Preparation, characterization and in vitro intestinal absorption of a dry emulsion formulation containing atorvastatin calcium.
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 microg/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.
Yin
Yong-Mei
YM
College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
Cui
Fu-De
FD
Kim
Jung Sun
JS
Choi
Min-Koo
MK
Choi
Byung Chul
BC
Chung
Suk-Jae
SJ
Shim
Chang-Koo
CK
Kim
Dae-Duk
DD
D000284:Administration, Oral; D000818:Animals; D000069059:Atorvastatin; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003912:Dextrins / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions; D005990:Glycerol / Q000031:analogs & derivatives / Q000737:chemistry; D006538:Heptanoic Acids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D008297:Male; D009829:Oleic Acids / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry; D011758:Pyrroles / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013997:Time Factors
D003912:Dextrins; D004337:Drug Carriers; D004655:Emulsions; D006538:Heptanoic Acids; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D009829:Oleic Acids; D011758:Pyrroles; D013501:Surface-Active Agents; D020442:Poloxamer; D000069059:Atorvastatin; D005990:Glycerol