Preparation, characterization and in vitro intestinal absorption of a dry emulsion formulation containing atorvastatin calcium

被引:28
作者
Yin, Yong-Mei [1 ,2 ,3 ]
Cui, Fu-De [3 ]
Kim, Jung Sun [4 ]
Choi, Min-Koo [1 ,2 ]
Choi, Byung Chul [5 ]
Chung, Suk-Jae [1 ,2 ]
Shim, Chang-Koo [1 ,2 ]
Kim, Dae-Duk [1 ,2 ]
机构
[1] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea
[2] Seoul Natl Univ, Pharmaceut Sci Res Inst, Seoul 151742, South Korea
[3] Shenyang Pharmaceut Univ, Coll Pharm, Shenyang, Peoples R China
[4] Dongseo Univ, Div Hlth Sci, Pusan, South Korea
[5] Chung Ang Univ, Coll Pharm, Seoul 156756, South Korea
关键词
Atorvastatin calcium; Dry emulsion; Spray drying; Dissolution; Absorption; SOLID-STATE EMULSIONS; DELIVERY SYSTEMS SMEDDS; FREEZE-DRIED TABLETS; DROPLET SIZE; DOSAGE FORM; BIOAVAILABILITY; CLASSIFICATION; DISEASE; OIL; CYCLOSPORINE;
D O I
10.1080/10717540802481380
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 mu g/cm(2) 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.
引用
收藏
页码:30 / 36
页数:7
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