Effect of external mechanical forces on the crystallographic solid form and dissolution rate of traditional Chinese medicine extracts——taking <i>Ligustrum lucidum</i> extract as an example

LIANG Linlin; WANG Zhiwei; HE Xiaoshuang; HENG Weili; QIAN Shuai; GAO Yuan; ZHANG Jianjun; WEI Yuanfeng

doi:10.11665/j.issn.1000-5048.2023122902

Journal of China Pharmaceutical University > 2024 > 55(6): 767-774. > DOI: 10.11665/j.issn.1000-5048.2023122902

LIANG Linlin, WANG Zhiwei, HE Xiaoshuang, et al. Effect of external mechanical forces on the crystallographic solid form and dissolution rate of traditional Chinese medicine extracts——taking Ligustrum lucidum extract as an example[J]. J China Pharm Univ, 2024, 55(6): 767 − 774. DOI: 10.11665/j.issn.1000-5048.2023122902

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Effect of external mechanical forces on the crystallographic solid form and dissolution rate of traditional Chinese medicine extracts——taking Ligustrum lucidum extract as an example

1.
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198
2.
Zhejiang Cheng Yi Pharmaceutical Co., Ltd., Wenzhou 325700
3.
School of Pharmacy, Nanjing Tech University, Nanjing 211816
4.
School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China

Funds: This study was supported by the National Natural Science Foundation of China (No.82104401, No.82274217, No.82204636, No.82373824)

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Received Date: December 28, 2023

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Abstract

Abstract

Taking the Ligustrum lucidum extract as an example, this study investigated the influence of external mechanical forces under different processing conditions on the crystallographic solid form and the key parameter of drug dissolution rate, so as to provide guidance for the preparation and quality control of traditional Chinese medicine preparations. Under different pulverization and tableting conditions, the change of crystallographic solid form of L. lucidum extract was observed by polarizing light microscope. Meanwhile, the effect of this change on the dissolution rate was investigated, and the mathematical relationship between crystal content and dissolution rate was analyzed. The results showed that the process of ball milling and tableting had a significant impact on the crystallographic solid form of L. lucidum extract. The amorphous extract displayed crystal transformation, which induced a significant decline in dissolution rate. Further studies revealed that there was a negative linear relationship between crystal content and dissolution rate. The results of this study indicated that the crystallographic solid form transformation of traditional Chinese medicine extracts might occur during the preparation process, which may cause potential risks to the quality of traditional Chinese medicine preparations. It is suggested that we should pay attention to and strengthen the investigation of the crystallographic solid form during the preparation process, so as to guarantee the safety, effectiveness, and quality controllability of traditional Chinese medicine preparations.

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[1]	Zhou YN, Wang JK, Xiao Y, et al. The effects of polymorphism on physicochemical properties and pharmacodynamics of solid drugs[J]. Curr Pharm Des, 2018, 24(21): 2375-2382. doi: 10.2174/1381612824666180515155425
[2]	Zier KI, Schultze W, Leopold CS. Factors influencing the properties and the stability of spray-dried Sennae fructus extracts[J]. Drug Dev Ind Pharm, 2018, 44(10): 1659-1667. doi: 10.1080/03639045.2018.1483397
[3]	Wang B, Liu FL, Xiang J, et al. A critical review of spray-dried amorphous pharmaceuticals: synthesis, analysis and application[J]. Int J Pharm, 2021, 594: 120165. doi: 10.1016/j.ijpharm.2020.120165
[4]	Laitinen R, Löbmann K, Strachan CJ, et al. Emerging trends in the stabilization of amorphous drugs[J]. Int J Pharm, 2013, 453(1): 65-79. doi: 10.1016/j.ijpharm.2012.04.066
[5]	Dong LP, Wang B, Chen L, et al. Solubilization and in vitro physical and chemical properties of the amorphous spray-dried lactose-luteolin system[J]. J Nanomater, 2022, 2022: 2137188. doi: 10.1155/2022/2137188
[6]	Wang BY, Wang XL, Zhu YJ, et al. Characterization of nimodipine amorphous nanopowder prepared by quenching cooling combined with wet milling and spray drying[J]. Int J Pharm, 2022, 628: 122332. doi: 10.1016/j.ijpharm.2022.122332
[7]	Fael H, Demirel AL. Indomethacin co-amorphous drug-drug systems with improved solubility, supersaturation, dissolution rate and physical stability[J]. Int J Pharm, 2021, 600: 120448. doi: 10.1016/j.ijpharm.2021.120448
[8]	Sadeghi F, Torab M, Khattab M, et al. Improvement of physico-mechanical properties of partially amorphous acetaminophen developed from hydroalcoholic solution using spray drying technique[J]. Iran J Basic Med Sci, 2013, 16(10): 1100-1108.
[9]	Xiong ZW, Yang B, Zhao YX, et al. A new direct compression mechanism of structural transition in Poria cocos extract composite particles[J]. Int J Pharm, 2022, 623: 121913. doi: 10.1016/j.ijpharm.2022.121913
[10]	Almotairy A, Almutairi M, Althobaiti A, et al. Investigation of hot melt extrusion process parameters on solubility and tabletability of atorvastatin calcium in presence of Neusilin^® US₂[J]. J Drug Deliv Sci Technol, 2023, 79: 104075. doi: 10.1016/j.jddst.2022.104075
[11]	Zhao YL, Liang LL, He XS, et al. 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]. J China Pharm Univ (中国药科大学学报), 2023, 54(1): 68-76.
[12]	Morris KR, Griesser UJ, Eckhardt CJ, et al. Theoretical approaches to physical transformations of active pharmaceutical ingredients during manufacturing processes[J]. Adv Drug Deliv Rev, 2001, 48(1): 91-114. doi: 10.1016/S0169-409X(01)00100-4
[13]	Liu MH, Zou ZR. Research progress on chemical constituents, pharmacological effects and pharmacokinetics of Ligustri lucidi fructus[J]. J Trop Subtrop Bot(热带亚热带植物学报), 2022, 30: 446-460.
[14]	Zhu KN, Wu ZF, Jiang CH, et al. Advances on hypoglycemic activity and mechanism of triterpenoids[J]. J China Pharm Univ (中国药科大学学报), 2015, 46(6): 764-770.
[15]	Xu HR, Cheng GL, Huang ZW, et al. Research progress on medicinal value of Ligustrum lucidum and related marketed drugs[J]. Chin Tradit Herb Drugs(中草药), 2023, 54: 1663-1671.
[16]	Hu L, Li RL, Wang XB, et al. Determination of oleanolic acid in Achyranthes aspera L. with different plant origins by HPLC[J]. J Pharm Res(药学研究), 2021, 40: 726-729.
[17]	Liang H, Ni ZC, Yan MQ, et al. Preparation technology and physico-chemical characteristics of Olibanum ultramicro powders[J]. Chin Tradit Herb Drugs (中草药), 2017, 48(7): 1321-1326.
[18]	Shah B, Kakumanu VK, Bansal AK. Analytical techniques for quantification of amorphous/crystalline phases in pharmaceutical solids[J]. J Pharm Sci, 2006, 95(8): 1641-1665. doi: 10.1002/jps.20644
[19]	Chieng N, Rades T, Aaltonen J. An overview of recent studies on the analysis of pharmaceutical polymorphs[J]. J Pharm Biomed Anal, 2011, 55(4): 618-644. doi: 10.1016/j.jpba.2010.12.020
[20]	Venter C, Niesler CU. Rapid quantification of cellular proliferation and migration using ImageJ[J]. Biotechniques, 2019, 66(2): 99-102. doi: 10.2144/btn-2018-0132
[21]	Avdeef A, Tsinman O. Miniaturized rotating disk intrinsic dissolution rate measurement: effects of buffer capacity in comparisons to traditional wood’s apparatus[J]. Pharm Res, 2008, 25(11): 2613-2627. doi: 10.1007/s11095-008-9679-z
[22]	Park H, Jung C, Yi S, et al. Elucidating the ball-milling-induced crystallization mechanism of amorphous NbCo_1.1Sn via atomic-scale compositional analysis[J]. J Alloys Compd, 2023, 968: 172014. doi: 10.1016/j.jallcom.2023.172014
[23]	Park H, Kim JS, Hong S, et al. Tableting process-induced solid-state polymorphic transition[J]. J Pharm Investig, 2022, 52(2): 175-194. doi: 10.1007/s40005-021-00556-6
[24]	Krishna Kumar NS, Suryanarayanan R. Crystallization propensity of amorphous pharmaceuticals: kinetics and thermodynamics[J]. Mol Pharm, 2022, 19(2): 472-483. doi: 10.1021/acs.molpharmaceut.1c00839
[25]	Bagwan NUS, Sheokand S, Kaur A, et al. Role of surface molecular environment and amorphous content in moisture sorption behavior of milled terbutaline sulphate[J]. Eur J Pharm Sci, 2021, 161: 105782. doi: 10.1016/j.ejps.2021.105782
[26]	Ke WR, Kwok PCL, Khanal D, et al. Co-spray dried hydrophobic drug formulations with crystalline lactose for inhalation aerosol delivery[J]. Int J Pharm, 2021, 602: 120608. doi: 10.1016/j.ijpharm.2021.120608
[27]	Martínez LM, Cruz-Angeles J, Vázquez-Dávila M, et al. Mechanical activation by ball milling as a strategy to prepare highly soluble pharmaceutical formulations in the form of co-amorphous, co-crystals, or polymorphs[J]. Pharmaceutics, 2022, 14(10): 2003. doi: 10.3390/pharmaceutics14102003
[28]	Barnard T, Sosso GC. Combining machine learning and molecular simulations to predict the stability of amorphous drugs[J]. J Chem Phys, 2023, 159(1): 014503. doi: 10.1063/5.0156222

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Effect of external mechanical forces on the crystallographic solid form and dissolution rate of traditional Chinese medicine extracts——taking Ligustrum lucidum extract as an example

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