Exploration of enalapril-lacidipine co-amorphous system with superior dissolution, in vivo absorption and physical stability via incorporated into mesoporous silica

IF 4.3 3区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutical Sciences Pub Date : 2025-02-05 DOI:10.1016/j.ejps.2025.107033

Yuhan Guo , Hanyu Wang , Qiang Zhu , Ying Mao , Xiangce Wen , Xin Zhang , Shirui Mao , Huiya Yuan , Jian Guan

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引用次数: 0

Abstract

In the present study, enalapril (ENP) was taking as a potential co-former to fabricate co-amorphous system with lacidipine (LCDP). The ENP/LCDP co-amorphous system was firstly prepared with or without mesoporous SiO₂ and characterized by DSC, XRD and SEM technologies. The potential molecular interactions were evaluated by FTIR spectrums. Furthermore, the dissolution and pharmacokinetics behavior of various formulations were also carried out. It was demonstrated that the completely co-amorphization was obtained at ENP/LCDP 2:1 molar ratio by the intermolecular interactions between ENP and LCDP. The ENP/LCDP co-amorphous system significantly improve the dissolution rate of LCDP and ENP respectively. Compared to the naked ENP/LCDP co-amorphous system, remarkable enhancement of dissolution rate and bioavailability of model drugs was observed by incorporated the co-amorphous system into mesoporous SiO₂, and a superior physical stability was also observed after accelerated study. Raman mapping revealed that the less microstructure phase separation could be the main reason for the better stability in presence of mesoporous SiO₂. In conclusion, ENP could be successfully used as a potential co-former to fabricate co-amorphous system with poorly water-soluble drugs and collaborates the co-amorphous with mesoporous SiO₂ become a promising strategy to achieve stable amorphous formulation for further enhancement of dissolution rate and bioavailability.

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来源期刊

European Journal of Pharmaceutical Sciences 医学-药学

CiteScore

9.60

自引率

2.20%

发文量

248

审稿时长

50 days

期刊介绍： The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.