Merging konjac glucomannan with other copolymeric hydrogels as a cutting-edge liquid raft system for dual delivery of etoricoxib and famotidine.

IF 6.5 2区 医学 Q1 PHARMACOLOGY & PHARMACY Drug Delivery Pub Date : 2023-12-01 DOI:10.1080/10717544.2023.2189630
Nabil A Shoman, Marwa Saady, Mahmoud Teaima, Rehab Abdelmonem, Mohamed A El-Nabarawi, Sammar Fathy Elhabal
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Abstract

This study aimed to formulate and evaluate a floating raft system for the co-delivery of etoricoxib (ETO) and famotidine (FAM) using a combination of glucomannan with natural/semi-synthetic polysaccharides. Formulation variables affect gelation lag time (GLT), floating lag time (FLT), and release percentage of drugs after 1-8 h, Stability, and viscosity parameters were evaluated. In vivo X-ray studies, followed by the pharmacokinetic study, were performed on human volunteers. Formulations exhibited pseudoplastic behavior for ease of swallowing. The optimum raft system (ORS) comprised 1% Na alginate, 0.1% Low Methoxyl (LM) pectin, 0.8% Konjac glucomannan (KGL), 1% Precirol, and 1% CaCO3. ORS exhibited rapid GLT and FLT (around 42 and 8 sec respectively) in 0.1 N HCl as well as controlled release of ETO (15% in 1 h and 82% in 8 h) and FAM (29% in 1 h and 85% in 8 h). Formulation stability with the absence of any drug-excipient interactions was observed. The X-ray imaging showed a promising buoyancy ability for approximately 8 h. Compared with marketed products, ORS showed superior relative bioavailability for both drugs. These findings revealed the successful preparation of a promising raft system with improved dual drug delivery.

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将魔芋葡甘露聚糖与其他共聚水凝胶合并,作为一种尖端的液体筏系统,用于双重递送依托昔布和法莫替丁。
本研究旨在使用葡甘聚糖与天然/半合成多糖的组合,制备并评估用于联合递送依托里昔布(ETO)和法莫替丁(FAM)的浮筏系统。配方变量影响1-8后药物的凝胶滞后时间(GLT)、漂浮滞后时间(FLT)和释放百分比 h、 对稳定性和粘度参数进行了评估。对人体志愿者进行体内X射线研究,然后进行药代动力学研究。配方表现出假塑性行为,便于吞咽。最佳筏板体系(ORS)包括1%藻酸钠、0.1%低甲氧基(LM)果胶、0.8%魔芋葡甘聚糖(KGL)、1%Precisrol和1%CaCO3。口服补液盐表现出快速GLT和FLT(约42和8 秒),单位为0.1 N HCl以及ETO的控制释放(1 h和82% h) 和FAM(29% h和85% h) 。在没有任何药物-赋形剂相互作用的情况下观察到制剂的稳定性。X射线成像显示,大约8 h.与市场上的产品相比,口服补液盐对这两种药物都显示出优越的相对生物利用度。这些发现揭示了一种具有改进的双重药物递送的有前景的raft系统的成功制备。
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来源期刊
Drug Delivery
Drug Delivery 医学-药学
CiteScore
11.80
自引率
5.00%
发文量
250
审稿时长
3.3 months
期刊介绍: Drug Delivery is an open access journal serving the academic and industrial communities with peer reviewed coverage of basic research, development, and application principles of drug delivery and targeting at molecular, cellular, and higher levels. Topics covered include all delivery systems including oral, pulmonary, nasal, parenteral and transdermal, and modes of entry such as controlled release systems; microcapsules, liposomes, vesicles, and macromolecular conjugates; antibody targeting; protein/peptide delivery; DNA, oligonucleotide and siRNA delivery. Papers on drug dosage forms and their optimization will not be considered unless they directly relate to the original drug delivery issues. Published articles present original research and critical reviews.
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