Shuai Sun , Mengjun Wang , Jin Chen , Xiaoli Ju , Furong Zhang , Meilin He , Dongfang Cheng , Shumeng Kong
{"title":"高生物利用度塞来昔布冻干口腔崩解片的制备与评价","authors":"Shuai Sun , Mengjun Wang , Jin Chen , Xiaoli Ju , Furong Zhang , Meilin He , Dongfang Cheng , Shumeng Kong","doi":"10.1016/j.ejpb.2025.114756","DOIUrl":null,"url":null,"abstract":"<div><div>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.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"213 ","pages":"Article 114756"},"PeriodicalIF":4.3000,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Preparation and evaluation of celecoxib lyophilized orally disintegrating tablets with high bioavailability\",\"authors\":\"Shuai Sun , Mengjun Wang , Jin Chen , Xiaoli Ju , Furong Zhang , Meilin He , Dongfang Cheng , Shumeng Kong\",\"doi\":\"10.1016/j.ejpb.2025.114756\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>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.</div></div>\",\"PeriodicalId\":12024,\"journal\":{\"name\":\"European Journal of Pharmaceutics and Biopharmaceutics\",\"volume\":\"213 \",\"pages\":\"Article 114756\"},\"PeriodicalIF\":4.3000,\"publicationDate\":\"2025-05-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Pharmaceutics and Biopharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S093964112500133X\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmaceutics and Biopharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S093964112500133X","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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.
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.