KIM, MYUNG HWA,김명화,CHUN, KWANG WOO,천광우,YE, IN HAE,예인해,CHOI, JONG HEE,최종희
申请号：
KR1020120002014
公开号：
KR1020120140591A
申请日:
2012.01.06
申请国别(地区):
KR
年份:
2012
代理人:
摘要：
PURPOSE: A pharmaceutical composition with improved solubility of refractory tricyclic compound is provided to have a nano particle able to solubilize a highly concentrated and less soluble derivative of tricyclic without solubilizing agent, keep highly improved solubility for an injection after adding water and have high stability in long term preservation.CONSTITUTION: A pharmaceutical composition with improved solubility derivative of refractory tricyclic compound comprises phospholipid, cholesterol, the lipid mixture of ionic lipid and nano particles made of a refractory tricyclic compound expressed as structural formula 1. The phospholipid is hydrogenated soy phospatidylcholine(HSPC). The ionic lipid is dipalmitoyl phosphatidic acid(DPPA). In the lipid mixture, phospholipid to cholesterol to ionic lipid ratio part by weight is 0-100:0-20:0-10. In the lipid mixture phospholipid to cholesterol to ionic lipid ratio par by weight is 0-20:0-7:1-3. In the lipid mixture, phospholipid to cholesterol to ionic lipid ratio part by weight is 7:3:1. The lipid mixture to the derivative of tricyclic ratio part by weight is 1-20:1. The lipid mixture to the derivative of tricyclic ratio part by weight is 3:1. A pharmaceutical composition comprises no agent for solubilizing. Oral medication is manufactured, adding pharmaceutically acceptable additive to a pharmaceutical composition with improved solubility derivative of tricyclic.COPYRIGHT KIPO 2013본 발명은 인지질, 콜레스테롤, 이온성지질 및 트리사이클릭 유도체 화합물로 이루어지는 나노입자를 포함하는 트리사이클릭 유도체 화합물의 용해도가 향상된 약학적 조성물에 관한 것으로, 본 발명에 의하면 지질나노입자를 제조함으로써 난용성인 트리사이클릭 유도체 화합물을 인체에 유해한 용해보조제를 사용하지 않고도 고농도로 가용화시키는 것이 가능하고, 후에 주사제로 사용하기 위해서 물을 가하더라도 향상된 용해도를 유지하며, 장기간 보관시에도 안정성을 나타낸다. 따라서, 본 발명의 지질나노입자는 난용성 트리사이클릭 유도체 화합물을 유효성분으로 하는 약학적 제제의 제조에 유용하게 사용될 수 있다.
