目的 以陳皮Citri Reticulatae Pericarpium生粉為模型藥物，研究改性劑微粉硅膠的不同加入方式與用量對陳皮生粉的粉體學(xué)性質(zhì)以及直壓性能的影響。方法 采用液相分散法以外加法、內(nèi)加法及內(nèi)外加法將微粉硅膠與陳皮共處理制備陳皮改性復(fù)合粉體，測定并比較各粉體的密度、流動性、粒徑、孔隙率、壓縮成型性等粉體學(xué)性質(zhì)和抗張強(qiáng)度、功與能等相關(guān)壓片性質(zhì)，并繪制物理指紋圖譜。結(jié)果 微粉硅膠的加入方法不同，陳皮改性粒子的粉體學(xué)和壓縮性質(zhì)改善程度不同，與陳皮原料藥相比，內(nèi)加法和內(nèi)外加法所制備的改性粉體（樣品S3、S6～S9）的流動性、均勻度、密度均得到改善，吸濕性降低約30.46%～42.00%，可壓性增強(qiáng)（TS 7.01～12.08倍），比表面積增大（1.63～2.42倍），有效功和能增加，崩解時(shí)間降低，約為250～384 s，直壓性能明顯改善。其中內(nèi)加法（樣品S3）和內(nèi)外加法粉混小比例（樣品S9）的改性粉體改善最顯著。然而，外加法和物理混合法所制備的改性粉體樣品（樣品S2、S4、S5）流動性和比表面積也有所改善，但二者具有較小的堆密度與振實(shí)密度，自身無法壓制成片。這可能是與微粉硅膠的加入方式有關(guān)，因?yàn)槲⒎酃枘z外加（樣品S2、S4、S5），大部分輔料不能有效地與中藥粉體結(jié)合，浮在粉體表面，微粉硅膠自身性質(zhì)發(fā)揮主要作用。而內(nèi)加法/內(nèi)外加法（樣品S3、S6、S8、S9），由于固體橋和析出活性成分的包裹作用，部分微粉硅膠更緊密地包裹在主體粒子表面，部分進(jìn)入主體粒子內(nèi)部。在壓片過程中，表面分布的納米微粉硅膠起到促進(jìn)粒子重排的作用，并且給粒子提供了納米級的粗糙表面，在壓縮過程中轉(zhuǎn)變?yōu)楦蟮慕Y(jié)合面積，從而顯著提高片劑的TS。相較于外加法，其具有較大的密度和較好的均勻性和可壓性。結(jié)論 采用液相分散法將微粉硅膠以內(nèi)加法及內(nèi)外加法與陳皮生粉共處理能顯著改善其生粉的直壓性質(zhì)，可為一些中藥提取物片劑制備性質(zhì)的改善提供一個(gè)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

2024年度高校國內(nèi)訪問學(xué)者“教師專業(yè)發(fā)展項(xiàng)目”（FX2024099）；寧波市公益類科技計(jì)劃項(xiàng)目（2024S181）；江西中醫(yī)藥大學(xué)現(xiàn)代中藥制劑教育部重點(diǎn)實(shí)驗(yàn)室開放基金項(xiàng)目（Zdsys-202302）；2023年度寧波市醫(yī)藥文化研究基地項(xiàng)目（NY202307）；2024年度浙江藥科職業(yè)大學(xué)校級科研項(xiàng)目“經(jīng)典名方烏藥湯揮發(fā)性成分在臨方制劑不同劑型中的量值傳遞研究”（校2025034）