Crystallization transformation of amorphous extracts of traditional Chinese medicine and its effect on dissolution behavior — Taking total flavonoids from<i> Pueraria lobata</i> as an example

ZHAO Yili; LIANG Linlin; HE Xiaoshuang; HENG Weili; PANG Zunting; QIAN Shuai; GAO Yuan; ZHANG Jianjun; WEI Yuanfeng

doi:10.11665/j.issn.1000-5048.20221124002

Journal of China Pharmaceutical University > 2023 > 54(1): 68-76. > DOI: 10.11665/j.issn.1000-5048.20221124002

ZHAO Yili, LIANG Linlin, HE Xiaoshuang, HENG Weili, PANG Zunting, QIAN Shuai, GAO Yuan, ZHANG Jianjun, WEI Yuanfeng. Crystallization transformation of amorphous extracts of traditional Chinese medicine and its effect on dissolution behavior — Taking total flavonoids from Pueraria lobata as an example[J]. Journal of China Pharmaceutical University, 2023, 54(1): 68-76. DOI: 10.11665/j.issn.1000-5048.20221124002

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Crystallization transformation of amorphous extracts of traditional Chinese medicine and its effect on dissolution behavior — Taking total flavonoids from Pueraria lobata as an example

1.
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198
2.
School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China

Funds: This study was supported by the National Natural Science Foundation of China (No. 81873012, No.82074029, No.82104401, No.82274217, No.82204636), China Postdoctoral Science Foundation (No.2021M693517), Key project of the Fundamental Research Funds for the Central Universities (No.2632021ZD15), and Postdoctoral Research Grant of Jiangsu Province

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Received Date: November 23, 2022
Revised Date: February 12, 2023

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Abstract

In order to guarantee the quality of traditional Chinese medicines (TCMs), the crystallization transformation of complex extracts of TCMs and the influence of solid form on their physicochemical properties were studied.The extract of total flavonoids from Pueraria lobata was taken as a model.Crystallization transformation happened when lofting under different conditions, and the intrinsic dissolution tests were carried out.It was found that humidity was the key factor to induce crystallization of total flavonoids from Pueraria lobata.The greater the wettability was, the more the crystallization was.The dissolution rate of total flavonoids from Pueraria lobata with the most crystallization amount significantly decreased by 96.51% compared to the sample without crystallization.After further simulating the preparation process of total flavonoids from Pueraria lobata, it was found that the wet granulation process with introduced water would also lead to crystallization and reduced dissolution rate.As for all crystallization samples, there was an inversely proportional relationship between the dissolution rates and the amount of crystallization.The risk of crystallization existed both in the storage and preparation process of TCM extracts.Crystallization would significantly affect the dissolution rate, and thus the quality of TCM products.In this study, the crystallization transformation of amorphous complex TCM extracts was discovered, and the effect of the crystallization transformation on its dissolution behavior was systematically studied, which provides a new research idea for assuring the quality of TCM products and promoting the improvement of TCM preparation level.
- TCM extracts,
- amorphous state,
- crystallization transformation,
- total flavonoids from pueraria lobata,
- dissolution rate

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Crystallization transformation of amorphous extracts of traditional Chinese medicine and its effect on dissolution behavior — Taking total flavonoids from Pueraria lobata as an example

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