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Preparation and evaluation of solid dispersion for nitrendipine-carbopol and nitrendipine-HPMCP systems using a twin screw extruder.

机译:使用双螺杆挤出机制备和评价尼群地平-卡波姆和尼群地平-HPMCP系统的固体分散体。

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摘要

In the present study, we prepared solid dispersions of the poorly water-soluble drug nitrendipine (NIT) using the twin screw extruder method with high-molecular-weight substances, hydroxypropylmethylcellulosephthalate (HPMCP) and Carbopol (CAR), as carriers. Powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) evaluation showed that solid dispersions can be formed when NIT-HPMCP and NIT-CAR mixtures are treated with the twin screw extruder method. Fourier Transformation IR Spectroscopy (FT-IR) obtained with NIT-HPMCP and NIT-CAR solid dispersions indicated the presence of hydrogen bonding between the drug and the carriers. NIT-CAR solid dispersions were found to give somewhat higher dissolution than crystalline NIT and physical mixtures, while the dissolution of NIT-HPMCP solid dispersions was markedly decreased compared with the crystalline NIT and physical mixtures. These findings indicated that CAR has a greater ability to improve the dissolution of NIT than HPMCP when a twin screw extruder was employed to prepare the solid dispersions. The twin screw extruder method can be used as a simple and effective method for the preparation of solid dispersions to improve the dissolution properties of poorly water-soluble drugs when choosing proper polymers as carriers.
机译:在本研究中,我们使用高分子量物质,羟丙基甲基纤维素邻苯二甲酸酯(HPMCP)和Carbopol(CAR)作为载体,使用双螺杆挤出机方法制备了水溶性差的药物硝苯地平(NIT)的固体分散体。粉末X射线衍射(PXRD)和差示扫描量热法(DSC)评估表明,使用双螺杆挤出机方法处理NIT-HPMCP和NIT-CAR混合物时,可以形成固体分散体。使用NIT-HPMCP和NIT-CAR固体分散体获得的傅立叶变换红外光谱(FT-IR)表明,药物与载体之间存在氢键。发现NIT-CAR固体分散体比结晶NIT和物理混合物具有更高的溶解度,而与结晶NIT和物理混合物相比,NIT-HPMCP固体分散体的溶解度明显降低。这些发现表明,当使用双螺杆挤出机制备固体分散体时,CAR具有比HPMCP更大的改善NIT溶解的能力。当选择合适的聚合物作为载体时,双螺杆挤出机方法可以用作制备固体分散体的简单有效的方法,以改善水溶性差的药物的溶解性能。

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