Zhang Meng-Shan, Luo Yu, Gao Ya-Ting, Li Yi-Ping, Hong Yan-Long, Lin Xiao
School of Pharmacy, Shanghai University of Traditional Chinese Medicine Shanghai 201203, China.
Zhongguo Zhong Yao Za Zhi. 2022 Feb;47(4):931-937. doi: 10.19540/j.cnki.cjcmm.20210422.303.
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.
为解决干姜醇提物成型性差的问题,本研究探讨了采用少量羟丙基甲基纤维素(HPMC)共喷雾干燥对其进行物理改性的可行性。基于单因素分析,采用中心复合设计研究了两个自变量(产品中HPMC含量和喷雾物料固含量)对干燥产品粉体性质和片剂性质的影响。以片剂的抗张强度和崩解时间为评价指标,确定最佳处方如下:HPMC含量为15%,喷雾物料固含量为25.6%。验证了所建立的预测片剂抗张强度和崩解时间的回归模型的准确性,结果表明实测值与预测值接近,偏差分别为0.47%和-8.2%,表明模型具有良好的预测性和重现性。采用最佳处方制备的片剂抗张强度(4.24MPa)是干姜喷雾干燥粉体片剂抗张强度(1.18MPa,远低于合格片剂2MPa的基线)的3.59倍。另一方面,由于添加了HPMC,片剂的崩解时间从7.3分钟增加到24.6分钟。总体而言,本研究为解决中药原料普遍存在的成型性差问题提供了一种新策略,有助于成功制备高载药量的中药片剂。