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1010 INTRAVENOUS FORMULATIONS OF COENZYME Q10 CoQ10 AND METHODS OF USE THEREOF
专利权人:
베르그 엘엘씨
发明人:
나라인 니벤 라진,맥쿡 존 패트릭
申请号:
KR1020187028687
公开号:
KR1020086580000B1
申请日:
2011.03.11
申请国别(地区):
KR
年份:
2019
代理人:
摘要:
Described herein are formulations suitable for parenteral administration of certain hydrophobic active agents, such as coenzyme Q10. Also provided herein are methods of making the same and methods of treating tumorous diseases using the same. The formulation is an aqueous solution; Hydrophobic actives that are dispersed to form colloidal nano-dispersions of the particles; And a dispersion stabilizer and an opsonization reducer, wherein the colloidal nano-dispersion of the active agent is dispersed into nano-dispersion particles having an average size of less than 200-nm. Methods for preparing parenteral formulations include (1) forming a hydrophobic active agent / water mixture by adding hydrophobic active agent to a water bath at 65 ° C. and mixing; (2) adding a dispersion stabilizer to the hydrophobic active agent / water mixture and mixing at 65 ° C. to form a hydrophobic active agent / water / stabilizer mixture; (3) adding an opsonization reducer to form a hydrophobic active agent / water / stabilizer / opsonization reducer mixture; (4) pre-heating the microfluidizer to 65 ° C; And (5) processing the hydrophobic active agent / water / stabilizer / opsonization reducer mixture in a microfluidizer at 65 ° C. to form a hydrophobic active agent colloidal nano-dispersion having an average particle size of less than 200-nm. Dispersing the hydrophobic active agent by high pressure homogenization with. Also provided herein are methods of treating a neoplastic disease by administering to a subject a formulation described herein to thereby treat or prevent the neoplastic disease.본원에는 코엔자임 Q10과 같은 특정의 소수성 활성제의 비경구 투여에 적합한 제형이 기재되어 있다. 이를 제조하는 방법 및 이를 사용하여 종양성 질환을 치료하는 방법이 또한 본원에 제공된다. 당해 제형은 수용액; 분산되어 입자의 콜로이드성 나노-분산물을 형성하는 소수성 활성제; 및 분산 안정화제 및 옵소닌화 감소제 중 적어도 하나를 포함하며, 여기서 활성제의 콜로이드성 나노-분산물이, 평균 크기가 200-nm 미만인 나노-분산 입자내로 분산된다. 비경구 제형을 제조하는 방법은 (1) 소수성 활성제를 65℃의 수욕에 가하여 혼합함으로써 소수성 활성제/물 혼합물을 형성하는 단계; (2) 분산 안정화제를 소수성 활성제/물 혼합물에 첨가하여 65℃에서 혼합함으로써 소수성 활성제/물/안정화제 혼합물을 형성하는
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