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
目的探讨黏膜黏附化疗药物HPC-MMC预防肿瘤复发的效果.方法对46例表浅膀胱癌患者于TURBt术后随机分两组行膀胱灌注化疗,黏膜黏附化疗药物组20例,以20 mg/20 ml 1%HPC-MMC膀胱灌注;MMC组26例,以20 mg/20 ml MMC膀胱灌注.疗程1年.HPC-MMC...目的探讨黏膜黏附化疗药物HPC-MMC预防肿瘤复发的效果.方法对46例表浅膀胱癌患者于TURBt术后随机分两组行膀胱灌注化疗,黏膜黏附化疗药物组20例,以20 mg/20 ml 1%HPC-MMC膀胱灌注;MMC组26例,以20 mg/20 ml MMC膀胱灌注.疗程1年.HPC-MMC组总灌注次数少于MMC组4次.随访6～36个月.结果 HPC-MMC组未发现出血性膀胱炎,无明显尿路刺激症状.平均随访27.4个月,7例复发,1年复发率为16.7%,3年总复发率38.9%.MMC组平均随访26.8个月,9例复发,1年复发率为22.7%,3年总复发率40.9%.结论黏膜黏附化疗药物HPC-MMC膀胱灌注防止肿瘤复发优于单用MMC,同时可降低副作用,减轻患者痛苦及经济负担.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.
文摘目的探讨黏膜黏附化疗药物HPC-MMC预防肿瘤复发的效果.方法对46例表浅膀胱癌患者于TURBt术后随机分两组行膀胱灌注化疗,黏膜黏附化疗药物组20例,以20 mg/20 ml 1%HPC-MMC膀胱灌注;MMC组26例,以20 mg/20 ml MMC膀胱灌注.疗程1年.HPC-MMC组总灌注次数少于MMC组4次.随访6～36个月.结果 HPC-MMC组未发现出血性膀胱炎,无明显尿路刺激症状.平均随访27.4个月,7例复发,1年复发率为16.7%,3年总复发率38.9%.MMC组平均随访26.8个月,9例复发,1年复发率为22.7%,3年总复发率40.9%.结论黏膜黏附化疗药物HPC-MMC膀胱灌注防止肿瘤复发优于单用MMC,同时可降低副作用,减轻患者痛苦及经济负担.
