Optimization of the forming process and establishment of a physical fingerprint for Kaixin granules
- VernacularTitle:开心颗粒成型工艺优化及其物理指纹图谱构建
- Author:
Zuomin WU
1
;
Yunzhi WANG
1
;
Meng NING
1
;
Shuxian BAI
1
;
Huifen MA
2
;
Zhishen XIE
2
;
Zhenqiang ZHANG
2
;
Xiaotao YU
1
;
Jingyuan DONG
1
Author Information
1. Dept. of Pharmacy，Luohe Central Hospital，Henan Luohe 462000，China
2. Academy of Chinese Medical Sciences，Henan University of Chinese Medicine，Zhengzhou 450046，China
- Publication Type:Journal Article
- Keywords:
Kaixin granules;
forming process;
physical fingerprint;
Plackett-burman design;
Box-Behnken response surface methodology;
analytic hierarchy process-entropy weight method
- From:
China Pharmacy
2026;37(20):2673-2678
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To optimize the forming process of Kaixin granules and establish its physical fingerprint.METHODS Using particle forming rate， hygroscopicity rate， dissolution rate， and angle of repose as indices， the key process parameters of the granule forming process were determined by Plackett-Burman design. The analytic hierarchy process （AHP） combined with the entropy weight method was used to comprehensively weight the indices， and the forming process of Kaixin granules was optimized and validated by Box-Behnken response surface methodology. A physical fingerprint of Kaixin granules was established based on the following physical indices： angle of repose， Hausner ratio， bulk density， tapped density， moisture content， hygroscopicity ratio， and relative uniformity index， with similarity evaluation was performed. Cluster analysis and partial least squares discriminant analysis （PLS-DA） were performed using SPSS 20.0 and the SPSSPRO online analysis platform， respectively.RESULTS The key process parameters were ethanol volume fraction， ethanol amount， and the drug-excipient ratio. The optimal forming conditions were as follows： ethanol volume fraction of 87%， ethanol amount of 27%， and a drug-excipient ratio of 1∶1. Validation showed that the average comprehensive scores of three batches were 97.82， with an RSD of 0.19%. The similarity of the physical fingerprints of ten batches of Kaixin granules prepared under the optimal forming process were greater than 0.98. The results of cluster analysis showed that the ten batches were divided into two groups： S4， S5， S7， S8 and S10 in one cluster， and S1-S3， S6 and S9 in another. The variable importance in projection values of Hausner ratio， relative uniformity index， bulk density， and moisture content were greater than 1.CONCLUSIONS The optimized forming process is stable and feasible. The established physical fingerprint can effectively characterize the overall physical properties of Kaixin granules. Hausner ratio， relative uniformity index， bulk density， and moisture content are the key physical indices.
