{"title":"喷雾干燥法制备的普罗布考与阿托伐他汀钙三水合物共晶溶解性能的改进","authors":"Shinji Oyama, Noriko Ogawa, Kaori Kawai, Kanako Iwai, Toshiya Yasunaga, Hiromitsu Yamamoto","doi":"10.1248/cpb.c23-00673","DOIUrl":null,"url":null,"abstract":"</p><p>A co-amorphous model drug was prepared by the spray-drying (SD) of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as low water solubility and co-former components, respectively. The physicochemical properties of the prepared samples were characterized by powder X-ray diffraction (PXRD) analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and dissolution tests. Stability tests were also conducted under a stress environment of 40 °C and 75% relative humidity. The results of PXRD measurements and thermal analysis suggested that PC and ATO form a co-amorphous system by SD. Thermal analysis also indicated an endothermic peak that followed an exotherm in amorphous PC and a physical mixture (PM) of amorphous PC and ATO; however, no endothermic peak was detected in the co-amorphous system. The dissolution profiles for PC in the co-amorphous sample composed of PC and ATO were improved compared to those for raw PC crystals or the PM. Stability tests indicated that the co-amorphous material formed by PC and ATO can be stored for 35 d without crystallization, whereas amorphous PC became crystallized within a day. Therefore, co-amorphization of PC and ATO prepared by SD is considered to be a useful method to improve the solubility of PC in water.</p>\n<p></p>\n<img alt=\"\" src=\"https://www.jstage.jst.go.jp/pub/cpb/72/2/72_c23-00673/figure/72_c23-00673.png\"/>\n<span style=\"padding-left:5px;\">Fullsize Image</span>","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.5000,"publicationDate":"2024-02-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Improved Dissolution Properties of Co-amorphous Probucol with Atorvastatin Calcium Trihydrate Prepared by Spray-Drying\",\"authors\":\"Shinji Oyama, Noriko Ogawa, Kaori Kawai, Kanako Iwai, Toshiya Yasunaga, Hiromitsu Yamamoto\",\"doi\":\"10.1248/cpb.c23-00673\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"</p><p>A co-amorphous model drug was prepared by the spray-drying (SD) of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as low water solubility and co-former components, respectively. The physicochemical properties of the prepared samples were characterized by powder X-ray diffraction (PXRD) analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and dissolution tests. Stability tests were also conducted under a stress environment of 40 °C and 75% relative humidity. The results of PXRD measurements and thermal analysis suggested that PC and ATO form a co-amorphous system by SD. Thermal analysis also indicated an endothermic peak that followed an exotherm in amorphous PC and a physical mixture (PM) of amorphous PC and ATO; however, no endothermic peak was detected in the co-amorphous system. The dissolution profiles for PC in the co-amorphous sample composed of PC and ATO were improved compared to those for raw PC crystals or the PM. Stability tests indicated that the co-amorphous material formed by PC and ATO can be stored for 35 d without crystallization, whereas amorphous PC became crystallized within a day. Therefore, co-amorphization of PC and ATO prepared by SD is considered to be a useful method to improve the solubility of PC in water.</p>\\n<p></p>\\n<img alt=\\\"\\\" src=\\\"https://www.jstage.jst.go.jp/pub/cpb/72/2/72_c23-00673/figure/72_c23-00673.png\\\"/>\\n<span style=\\\"padding-left:5px;\\\">Fullsize Image</span>\",\"PeriodicalId\":9773,\"journal\":{\"name\":\"Chemical & pharmaceutical bulletin\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2024-02-16\",\"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.c23-00673\",\"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.c23-00673","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
通过喷雾干燥法（SD）制备了一种共晶模型药物，其成分分别为低水溶性的丙磺舒（PC）和阿托伐他汀钙三水合物（ATO）。通过粉末 X 射线衍射（PXRD）分析、热分析、傅立叶变换红外光谱（FTIR）和溶解试验对制备样品的理化性质进行了表征。此外，还在 40 °C 和 75% 相对湿度的应力环境下进行了稳定性测试。PXRD 测量和热分析结果表明，PC 和 ATO 通过 SD 形成了共晶体系。热分析还表明，在非晶态 PC 和非晶态 PC 与 ATO 的物理混合物（PM）中，放热后出现了一个内热峰；但在共晶体系中没有检测到内热峰。与未加工的 PC 晶体或 PM 相比，由 PC 和 ATO 组成的共晶样品中 PC 的溶解曲线有所改善。稳定性测试表明，PC 和 ATO 形成的共晶材料可存放 35 天而不结晶，而无定形 PC 在一天内就会结晶。因此，用 SD 法制备的 PC 和 ATO 共晶被认为是提高 PC 水溶性的有效方法。
Improved Dissolution Properties of Co-amorphous Probucol with Atorvastatin Calcium Trihydrate Prepared by Spray-Drying
A co-amorphous model drug was prepared by the spray-drying (SD) of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as low water solubility and co-former components, respectively. The physicochemical properties of the prepared samples were characterized by powder X-ray diffraction (PXRD) analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and dissolution tests. Stability tests were also conducted under a stress environment of 40 °C and 75% relative humidity. The results of PXRD measurements and thermal analysis suggested that PC and ATO form a co-amorphous system by SD. Thermal analysis also indicated an endothermic peak that followed an exotherm in amorphous PC and a physical mixture (PM) of amorphous PC and ATO; however, no endothermic peak was detected in the co-amorphous system. The dissolution profiles for PC in the co-amorphous sample composed of PC and ATO were improved compared to those for raw PC crystals or the PM. Stability tests indicated that the co-amorphous material formed by PC and ATO can be stored for 35 d without crystallization, whereas amorphous PC became crystallized within a day. Therefore, co-amorphization of PC and ATO prepared by SD is considered to be a useful method to improve the solubility of PC in water.
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
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Health statistics
Forensic science
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Pharmacology
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Medicinal chemistry
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Physical pharmacy
Natural product chemistry
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Biopharmacy and pharmacokinetics
Pharmaceutical education
Chemical biology
Physical chemistry
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Regulatory science
Immunology and microbiology
Clinical pharmacy
Miscellaneous.
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