该研究就中药生物药剂学分类系统（biopharmaceutics classification system of Chinese materia medica,CMMBCS）中的特性溶出速率问题,利用旋转盘系统考察人工制造的多成分环境对特性溶出速率的影响,并利用所获数据进行分析总结相关...该研究就中药生物药剂学分类系统（biopharmaceutics classification system of Chinese materia medica,CMMBCS）中的特性溶出速率问题,利用旋转盘系统考察人工制造的多成分环境对特性溶出速率的影响,并利用所获数据进行分析总结相关规律。采用递进式设计,分别研究了单一成分（葛根素、黄芩苷和甘草酸）、2成分（葛根素＋黄芩苷,葛根素＋甘草酸,黄芩苷＋甘草酸）和3成分（葛根素＋黄芩苷＋甘草酸）环境对小檗碱特性溶出速率的影响趋势,为多成分环境下中药成分的吸收相关研究奠定基础。展开更多
Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible structures, 1H- and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the so...Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible structures, 1H- and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the solid-state, both tautomers can be isolated as crystal forms A (1H-tautomer) and B (2H-tautomer). Studies have reported that IBS is a polymorphic system and its forms A and B are related monotropically. These reports indicate form B as the most stable and less soluble form. Therefore, the goal of this contribution is to demonstrate through a complete solid-state characterization, thermodynamic study and dissolution properties that the IBS forms are desmotropes that are not related monotropically. However, the intention is also to call attention to the importance of conducting strict chemical and in solid-state quality controls on the IBS raw materials. Hence, powder X-ray diffraction (PXRD) and Raman spectroscopy (RS) at ambient and non-ambient conditions, differential scanning calorimetry (DSC), hot stage microscopy (HSM), Fourier transform infrared (FT-IR) and scanning electron microscopy (SEM) techniques were applied. Furthermore, intrinsic dissolution rate (IDR) and structural stability studies at 98% relative humidity (RH), 25℃ and 40 ℃ were conducted as well. The results show that in fact, form A is approximately four-fold more soluble than form B. In addition, both IBS forms are stable at ambient conditions. Nevertheless, structural and/or chemical instability was observed in form B at 40℃ and 98% RH. IBS has been confirmed as a desmotropic system rather than a polymorphic one. Consequently, forms A and B are not related monotropically.展开更多
文摘该研究就中药生物药剂学分类系统（biopharmaceutics classification system of Chinese materia medica,CMMBCS）中的特性溶出速率问题,利用旋转盘系统考察人工制造的多成分环境对特性溶出速率的影响,并利用所获数据进行分析总结相关规律。采用递进式设计,分别研究了单一成分（葛根素、黄芩苷和甘草酸）、2成分（葛根素＋黄芩苷,葛根素＋甘草酸,黄芩苷＋甘草酸）和3成分（葛根素＋黄芩苷＋甘草酸）环境对小檗碱特性溶出速率的影响趋势,为多成分环境下中药成分的吸收相关研究奠定基础。
基金financial support of FEES-CONARE (Ref 115B5662)the University of Costa Rica (UCR)+1 种基金the Costa Rica Institute of Technology (TEC)the National Laboratory of Nanotechnology (LANOTEC)
文摘Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible structures, 1H- and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the solid-state, both tautomers can be isolated as crystal forms A (1H-tautomer) and B (2H-tautomer). Studies have reported that IBS is a polymorphic system and its forms A and B are related monotropically. These reports indicate form B as the most stable and less soluble form. Therefore, the goal of this contribution is to demonstrate through a complete solid-state characterization, thermodynamic study and dissolution properties that the IBS forms are desmotropes that are not related monotropically. However, the intention is also to call attention to the importance of conducting strict chemical and in solid-state quality controls on the IBS raw materials. Hence, powder X-ray diffraction (PXRD) and Raman spectroscopy (RS) at ambient and non-ambient conditions, differential scanning calorimetry (DSC), hot stage microscopy (HSM), Fourier transform infrared (FT-IR) and scanning electron microscopy (SEM) techniques were applied. Furthermore, intrinsic dissolution rate (IDR) and structural stability studies at 98% relative humidity (RH), 25℃ and 40 ℃ were conducted as well. The results show that in fact, form A is approximately four-fold more soluble than form B. In addition, both IBS forms are stable at ambient conditions. Nevertheless, structural and/or chemical instability was observed in form B at 40℃ and 98% RH. IBS has been confirmed as a desmotropic system rather than a polymorphic one. Consequently, forms A and B are not related monotropically.
