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用于小鼠模型感染的阿莫西林和克拉霉素黏膜黏附递送系统:表征、药代动力学及疗效

Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy.

作者信息

Villegas Isabel, Rosillo María Ángeles, Alarcón-de-la-Lastra Catalina, Vázquez-Román Victoria, Llorente Maria, Sánchez Susana, Gil Ana Gloria, Alcalde Pilar, González Esther, Rosell Elisabet, Nieto Carles, Fernandez-Campos Francisco

机构信息

Department of Pharmacology, Faculty of Pharmacy, University of Seville, Profesor García González Street, 2, 41012 Seville, Spain.

Department of Normal and Pathological Cytology and Histology, Faculty of Medicine, University of Seville, Avda. Dr. Fedriani, s/n. 41009 Sevilla, Spain.

出版信息

Pharmaceutics. 2021 Jan 24;13(2):153. doi: 10.3390/pharmaceutics13020153.

Abstract

is the main pathogen responsible for gastric ulcers and a predisposing factor of stomach cancer. Although current treatment is usually successful, it requires high doses and frequent administration. An innovative mucoadhesive system (Mucolast) loaded with amoxicillin and clarithromycin is proposed to improve the efficacy of treatment against . The drug product was optimized based on its viscoelastic properties to obtain long-term stability of the vehicle. The drug release mechanisms were different for both antibiotics based on their solubilization status. A systemic and stomach pharmacokinetic profile was obtained after three different doses were administered to mice, obtaining similar systemic exposure levels but an increase in drug concentration in the stomach. The efficacy results in mice infected with also demonstrated the superiority of the antibiotics when administered in Mucolast, as shown by the bacterial count in stomach tissue and under histopathological and biochemical evaluation. The proposed treatment was efficacious and safe and is presented as a realistic alternative to current treatment options to improve patient compliance and to reduce bacterial resistance.

摘要

是导致胃溃疡的主要病原体和胃癌的诱发因素。尽管目前的治疗通常是成功的,但需要高剂量和频繁给药。提出了一种负载阿莫西林和克拉霉素的创新型粘膜粘附系统(Mucolast),以提高针对的治疗效果。该药物产品基于其粘弹性特性进行了优化,以获得载体的长期稳定性。两种抗生素的药物释放机制因其溶解状态而异。对小鼠给予三种不同剂量后获得了全身和胃部药代动力学特征,全身暴露水平相似,但胃部药物浓度增加。在感染的小鼠中进行的疗效结果也证明了在Mucolast中给药时抗生素的优越性,胃组织中的细菌计数以及组织病理学和生化评估结果均表明了这一点。所提出的治疗方法有效且安全,是当前治疗选择的一种切实可行的替代方案,可提高患者的依从性并降低细菌耐药性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5774/7911155/6ae7f0d0b210/pharmaceutics-13-00153-g001.jpg

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