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采用响应面法对盐酸伊托必利缓释骨架片的处方工艺进行优化及释放动力学评价。

Formulation development and optimization of sustained release matrix tablet of Itopride HCl by response surface methodology and its evaluation of release kinetics.

机构信息

Particle Design Research Group, Universiti Teknologi MARA, 42300 Puncak Alam, Selangor, Malaysia ; Non-Destructive Biomedical and Pharmaceutical Research Centre, Universiti Teknologi MARA, 42300 Puncak Alam, Selangor, Malaysia.

出版信息

Saudi Pharm J. 2013 Apr;21(2):201-13. doi: 10.1016/j.jsps.2012.03.006. Epub 2012 Apr 12.

Abstract

The objective of this present investigation was to develop and formulate sustained release (SR) matrix tablets of Itopride HCl, by using different polymer combinations and fillers, to optimize by Central Composite Design response surface methodology for different drug release variables and to evaluate drug release pattern of the optimized product. Sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and polyvinyl pyrolidine (pvp) and lactose as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was further subjected to scanning electron microscopy to reveal its release pattern. The in vitro study revealed that combining of HPMC K100M (24.65 MG) with pvp(20 mg)and use of LACTOSE as filler sustained the action more than 12 h. The developed sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.

摘要

本研究的目的是开发和制备盐酸伊托必利的缓控释(SR)基质片剂,使用不同的聚合物组合和填充剂,通过中心组合设计响应面法优化不同药物释放变量,并评估优化产品的药物释放模式。采用纤维素类聚合物:羟丙甲纤维素(HPMC)和聚乙烯吡咯烷酮(pvp)和乳糖作为填充剂,制备了各种组合的缓控释基质片剂。预压和后压参数的研究有助于筛选出具有最佳特性的配方,该配方通过响应面法(中心组合设计)进行了优化研究。进一步对优化后的片剂进行扫描电子显微镜观察,揭示其释放模式。体外研究表明,将 HPMC K100M(24.65MG)与 pvp(20mg)结合使用乳糖作为填充剂,可使作用持续 12 小时以上。开发的具有改善疗效的缓控释基质片剂在治疗上可能优于传统片剂。

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