{"title":"比较磷酸盐缓冲溶液和碳酸氢盐缓冲溶液作为预测非布索坦制剂生物等效性的溶出试验介质","authors":"Masaki Higashino, Kiyohiko Sugano","doi":"10.1248/cpb.c24-00526","DOIUrl":null,"url":null,"abstract":"<p><p>The purpose of the present study was to compare phosphate buffer (PPB) and bicarbonate buffer (BCB) solutions as dissolution test media for predicting the bioequivalence (BE) of an immediate-release (IR) formulation. Febuxostat was used as a model of free acid drugs. One reference formulation (RF) and three test formulations (TF) were employed in this study. The clinical BE studies involved 18 to 24 healthy adult volunteers. Each formulation was orally administered in the fasted state. The compendial paddle apparatus was used for the dissolution tests (500 mL, 37 °C, 25 or 50 rpm). BCB (10 mM, pH 6.8, 140 mM NaCl) and PPB (2.5 to 25 mM, pH 6.8, 140 mM NaCl) were used as dissolution media. The pH value of BCB was maintained by the floating lid method. In the clinical BE studies, two TFs were BE to RF, whereas one TF was non-BE. At a paddle speed of 50 rpm, RF and TFs showed little or no difference in the dissolution profiles in all buffer solutions. At 25 rpm, the dissolution profiles in 2.5 mM PPB and 10 mM BCB were consistent with the clinical BE results. The in vitro-in vivo correlation between C<sub>max</sub> ratio and dissolved% ratio at each time point was highest for 10 mM BCB at 25 rpm. These results suggest that the use of BCB increases the BE predictability of dissolution tests.</p>","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 11","pages":"989-995"},"PeriodicalIF":1.5000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Comparison of Phosphate and Bicarbonate Buffer Solutions as Dissolution Test Media for Predicting Bioequivalence of Febuxostat Formulation.\",\"authors\":\"Masaki Higashino, Kiyohiko Sugano\",\"doi\":\"10.1248/cpb.c24-00526\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The purpose of the present study was to compare phosphate buffer (PPB) and bicarbonate buffer (BCB) solutions as dissolution test media for predicting the bioequivalence (BE) of an immediate-release (IR) formulation. Febuxostat was used as a model of free acid drugs. One reference formulation (RF) and three test formulations (TF) were employed in this study. The clinical BE studies involved 18 to 24 healthy adult volunteers. Each formulation was orally administered in the fasted state. The compendial paddle apparatus was used for the dissolution tests (500 mL, 37 °C, 25 or 50 rpm). BCB (10 mM, pH 6.8, 140 mM NaCl) and PPB (2.5 to 25 mM, pH 6.8, 140 mM NaCl) were used as dissolution media. The pH value of BCB was maintained by the floating lid method. In the clinical BE studies, two TFs were BE to RF, whereas one TF was non-BE. At a paddle speed of 50 rpm, RF and TFs showed little or no difference in the dissolution profiles in all buffer solutions. At 25 rpm, the dissolution profiles in 2.5 mM PPB and 10 mM BCB were consistent with the clinical BE results. The in vitro-in vivo correlation between C<sub>max</sub> ratio and dissolved% ratio at each time point was highest for 10 mM BCB at 25 rpm. These results suggest that the use of BCB increases the BE predictability of dissolution tests.</p>\",\"PeriodicalId\":9773,\"journal\":{\"name\":\"Chemical & pharmaceutical bulletin\",\"volume\":\"72 11\",\"pages\":\"989-995\"},\"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.c24-00526\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemical & pharmaceutical bulletin","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1248/cpb.c24-00526","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
摘要
本研究旨在比较磷酸盐缓冲液(PPB)和碳酸氢盐缓冲液(BCB)作为溶出度测试介质,以预测速释(IR)制剂的生物等效性(BE)。非布索坦被用作游离酸药物的模型。本研究采用了一个参考制剂(RF)和三个试验制剂(TF)。18至24名健康成年志愿者参与了临床BE研究。每种配方均在空腹状态下口服。溶解试验采用药典规定的桨式仪器(500 mL、37 °C、25 或 50 rpm)。溶解介质为 BCB(10 mM,pH 6.8,140 mM NaCl)和 PPB(2.5 至 25 mM,pH 6.8,140 mM NaCl)。BCB 的 pH 值通过浮盖法保持。在临床 BE 研究中,两个 TF 为 BE 至 RF,一个 TF 为非 BE。桨速为 50 转/分钟时,RF 和 TF 在所有缓冲溶液中的溶解曲线差异很小或没有差异。在 25 rpm 转速下,2.5 mM PPB 和 10 mM BCB 中的溶解曲线与临床 BE 结果一致。在 25 rpm 时,10 mM BCB 在各时间点的 Cmax 比值和溶出率之间的体外-体内相关性最高。这些结果表明,BCB 的使用提高了溶出试验的 BE 可预测性。
Comparison of Phosphate and Bicarbonate Buffer Solutions as Dissolution Test Media for Predicting Bioequivalence of Febuxostat Formulation.
The purpose of the present study was to compare phosphate buffer (PPB) and bicarbonate buffer (BCB) solutions as dissolution test media for predicting the bioequivalence (BE) of an immediate-release (IR) formulation. Febuxostat was used as a model of free acid drugs. One reference formulation (RF) and three test formulations (TF) were employed in this study. The clinical BE studies involved 18 to 24 healthy adult volunteers. Each formulation was orally administered in the fasted state. The compendial paddle apparatus was used for the dissolution tests (500 mL, 37 °C, 25 or 50 rpm). BCB (10 mM, pH 6.8, 140 mM NaCl) and PPB (2.5 to 25 mM, pH 6.8, 140 mM NaCl) were used as dissolution media. The pH value of BCB was maintained by the floating lid method. In the clinical BE studies, two TFs were BE to RF, whereas one TF was non-BE. At a paddle speed of 50 rpm, RF and TFs showed little or no difference in the dissolution profiles in all buffer solutions. At 25 rpm, the dissolution profiles in 2.5 mM PPB and 10 mM BCB were consistent with the clinical BE results. The in vitro-in vivo correlation between Cmax ratio and dissolved% ratio at each time point was highest for 10 mM BCB at 25 rpm. These results suggest that the use of BCB increases the BE predictability of dissolution tests.
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.
Topics: Organic chemistry
In silico science
Inorganic chemistry
Pharmacognosy
Health statistics
Forensic science
Biochemistry
Pharmacology
Pharmaceutical care and science
Medicinal chemistry
Analytical chemistry
Physical pharmacy
Natural product chemistry
Toxicology
Environmental science
Molecular and cellular biology
Biopharmacy and pharmacokinetics
Pharmaceutical education
Chemical biology
Physical chemistry
Pharmaceutical engineering
Epidemiology
Hygiene
Regulatory science
Immunology and microbiology
Clinical pharmacy
Miscellaneous.