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    • 8. 发明公开
    • METHODS OF MAKING LIPOSOMES CONTAINING HYDRO-MONOBENZOPORPHYRIN PHOTOSENSITIZERS
    • 制备含有氢醌单卟啉光敏剂的脂质体的方法
    • EP0843547A1
    • 1998-05-27
    • EP96925614.0
    • 1996-07-29
    • QLT Phototherapeutics, Inc.
    • RON, Liu
    • A61K9A61K31A61K41
    • A61K9/127A61K9/1277A61K31/409A61K41/0071
    • Methods for making a pharmaceutical composition containing liposomes, which liposomes comprise a therapeutically acceptable amount of a hydro-monobenzoporphyrin photosensitizer and a mixture of phospholipids comprising egg phosphatidyl glycerol ('EPG') and dimyristoyl phosphatidyl choline ('DMPC'). The method comprises the steps of: a) combining the photosensitizer and the phospholipids in a molar ratio of about 1:7.0 or more phospholipid in the presence of an organic solvent; b) removing the organic solvent to form a lipid film; c) hydrating the lipid film with an aqueous solution at a temperature below about 300 °C, to form coarse liposomes containing a photosensitizer-phospholipid complex; and d) homogenizing or reducing the particle size of the coarse liposomes to a particle size range of about 150 to 300 nm at a temperature below about 300 °C. The invention also contemplates the liposomal pharmaceutical compositions themselves.
    • 制备含有脂质体的药物组合物的方法,所述脂质体包含治疗可接受量的氢化单苯并卟啉光敏剂和包含卵磷脂酰甘油('EPG')和二肉豆蔻酰磷脂酰胆碱('DMPC')的磷脂混合物。 该方法包括以下步骤:a)在有机溶剂存在下,以约1:7.0或更高的磷脂摩尔比使光敏剂和磷脂结合; b)去除有机溶剂以形成脂质膜; c)在低于约300℃的温度下用水溶液水合脂质膜以形成含有光敏剂 - 磷脂复合物的粗脂质体; 和d)在低于约300℃的温度下将粗脂质体的粒径均化或减小至约150-300nm的粒度范围。 本发明还考虑了脂质体药物组合物本身。