{"title":"Dissolution Profiles of Oral Disintegrating Tablet with Taste Masking Granule Polymer Coating in Biorelevant Bicarbonate Buffer.","authors":"Masaki Higashino, Kiyohiko Sugano","doi":"10.1248/cpb.c23-00783","DOIUrl":null,"url":null,"abstract":"<p><p>The current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra<sup>®</sup> as the reference formulation, and generic formulations A and B as the test formulations. Allegra<sup>®</sup>, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit<sup>®</sup> E, EUD-E), a basic polymer commonly used to mask the bitter taste of drugs. Both generic A and generic B have been known to be bioequivalent to Allegra<sup>®</sup>. The dissolution tests were conducted using a compendial paddle, with either bicarbonate (10 mM, pH 6.8) or phosphate buffer (25 mM, pH 6.8) as the dissolution media. A floating lid was employed to cover the surface of the bicarbonate buffer to prevent volatilization. Results indicated that in phosphate buffer, the dissolution profiles of Allegra and generic B significantly varied from that of generic A, whereas in the bicarbonate buffer, the dissolution profiles of Allegra, generic A, and generic B were comparable. These findings suggest that the use of bicarbonate buffer may offer a more precise prediction of human bioequivalence compared to phosphate buffer.</p>","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.5000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemical & pharmaceutical bulletin","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1248/cpb.c23-00783","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra® as the reference formulation, and generic formulations A and B as the test formulations. Allegra®, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit® E, EUD-E), a basic polymer commonly used to mask the bitter taste of drugs. Both generic A and generic B have been known to be bioequivalent to Allegra®. The dissolution tests were conducted using a compendial paddle, with either bicarbonate (10 mM, pH 6.8) or phosphate buffer (25 mM, pH 6.8) as the dissolution media. A floating lid was employed to cover the surface of the bicarbonate buffer to prevent volatilization. Results indicated that in phosphate buffer, the dissolution profiles of Allegra and generic B significantly varied from that of generic A, whereas in the bicarbonate buffer, the dissolution profiles of Allegra, generic A, and generic B were comparable. These findings suggest that the use of bicarbonate buffer may offer a more precise prediction of human bioequivalence compared to phosphate buffer.
本研究旨在探讨缓冲剂种类对含碱性聚合物的口腔崩解片(ODT)溶出行为的影响及其对生物等效性(BE)预测的影响。盐酸非索非那定口腔崩解片制剂作为模型制剂,Allegra®作为参比制剂,普通制剂A和B作为试验制剂。Allegra®、普通制剂 A 和普通制剂 B 都是含有甲基丙烯酸氨基烷基共聚物 E(Eudragit® E,EUD-E)的 ODT 制剂,EUD-E 是一种碱性聚合物,常用来掩盖药物的苦味。据了解,仿制药 A 和仿制药 B 与 Allegra® 具有生物等效性。溶解试验使用药典桨进行,溶解介质为碳酸氢盐(10 mM,pH 6.8)或磷酸盐缓冲液(25 mM,pH 6.8)。使用浮盖覆盖碳酸氢盐缓冲液表面以防止挥发。结果表明,在磷酸盐缓冲液中,阿莱格拉和非专利药 B 的溶出曲线与非专利药 A 的溶出曲线差异很大,而在碳酸氢盐缓冲液中,阿莱格拉、非专利药 A 和非专利药 B 的溶出曲线相当。这些发现表明,与磷酸盐缓冲液相比,使用碳酸氢盐缓冲液可以更精确地预测人体生物等效性。
期刊介绍:
The CPB covers various chemical topics in the pharmaceutical and health sciences fields dealing with biologically active compounds, natural products, and medicines, while BPB deals with a wide range of biological topics in the pharmaceutical and health sciences fields including scientific research from basic to clinical studies. For details of their respective scopes, please refer to the submission topic categories below.
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