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http://dx.doi.org/10.4333/KPS.2002.32.4.267

Improvement of Bioavailability for Lovastatin using Self-microemulsifying Drug Delivery System  

Yoon, Bok-Young (Department of Advanced Organic Materials Engineering, Chonbuk National University)
Kang, Bok-Ki (Department of Advanced Organic Materials Engineering, Chonbuk National University)
Jeung, Sang-Young (Biomaterials Laboratory, Korea Research Institute of Chemical Technology)
Lee, Young-Won (College of Veterinary Medicine, Chungnam National University)
Lee, Si-Beum (College of Pharmacy, Chungnam National University)
Hwang, Sung-Joo (College of Pharmacy, Chungnam National University)
Yuk, Soon-Hong (Department of Macromolecular Science, Hannam University)
Khang, Gil-Son (Department of Advanced Organic Materials Engineering, Chonbuk National University)
Lee, Hai-Bang (Biomaterials Laboratory, Korea Research Institute of Chemical Technology)
Cho, Sun-Hang (Biomaterials Laboratory, Korea Research Institute of Chemical Technology)
Publication Information
Journal of Pharmaceutical Investigation / v.32, no.4, 2002 , pp. 267-275 More about this Journal
Abstract
A self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and ultimately bioavailability of a poorly water soluble drug, lovastatin. SMEDDS was thε mixtures of oils, surfactants, and cosurfactants, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastro-intestinal (GI) tract. Various types of self-emulsifying formulations were prepared using four types of oil (Capryol 90, Lauroglycol 90, Labrafil M 1944 CS and Labrafil M 2125), two surfactants (Cremophor EL and Tween 80), and three cosurfactants (Carbitol, PEG 400 and propylene glycol). Thε efficiency of emulsification was studied using a laser diffraction size analyzer to determine particle size distributions of the resultant emulsions. Optimized formulations selected for bioavailability assessment were Carpryol 90 (40%), Cremophor EL (30%) and Carbitol (30%). SMEDDS containing lovastatin (20 mg and 5 mg) were compared to a conventional lovastatin tablet $(Mevacor^{\circledR},\;20\;mg/tab)$ by the oral administration as prefilled hard gelatin capsules to fasted beagle dogs for in vivo study. The arεa under the serum concentration-time curve from time zero to the last measured time in serum, $AUC_{0{\rightarrow}24h}$, was significantly greater in SMEDDS, suggesting that bioavailability increase 130% and 192% by the SMEDDS, respectively. The self-emulsifying formulations of lovastatin afforded the improvement in absolute oral bioavailability relative to previous data of lovastatin tablet formulation. These data indicate the utility of dispersed self-emulsifying formulations for the oral delivery of lovastatin and potentially other poorly absorbed drugs.
Keywords
Self-microemulsifying drug delivery system; Lovastatin; Bioavailability;
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