高生物利用度塞来昔布冻干口腔崩解片的制备与评价

IF 4.3 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Shuai Sun , Mengjun Wang , Jin Chen , Xiaoli Ju , Furong Zhang , Meilin He , Dongfang Cheng , Shumeng Kong
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引用次数: 0

摘要

本研究旨在开发具有高生物利用度、起效快的塞来昔布纳米冻干口腔崩解片。采用介质碾磨法结合冷冻干燥技术制备了塞来昔布纳米级冻干口腔崩解片。单因素试验设计和Box-Behnken统计试验设计优化了工艺和配方。优化后的配方中塞来昔布含量为49.5%,PVP K30含量为11.3%,SDS含量为2.6%,甘露醇含量为36.6%。片剂在5 s内崩解,分散后平均药物粒径为351nm。塞来昔布的溶解度在所有测试的pH值水平下显著增加。体外释放研究表明,超过90%的塞来昔布在3分钟内从片剂中释放出来。在大鼠和比格犬体内研究显示,与西乐葆®相比,塞来昔布的相对生物利用度分别为155%和292%,tmax分别降低了25.5%和33.5%。该研究成功开发了一种基于纳米技术的塞来昔布冻干口腔崩解片,提高了生物利用度,为低剂量非甾体抗炎药制剂提供了一条有希望的途径。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preparation and evaluation of celecoxib lyophilized orally disintegrating tablets with high bioavailability

Preparation and evaluation of celecoxib lyophilized orally disintegrating tablets with high bioavailability
This study aimed to develop industrially feasible nano-lyophilized orally disintegrating tablets of celecoxib with high bioavailability and rapid onset of action. Nano-lyophilized orally disintegrating tablets were prepared using a media milling method combined with freeze-drying technology, in which the particle size of celecoxib was at the nanoscale. Single-factor experimental design and Box–Behnken statistical experimental design optimized the process and formulation. The optimized formulation contained 49.5 % celecoxib, 11.3 % PVP K30, 2.6 % SDS and 36.6 % mannitol. The tablets disintegrated within 5 s, with an average drug particle size of 351 nm after dispersion. The solubility of celecoxib increased significantly across all tested pH levels. In vitro release studies demonstrated that over 90 % of celecoxib was released from the tablets within 3 min. In vivo studies in rats and beagle dogs showed relative bioavailabilities of 155 % and 292 %, respectively, compared to Celebrex®, and tmax was reduced by 25.5 % and 33.5 %. The study successfully developed a nanotechnology-based lyophilized orally disintegrating tablet of celecoxib with enhanced bioavailability, offering a promising approach for low-dose NSAID formulations.
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来源期刊
CiteScore
8.80
自引率
4.10%
发文量
211
审稿时长
36 days
期刊介绍: The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.
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