HPMC共喷雾干燥改善干姜醇提物压缩成型性的研究

Improvement on compactibility of the alcoholic extract of Zingiberis Rhizoma by co-spray drying with HPMC

针对干姜醇提物压缩成型性较差的问题,探究将其与少量羟丙基甲基纤维素(hydroxypropyl methyl cellulose,HPMC)共喷雾干燥进行物理改性的可行性。在单因素考察的基础上,利用星点设计考察2个自变量(产品中HPMC含量与喷雾物料固含量)对共喷雾干燥产物粉体学性质和片剂性质的影响。以片剂抗张强度和崩解时间作为考察指标,确定最优的处方条件:HPMC质量分数15%,喷雾物料固体质量分数25.6%。对所建抗张强度和崩解时间的回归模型预测的准确性进行验证,结果各实测值与预测值接近(偏差分别为0.47%和-8.2%),表明模型预测良好,优化处方性能具有较好的重复性。优化处方所压片剂的抗张强度为干姜醇提物自喷粉的3.59倍,从远低于合格片剂基准2 MPa的1.18 MPa改善至4.24 MPa;另一方面,由于HPMC的引入,改性片剂崩解时间从原来的7.3 min延长至24.6 min。该研究为解决中药制剂原料压缩成型差的共性问题提供了一种新的解决方案,有助于高载药量中药片剂的成功制备。

Aiming to solve the poor compactibility of the alcoholic extract of Zingiberis Rhizoma(ZR),this study explored the feasibility of its physical modification using co-spray drying with a small amount of hydroxypropyl methyl cellulose(HPMC).Based on the univariate analysis,the influence of two independent variables(the HPMC content in the product and the solid content of spray material)on the powder properties and tablet properties of the dried product was investigated by the central composite design.With the tensile strength and disintegration time of the tablets as the evaluation indexes,the optimal prescription was determined as follows:the HPMC content was 15%and the solid content of spray material was 25.6%.The accuracy of the regression model established for predicting tensile strength and disintegration time of tablets was verified,and the results revealed that the measured values were close to the predicted ones with deviations of 0.47%and-8.2%,indicating good prediction and reproducibility of the model.The tensile strength(4.24 MPa)of tablets prepared with the optimal prescription was 3.59 times that(1.18 MPa,far lower than the baseline of 2 MPa for qualified tablets)with the spray-dried powder of the ZR.On the other hand,due to the addition of HPMC,the disintegration time of tablets increased from 7.3 min to 24.6 min.On the whole,this study provided a new strategy to solve the common problem of poor compactibility of raw Chinese medicinal materials,which facilitated the successful preparation of Chinese medicinal tablets with high drug loads.