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KMID : 0369820110410020103
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Jorunal of Korean Pharmaceutical Sciences
2011 Volume.41 No. 2 p.103 ~ p.109
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Development of Self-microemulsifying Drug Delivery System for Enhancing the Bioavailability of Atorvastatin
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Jin Shun-Ji
Cho Won-Kyung
Park Hee-Jun
Cha Kwang-Ho
Park Jun-sung
Koo Ja-Seong
Wang Hun-Sik
Kim Jeong-Soo
Kim Min-Soo
Hwang Sung-Joo
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Abstract
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The objective of the study was to prepare self-microeulsifying drug delivery system (SMEDDS) incorporating atorvastatin calcium and evaluate its properties and oral bioavailability. Solubility of atorvastatin in various vehicles was determined. Pseudo-ternary phase diagrams were constructed to identify the good self-emulsification region. The droplet size distributions of the resultant emulsions were determined by dynamic light scattering measurement. The mean droplet size of chosen formulation (20% ethyl oleate, 40% tween-80, 40% Carbitol®) was 23.4±1.3 nm. The SMEDDS incorporating atorvastatin calcium appeared to be associated with better performance in dissolution and pharmacokinetic studies, compared with raw atorvastatin calcium. In dissolution test, the release percentage of atorvastatin from SMEDDS mixture
could rapidly reach more than 95% within 3 min. Oral AUC0→8hrvalues in SD rats was 1994±335 ng·hr/mL, which significantly increased (P<0.05) compared with raw atorvastatin calcium. The SMEDDS formulation was relatively stable when stored at 4o C during 3 months. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin, by the oral route.
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KEYWORD
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Atorvastatin calcium, SMEDDS, Phase diagram, Bioavailability, Stability
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