Article
  • Development of Metformin Hydrochloride-Linagliptin Controlled Release Tablet Using Hydrophilic Polymers for Type 2 Diabetes in Asians

  • Sunjae Park*, Pil Yun Kim*, Na Eun Kim*, Youngeun Song*, Ga Young Jeon*, Nomin-Erdene Tumursukh*, 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

  • 아시아인의 제2형 당뇨병 치료를 위한 친수성 고분자를 사용한 메트포르민 염산염-리나글립틴 방출제어형 정제 개발

  • 박선재* · 김필윤* · 김나은* · 송영은* · 전가영* · 투무르수흐너밍에르덴* · 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

Metformin hydrochloride, used for treatment of type 2 diabetes, is a drug belonging to the biopharmaceutical classification system III and has a high solubility in water. Therefore, hypoglycemia occurs in Asians who have lower weight and body fat than Westerners because of the rapid initial release. Accordingly, a hydrophilic polymer was used to reduce the risk of hypoglycemia due to the rapid increase in blood concentration of the drug, and a combination of metformin hydrochloride and linagliptin fixed -dose triple -layer tablet was prepared through a wet granulation process. The crystallinity and inclusion of drugs were evaluated through X-ray diffractometer (XRD), and chemical changes were confirmed through Fourier transform infrared spectroscopy (FTIR). Finally, tablets prepared by inducing a sustained release pattern and Trajenta duo tablets were analyzed by comparative dissolution test and confirmed to be available as type 2 diabetes treatments suitable for Asians.


제2형 당뇨병 치료제 메트포르민 염산염은 생물약제학적 분류체계 III에 속하는 약물로 물에 대한 용해도가 높다. 따라서 초기 방출이 급격하게 일어나기 때문에 서구인에 비해 낮은 체중과 체지방을 가진 아시아인들에게는 저혈당증이 발생한다. 이에 급격한 약물 혈중농도 증가에 의한 저혈당증 위험의 발생률을 낮출 수 있도록 친수성 고분자를 사용하였고, 습식과립공정을 통하여 메트포르민 염산염과 리나글립틴 고정 용량 조합 삼중층 정제를 제조하였다. X-ray diffractometer(XRD)를 통해 약물의 결정성 및 포접을 평가했고, Fourier transform infrared spectroscopy (FTIR)을 통해 물리·화학적 변화를 확인하였다. 최종적으로, 본 연구의 서방정제와 트라젠타듀오정과의 비교용출 시험을 수행하여, 아시아인들에 적합한 제2형 당뇨병 치료제로 개발 가능함을 확인하였다.


Keywords: metformin hydrochloride, linagliptin, wet granulation, poly(ethylene oxide), 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(2): 159-164

    Published online Mar 25, 2022

  • 10.7317/pk.2022.46.2.159
  • Received on Oct 13, 2021
  • Revised on Dec 7, 2021
  • Accepted on Dec 14, 2021

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