[關鍵詞]
[摘要]
目的 采用表面改性技術優(yōu)化黃芩(Scutellariae Radix,SR)、黃連(Coptidis Rhizoma,CR)浸膏粉的綜合性能,優(yōu)選最佳改性劑及改性工藝,為后續(xù)制劑開發(fā)提供依據(jù)。方法 制備黃芩、黃連浸膏粉及流浸膏,選擇二氧化硅(silicon dioxide,S)、微粉硅膠(micronized silica gel,M)、羥丙基甲基纖維素(hydroxypropyl methylcellulose,H)3種改性劑,采用表面包覆(surface cladding,SC)和微囊化包衣(microencapsulation coating,MC)2種改性技術分別制備改性浸膏粉。測定各浸膏粉的吸濕率(H)、含水量(HR)、休止角(α)、松密度(Da)、振實密度(Dc)、豪斯納比(IH)、卡爾指數(shù)(IC)、間隙率(Ie)、中值徑(D50)、粒徑分布寬度(span)、粒徑范圍(width)及比表面積(SSA)總計12個二級指標,進行歸一化處理,繪制物理指紋圖譜并進行相似度分析。將二級指標轉換成均一性、堆積性、流動性、可壓性和穩(wěn)定性共5個一級指標,采用熵權-變異系數(shù)法獲得權重系數(shù),并計算各浸膏粉綜合性能評分。選用主成分分析法(principal component analysis,PCA)評價各二級指標對浸膏粉綜合性能的貢獻率,針對影響浸膏粉均一性最為顯著的D50進行偏最小二乘法(partial least squares,PLS)分析,明確各二級指標與其相關性。結果 SC和MC改性技術,制備獲得SR、CR浸膏粉及6種改性浸膏粉,各浸膏粉二級指標歸一化處理,繪制物理指紋圖譜。相似度研究得出:黃芩SR與SC改性組SR-SC-S、SR-SC-M、SR-SC-H的相似度分別為0.977、0.971、0.978;SR與囊化包衣改性組SR-MC-S、SR-MC-M、SR-MC-H的相似度分別為0.717、0.739和0.693。黃連CR與SC改性組CR-SC-S、CR-SC-M、CR-SC-H的相似度分別為0.904、0.902和0.955,CR與囊化包衣改性組CR-MC-S、CR-MC-M、CR-MC-H浸膏粉的相似度分別為0.729、0.737和0.716。MC改性的SR、CR與未改性浸膏粉相比具有顯著性差異,羥丙甲基纖維素改性劑差異最顯著,SC改性工藝改性組效果不明顯,無顯著性差異。熵權變異系數(shù)法計算得出,黃芩耦合權重系數(shù)wjSR:穩(wěn)定性(0.121 0)、均一性(0.484 0)、流動性(0.186 7)、堆積性(0.099 0)、可壓性(0.109 3);黃連耦合權重系數(shù)wjCR:穩(wěn)定性(0.013 4)、均一性(0.394 1)、流動性(0.173 1)、堆積性(0.288 5)、可壓性(0.130 9)。浸膏粉性能綜合性能評分結果顯示,黃芩SR浸膏粉綜合性能評分49.13,MC改性SR-MC-H、SR-MC-M、SR-MC-S綜合性能評分分別為62.90、61.78、61.64,相比具顯著差異,SR-MC-H綜合性能評分較浸膏粉提高了28.0%,改性最佳,SC改性效果略差。黃連CR浸膏粉綜合性能評分為50.21,MC改性綜合性能評分均大于61.00,與浸膏粉相比差異具有顯著性,CR-MC-H綜合性能評分61.68,較未改性組提高了22.8%,效果最佳,SC改性,二氧化硅及微粉硅膠組浸膏粉綜合性能評分分別為56.35、56.25,也有顯著性差異。PCA結果表明α、SSA、HR、width、span這5個二級指標對SR、CR浸膏粉綜合性能貢獻率較大。針對D50進行PLS分析,得出width、span、H及Dc等指標對浸膏粉D50影響較為顯著。結論 表面改性技術可提高黃芩、黃連浸膏粉的綜合性能,MC改性工藝改性效果較好,羥丙基甲基纖維素作為改性劑綜合性能評分最高。
[Key word]
[Abstract]
Objective Surface modification technology was used to optimize the comprehensive properties of Scutellariae Radix (SR) and Coptidis Rhizoma (CR) extract powders. The study aimed to select the best modifier and process, providing a foundation for the development of subsequent formulations. Methods SR and CR extract powders and crude extracts were prepared. Three modifiers , silicon dioxide (S), micronized silica gel (M) and hydroxypropyl methylcellulose (H), were selected, and the modified technology of surface cladding (SC) and microencapsulation coating (MC) was used to prepare modified extract powder. Powders were measured secondary indexes, including H, HR, α, Da, Dc, IH, IC, Ie, D50, span, width and SSA. All secondary indexes were normalized and a physical fingerprint diagram was drawn and similarity analysis was conducted. The secondary indexes were converted into five primary indexes of uniformity, accumulability, flowability,compressibility and stability, and the weight coefficients were obtained by using the entropy weighted coefficient of variation method. The comprehensive performance scores of the extract powders were calculated. PCA was used to evaluate the contribution rate of each secondary index to the comprehensive performance of the extract powders, and PLS was used to analyze the correlation between each secondary index and the comprehensive performance of the extract powders, focusing on the D50 that the greatest impact on the homogeneity of the extract powders. Results Using SC and MC modification techniques, SR, CR, and six modified extract powders were prepared. The secondary indexes of each extract powder were normalized, and physical fingerprint profiles were created. The similarity analysis results were as follows: The similarity between SR and SC modified groups SR-SC-S, SR-SC-M, and SR-SC-H was 0.977, 0.971, and 0.978, respectively. The similarity between SR and MC modified groups SR-MC-S, SR-MC-M, and SR-MC-H was 0.717, 0.739, and 0.693, respectively. The similarity between CR and SC modified groups CR-SC-S, CR-SC-M, and CR-SC-H was 0.904, 0.902, and 0.955, respectively. The similarity between CR and MC modified groups CR-MC-S, CR-MC-M, and CR-MC-H was 0.729, 0.737, and 0.716, respectively. Significant differences were observed between the MC modified SR and CR powders compared to the unmodified extract powders, with hydroxypropyl methylcellulose showing the most significant difference. The SC modification showed no significant effect. The entropy weight coefficient of variation method yielded the following coupling weight coefficients wjSR: stability (0.121 0), uniformity (0.484 0), flowability (0.186 7), accumulability (0.099 0), and compressibility (0.109 3); wjCR: stability (0.013 4), uniformity (0.394 1), flowability (0.173 1), accumulability (0.288 5), and compressibility (0.130 9). The results of comprehensive performance scores of the extract powders showed the comprehensive performance score of SR extract powder was 49.13. The MC modified SR-MC-H, SR-MC-M, and SR-MC-S had comprehensive performance scores of 62.90, 61.78, and 61.64, respectively, showing significant differences compared to the unmodified powder. The SR-MC-H comprehensive performance score improved by 28.0% over the unmodified extract powder, indicating the best modification effect, while the effect of SC modification was slightly worse. The comprehensive performance score of CR extract powder was 50.21. The MC modified powders had comprehensive performance scores above 61.00, showing significant differences compared to the unmodified powder. The CR-MC-H had a comprehensive performance score of 61.68, an improvement of 22.8% over the unmodified group, indicating the best effect. The SC modification with silicon dioxide and micronized silica gel resulted in comprehensive performance scores of 56.35 and 56.25, respectively, also showing significant differences. PCA analysis indicated that five secondary indexes α, SSA, HR, width, and span had a large contribution to the overall performance of SR and CR extract powders. PLS analysis of D50 revealed that width, span, H, and Dc had significant effects on the D50 of the extract powders. Conclusion Surface modification technology can improve the comprehensive properties of SR and CR extract powders. The MC modification technology showed the best results, with hydroxypropyl methylcellulose achieving the highest comprehensive performance score as a modifier.
[中圖分類號]
R283.6
[基金項目]
江蘇省“青藍工程”優(yōu)秀教學團隊資助項目(2024年);泰州市科技支撐計劃(社會發(fā)展)項目(TS202425,SSF20230030);泰州職業(yè)技術學院科研課題(TZYKY-21-5);江蘇省大學生創(chuàng)新創(chuàng)業(yè)訓練計劃項目(202413981004Y)