Human bioequivalence evaluation of two losartan potassium tablets under fasting conditions

Abstract

The bioequivalence of two different tablet formulations containing losartan potassium 100 mg was determined in healthy volunteers after a single oral dose in a randomized crossover study. Test and reference products were administered to 60 volunteers with 240 ml water after overnight fasting. Plasma concentrations of losartan and its active carboxylic acid metabolite were monitored over a period of 36 h after drug administration by validated LC/MS/MS analytical method. The pharmacokinetic parameters Cmax, AUC0-t, AUC0-∞, AUC0-t/AUC0-∞, tmax, Kel and t½ were determined from plasma concentration time profile of both formulations for losartan and its active metabolite losartan carboxylic acid and were found to be in good agreement. The carboxylic acid metabolite was considered for profiling purpose only. The analysis of variance did not show any significant difference between the two formulations and 90% confidence intervals for the ratio of Cmax (84.89-104.09%), AUC0-t (95.84-102.84%) and AUC0-∞ (96.43-103.25%) values for losartan between the test and reference products were within the 80-125% interval, satisfying the bioequivalence criteria of the US FDA guidelines. These results indicate that the test and the reference products of losartan potassium are bioequivalent and, thus, may be prescribed interchangeably.

Human extinction learning is accelerated by an angiotensin antagonist via ventromedial prefrontal cortex and its connections with basolateral amygdala

“…The experiment consisted of three sequential stages: (1) routinely prescribed for the management of hypertension 48 and penetrates the bloodbrain barrier 49 . In line with the pharmacodynamic profile of LT 50 and previous studies examining the cognitive enhancing properties of LT in healthy subjects 46 the experimental paradigm (extinction) started 90 minutes after administration.…”

Normalizing granuloma vasculature and matrix improves drug delivery and reduces bacterial burden in tuberculosis-infected rabbits

“…Low-dose (50 mg tablet, ~12.5 mg/kg) or high-dose (100 mg tablet, ~25 mg/kg) losartan treatment was administered via daily pilling (Organon, Jersey City, NJ) for up to 4 wk based on previous studies showing these doses reduced tissue-injury fibrosis in mice and rabbits ( 47 , 48 ). The C max of the 100 mg tablet was 0.6 ± 0.09 µg/mL (mean ± SD), which was not significantly different than what has been observed in humans at the same dose ( 49 ); the 50 mg/kg dose in rabbits was more variable (0.4 ± 0.24 µg/mL). Losartan did not have an antibacterial effect on Mycobacterium tuberculosis ( Mtb ) in the concentration range as determined by MIC assay ( 50 ).…”

Telmisartan and losartan: The marked differences between their chemical and pharmacological properties may explain the difference in therapeutic efficacy in hospitalized patients with COVID‐19

“…Plasma C max (ng/mL) 1520 799 -Plasma C max values are presented after administration of telmisartan 160 mg/day orally 15 or losartan 100 mg orally single dose. 16 The accumulation observed with telmisartan, based on its t Telmisartan is an AT1 receptor blocker with an affinity (potency) greater than that observed for both losartan and its active metabolite EXP3174. 13 (Continues) of the main chemical and pharmacological properties of these two drugs (Table 1) allows us to predict that administered in equivalent antihypertensive doses, telmisartan, penetrating the lung interstitium, will reach effective pulmonary tissue concentrations that support the effectiveness obtained with telmisartan 4 and may explain the lack of effectiveness with losartan 5 in hospitalized patients with COVID-19.…”