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醋氯芬酸速崩片制剂:不同浓度的直压型微晶纤维素 PH102 对其压缩性、机械性能和药物释放特性的影响。

Aceclofenac fast dispersible tablet formulations: Effect of different concentration levels of Avicel PH102 on the compactional, mechanical and drug release characteristics.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.

出版信息

PLoS One. 2020 Feb 12;15(2):e0223201. doi: 10.1371/journal.pone.0223201. eCollection 2020.

DOI:10.1371/journal.pone.0223201
PMID:32050259
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7015698/
Abstract

The objective of this study was based on the formulation development of fast dispersible Aceclofenac tablets (100 mg) and to evaluate the influence of pharmaceutical mixtures of directly compressible Avicel PH102 with Mannitol and Ac-di-sol on the compressional, mechanical characteristics and drug release properties. Fast dispersible Aceclofenac formulations were developed by central composite design (CCD). Among them the best possible formulation was selected on the basis of micromeritic properties, appropriate tablet weight and disintegration time for further study. Tablets were directly compressed using manual hydraulic press with a compressional force ranging from 7.2 to 77.2 MN/m2. Pre and post compression studies were performed and the compressed formulations (FA-FF) were assessed for different quality tests. The Heckel and Kawakita equations were applied for determination of compressional behavior of formulations. The quality attributes suggested that formulation (FB) containing avicel PH 102 (20%), mannitol (25%) and ac-di-sol (3%) as best optimized formulation showing better mechanical strength i.e. hardness 35.40 ± 6.93N, tensile strength 0.963 MN/m2, and friability 0.68%. Furthermore, compressional analysis of FB showed lowest PY value 59.520 MN/m2 and Pk value 1.040 MN/m2 indicating plasticity of the material. Formulation FB disintegrated rapidly within 21 seconds and released 99.92% drug after 45 min in phosphate buffer pH 6.8. Results of drug release kinetics showed that all formulations followed Weibull and First-order models in three different dissolution media. Avicel PH102 based formulation mixture exhibit excellent compactional strength with rapid disintegration and quick drug release.

摘要

本研究的目的是基于快速分散的醋氯芬酸片剂(100mg)的配方开发,并评估直接可压缩的 Avicel PH102 与甘露醇和 Ac-di-sol 的药物混合物对压缩性、机械特性和药物释放性能的影响。快速分散的醋氯芬酸制剂是通过中心复合设计(CCD)开发的。其中,根据微粉学特性、适当的片剂重量和崩解时间,选择了最佳的配方进行进一步研究。采用手动液压机直接压缩,压缩力范围为 7.2 至 77.2 MN/m2。进行了预压缩和后压缩研究,并对压缩制剂(FA-FF)进行了不同质量测试的评估。应用 Heckel 和 Kawakita 方程来确定制剂的压缩行为。质量属性表明,含有 Avicel PH 102(20%)、甘露醇(25%)和 Ac-di-sol(3%)的配方(FB)是最佳优化配方,具有更好的机械强度,即硬度为 35.40±6.93N、拉伸强度为 0.963 MN/m2 和脆碎度为 0.68%。此外,FB 的压缩分析显示最低的 PY 值为 59.520 MN/m2 和 Pk 值为 1.040 MN/m2,表明材料具有塑性。配方 FB 在 21 秒内迅速崩解,在磷酸盐缓冲液 pH 6.8 中 45 分钟后释放 99.92%的药物。药物释放动力学的结果表明,所有制剂在三种不同的溶解介质中均遵循 Weibull 和一级模型。基于 Avicel PH102 的配方混合物具有良好的可压缩性,崩解迅速,药物释放迅速。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/40aebfc8c779/pone.0223201.g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/cfbdea00d52e/pone.0223201.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/a3bff3a703a9/pone.0223201.g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/40aebfc8c779/pone.0223201.g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/cfbdea00d52e/pone.0223201.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/a3bff3a703a9/pone.0223201.g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/baf4221bc415/pone.0223201.g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de5d/7015698/40aebfc8c779/pone.0223201.g004.jpg

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