1-3--1---5--4- Composite formulation for oral administration comprising 1-3-cyano-1-isopropyl-indol-5-ylpyrazol-4-carboxyl acid

• Main Authors: LIM DO HYUNG, YOO SEOK CHEOL, JANG JOO MYUNG, SEO JIN A
• Format: Patent
• Language: English; Korean
• Published: 25.10.2022
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

The present invention relates to an oral formulation containing API selected from 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid or a pharmaceutically acceptable salt thereof, wherein the particle size D (0.9), which is the maximal particle size for 90% of the particles in cumulative particle size distribution, is 80 μm to 300 μm (both inclusive). Although including a high content of API, the oral formulation according to the present invention exhibits low friability and an increased dissolution rate by controlling the particle size of the API to a specific range. 본 발명은 입도 누적분포에서 최대 입도에 대해 90%에 해당하는 과립에 대한 입도(D(0.9))가 80 ㎛ 이상 300 ㎛ 이하인 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산 또는 이의 약학적으로 허용가능한 염에서 선택되는 API를 함유하는 경구용 제제에 관한 것이다. 본 발명에 따른 경구용 제제는 API의 입도를 특정 범위로 조절함으로써, 높은 함량의 API를 포함함에도 불구하고, 낮은 마손도 및 증가된 용출률을 가진다.