高效液相色谱法测定乙醇对格列吡嗪控释片体外释放行为的影响

doi:10.19803/j.1672-8629.20230412

中国药物警戒 ›› 2024, Vol. 21 ›› Issue (6): 638-643.
DOI: 10.19803/j.1672-8629.20230412

高效液相色谱法测定乙醇对格列吡嗪控释片体外释放行为的影响

苏海, 昝孟晴, 牛剑钊, 马玲云^#, 刘倩^*

中国食品药品检定研究院化学药品检定所,国家药品监督管理局化学药品质量研究与评价重点实验室,北京 100050

收稿日期:2023-06-28 出版日期:2024-06-15 发布日期:2024-06-18
通讯作者: ^*刘倩,女,研究员,药品检验研究。E-mail: liuqian@nifdc.org.cn; ^#为共同通信作者。
作者简介:苏海,男,在读硕士,药品检验研究。
基金资助:
国家重点研发计划（2020YFE0201700）; 国家药品监督管理局重点实验室学科建设课题（2023HYZX13、2024HYZX04）

Effect of ethanol on release behavior of glipizide controlled release tablets by HPLC

SU Hai, ZAN Mengqing, NIU Jianzhao, MA Lingyun^#, LIU Qian^*

National Medical Products Administration Key Laboratory for Quality Research and Evaluation of Chemical Drugs, Institute for Chemical Drug Control, National Institutes for Food and Drug Control, Beijing 100050, China

Received:2023-06-28 Online:2024-06-15 Published:2024-06-18

摘要/Abstract

摘要： 目的采用国家药品监督管理局发布的指导原则对不同企业格列吡嗪控释片仿制制剂及其参比制剂的乙醇剂量倾泻情况进行对比研究。方法采用高效液相色谱法测定格列吡嗪控释片仿制制剂及其参比制剂在不同乙醇浓度中的体外释放行为,绘制溶出曲线,采用溶出相对变化率来评价乙醇对药物释放的增速作用,并通过计算相似因子（f₂）评价不同制剂体外释放的相似性。结果随着乙醇浓度的升高,在5%、20%乙醇溶液中仿制制剂与参比制剂的体外释放量几乎无变化,在40%乙醇中释放量均出现了一定的升高,但其相似因子f₂均未低于50,与无乙醇的盐酸介质释放特性相似,同时仿制制剂体外释放行为与参比制剂相似。结论仿制制剂符合一致性评价质量标准。0%~40%浓度的乙醇对格列吡嗪控释片的体外释放行为无显著性影响,推测制剂中的亲水性辅料及独特的双层渗透泵结构是消除乙醇剂量倾泻影响的关键因素,对格列吡嗪与酒精饮料同服的合理用药与安全风险预测具有一定的参考价值。

关键词: 剂量倾泻, 格列吡嗪, 控释片, 乙醇, 高效液相色谱法, 溶出曲线, 安全性, 参比制剂, 仿制制剂

Abstract: Objective To comparatively study the alcohol-induced dose dumping in glipizide controlled-release tablets from different manufacturers and their reference formulation according to the National Medical Products Administration (NMPA) guidelines. Methods The in vitro release of glipizide from generic and reference formulations at different concentrations of ethanol was examined using high-performance liquid chromatography (HPLC). Dissolution profiles were meticulously generated, and the relative change in the rate of dissolution due to ethanol was used as an index to assess its effect on drug release kinetics. Additionally, the similarity in in vitro release patterns across various formulations was quantitatively evaluated by calculating the similarity factor (f₂). Results It was observed that the in vitro release profiles of generic formulations and the reference formulation underwent minimal changes at ethanol concentrations of 5% and 20%, with a noticeable increase at 40% ethanol, much like the release observed in a hydrochloric acid medium without ethanol (f₂>50), indicating that the in vitro release behavior of the generic formulations closely paralleled that of the reference formulation. Conclusion The generic formulations meet the quality standards for consistency evaluation. Ethanol concentrations ranging from 0% to 40% do not significantly affect the in vitro release behavior of glipizide controlled-release tablets. The presence of hydrophilic excipients and the unique push-pull osmotic pump structure within the formulation may play critical roles in mitigating the risk of alcohol-induced dose dumping. These findings can help predict appropriate dosing and assess the safety risk associated with consuming glipizide alongside alcoholic beverages.

Key words: dose dumping, glipizide, controlled-release tablets, ethanol, high-performance liquid chromatography, dissolution profile, safety, reference formulation, generic formulation

中图分类号:

R917

苏海, 昝孟晴, 牛剑钊, 马玲云, 刘倩. 高效液相色谱法测定乙醇对格列吡嗪控释片体外释放行为的影响[J]. 中国药物警戒, 2024, 21(6): 638-643.

SU Hai, ZAN Mengqing, NIU Jianzhao, MA Lingyun, LIU Qian. Effect of ethanol on release behavior of glipizide controlled release tablets by HPLC[J]. Chinese Journal of Pharmacovigilance, 2024, 21(6): 638-643.

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高效液相色谱法测定乙醇对格列吡嗪控释片体外释放行为的影响

Effect of ethanol on release behavior of glipizide controlled release tablets by HPLC

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