苦杏仁提取物乳剂的处方研究

Emulsion formulation optimization of extracts from Armeniacae Semen

中药苦杏仁中含有苦杏仁苷等有效成分,小剂量口服给药之后具有止咳平喘的生物活性。结合乳剂给药剂型在药物递送方面的优势,将苦杏仁提取物制备成稳定的水包油型乳剂,并通过相关处方工艺筛选,得到了分散均一、稳定性良好的制剂。首先通过超声浸提法对苦杏仁中的有效组分进行提取,并将其减压浓缩,得到提取物浸膏;之后,以分散均一性、离心稳定性以及耐寒耐热性的综合评分结果为评价指标,通过正交设计法对油相、乳化剂以及稳定剂的用量进行筛选,确定了苦杏仁提取物乳剂的最优处方。该乳剂以中链油为油相,磷脂为乳化剂,西黄蓍胶为稳定剂,优选处方下,油相、磷脂以及西黄蓍胶的质量比例(m/m)分别为30.0%、1.5%以及1.2%。根据筛选得到的优选处方,制备得到的苦杏仁提取物乳剂稳定性良好,分散均一,为中药提取物的新剂型研究及应用奠定了基础。

Amygdalin is abundant in effective extracts from Armeniacae Semen with bioactivities of relieving cough and asthma through oral administration in lower dose.Combining advantages of emulsion in drug delivery,homogeneous and stable water-in-oil type emulsion was established successfully after relevant formulation optimization.In this study,effective extracts were acquired through ultrasonic extraction firstly.Afterwards,comprehensive scoring of homogeneity,centrifugal stability and cold/heat resistance were set as the evaluation indicators in orthogonal screening.And optimal proportion of oil phase,emulsifier and stabilizer were obtained for the preparation of Armeniacae Semen extracts emulsion.In the optimal formulation,medium-chain triacylglycerol was used as the oil phase and soybean lecithin was chosen as emulsifier with the mass percentage of 30%and 1.5%respectively.Moreover,tragacanth was added as stabilizer with addition amount of 1.2%.Under the optimal formulation,3 batches of Armeniacae Semen extracts emulsion were prepared with favorable stability and homogeneity.This study provides the basis for further application of Armeniacae Semen extracts emulsion.