Polyethylene Glycol-Based Solid Dispersions to Enhance Eprosartan Mesylate Dissolution and Bioavailability

Abstract

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