右佐匹克隆口腔崩解片的制备及处方优化
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摘要
目的:制备右佐匹克隆口腔崩解片,并优化其处方。方法:采用粉末直接压片法制备右佐匹克隆口腔崩解片,以物料休止角、崩解时限、口感评价为指标,单因素试验筛选处方中填充剂、崩解剂、润滑剂、矫味剂种类或用量;以崩解时限为指标,正交试验优化处方中填充剂比例、崩解剂用量、润滑剂用量、矫味剂用量,并考察最优处方所制右佐匹克隆口腔崩解片的硬度和主成分含量。结果:最优处方中填充剂甘露醇-微晶纤维素质量比为1∶4、崩解剂交联聚维酮用量为15%、润滑剂硬脂酸镁用量为1.0%、矫味剂甜菊苷用量为3.0%。所制3批右佐匹克隆口腔崩解片的表面光滑、口感微甜,崩解时限分别为(26.7±1.2)、(26.7±0.6)、(27.6±0.9)s,硬度分别为(3.59±0.19)、(3.49±0.18)、(3.27±0.16)kg,右佐匹克隆含量分别为(99.47±0.15)%、(99.53±0.05)%、(99.46±0.20)%,RSD均≤0.87%(n=3)。结论:所制右佐匹克隆口腔崩解片各项质量指标均符合口腔崩解片的要求。
OBJECTIVE:To prepare Dexzopiclone orally disintegrating tablets(DODT),and to optimize its formulation.METHODS:Direct powder compression method was used to prepare DODT. Using repose angle of material,disintegration time and taste evaluation as indexes,single factor test was used to screen the types or amount of bulking agent,disintegrating agent,glidant and flavoring agent;using disintegration time as index,orthogonal experiment was applied to optimize the proportion of bulking agent,the amount of disintegrating agent,glidant and flavoring agent. Then the hardness and main component contents of DODT prepared by optimal formulation were determined. RESULTS:The optimal formulation was as follows as the ratio of mannitol-MCC 1 ∶ 4,the amount of disintegrating agent PVPP was 15%,the amount of glidant magnesium stearate was 1.0%,the amount of flavoring agent stevia was 3.0%. Three batches of prepared DODT were smooth in surface and good in taste;their disintegration time were(26.7±1.2),(26.7±0.6),(27.6±0.9)s,hardness were(3.59±0.19),(3.49±0.18),(3.27±0.16)kg,and contents were(99.47±0.15)%,(99.53±0.05)%,(99.46±0.20)%,respectively(all RSDs≤0.87%,n=3). CONCLUSIONS:Prepared DODT are all in line with the quality requirements of orally disintegrating tablets.
OBJECTIVE:To prepare Dexzopiclone orally disintegrating tablets(DODT),and to optimize its formulation.METHODS:Direct powder compression method was used to prepare DODT. Using repose angle of material,disintegration time and taste evaluation as indexes,single factor test was used to screen the types or amount of bulking agent,disintegrating agent,glidant and flavoring agent;using disintegration time as index,orthogonal experiment was applied to optimize the proportion of bulking agent,the amount of disintegrating agent,glidant and flavoring agent. Then the hardness and main component contents of DODT prepared by optimal formulation were determined. RESULTS:The optimal formulation was as follows as the ratio of mannitol-MCC 1 ∶ 4,the amount of disintegrating agent PVPP was 15%,the amount of glidant magnesium stearate was 1.0%,the amount of flavoring agent stevia was 3.0%. Three batches of prepared DODT were smooth in surface and good in taste;their disintegration time were(26.7±1.2),(26.7±0.6),(27.6±0.9)s,hardness were(3.59±0.19),(3.49±0.18),(3.27±0.16)kg,and contents were(99.47±0.15)%,(99.53±0.05)%,(99.46±0.20)%,respectively(all RSDs≤0.87%,n=3). CONCLUSIONS:Prepared DODT are all in line with the quality requirements of orally disintegrating tablets.
引文
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[2]蒋文婧.艾司佐匹克隆的药物化学[J].中国民族民间医药,2009,18(8):21-22.
[3]HIRANI JJ,RATHOD DA,VADALIA KR.Orally disintegrating tablets:a review[J].Trop J Pharm Res,2011,2(4):81-88.
[4]曾富荣,程英.右佐匹克隆治疗脑卒中后焦虑抑郁伴失眠的临床疗效[J].中国现代医生,2012,50(36):159-160.
[5]班春霞,郭本玉,陈青,等.住院精神病患者精神药物应用时点调查[J].临床心身疾病杂志,2014,20(6):90-91.
[6]林伟豪,朱新华.阿司匹林口崩片的制备[J].华西药学杂志,2012,27(5):547-549.
[7]国家药典委员会.中华人民共和国药典:四部[S].2015年版.北京:中国医药科技出版社,2015:通则0921.
[8]吴旖,谢敏.百部新碱口腔崩解片的制备[J].中国药房,2016,27(16):2268-2271.
[9]田朋鑫,罗永煌,刘艳玲,等.甲磺酸普立地诺口腔崩解片的研制及质量评价[J].中国药房,2012,23(1):48-51.
[10]张爱丽,邵杰,张庆芬.橘红痰咳口腔崩解片的制备[J].中成药,2015,37(7):1462-1466.
[11]张招磊.右旋佐匹克隆片的制备工艺及质量评价[D].哈尔滨:黑龙江中医药大学,2014.
[12]李标,蒲道俊.口腔崩解片的研究进展[J].中国医院用药评价与分析,2010,10(2):159-160.
[13]U.S.Food and Drug Administration.Guidance for industry orally disintegrating tablets[EB/OL].(2008-11)[2017-10-05].http://www.fda.gov/cder/guidance/index.htm.