A water-soluble multi-use eyedrops composition for the treatment of dry eye syndrome containing rebamipide and a method for solubilization and stabilization thereof
HWANG SUNG WOO,황성우,YOON SI YEOL,윤시열,CHO KWAN HYUNG,조관형,JI YOUNG HOON,지용훈
申请号：
KR1020180094992
公开号：
KR1020200019451A
申请日:
2018.08.14
申请国别(地区):
KR
年份:
2020
代理人:
摘要：
The present invention relates to a water-soluble multi-use eye drop composition for treating dry eye syndrome, containing rebamipide, and a method of solubilizing and stabilizing the same. More specifically, the present invention relates to an eye drop composition for treating dry eye syndrome, which remains in an aqueous solution state by using a buffer that does not contain components with anti-inflammatory effects, such as aminocaproic acid, etc., and has excellent preservative effect, and to a preparation method of the same. The eye drop composition for treating dry eye syndrome of the present invention contains an alkali for solubilizing rebamipide, contains a stabilizer for maintaining a stable supersaturated state, preservatives, and a chelating agent for enhancing the effect of the preservatives, and contains a specific kind of buffer for maintaining a physiologically compatible pH of 7 to 8, and an osmotic regulator. The preparation method comprises the steps of: dissolving preservatives in water, and adding and dissolving therein rebamipide or a pharmaceutically acceptable salt thereof, a stabilizer, and an alkali, to produce a water-soluble eye drop solution of pH 10 to 11； adding and dissolving in the eye drop solution, a buffer and at least one osmotic regulator selected from non-ionic osmotic regulators； adding and dissolving therein a chelating agent； adjusting the same to the pH of 7 to 8 by boric acid； filtering the same by a syringe filter； and sterilizing the same. The eye drop solution thus prepared is in an aqueous solution state, is stable when frozen, refrigerated, or at room temperature, and is stable even when stored frozen or at room temperature.본 발명은 레바미피드를 함유하는 안구 건조증 치료용 수용성 다회용 점안제 조성물 및 이의 가용화 및 안정화 방법에 관한 것으로, 아미노카프론산 등과 같이 항염증 효과 같은 효능을 포함하지 않는 완충제를 사용하여 수용액 상태를 유지하며 방부효과가 뛰어난 조성물이며, 안구건조증 치료용 점안제 조성물 및 그 제조방법에 관한 것이다.본 발명의 안구건조증 치료용 점안제 조성물은 레바미피드를 가용화하기 위한 염기를 포함하며, 과포화 안정화 상태를 유지하기 위한 안정화제, 방부제, 방부제의 효과를 높여주는 킬레이트제를 포함하며, 생체 적합한
