Formulation, characterization and evaluation to establish the bioavailability of gastroretentive mucoadhesive dosage of atenolol in human subjects with possible in-vitro-in-vivo correlation

Q4 Pharmacology, Toxicology and Pharmaceutics
K. Kumar, Gurunath Surampalli, Y. Rao, M. Ajitha
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引用次数: 0

Abstract

Objective: This study was planned to formulate, characterize and evaluate to establish the bioavailability of gastroretentive mucoadhesive dosage of atenolol in human subjects with possible in-vitro-in-vivo correlation. Method: In this investigation gastroretentive mucoadhesive dosage of Atenolol was formulated using HPMCK4M, chitosan and Isabgul husk by wet granulation technique. The prepared tablets were subjected to physical evaluation, in-vitro drug release and in-vivo X-ray studies, followed by the pharmacokinetic study in human volunteers. Results: All the prepared tablets showed physicochemical properties within the limits and good in-vitro mucoadhesion. Formulation F2 was selected based on the in-vitro characteristics and in-vivo radiographic studies by replacing part of the drug by adding barium sulphate. From the radiographic studies it was found that the F2 could be successfully retained in stomach for more than 6 hours. Pharmacokinetic studies showed a significant improvement in AUC0-14; 6414.93 ± 58.221 ng.h/mL (p < 0.05) when compared to reference AUC0-14; 4752.18 ± 76.759 ng.h/mL in healthy human volunteers with good invitro-invivo correlation. Conclusion: Based on in-vitro characteristics and in-vivo radiographic studies, F2 was selected as optimized gastroretentive mucoadhesive dosage form with improved bioavailability for better patient compliance and disease management.
阿替洛尔胃滞留粘附剂剂量在人体内的生物利用度的配方、表征和评估
目的:本研究拟制定、表征和评价胃保留黏附剂阿替洛尔在人体中的生物利用度,并可能存在体内外相关性。方法:以HPMCK4M、壳聚糖和蚕豆壳为原料,采用湿法制备阿替洛尔胃保留黏附剂。对制备的片剂进行了物理评价、体外释药和体内x线研究,并在人体志愿者体内进行了药代动力学研究。结果:所制片剂理化性质均在限定范围内,体外黏附良好。配方F2是根据体外特性和体内放射学研究选择的,通过添加硫酸钡代替部分药物。放射学研究发现,F2可在胃中成功滞留6小时以上。药代动力学研究显示AUC0-14显著改善;6414.93±58.221 ng.h/mL (p < 0.05);4752.18±76.759 ng.h/mL,具有良好的体内外相关性。结论:基于体外特性和体内放射学研究,F2是最佳的胃保留黏附剂剂型,具有更好的生物利用度,可提高患者的依从性和疾病管理。
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来源期刊
Iranian Journal of Pharmaceutical Sciences
Iranian Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.50
自引率
0.00%
发文量
0
期刊介绍: Iranian Journal of Pharmaceutical Sciences (IJPS) is an open access, internationally peer-reviewed journal that seeks to publish research articles in different pharmaceutical sciences subdivisions: pharmacology and toxicology, nanotechnology, pharmaceutics, natural products, biotechnology, pharmaceutical chemistry, clinical pharmacy and other pharmacy related topics. Each issue of the journal contents 16 outstanding research articles in area of pharmaceutical sciences plus an editorial written by the IJPS editors on one of the most up to date advances topics in pharmacy. All articles published by IJPS would be permanently accessible online freely without any subscription charges. Authors of the published articles have granted the right to use and disseminate their article to third parties.
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