卡托普利择时渗透泵片的处方优化
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篇名: 卡托普利择时渗透泵片的处方优化
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摘要: 目的:优化卡托普利择时渗透泵片的处方。方法:以卡托普利择时渗透泵片的累积释放百分率(Q)为指标,采用单因素法考察阻滞层包衣增质量,半透膜包衣增质量,含药层聚环氧乙烷(PEO)种类及含药层PEO(3×105)、羟丙基甲基纤维素(HPMC)用量,助推层PEO(7×106)、氯化钠(NaCl)用量对释药情况的影响;在单因素考察基础上,以释放行为综合评分(L)为指标,以含药层PEO(3×105)和HPMC用量、助推层PEO(7×106)和NaCl用量为主要因素,按L9(43)表进行正交试验优化片芯处方,并进行验证。结果:片芯最优处方为含药层PEO(3×105)用量71 mg,含药层HPMC用量15 mg,助推层PEO(7×106)用量61 mg,助推层NaCl用量18 mg;阻滞层包衣增质量为7%,半透膜包衣增质量为10%。按优化处方制备的渗透泵片4 h之后开始释药,4~20 h的体外释药回归方程为Q=5.118t-21.441(R2=0.995 6),符合零级释药特征。结论:优化的处方稳定可行、质量可控,可为卡托普利择时渗透泵片的进一步开发提供参考。
ABSTRACT: OBJECTIVE: To optimize the formula of Captopril timing osmotic pump tablets. METHODS: Using accumulative release rate (Q) as index, single factor test was used to investigate the effects of blocking layer coating weight gain, semipermeable membrane coating weight gain, the type of polyepoxide (PEO),the amount of PEO (3×105) and HPMC in drug bearing layer, the amount of PEO (7×106) and NaCl in booster layer on drug release of Captopril timing osmotic pump tablets. Based on single factor investigation, using comprehensive score of release behavior (L) as index, the amount of PEO (3×105) and HPMC in drug bearing layer, the amount of PEO (7×106) and NaCl in booster layer as factors, L9(43) orthogonal test was used to optimize the formula of tablet core validation test was conducted. RESULTS: The optimal formula of tablet core included PEO(3×105) 71 mg and HPMC 15 mg in drug bearing layer, PEO (7×106) 61 mg and NaCl 18 mg in booster layer, coating weight gain 7% and semipermeable membrane coating weight gain 10% in blocking layer.  The osmotic pump tablet prepared by optimized formula released after 4 h; in vitro drug release regression equation was Q=5.118t-21.441(R2=0.995 6), which was in line with zero-order release characteristics. CONCLUSIONS: The optimal formula is stable, feasible and controllable in quality, and can provide reference for further development of Captopril timing osmotic pump tablets.
期刊: 2018年第29卷第10期
作者: 叶吴琦,左丁,张子豪,陈天民,焦敏芬,韩翠艳
AUTHORS: YE Wuqi,ZUO Ding,ZHANG Zihao,CHEN Tianmin,JIAO Minfen,HAN Cuiyan
关键字: 卡托普利;择时渗透泵片;单因素考察;正交试验;处方优化
KEYWORDS: Captopril; Timing osmotic pump tablets; Single factor investigation; Orthogonal test; Formula optimization
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