卡前列甲酯-羟丙基-β-环糊精包合物舌下片的制备及质量评价

发布时间：2018-09-17 08:47

【摘要】：目的:制备卡前列甲酯-羟丙基-β-环糊精(HP-β-CD)包合物舌下片,并进行质量评价。方法:采用湿法制粒法制备卡前列甲酯-HP-β-CD包合物舌下片,以片剂的外观、崩解时间、润湿时间、主药含量为考察指标,以处方中甘露醇-乳糖的质量比、聚维酮的体积分数、低取代羟丙纤维素(L-HPC)的用量为因素,采用正交试验筛选处方。评价最优处方所制舌下片的崩解时间、润湿时间、主药含量、含量均匀度及溶出度。结果:最优处方为卡前列甲酯-HP-β-CD包合物78.82 mg(含卡前列甲酯1 mg),甘露醇-乳糖(质量比9:1)的混合粉末100 mg,2%的PVP溶液适量,L-HPC 30 mg,硬脂酸镁1 mg。所制3批舌下片的崩解时间为(25.30±3.21)~(26.53±2.69)s,润湿时间为(64.65±8.07)~(65.54±7.21)s,主药含量为(96.13±0.43)%~(97.06±0.82)%,含量均匀度为5.95~7.68,10 min内累积溶出度均超过50%,30 min内可完全溶出。结论:成功制得质量符合要求的卡前列甲酯-HP-β-CD包合物舌下片。
[Abstract]:Aim: to prepare sublingual tablets of HP- 尾-CD inclusion compound and evaluate its quality. Methods: carboprost methyl ester -HP- 尾 -CD inclusion compound sublingual tablets were prepared by wet granulation method. The appearance, disintegration time, wetting time and main drug content of the tablets were used as indexes. The mass ratio of mannitol and lactose in the prescription and the volume fraction of polyviridone were used as the index. The dosage of low substituted hydroxypropyl cellulose (L-HPC) was selected by orthogonal test. To evaluate the disintegration time, wetting time, main drug content, content uniformity and dissolution of sublingual tablets. Results: the optimal formulation was 78.82 mg (1 mg), mannitol-lactose mixed powder containing Carprost methyl ester HP- 尾 -CD) in PVP solution of 100 mg,2% mixed powder with L-HPC 30 mg, magnesium stearate 1 mg.. The disintegration time of the three sublingual tablets was (25.30 卤3.21) ~ (26.53 卤2.69) s, the wetting time was (64.65 卤8.07) ~ (65.54 卤7.21) s, the content of the main drug was (96.13 卤0.43) ~ (97.06 卤0.82), and the content uniformity was 5.95 卤7.6810 min. Conclusion: the sublingual tablets of carprost methyl ester-尾-CD inclusion compound were successfully prepared.
【作者单位】：重庆市急救医疗中心药剂科;陆军军医大学第三附属医院药剂科;重庆医药高等专科学校药学院;重庆市第五人民医院药剂科;
【基金】：重庆市卫生和计划生育委员会医学科研计划项目(No.20142078)
【分类号】：R943

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