Preparation and in Vivo Evaluation of a Dutasteride-Loaded Solid-Supersaturatable Self-Microemulsifying Drug Delivery System

International Journal of Molecular Sciences

Min-Soo Kim²  Eun-Sol Ha²  Gwang-Ho Choo²  In-Hwan Baek¹ 

[1] College of Pharmacy, Kyungsung University, Busan 608-736, Korea; E-Mail:;College of Pharmacy, Pusan National University, Busan 609-735, Korea; E-Mails:

关键词: self-emulsifying;    bioavailability;    dutasteride;    cellulose;    drug delivery;   

DOI  :  10.3390/ijms160510821

来源: mdpi

【 摘 要 】

The purpose of this study was to prepare a dutasteride-loaded solid-supersaturatable self-microemulsifying drug delivery system (SMEDDS) using hydrophilic additives with high oral bioavailability, and to determine if there was a correlation between the in vitro dissolution data and the in vivo pharmacokinetic parameters of this delivery system in rats. A dutasteride-loaded solid-supersaturatable SMEDDS was generated by adsorption of liquid SMEDDS onto Aerosil 200 colloidal silica using a spray drying process. The dissolution and oral absorption of dutasteride from solid SMEDDS significantly increased after the addition of hydroxypropylmethyl cellulose (HPMC) or Soluplus. Solid SMEDDS/Aerosil 200/Soluplus microparticles had higher oral bioavailability with 6.8- and 5.0-fold higher peak plasma concentration (C_max) and area under the concentration-time curve (AUC) values, respectively, than that of the equivalent physical mixture. A linear correlation between in vitro dissolution efficiency and in vivo pharmacokinetic parameters was demonstrated for both AUC and C_max values. Therefore, the preparation of a solid-supersaturatable SMEDDS with HPMC or Soluplus could be a promising formulation strategy to develop novel solid dosage forms of dutasteride.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.