화학공학소재연구정보센터
Polymer(Korea), Vol.46, No.6, 752-756, November, 2022
Eudragit RS/RL을 이용한 고체분산에 의한 티카그렐러 서방형 제형 설계
Formulation Design of Sustained-release Dosage form of Ticagrelor by Solid Dispersion Using Eudragit RS/RL
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초록
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 습식 과립공정을 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.
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.
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