目的 擬制備黃芩苷-Eudragit L100-55腸溶固體分散體，考察黃芩苷腸溶制劑的可行性。方法 采用溶劑蒸發(fā)法制備黃芩苷-Eudragit L100-55 (EL) 腸溶固體分散體，運(yùn)用差示掃描量熱法（DSC）、掃描電鏡法（SEM）、X射線粉末衍射法（XRD）和傅里葉變換紅外光譜（FTIR）等分析方法對(duì)其微觀結(jié)構(gòu)和理化性質(zhì)進(jìn)行了分析，并對(duì)其體外釋放性能進(jìn)行考察。結(jié)果 DSC和XRD分析結(jié)果顯示黃芩苷以無(wú)定形形式分散在固體分散體中，F(xiàn)TIR結(jié)果表明黃芩苷與EL之間存在非共價(jià)鍵作用。體外釋放度測(cè)定結(jié)果表明，黃芩苷-EL比例達(dá)到1∶6時(shí)所制備的固體分散體，黃芩苷在pH 1.2的稀鹽酸溶液中2 h的釋放量小于3%，在pH 6.8的磷酸緩沖液中，2 h累積溶出度達(dá)到90%以上。結(jié)論 所制備的腸溶固體分散體能夠達(dá)到黃芩苷在人工腸液中的快速釋放和增加局部藥物濃度的目的，從而改善黃芩苷的口服吸收。

Objective To prepare the baicalin-Eudragit L100-55 (EL) enteric coated solid dispersion and to investigate the feasibility of this baicalin preparation. Methods Baicalin-EL enteric coated solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD), and infrared vibrational spectra (IR). And its in vitro release was also investigated. Results DSC and XRD analyses suggested that baicalin may be present in enteric coated solid dispersion as amorphous substance. IR results indicated the presence of interactions between baicalin and EL. The in vitro release showed the accumulated dissolution rate of baicalin was less than 3% in artificial pH 1.2 dilute hydrochloric acid solution for 2 h, but an accumulated dissolution rate exceeding 90% in pH 6.8 phosphate buffer solution for 2 h when baicalin-EL ratio reached 1∶6. Conclusion Baicalin-EL enteric coated solid dispersion prepared could release drug rapidly and increase local drug concentration and then improve the oral absorption of baicalin.

國(guó)家“十一五”科技支撐計(jì)劃（2008BAI51B03）；江蘇省社會(huì)發(fā)展科技支撐計(jì)劃（BE2010756）；江蘇省中醫(yī)藥科技項(xiàng)目（LZ11065）