Short communication: in vivo evaluation of microemulsion system for oral and parenteral delivery of rutaecarpine to rats.
Rutaecarpine-loaded microemulsion composed of 10.8% polyethylene glycol 400, 7.2% Tween 80, 20% caster oil, and 62% water were previously reported to be physically and chemically stable for at least 6 months. For the development of a Rutaecarpine-loaded microemulsion, here we studied the pharmacokinetic profiles of rutaecarpine after oral and intravenous administration of rutaecarpine-loaded microemulsion compared to suspension. The AUC of rutaecarpine from microemulsion after oral and intravenous administration increased about three-fold compared with that from suspension. Furthermore, the rutaecarpine-loaded microemulsion gave significantly higher AUC and Cmax than did suspension, suggesting that the oral bioavailability of rutaecarpine in this microemulsion system could be enhanced due to the enhanced solubility of rutaecarpine by microemulsion. Thus, our results indicated that the microemulsion system composed of castor oil, polyethylene glycol 400, Tween 80, and water could be a more effective oral and parenteral dosage form for rutaecarpine.
Yong
Chul-Soon
CS
College of Pharmacy, Yeungnam University, Dae-Dong, Gyongsan, South Korea.
Park
Byung-Joo
BJ
Kim
Dong-Hyun
DH
Yoo
Bong-Kyu
BK
Woo
Jong Soo
JS
Bhamdari
Krisna
K
Jahng
Yurngdong
Y
Choi
Han-Gon
HG
Lee
Mann Hyung
MH
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002368:Castor Oil / Q000737:chemistry; D004355:Drug Stability; D004356:Drug Storage; D004655:Emulsions; D005079:Excipients / Q000737:chemistry*; D026121:Indole Alkaloids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D008297:Male; D011092:Polyethylene Glycols / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D011799:Quinazolines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013535:Suspensions; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014867:Water; D052999:Quinazolinones
D002368:Castor Oil; D004655:Emulsions; D005079:Excipients; D026121:Indole Alkaloids; D011092:Polyethylene Glycols; D011136:Polysorbates; D011799:Quinazolines; D013535:Suspensions; D014665:Vasodilator Agents; D014867:Water; C028632:rutecarpine; D052999:Quinazolinones