The purpose of this study was to develop an extended-release(ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combinati...The purpose of this study was to develop an extended-release(ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combination of enteric polymer and hydrophilic polymer. Hypromellose acetate succinate(HPMCAS) and hydroxypropylcellulose(HPC) were selected as ER polymers for the ER matrix tablet(HPMCAS/HPC ER matrix tablet). Oxycodone hydrochloride was employed as a model drug. Dissolution properties of the HPMCAS/HPC ER matrix tablets were evaluated and were not affected by the pH of the test medium or paddle rotating speed.In a USP apparatus 3(bio-relevant dissolution method), dissolution profiles of the HPMCAS/HPC ER matrix tablets containing oxycodone hydrochloride were similar to that of the reference product(OxyC ontin). Moreover, in vivo performance after oral administration of the HPMCAS/HPC ER matrix tablets to humans was simulated by GastroP lus based on dissolution profiles from the USP apparatus 3. The plasma concentration-time profile simulated was similar to that of the reference product. These results suggest that the combination of HPMCAS and HPC shows a robust dissolution profile against pH and paddle rotating speed and indicates the appropriate extended-release profile in humans.展开更多
目的:通过测定纯水残氧量、气体分压和air量,分析与评价真空脱气仪的脱气效果,并与抽滤、煮沸、超声等方法进行比较,选出适宜的溶出介质脱气方法,指导用于日常检验工作中。方法:采用单路水质在线监控仪和Carbo QC Anton Pear仪分别测定...目的:通过测定纯水残氧量、气体分压和air量,分析与评价真空脱气仪的脱气效果,并与抽滤、煮沸、超声等方法进行比较,选出适宜的溶出介质脱气方法,指导用于日常检验工作中。方法:采用单路水质在线监控仪和Carbo QC Anton Pear仪分别测定纯水残氧量,气体分压和air量。对真空脱气仪在负压、脱气时间等方面进行脱气效果考察,并与抽滤、煮沸、超声等脱气效果进行比较。结果:真空脱气仪在负压0.06 MPa、介质温度41℃、脱气时间为30 min情况下,脱气效果明显。抽滤、煮沸脱气效果与真空脱气仪脱气效果相当。超声脱气效果不明显。结论:真空脱气仪使用快捷方便、高效,脱气效果明显,适宜用于溶出介质的脱气处理。展开更多
文摘The purpose of this study was to develop an extended-release(ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combination of enteric polymer and hydrophilic polymer. Hypromellose acetate succinate(HPMCAS) and hydroxypropylcellulose(HPC) were selected as ER polymers for the ER matrix tablet(HPMCAS/HPC ER matrix tablet). Oxycodone hydrochloride was employed as a model drug. Dissolution properties of the HPMCAS/HPC ER matrix tablets were evaluated and were not affected by the pH of the test medium or paddle rotating speed.In a USP apparatus 3(bio-relevant dissolution method), dissolution profiles of the HPMCAS/HPC ER matrix tablets containing oxycodone hydrochloride were similar to that of the reference product(OxyC ontin). Moreover, in vivo performance after oral administration of the HPMCAS/HPC ER matrix tablets to humans was simulated by GastroP lus based on dissolution profiles from the USP apparatus 3. The plasma concentration-time profile simulated was similar to that of the reference product. These results suggest that the combination of HPMCAS and HPC shows a robust dissolution profile against pH and paddle rotating speed and indicates the appropriate extended-release profile in humans.
