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Preparation,characterization and in vitro intestinal absorption of a dry emulsion formulation containing atorvastatin calcium
Authors:Yong-Mei Yin  Fu-De Cui  Jung Sun Kim  Min-Koo Choi  Byung Chul Choi  Suk-Jae Chung
Affiliation:1. College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China;2. College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul, South Korea;3. Division of Health Science, Dongseo University, Busan, South Korea;4. College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul, South Korea
Abstract:A redispersible dry emulsion (DE) formulation of atorvastatin calcium (AC) was developed to enhance the in vitro dissolution of AC, thereby increasing its gastrointestinal absorption. The spray-drying technology was used where Plurol Oleique CC 497 was chosen as the oil phase. Effects of carriers, surfactants, and homogenizers on the characteristics of DE containing AC were systematically investigated. The final formulation consisted of dextrin and Poloxamer 188 as carrier and surfactant, respectively, and was homogenized by a high pressure homogenizer before spray drying. The in vitro release of AC from the optimized DE was significantly higher than that of pure AC powder (76% vs. 30% at 24 hr). The in vitro intestinal absorption of AC from the DE formulation was 0.77 μg/cm2 at 2 hr, which was a 2.33-fold increase compared to the pure unformulated AC powder. These results suggest that the oral dry emulsion formulation could improve the intestinal absorption of AC.
Keywords:Atorvastatin calcium  Dry emulsion  Spray drying  Dissolution    Absorption
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