A sensitive and efficient LC–MS/MS method for the bioanalysis of fosinopril diacid from human plasma and its application for a bioequivalence study in humans

Abstract

Fosinopril diacid is an angiotensin converting enzyme inhibitor with efficient antihypertensive action. It is an active metabolic product formed in the body from hydrolysis of its prodrug Fosinopril. A sensitive, rapid method with high recovery for Fosinopril diacid from human plasma was developed. Solid‐phase extraction technique employing Waters Oasis SPE cartridges gave clean samples with very high recovery of 97%. The analyte along with its internal standard (Benazepril hydrochloride) were chromatographed on an XTerra RP8 column (4.6 × 50 mm, 5 μm) using methanol–ammonium acetate buffer (10 mm; 90:10, v/v) as the mobile phase. A triple quadrupole mass spectrometer equipped with electrospray ionization source operated in the negative ion mode was used for detection. Multiple reaction monitoring scan mode was used for monitoring the transitions from m/z 434.00 → 237.15 for Fosinopril diacid and m/z 423.10 → 174.00 for Benazepril hydrochloride. Beer–Lambert’s law was obeyed in the range of 0.50–1,500.00 ng/ml (r = 0.9993). The stability of the drugs in human plasma and in stock solution was proved by performing stability tests as per US Food and Drug Administration guidelines. The method was successfully applied for a bioequivalence study of Fosinopril diacid in 36 healthy, adult, male volunteers under fasting conditions.

Identification of novel α-glucosidase and ACE inhibitory peptides from Douchi using peptidomics approach and molecular docking

“…The ACE promotes the conversion of type I angiotensin to type II, thereby inhibiting angiotensin activity while simultaneously leading to increase in blood pressure and risk of cardiovascular disease ( Ramírez-Sánchez, 2021 ). Although some ACE inhibitors such as fosinopril ( Bhende, Varanasi, & Abbulu, 2020 ) have rapid and strong efficacy, damage to renal function often occurs when these drugs are used. Peptides isolated from natural foods have demonstrated ACE inhibitory activity and fewer side effects, therefore constituting a research hot area ( Zhang, He, Rui, & Simpson, 2021 ).…”