CAS Number: 76547-98-3 / 77726-95-5
Lisinopril | 76547-98-3 / 77726-95-5
Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor drug widely prescribed to treat hypertension and heart failure, but it has also emerged as an environmental contaminant detected in water sources, fish, and even groundwater, where it persists due to inefficient removal by conventional wastewater treatment. Thermodynamic studies in aqueous sodium chloride solutions reveal that lisinopril forms complexes with metal ions such as Cu²⁺, Zn²⁺, Ca²⁺, and Mg²⁺, with a greater sequestering ability for Cu²⁺ than for Zn²⁺; speciation modeling shows that at seawater pH (8.2), approximately 75% of lisinopril is complexed by Cu²⁺ and 92% by Zn²⁺. Additionally, a novel, environmentally friendly fluorescence quenching method using boron and nitrogen co-doped carbon quantum dots (B,N CQDs) has been developed for sensitive lisinopril determination, operating via static quenching with a binding energy of −33.58 kJ mol⁻¹ and achieving a detection limit of 6.21 ng mL⁻¹. Furthermore, a quality-by-design approach using β-cyclodextrin inclusion complexes prepared by the kneading method has been shown to significantly improve the solubility and oral bioavailability of lisinopril, with optimized formulations achieving 90.16% in vitro drug release at 24 hours and a two-fold increase in oral bioavailability compared to the pure drug.
Product Information
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References
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Quality by Design Enabled β-Cyclodextrin Complexes of Lisinopril by Kneading Method: Improved Solubility and Bioavailability
The FT-IR analysis study confirmed the selected drug, polymers, and other excipients showed no physical interactions. The prepared inclusion complexes' particle sizes and encapsulation efficiency were between 802 to 3259µm, 19.22 to 93.28%. The optimized formulation batch (F5) showed 90.16% in vitro drug release at 24h compared to the pure drug. From the in vivo study, the pharmacokinetic parameters for the optimized formulation (F5) were found to be Cmax of 94.336 ng/ml, Tmax of 12h, and AUC 94.336 ng.h/ml, Kel of 0.0395h-1 and t1/2 of 12h. After three months, stability studies for the optimized formulation batch indicate no change in drug entrapment efficiency and other parameters.
DOI: 10.2174/2666145416666230407100318 -
Oral combined hydrochlorothiazide and lisinopril vs nifedipine for postpartum hypertension: a comparative-effectiveness pilot randomized controlled trial
Of 111 eligible individuals, 70 (63%) agreed and were randomized (31 in the hydrochlorothiazide and lisinopril group and 36 in the nifedipine group; 3 withdrew consent after randomization), and the characteristics were similar at baseline between the groups. The primary outcome was unavailable for 9 (12.8%) participants. The primary outcome occurred in 27% of participants in the hydrochlorothiazide and lisinopril group and in 43% of the participants in the nifedipine group (posterior adjusted relative risk, 0.74; 95% credible interval, 0.40–1.31). Bayesian analysis indicated an 85% posterior probability of a reduction in the primary outcome with combined hydrochlorothiazide and lisinopril therapy relative to nifedipine treatment. No differences were noted in the secondary outcomes or adverse medication events.
DOI: 10.1016/j.ajog.2023.01.015