Article
  • Formulation Design of Sustained-release Dosage form of Ticagrelor by Solid Dispersion Using Eudragit RS/RL

  • Byungkwan Moon*, Younghun Lee*, Seung Jae Kim*, Suyoung Been*, Na Eun Kim*, Seong Won Lee*, Sunjae Park*, Jeong Eun Song*, and Gilson Khang*, **, ***,†

  • *Department of Bionanotechnology and Bio-Convergence Engineering, Jeonbuk National University, 567 Baekje-daero, Deokjin-gu, Jeonju-si, Jeollabuk-do 54896 Korea
    **Department of Polymer Nano Science & Technology, Jeonbuk National University, 567 Baekje-daero, Deokjin-gu, Jeonju-si, Jeollabuk-do 54896 Korea
    ***Polymer Materials Fusion Research Center, Jeonbuk National University, 567 Baekje-daero,
    Deokjin-gu, Jeonju-si, Jeollabuk-do 54896 Korea

  • Eudragit RS/RL을 이용한 고체분산에 의한 티카그렐러 서방형 제형 설계

  • 문병관* · 이영훈* · 김승재* · 빈수영* · 김나은* · 이성원* · 박선재* · 송정은* · 강길선*, **, ***,†

  • *전북대학교 바이오나노융합공학과, **전북대학교 고분자나노공학과, ***전북대학교 고분자융합소재연구소

  • Reproduction, stored in a retrieval system, or transmitted in any form of any part of this publication is permitted only by written permission from the Polymer Society of Korea.

Abstract

Ticagrelor is a drug that prevents stroke and heart attack in patients with acute coronary syndrome and belongs to the biopharmaceutical classification system IV with low solubility and permeability. Therefore, in order to increase the bioavailability, the drug solubilization process is essential. To this end, a solid dispersion was produced through a wet granulation process by a spray-drying method using hydrophilic and pH-independent polymers Eudragit RL PO and Eudragit RS PO. Crystallinity and saturation were confirmed through X-ray diffractometer and differential scanning calorimetry whether the drug was dispersed in a polymer matrix in an amorphous form, and a chemical change was confirmed through Fourier transform infrared spectroscopy. Finally, it was confirmed that the release control of the drug was well performed through the dissolution test, and it was possible to develop a formulation that reduced the number of doses and improved the patient's compliance with the dose.


티카그렐러는 급성관상동맥증후군 환자의 뇌졸중과 심장마비를 예방하는 약물로서 용해도와 생체막 투과성이 낮은 생물약제학적 분류체계 IV에 속하는 약물이다. 이에 생체이용률을 높이기 위해서는 약물가용화 과정이 필수적이다. 이를 위해 친수성이고 pH 비의존적 고분자 Eudragit RL PO, Eudragit RS PO을 사용해 분무건조법으로 습식과립공정을 통해 고체 분산체를 제조하였다. 약물이 무정형으로 고분자 매트릭스에 분산되었는지 X-ray diffractometer, differential scanning calorimetry를 통해 결정성 및 포접을 확인하였고, Fourier transform infrared spectroscopy을 통해 화학적 변화를 확인하였다. 최종적으로, 용출시험을 통해 약물의 방출제어가 잘 이루어졌는지 확인하여, 복용 회수를 줄이고 환자의 복약 순응도를 높인 제형으로 개발 가능함을 확인하였다.


Keywords: ticagrelor, solid dispersion, wet granulation, eudragit, sustained release.

  • Polymer(Korea) 폴리머
  • Frequency : Bimonthly(odd)
    ISSN 0379-153X(Print)
    ISSN 2234-8077(Online)
    Abbr. Polym. Korea
  • 2022 Impact Factor : 0.4
  • Indexed in SCIE

This Article

  • 2022; 46(6): 752-756

    Published online Nov 25, 2022

  • 10.7317/pk.2022.46.6.752
  • Received on May 30, 2022
  • Revised on Jul 18, 2022
  • Accepted on Sep 13, 2022

Correspondence to

  • Gilson Khang

  • *Department of Bionanotechnology and Bio-Convergence Engineering, Jeonbuk National University, 567 Baekje-daero, Deokjin-gu, Jeonju-si, Jeollabuk-do 54896 Korea
    **Department of Polymer Nano Science & Technology, Jeonbuk National University, 567 Baekje-daero, Deokjin-gu, Jeonju-si, Jeollabuk-do 54896 Korea
    ***Polymer Materials Fusion Research Center, Jeonbuk National University, 567 Baekje-daero,
    Deokjin-gu, Jeonju-si, Jeollabuk-do 54896 Korea

  • E-mail: gskhang@jbnu.ac.kr