• 제목/요약/키워드: ticagrelor

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다공성의 캐리어를 이용한 티카그렐러 함유 고형의 자가 나노유화 약물전달시스템 개발 (Development of Solid Self-nanoemulsifying Drug Delivery Systems of Ticagrelor Using Porous Carriers)

  • 최형주;김경수
    • 생명과학회지
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    • 제31권5호
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    • pp.502-510
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    • 2021
  • 자가 나노유화 약물전달시스템(SNEDDS)은 오일, 계면활성제, 공계면활성제의 균질한 혼합물로서 가벼운 교반에 의해도 에멀전 형성이 가능하고 분산 시 200 nm 이하 범위의 입자 크기를 갖는 나노 에멀전을 형성하는 약물 수송체를 말한다. SNEDDS는 난용성이며 생체이용률이 낮은 소수성약물의 흡수율을 높일 수 있는 뛰어난 가용화 방법으로 알려져 있다. 본 연구에서는 난용성인 티카그렐러에 대한 용해도가 높은 유상으로 MCT oil과, 계면활성제로 Tween 80, 공계면활성제로 Labrafil M1944CS를 사용하여 SNEDDS를 개발하고, 분무건조기술을 이용하여 다양한 다공성의 캐리어에 흡착시켜 고형의 SNEDDS를 제조하였다. 제조된 고형의 SNEDDS에 대하여 물리화학적 특성 및 분말특성을 평가한 후 용출시험을 진행하였다. 본 연구를 통해 얻어진 다공성의 캐리어에 흡착시켜 만들어진 다양한 고형 SNEDDS에서 티카그렐러의 결정형은 무정형으로 변환된 것을 확인할 수 있었다. 또한 제조된 고형의 SNEDDS 조성물들은 모두 원료에 비하여 우수한 용출양상을 나타내는 것을 확인할 수 있었다. 특히 이산화규소를 통해 얻어진 고형의 SNEDDS 조성물의 입자크기와 다분산지수가 제일 작았으며 흐름성과 압축성도 제일 우수하였다. 따라서 이산화규소를 통해 얻어진 고형의 SNEDDS 조성물은 난용성인 티카그렐러의 경구 고형제제화 연구에 적합한 약물 전달 시스템인 것을 확인할 수 있었다.

Ticagrelor Monotherapy After 3-Month Dual Antiplatelet Therapy in Acute Coronary Syndrome by High Bleeding Risk: The Subanalysis From the TICO Trial

  • Yong-Joon Lee;Yongsung Suh;Jung-Sun Kim;Yun-Hyeong Cho;Kyeong Ho Yun;Yong Hoon Kim;Jae Young Cho;Ae-Young Her;Sungsoo Cho;Dong Woon Jeon;Sang-Yong Yoo;Deok-Kyu Cho;Bum-Kee Hong;Hyuckmoon Kwon;Sung-Jin Hong;Chul-Min Ahn;Dong-Ho Shin;Chung-Mo Nam;Byeong-Keuk Kim;Young-Guk Ko;Donghoon Choi;Myeong-Ki Hong;Yangsoo Jang;TICO investigators
    • Korean Circulation Journal
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    • 제52권4호
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    • pp.324-337
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    • 2022
  • Background and Objectives: Identifying patients with high bleeding risk (HBR) is important when making decisions for antiplatelet therapy strategy. This study evaluated the impact of ticagrelor monotherapy after 3-month dual antiplatelet therapy (DAPT) according to HBR in acute coronary syndrome (ACS) patients treated with drug eluting stents (DESs). Methods: In this post-hoc analysis of the TICO trial, HBR was defined by 2 approaches: meeting Academic Research Consortium for HBR (ARC-HBR) criteria or Predicting Bleeding Complications in Patients Undergoing Stent Implantation and Subsequent DAPT (PRECISE-DAPT) score ≥25. The primary outcome was a 3-12 months net adverse clinical event (composite of major bleeding and adverse cardiac and cerebrovascular events). Results: Of the 2,980 patients without adverse events during the first 3 months after DES implantation, 453 (15.2%) were HBR by ARC-HBR criteria and 504 (16.9%) were HBR by PRECISE-DAPT score. The primary outcome rate was higher in HBR versus non-HBR patients (by ARC-HBR criteria: hazard ratio [HR], 2.87; 95% confidence interval [CI], 1.76-4.69; p<0.001; by PRECISE-DAPT score: HR, 3.09; 95% CI, 1.92-4.98; p<0.001). Ticagrelor monotherapy after 3-month DAPT was associated with lower primary outcome rate than ticagrelor-based 12-month DAPT regardless of HBR by ARC-HBR criteria, with similar magnitudes of therapy effect for HBR and non-HBR patients (p-interaction=0.400). Results were consistent by PRECISE-DAPT score (p-interaction=0.178). Conclusions: In ACS patients treated with DESs, ticagrelor monotherapy after 3-month DAPT was associated with lower rate of adverse clinical outcomes regardless of HBR, with similar magnitudes of therapy effect between HBR and non-HBR.

A Study on the prediction dyspnea-induced attributes of linear regression-based Article

  • Lee, Kwang-Keun;Jeon, Gyu-Hyeon
    • 한국인공지능학회지
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    • 제6권2호
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    • pp.17-22
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    • 2018
  • According to the World Health Organization, the top 10 causes of death worldwide include heart disease. Heart diseases include coronary disease, which induces acute myocardial infarction. Ticagrelor drugs are being used to treat acute alliances, but it has become difficult to breathe due to the drugs. In a related study, Tobias predicted that uric acid causes acute respiratory distress independently of other factors, including BNP. And in the Ahmad study, serum uric acid numbers were related to the left ventricle depending on the level of uric acid. Experimental data are data used after 155 patients who received coronary intervention took ticagrelor. The research methods were leveraged by gradient decent algorithm and linear regression. In order to avoid overfitting in the experiment, training data and test data were separated into 70 and 30 percent respectively. The experimental results lacked the predictability of other attributes except DT in the correlation coefficient and crystal coefficient. However, all attributes related to dyspnea other than DT are determined to be related to causing relaxation of the heart in the left ventricle. Therefore, the attribute causing dyspnea is determined to be an attribute causing relaxation of the heart of the DT and left ventricle.

급성관상동맥 증후군 치료를 위한 국내·외 항혈소판제 약물요법 가이드라인 비교 연구 (A Comparative Study the USA, Europe and Korea Guidelines of Antiplatelet Therapy for Patients with Acute Coronary Syndrome)

  • 정은주;이채원;백인환
    • 한국임상약학회지
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    • 제25권3호
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    • pp.200-208
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    • 2015
  • Objective: Patients with acute coronary syndrome (ACS) are typically managed with dual antiplatelet therapy of acetylsalicylic acid (aspirin) and $P2Y_{12}$ receptor inhibitor. In this study, we discussed current and previous antiplatelet therapy guidelines and compared with guidelines of the USA (ACC/AHA), Europe (ESC) and Korea (KSC). Method: This study investigated from ACC/AHA Joint Guidelines (the USA), ESC Clinical Practice Guidelines (Europe) and Korea Society of Interventional Cardiology (Korea) web site, respectively. Results: It is significant that difference between the current and the previous guidelines was integration of terminology from clopidogrel to $P2Y_{12}$ receptor inhibitors since prasugrel and ticagrelor, new antiplatelet drugs, has been added. The other difference was all three guidelines has differences in dose of aspirin. The most notable difference was class of recommendation(COR) in $P2Y_{12}$ receptor inhibitors. ACC/AHA and Korean guidelines recommend clopidogrel, prasugrel, and ticagrelor with COR IB; whereas, ESC recommend prasugrel and ticagrelor with IB which is higher than clopidogrel with IC. Conclusion: This research addresses important movement to revise the Korean existing guideline recommendations. New Korean antiplatelet therapy guideline should be avoiding obvious differences in ACC/AHA and ESC guidelines and harmonizing international guidelines.

Pharmacological Approaches to Limit Ischemic and Reperfusion Injuries of the Heart: Analysis of Experimental and Clinical Data on P2Y12 Receptor Antagonists

  • Leonid N. Maslov;Sergey V. Popov;Alexandr V. Mukhomedzyanov;Ivan A. Derkachev;Vyacheslav V. Ryabov;Alla A. Boshchenko;N. Rajendra Prasad;Galina Z. Sufianova;Maria S. Khlestkina;Ilgiz Gareev
    • Korean Circulation Journal
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    • 제52권10호
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    • pp.737-754
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    • 2022
  • Ischemic and reperfusion injuries of the heart underlie the pathogenesis of acute myocardial infarction (AMI) and sudden cardiac death. The mortality rate is still high and is 5-7% in patients with ST-segment elevation myocardial infarction. The review is devoted to pharmacological approaches to limitation of ischemic and reperfusion injuries of the heart. The article analyzes experimental evidence and the clinical data on the effects of P2Y12 receptor antagonists on the heart's tolerance to ischemia/reperfusion in animals with coronary artery occlusion and reperfusion and also in patients with AMI. Chronic administration of ticagrelor prevented adverse remodeling of the heart. There is evidence that sphingosine-1-phosphate is the molecule that mediates the infarct-reducing effect of P2Y12 receptor antagonists. It was discussed a role of adenosine in the cardioprotective effect of ticagrelor.