분무건조기를 이용한 아토르바스타틴 고체분산체의 용출율 개선 = Improved Dissolution of Solid Dispersed Atorvastatin Using Spray-Dryer

다국어 초록 (Multilingual Abstract)

Solid dispersions of poorly water-soluble drug, atorvastatin, were prepared with Eudragit L100 to improve the solubility by spray dryer. To investigate the correlation between physicochemical properties and dissolution rate of solid
dispersions, the samples were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and fourier transform infrared spectroscopy (FT-IR). SEM and DSC were found that atorvastatin is amorphous in the Eudragit L100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin and
Eudragit L100. The dissolution rate of solid dispersed atorvastatin was markedly increased compared to drug powder in stimulated intestinal juice (pH 6.8). Thus, the solid dispersed atorvastatin using the spray drying method with Eudragit L100 may be effective for the bioavailability.

참고문헌 (Reference)

1 강길선, "자가미세유화를 통한 아토르바스타틴 칼슘의 난용성 개선" 한국약제학회 37 (37): 339-347, 2007

2 김경환, "이우주의 약리학개론" 의학문화사 473-475, 1998

3 강길선, "아토르바스타틴 칼슘 고체분산체의 특성화 및 용출율 개선" 한국약제학회 38 (38): 111-117, 2008

4 강길선, "시부트라민 고체 분산체의 특성화 및 조절된 방출거동" 한��약제학회 38 (38): 119-126, 2008

5 박정수, "분무건조 방법으로 제조된 미립구에서 Sibutramine의 방출거동" 한국고분자학회 32 (32): 193-198, 2008

6 M. Asada, "Theophylline particle design using chitosan by the spray drying" 270 : 167-174, 2004

7 Röhm GmbH, "Specifications and test methods for EUDRAGITR L100 and EUDRAGITR S100" 2004

8 J.N. Gyabaah, "Solubility of lovastatin in a family of six alcohols: Ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, and 1-octanol" 359 (359): 111-117, 2008

9 M.S. Kim, "Preparation, characterization and in vivo evaluation of amorphous atorvastatin calcium nanoparticles using supercritical antisolvent(SAS) process" 69 (69): 454-465, 2008

10 T. Ozeki, "Preparation of two-drug composite microparticles to improve the dissolution of insoluble drug in water for use with a 4-fluid nozzle spray drier" 107 : 387-394, 2005

11 B.K. Kang, "Preparation of solid dosage form containing SMEDDS of simvastatin by microencapsulation" 33 (33): 121-127, 2003

12 H.R. Shen, "Preparation and evaluation of self-microemulsifying drug delivery systems(SMEDDS) contain- ing atorvastatin" 58 : 1183-1191, 2006

13 G. Khang, "Preparation and characterization of PLGA microspheres for the sustained release of AZT" 8 (8): 80-88, 2000

14 M.S. Kim, "Patent WO2003068191"

15 T. Mizoe, "One-step preparation of drug-containing microparticles to enhance the dissolution and absorption of poorly water-soluble drugs using a 4-fluid nozzle spray drier" 120 : 205-210, 2007

16 T.S. Chung, "Novel hollow fiber membranes with defined unit-step morphological change" 193 (193): 123-128, 2001

17 D.D. Cilla, "Multiple-dose pharmacokinetics, pharmacodynamic and safety of atorvastatin, an inhibitor of HMG-CoA reductase, in healthy subjects" 60 : 687-695, 1996

18 L.S. Porubcan, "Mechanism of adsorption of clindamycin and tetracycline by montmorillonite" 67 : 1081-, 1978

19 S.J. Lee, "Korea Patent, 10-2007-0094386"

20 Röhm Pharma, "Information sheet, “Eudragit L” (1998)"

21 K. Uekama, "Inclusion complexations of steroid hormones with cyclodextrins in water and in the solid-phase" 10 : 1-15, 1982

22 B.Y. Yoon, "Improvement of bioavailability for lovastatin using selfemulsifying drug delivery system" 32 (32): 267-274, 2002

23 D. Skorda, "Identification and quantitative determination of atorvastatin calcium polymorph in tablets using FT-Raman spectroscopy" 74 : 1066-1070, 2008

24 M. Otsuka, "Hygroscopic stability and dissolution properties of spray-dried solid dispersions of furosemide with Eudragit" 82 : 32-38, 1993

25 H.B. Lee, "Fentanyl-loaded PLGA microspheres for local anesthesia" 40 (40): 288-289, 1999

26 D.H. Choi, "Drug interaction between oral atorvastatin and verapamil in healthy subjects:Effects of atorvastatin on the pharmacokinetics of verapamil and norverapamil" 64 : 445-449, 2008

27 B.K. Kang, "Development of selfmicroemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs" 274 : 65-73, 2004

28 P.D. Martino, "Characterization and compaction behaviour of nimesulide crystal forms" 342 : 137-144, 2007