차의과학대학교 산학협력단;CHA UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
发明人:
AN, Ji Hun,안지훈,JUNG, Ki Won,정기원,PARK, Min Ho,박민호,LIM, Chang Jin,임창진
申请号：
KRKR2019/002079
公开号：
WO2020/013415A1
申请日:
2019.02.20
申请国别(地区):
KR
年份:
2020
代理人:
摘要：
In order to overcome the extreme insolubility (water solubility: 0.12㎍/L) and the oral absorptivity less than 1% of ursolic acid, which are very severe problems that make ursolic acid difficult to develop into a drug although the natural active substance ursolic acid is highly valuable as a drug, the present inventors provide a novel ursolic acid/citric acid cocrystal or composite agent having an optimal ratio to increase in water solubility and gastrointestinal pH solubility by 10000 fold, and in elution rate. The novel ursolic acid/citric acid cocrystal or composite agent is very useful as an optimal drug raw material capable of maximizing the utility of ursolic acid as a drug.Afin de surmonter l'insolubilité extrême (solubilité dans l'eau : 0,12 ㎍/L) et l'absorptivité orale inférieure à 1 % d'acide ursolique, qui sont des problèmes très sévères qui rendent l'acide ursolique difficile à transformer en médicament bien que l'acide ursolique de substance active naturelle soit très utile en tant que médicament, les présents inventeurs proposent un nouveau co-cristal d'acide ursolique/acide citrique ou un agent composite ayant un rapport optimal pour augmenter la solubilité dans l'eau et la solubilité dans le pH gastro-intestinal de 10000 fois, et dans le taux d'élution. Le nouveau co-cristal d'acide ursolique/acide citrique ou l'agent composite est très utile en tant que matière première de médicament optimale capable de maximiser l'utilité de l'acide ursolique en tant que médicament.본 발명자들은 약물로서 활용가치가 뛰어난 천연 활성물질인 우르솔릭산(ursolic acid)의 약물로서의 개발을 어렵게 만드는 매우 심각한 문제점인 극난용성(수용해도: 0.12㎍/L) 및 경구 흡수도 1% 미만을 극복하고자 수용해도 및 위장관 pH 용해도가 10000배 증가 되고, 용출속도가 증가 된 최적의 비율의 신규한 우르솔릭산/시트릭산 공결정 또는 복합제를 제공한다. 이 신규한 우르솔릭산/시트릭산 공결정 또는 복합제는 우르솔릭산의 약물로서 활용을 극대화 할 수 있는 최적의 원료의약물질로서 매우 유용하다.
