目的 篩選和優(yōu)化驅(qū)蟲斑鳩菊乳膏劑的處方。方法 將白凡士林、液體石蠟和單硬脂酸甘油酯（GMS）在 75 ℃水浴中加熱至融化混合均勻作為油相；驅(qū)蟲斑鳩菊有效部位（VAEP）先以聚氧乙烯40氫化蓖麻油（RH40）潤(rùn)濕后再加入水和二乙二醇單乙醚（Transcutol P）作為水相，水相在75 ℃水浴中加熱后以細(xì)流狀加入油相中，邊加邊攪拌，自水浴取出后繼續(xù)攪拌至半固體狀即得乳膏劑。以外觀性狀、涂展性、離心穩(wěn)定性、耐寒耐熱穩(wěn)定性為評(píng)價(jià)指標(biāo)，采用層次分析法（AHP）-基于指標(biāo)相關(guān)性的指標(biāo)權(quán)重確定方法（CRITIC）混合加權(quán)法確定各評(píng)價(jià)指標(biāo)的權(quán)重系數(shù)，結(jié)合D-最優(yōu)混料設(shè)計(jì)優(yōu)化驅(qū)蟲斑鳩菊乳膏的處方。按照最優(yōu)處方制備不同載藥量（1%、2%、4%、8%、16%）的乳膏，進(jìn)行綜合評(píng)分；制備載藥量分別為1%、2%和4%的乳膏，4 ℃放置30 d，以HPLC法對(duì)乳膏中斑鳩菊大苦素和3，5-二咖啡酰奎寧酸的含量變化率進(jìn)行初步考察。結(jié)果 按 AHP-CRITIC 混合加權(quán)法得到外觀性狀、涂展性、耐熱耐寒穩(wěn)定性和離心穩(wěn)定性的權(quán)重系數(shù)分別為 13.18%、16.01%、38.93%、31.89%，結(jié)合D-最優(yōu)混料設(shè)計(jì)確定驅(qū)蟲斑鳩菊乳膏的最優(yōu)處方為液體石蠟10%、凡士林45.48%、GMS 7.83%、RH40 10.31%、Transcutol P 6.65%、水19.73%。驅(qū)蟲斑鳩菊乳膏最大載藥量為4%。乳膏中斑鳩菊大苦素和3，5-二咖啡?？鼘幩岷孔兓试?0 d內(nèi)均＜4.3%。結(jié)論 優(yōu)化后的驅(qū)蟲斑鳩菊乳膏外觀均勻、半透明、細(xì)膩柔軟，易于涂抹，穩(wěn)定性好，制備工藝穩(wěn)定可行。

Objective To screen and optimize the matrix prescription of Vernonia anthelmintica cream. Method Heating white vaseline, liquid paraffin, and glycerol monostearate (GMS) in a 75 ℃ water bath until they are melted and mixed evenly as an oil phase. The effective fraction of V. anthelmintica (VAEP) was first moistened with polyoxyethylene 40 hydrogenated castor oil (RH40), and then added with water and diethylene glycol monoethyl ether (Transcutanol P) as the aqueous phase. The aqueous phase was heated in a water bath at 75 ℃, and then added in a thin stream to the oil phase, stirring while adding. After being taken out of the water bath, continue stirring until it was semi solid to obtain the cream. The weight coefficients of each evaluation index were determined using the Analytic Hierarchy Process (AHP) -Index Weight Determination Method Based on Index Correlation (CRITIC) hybrid weighting method, using the appearance characteristics, spreadability, centrifugal stability, and cold and heat resistance stability as evaluation indicators. The formulation of V. anthelmintica cream was optimized using the D-optimal mixture design. Prepare creams with different drug loads (1%, 2%, 4%, 8%, and 16%) according to the optimal prescription, and conduct comprehensive scoring. The cream with drug loading of 1%, 2%, and 4% was prepared and placed for 30 d at 4 ℃. The content change rate of vernonin and 3, 5-dicaffeoylquinic acid in the cream was preliminarily investigated by HPLC. Results According to AHP- CRITIC mixed weighting method, the weight coefficients of appearance characteristics, spreadability, heat and cold resistance stability, and centrifugal stability were 13.18%, 16.01%, 38.93%, and 31.89%, respectively. Combined with D-optimal mixture design, the optimal formulation of V. anthelmintica cream was determined to be liquid paraffin 10%, vaseline 45.48%, GMS 7.83%, RH40 10.31%, Transitol P 6.65%, and water 19.73%. The maximum drug loading of V. anthelmintica cream was 4%. The change rate of the content of vernonia macrocephalin and 3, 5-dicaffeoylquinic acid in the cream was less than 4.3% within 30 d. Conclusion The preferred V. Anthelmintica cream was uniform,translucent,delicate and soft,and easy to spread,with good stability,and the preparation process was stable and feasible.

R943

中國(guó)科學(xué)院生物資源規(guī)劃項(xiàng)目資助（KFJ-BRP-007-011）