Intravenous itraconazole emulsions produced by SolEmuls technology

被引:62
作者
Akkar, A
Müller, RH
机构
[1] Free Univ Berlin, Dept Pharmaceut Technol Biotechnol & Qual Managem, D-12169 Berlin, Germany
[2] Pharmasol GmbH, Berlin, Germany
关键词
itraconazole; emulsions; high pressure homogenisation; poorly soluble drugs; particle size; SolEmuls;
D O I
10.1016/S0939-6411(03)00063-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Itraconazole is a drug which is poorly soluble in both the water and oil phases of emulsions. Incorporation in parenteral emulsions was performed applying the SolEmuls(R) Technology, i.e. localising the drug in the interfacial lecithin layer of the emulsions by homogenising a hybrid dispersion of oil droplets and drug nanocrystals in water. The maximum loading capacity of the emulsion system was found to be 10 mg/ml; at 20 mg/ml the loading capacity was exceeded leading to remaining drug nanocrystals in the emulsion. Incorporation of itraconazole into the lecithin layer led to an enhanced dispersion effect, i.e. with increasing drug concentration the droplet size of the emulsions decreased. Physical long-term stability of the optimum emulsion with 10 mg/ml could be shown over a period of 3 months at room temperature. (C) 2003 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:29 / 36
页数:8
相关论文
共 27 条
[1]  
AKKAR A, THESIS FREE U BERLIN
[2]  
AKKAR A, 2003, 8 UKICRS S BELF 10 J
[3]  
AKKAR A, 2002, ARCH PHARM PHARM S1, V335, P56
[4]  
[Anonymous], 1948, THEORY STABILITY LYO
[5]  
[Anonymous], [No title captured]
[6]  
BRUNO RP, 2001, DISPERSION TECHNIQUE, P77
[7]  
BUCHMANN S, 1994, P ANN C INT ASS PHAR
[8]  
DAVIS SS, 1988, Patent No. 0296845
[9]   STUDIES ON THE MECHANISM OF MEMBRANE-FUSION - ROLE OF HEADGROUP COMPOSITION IN CALCIUM-INDUCED AND MAGNESIUM-INDUCED FUSION OF MIXED PHOSPHOLIPID-VESICLES [J].
DUZGUNES, N ;
WILSCHUT, J ;
FRALEY, R ;
PAPAHADJOPOULOS, D .
BIOCHIMICA ET BIOPHYSICA ACTA, 1981, 642 (01) :182-195
[10]   The role of plasma proteins in brain targeting:: species dependent protein adsorption patterns on brain-specific lipid drug conjugate (LDC) nanoparticles [J].
Gessner, A ;
Olbrich, C ;
Schröder, W ;
Kayser, O ;
Müller, RH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 214 (1-2) :87-91