isoflavone with self-microemulsifying drug delivery systems in vitro and in vivo].
OBJECTIVE
To evaluate the self-microemulsifying ability and dissolution behavior of pueraria lobata isoflavone in vitro and the pharmacokinetic behavior in rats.


METHODS
The self-microemulsifying rate was evaluated by the self-microemulsifying time and the self-microemulsifying efficiency was evaluated by the particle size of resultant microemulsions. The plasma concentrations were evaluated by HPLC and dissolution and pharmacokinetic behavior of self-microemulsifying drug delivery systems were evaluated by comparison with commercial tablets.


RESULTS
The system was self-microemulsified in 2 min and the particle size was less than 50 nm. The dis- solution of SMESC in distilled water was more than 90% at 10 min, while those of the commercial tablet were less than 50% at 120 min. 82% increase in the relative bioavailability was observed for the self microemulsifying drug delivery systems compared with Yufengningxin tablets. Tmax was smaller in the self-microemulsifying drug delivery systems compared with Yufengningxin tablets.


CONCLUSIONS
The self-microemulsifying drug delivery systems can increase drug dissolution in vitro and absorption in vivo significantly.
Cui
Sheng-Miao
SM
Department of Traditional Chinese Materia Medica, Guangdong Pharmaceutical University, Guangzhou 510006, China.
Zhao
Chun-Shun
CS
He
Zhong-Gui
ZG
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D016503:Drug Delivery Systems; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D045703:Emulsifying Agents / Q000737:chemistry; D004655:Emulsions; D007529:Isoflavones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D029908:Pueraria / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013997:Time Factors
D004365:Drugs, Chinese Herbal; D045703:Emulsifying Agents; D004655:Emulsions; D007529:Isoflavones; D011136:Polysorbates