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Antiarrhythmic Drugs: Class II Agents as β-Adrenergic Blockers01:24

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Adrenergic stimulation generally impacts cardiac rate and rhythm. Specifically, stimulation of the β-adrenoceptors triggers an increase in intracellular calcium ion influx and pacemaker currents, which may cause arrhythmias. Catecholamines like adrenaline also demonstrate β2-adrenoceptor-mediated hypokalemia, impacting cardiac action potential and disrupting the normal cardiac rhythm. Class II antiarrhythmic drugs are β-adrenoceptor antagonists or β-blockers, which...
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相关实验视频

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High-Throughput Cardiotoxicity Screening Using Mature Human Induced Pluripotent Stem Cell-Derived Cardiomyocyte Monolayers
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尖端装载的循环德克斯特林-卡维迪醇复合物微阵列补丁.

Qonita Kurnia Anjani1, Akmal Hidayat Bin Sabri2, Khuriah Abdul Hamid3

  • 1School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK; Fakultas Farmasi, Universitas Megarezky, Jl. Antang Raya No. 43, Makassar 90234, Indonesia.

Carbohydrate polymers
|September 2, 2023
PubMed
概括
此摘要是机器生成的。

这项研究开发了溶解微针贴片 (MAP) 用于通过皮肤输送心力衰竭药物卡维迪醇. 这些MAP提高了药物的生物可用性,并为口服提供了有前途的替代品.

关键词:
卡尔维迪醇是一种循环德克斯特林 (Cyclodextrin) 是一种循环德克斯特林.心脏衰竭是因为心脏衰竭.微阵列贴片的贴片三级包容复合体的第三级包容复合体.

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科学领域:

  • 制药科学 制药科学
  • 生物材料工程 生物材料工程

背景情况:

  • 卡维迪醇是心力衰竭的β抑制剂,由于代谢快速,其口服生物利用性较差.
  • 目前的口服输送方法面临着有效性和患者遵守的挑战.

研究的目的:

  • 开发和评估新型溶解微针贴片 (MAPs),以提高卡维迪醇的通过皮肤输送.
  • 改善卡维迪洛的生物可用性,并为慢性心力衰竭管理提供持续的药物释放.

主要方法:

  • 使用卡维迪醇与基基-基 (HPγCD) 和聚乙烯 (PVP) 的三元循环烯复合体制造MAP.
  • 使用DSC,XRD,NMR和SEM进行卡维迪洛-环极烯复合物的表征.
  • 评估MAPs在老鼠的皮肤透,溶解,生物相容性和体内药理学性能.

主要成果:

  • 三级复合物的形成降低了卡维迪醇的结晶性,提高了其适用于MAP的适度.
  • MAPs成功地穿透了ex vivo猪皮肤,针头在2小时内溶解,用于通过皮肤输送.
  • 与口服相比,对大鼠的体内研究显示,与口服相比,卡维迪醇AUC和持续的血水平显著更高,毒性最小.

结论:

  • 含有卡维迪醇的溶解MAP提供了一种可行的策略,可以改善通过皮肤递送药物.
  • 这种新的方法有可能通过提高药物的疗效和患者体验来彻底改变慢性心力衰竭的治疗.