García-Pérez Martha-Estrella, Lemus-Rodríguez Zoe, Hung-Arbelo Mario, Vistel-Vigo Marlen
a Laboratorio Farmacéutico Oriente , Santiago de Cuba , Cuba.
b Facultad de Químico-Farmacobiología , Universidad Michoacana de San Nicolás de Hidalgo , Morelia , Michoacán , Mexico.
Drug Dev Ind Pharm. 2017 Dec;43(12):2011-2015. doi: 10.1080/03639045.2017.1359621. Epub 2017 Aug 3.
Petiveria alliacea L. (Phytolaccaceae) is a perennial shrub used by its immunomodulatory, anticancerogenic and anti-inflammatory properties. This study determined the influence of polyvinylpyrrolidone (PVP), colloidal silicon dioxide (CSD) and microcrystalline cellulose (MC) on the technological characteristic of a high-dose P. alliacea tablet prepared by the wet granulation method.
The botanical and pharmacognostic analysis of the plant material was firstly performed, followed by a 2 factorial design considering three factors at two levels: (a) the binder (PVP) incorporated in formulation at 10% and 15% (w/w); (b) the compacting agent (CSD) added at 10% and 15% (w/w) and; (c) the diluent (MC) included at 7.33% and 12.46% (w/w). The analysis of pharmaceutical performance and the accelerated and long-term stability of the best prototype were also completed.
The binder, compacting agent and the interaction binder/diluent had a significant impact on breaking force of high-dose P. alliacea tablet. The optimum formula was found to contain 15% (w/w) of CSD, 7.33% (w/w) of MC and 10% (w/w) of PVP. At these conditions, the tablet shows a breaking force of 77.96 N, a friability of 0.39%, a total phenol content of 1.30 mg/tablet and a maximum disintegration time of 6 min.
The use of adequate amounts of PVP, MC and CSD as per the factorial design allowed the preparation of a tablet suitable for administration, despite the inappropriate flow and compressibility properties of the P. alliacea powder.
蒜藜芦（商陆科）是一种多年生灌木，因其具有免疫调节、抗癌和抗炎特性而被使用。本研究确定了聚乙烯吡咯烷酮（PVP）、胶体二氧化硅（CSD）和微晶纤维素（MC）对通过湿法制粒制备的高剂量蒜藜芦片剂工艺特性的影响。
首先对植物材料进行植物学和生药学分析，然后采用二因素设计，考虑三个因素，每个因素有两个水平：（a）制剂中加入的粘合剂（PVP），含量为10%和15%（w/w）；（b）加入的压片助剂（CSD），含量为10%和15%（w/w）；（c）稀释剂（MC），含量为7.33%和12.46%（w/w）。还完成了最佳原型的药物性能分析以及加速和长期稳定性研究。
粘合剂、压片助剂以及粘合剂/稀释剂的相互作用对高剂量蒜藜芦片剂的断裂力有显著影响。发现最佳配方包含15%（w/w）的CSD、7.33%（w/w）的MC和10%（w/w）的PVP。在这些条件下，片剂的断裂力为77.96 N，脆碎度为0.39%，总酚含量为1.30 mg/片，最大崩解时间为6分钟。
根据析因设计使用适量的PVP、MC和CSD，尽管蒜藜芦粉末的流动性和可压缩性不合适，但仍可制备出适合给药的片剂。
