目的 以陈皮Citri Reticulatae Pericarpium生粉为模型药物，研究改性剂微粉硅胶的不同加入方式与用量对陈皮生粉的粉体学性质以及直压性能的影响。方法 采用液相分散法以外加法、内加法及内外加法将微粉硅胶与陈皮共处理制备陈皮改性复合粉体，测定并比较各粉体的密度、流动性、粒径、孔隙率、压缩成型性等粉体学性质和抗张强度、功与能等相关压片性质，并绘制物理指纹图谱。结果 微粉硅胶的加入方法不同，陈皮改性粒子的粉体学和压缩性质改善程度不同，与陈皮原料药相比，内加法和内外加法所制备的改性粉体（样品S3、S6～S9）的流动性、均匀度、密度均得到改善，吸湿性降低约30.46%～42.00%，可压性增强（TS 7.01～12.08倍），比表面积增大（1.63～2.42倍），有效功和能增加，崩解时间降低，约为250～384 s，直压性能明显改善。其中内加法（样品S3）和内外加法粉混小比例（样品S9）的改性粉体改善最显著。然而，外加法和物理混合法所制备的改性粉体样品（样品S2、S4、S5）流动性和比表面积也有所改善，但二者具有较小的堆密度与振实密度，自身无法压制成片。这可能是与微粉硅胶的加入方式有关，因为微粉硅胶外加（样品S2、S4、S5），大部分辅料不能有效地与中药粉体结合，浮在粉体表面，微粉硅胶自身性质发挥主要作用。而内加法/内外加法（样品S3、S6、S8、S9），由于固体桥和析出活性成分的包裹作用，部分微粉硅胶更紧密地包裹在主体粒子表面，部分进入主体粒子内部。在压片过程中，表面分布的纳米微粉硅胶起到促进粒子重排的作用，并且给粒子提供了纳米级的粗糙表面，在压缩过程中转变为更大的结合面积，从而显著提高片剂的TS。相较于外加法，其具有较大的密度和较好的均匀性和可压性。结论 采用液相分散法将微粉硅胶以内加法及内外加法与陈皮生粉共处理能显著改善其生粉的直压性质，可为一些中药提取物片剂制备性质的改善提供一个可行策略。

Objective To investigate the effects of the amount and different adding methods of engineering colloidal silicon dioxide (CSD) on the powder properties and vertical compression properties of CRP using the directly pulverized powders of Chenpi (Citri Reticulatae Pericarpium, CRP) as the model drug. Methods Different proportions of CRP engineering composite powders were prepared by co-processing CSD with CPR using liquid dispersion with the external, the internal, and the internal and external addition. The density, flow properties, particle size, porosity, compressibility and compactibility, tensile strength, work and energy were measured and compared, and the physical fingerprints were drawn. Results The improvement degree in the powder and compression properties of engineering CRP particles varied depending on the adding method of CSD. The samples 3, 6—9 showed marked improvement in flowability, uniformity, density, hygroscopicity, tensile strength (TS), specific surface area (SSA), disintegration time (DT), the effective work and energy, which were about 7.01—12.08-fold (TS), 1.63—2.42-fold (SSA) higher than that of CRP, respectively. Meanwhile, the hygroscopicity and DT were reduced by about 30.46% to 42.00% and 250—384 s. Wherein, sample 3 from internal addition method and 9 from internal and external addition method show the most significant improvement. The samples 2, 4 and 5 from external addition method and physical mix method were also improved in the flowability and SSA, however, that cannot be compressed into tablets due to lower bulk and tap density. This may be related to the method of external adding of CSD, the excipients was difficult to effectively bind with traditional Chinese medicine powder. The CSD floated on the surface of the powder, which will play a greater role. For internal/internal and external addition (samples 3, 6, 8, and 9), some CSD were more tightly wrapped on the surface of the main particle, while others enter the interior of the main particle due to the coating effect of the solid bridge and the precipitation of active ingredients. In the process of compression process, the surface distribution of nanoparticle CSD can promote the rearrangement of particles, and provide the particles with a nanoscale rough surface, which transform into a larger binding area during compression, significantly improving the TS of the tableta. Compared with the external addition, it had higher density, better uniformity, and compressibility. Conclusion Co-processing with CRP and CSD via the different addition by liquid dispersion could improve the directly pulverized powders properties of CRP, which provides a feasible choice for improving the tableting properties of some traditional Chinese medicine extract powders.

R283.6

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