分散片常用辅料粉体学参数的测定及微粉硅胶对中药分散片崩解性能的影响

The determination of micromeritics parameters of dispersible tablet's common excipients and the effects of SiO_2 on TCM dispersible tablet's disintegrating properties

目的:研究中药分散片辅料微晶纤维素(MCC)、交联聚维酮(PVPP)、低取代羟丙纤维素(L-HPC)、羧甲基淀粉钠(CMS-Na)、微粉硅胶的性质以及微粉硅胶对中药分散片崩解性能的影响。方法:通过测定粒径分布、比表面积与孔隙度、微观形态、休止角、密度及溶胀性等粉体学参数掌握辅料的个性特征;通过微粉硅胶配伍前后辅料崩解性能的变化以及微粉硅胶不同加入方式对4种分散片崩解性能的影响,证明微粉硅胶研磨改性缩短分散片崩解时间的普适性。结果:CMS-Na为表面光滑的规则球状颗粒,粒径与比表面积小,流动性与填充性较好,可压性较差;PVPP为多孔不规则团块状,比表面积与微孔面积大,吸附性与可压性好,流动性与填充性差。L-HPC与MCC形状不规则,可压性好,流动性与填充性一般。微粉硅胶呈多孔球状结构,粒径很小,比表面积和孔隙率极大。配伍低剂量微粉硅胶后,各种辅料的崩解时间明显缩短;当微粉硅胶作为填充剂加入时,分散片崩解时间变化规律不一致,当微粉硅胶作为改性剂加入时,4种分散片的崩解时间均缩短,且明显小于原处方及作为填充剂加入。结论:通过微粉硅胶研磨改性,能使提取物的比表面积增大、润湿性及吸水性增强,形成利于崩解的微环境,显著降低崩解时间;且这种效应不是通过调整辅料用量来实现的。

OBJECTIVE To study the physical properties of TCM dispersible tablet excipients microcrystalline cellulose （MCC）, crosslinked povidone （PVPP）, low-substituted hydroxypropyl cellulose （L-HPC）, sodium carboxymethyl starch （CMS- Na） ,micro-silica and the effects of micro silica on TCM dispersible tablet＇s disintegrating properties. METHODS The micro- meritic properties were studied by measuring the particle size distribution, specific surface area and porosity, morphology, re pose angle, density and swelling. By studying the changes of excipients disintegrating properties of micro-silica before and after compatibility, and the influence of different adding method of micro-silica on disintegrating properties of four kinds of dispers ible tablets, a common applicability was proved that micro-silica grinding modification could shorten the disintegration time of dispersible tablets. RESULTS CMS-Na was the more regular spherical particle with smooth surface and small specific surface area, good mobility and fillibility, poor compressibility. PVPP was irregular porous mass with large surface area and size dis tribution, with good adsorbability and compressibility, poor mobility and fillibility. L HPC and MCC showed irregular shape, good compressibility, mobility and fillibitity in general. Micro-silica powder was porous spherical structure, small particle size, specific surface area and porosity greatly. The disintegration time was significantly shorter after excipients combined with low dose micro-silica. When Micro silica as filler added, some varieties of disintegration time was extended, tractional shortening, the law was not consistent. When micro-silica was added as a modifier, the disintegration time of all varieties was shortened, and significantly less than the original prescription and as a filler added. CONCLUSION Micro-silica modified by grinding could increase the specific surface area of extracts , enhanced the wettability and water absorptivity, benefited to the formation of dis- integrating microenvironment, and significantly reduced the disintegration time, And this effect was not achieved by adjusting the excipients ratio.