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輔酶Q10(CoQ10)之靜脈注射調配物及其使用方法
专利权人:
发明人:
NARAIN, NIVEN RAJIN,纳蓝 尼芬 拉金,納藍 尼芬 拉金,MCCOOK, JOHN PATRICK,麦库 约翰 派屈克,麥庫 約翰 派屈克
申请号:
TW100108581
公开号:
TWI602562B
申请日:
2011.03.14
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
Disclosed herein are formulations suitable for parenteral administration of certain hydrophobic active agents such as Coenzyme Q10. Methods of preparing the same and methods of treatment of oncological disorders using the same are also provided herein. The formulations comprise an aqueous solution a hydrophobic active agent dispersed to form a colloidal nano-dispersion of particles and at least one of a dispersion stabilizing agent and an opsonization reducer wherein the colloidal nano-dispersion of the active agent is dispersed into nano-dispersion particles having a mean size of less than 200-nm. Methods of preparing the parenteral formulations comprise dispersing the hydrophobic active agent by high pressure homogenization by (1) adding hydrophobic active agent to a 65℃ bath of water and mixing to form a hydrophobic active agent/water mixture (2) adding a dispersion stabilizing agent to the hydrophobic active agent/water mixture and mix at 65℃ to form a hydrophobic active agent/water/stabilizer mixture (3) adding an opsonization reducer to form a hydrophobic active agent/water/stabilizer/reducer mixture (4) pre-heating a Microfluidizer to 65℃ and (5) processing by mixing the hydrophobic active agent/water/stabilizer/reducer mixture in the Microfluidizer at 65℃ such that a hydrophobic active agent colloidal nano-dispersion having a mean particle size less than 200-nm is formed. Provided herein are also methods of treating oncological disorders by administering formulations described herein to a subject such that treatment or prevention of the oncological disorder occurs.本文揭示適於非經腸投與諸如輔酶Q10等某些疏水活性劑之調配物。本文亦提供其製備方法及使用其治療腫瘤病症之方法。該等調配物包含水溶液;疏水活性劑,其經分散以形成粒子之膠狀奈米分散液;及分散穩定劑及調理作用降低劑中之至少一者,其中活性劑之膠狀奈米分散液分散成平均大小小於200 nm之奈米分散粒子。製備非經腸調配物之方法包含以以下方式藉由高壓均質化分散疏水活性劑:(1)向65℃水浴中添加疏水活性劑並混合形成疏水活性劑/水混合物;(2)向該疏水活性劑/水混合物中添加分散穩定劑並於65℃下混合形成疏水活性劑/水/穩定劑混合物;(3)添加調理作用降低劑以形成疏水活性劑/水/穩定劑/降低劑混合物;(4)將微射流均質機預加熱至65℃;及(5)藉由於65℃下在微射流均質機中混合疏水活性劑/水/穩定劑/降低劑混合物來進行處理,以便形成平均粒徑小於200 nm之疏水活性劑膠狀奈米分散液。本文亦提供藉由將本文所述調
来源网站:
中国工程科技知识中心
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