聚乙二醇基固体分散体增强甲磺酸依普沙坦溶出度和生物利用度

Ismaiel A Tekko
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引用次数: 3

摘要

心血管疾病是世界上大多数死亡的原因,每年有惊人的1700万人死亡[1]。高血压是这些终身心血管疾病之一。高血压有一个无声的进展模式,导致只有四分之一的高血压患者寻求医疗护理[1]。高血压可以通过使用一种或多种药物的治疗策略来控制,如受体阻滞剂、血管紧张素转换酶抑制剂或血管紧张素II受体拮抗剂[2]。甲磺酸依普沙坦(ESM)是一种有效的抗高血压药物,作为口服片剂(Teventen®)销售。它通过拮抗血管紧张素II受体起作用,导致外周血管变宽和血压降低[3]。该药可减少交感神经去甲肾上腺素的产生,从而降低血压[4]。该药不仅耐受性良好,而且在脑血管事件的二级预防中也显示出有效的益处。ESM发生严重不良事件的可能性很低,与任何临床显著的药物相互作用无关。所有这些都表明ESM是一种很有前景的单用或联合降压药物[5]。ESM作为单药使用时,推荐的每日起始和维持剂量为735.8 mg,相当于600 mg依泊沙坦,可作为Teveten®600 ISSN: 2641-2020 DOI: 10.33552/APPR.2019.02.000537
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Polyethylene Glycol-Based Solid Dispersions to Enhance Eprosartan Mesylate Dissolution and Bioavailability
Cardiovascular diseases are the cause of most mortalities worldwide with a staggering 17 million deaths per year [1]. One of these lifelong cardiovascular diseases is hypertension. Hypertension has a silent mode of progression which results in only one out of four hypertensive people to seek medical care [1]. Hypertension can be controlled by different therapeutic strategies using one or combination of drugs that acts like beta blocker, angiotensin-converting enzyme inhibitors or Angiotensin II receptors antagonists [2]. Eprosartan mesylate (ESM) is a potent antihypertension drug marketed as oral tablets (Teventen®). It acts by antagonising the Angiotensin II receptors, resulting in peripheral blood vessels wideness and blood pressure reduction [3]. The drug decreases sympathetic norepinephrine production which also results in blood pressure reduction as well [4]. The drug is not only well-tolerated but it also presents effective benefit in the secondary prevention of cerebrovascular events. ESM has a low potential for serious adverse events and has not been associated with any clinically significant drug interactions. All of these demonstrate ESM as a promising agent for solo or combination antihypertensive strategies [5]. The recommended daily starting and maintenance dose of ESM when used as monotherapy is 735.8 mg, equivalent to 600 mg Eprosartan, available as the commercial Teveten® 600 ISSN: 2641-2020 DOI: 10.33552/APPR.2019.02.000537
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