Synthesis of a novel pharmaceutical excipient: An anion exchange resin

doi:10.5246/jcps.2025.02.009

Journal of Chinese Pharmaceutical Sciences ›› 2025, Vol. 34 ›› Issue (2): 109-125.DOI: 10.5246/jcps.2025.02.009

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Synthesis of a novel pharmaceutical excipient: An anion exchange resin

Zhannuan Yin¹^,⁴, Xianghuan Meng², Yingshu Feng³, Ke Li⁴, Xinyi Tang⁴, Hongfei Liu¹^,²^,⁴^,^*(), Haibing He⁴^,⁵^,^*(), Wei Mi⁶^,^*

¹ Anhui University of Chinese Medicine, Hefei 230000, Anhui, China
² College of Pharmacy, Jiangsu University, Zhenjiang 212013, Jiangsu, China
³ Zhenjiang Key Laboratory of Functional Chemistry, Institute of Medicine & Chemical Engineering, Zhenjiang College, Zhenjiang 212028, Jiangsu, China
⁴ Jiangsu Haizhihong Biopharmaceutical Co., Ltd., Nantong 226100, Jiangsu, China
⁵ Department of Pharmaceutics, Shen yang Pharmaceutical University, Shenyang 110016, Liaoning, China
⁶ Jiangxi Alpha Hi-tech Pharmaceutical Co., Ltd., Pingxiang, 337000, Jiangxi, China

Received:2024-10-13 Revised:2024-11-12 Accepted:2024-12-23 Online:2025-03-01 Published:2025-03-02
Contact: Hongfei Liu, Haibing He, Wei Mi
Supported by:
2023 Nantong Jianghai Talents Project, the Nantong Social Livelihood Science and Technology Plan for 2023, and the 2022 New Drugs and Platform Enhancement Project of the Yangtze Delta Drug Advanced Research Institute. Additionally, support was provided by the Zhenjiang Science and Technology Project (Grant No. SH2020048), the China Postdoctoral Science Foundation (Grant No. 2020M681532), the Jiangsu Planned Projects for Postdoctoral Research Funds (Grant No. 2020Z209), and the Natural Science Research Projects of Universities in Jiangsu Province (Grant No. 20KJD350001).

Abstract

Abstract:

The aim of this study was to develop a novel pharmaceutical excipient: an anion exchange resin. Initially, polystyrene-divinylbenzene (PS-DVB) microspheres were synthesized via suspension polymerization. Subsequently, these microspheres served as a substrate for chloromethylation using methanol, formaldehyde, and chlorosulfonic acid. By optimizing the reaction conditions, the chloromethylated microspheres were characterized using infrared spectroscopy, scanning electron microscopy, and the Mohr method. Under optimal reaction conditions, the resulting products exhibited uniformity and spherical morphology, with an average particle size of approximately 190 µm. The PS-DVB microspheres effectively incorporated chloromethyl groups, as evidenced by a chlorine content of 14.67%. Scanning electron microscopy analysis indicated that the appearance of the microspheres remained largely unchanged post-reaction. Overall, the research findings demonstrated the successful preparation of the anion exchange resin. Characterization and quality assessment confirmed that the ion exchange resin met the required standards.

Key words: Suspension polymerization reaction, Polystyrene-divinylbenzene, Quaternarization reaction, Anion exchange resin, Fluidized bed coating method, Pharmacokinetic research

Supporting:

Zhannuan Yin, Xianghuan Meng, Yingshu Feng, Ke Li, Xinyi Tang, Hongfei Liu, Haibing He, Wei Mi. Synthesis of a novel pharmaceutical excipient: An anion exchange resin[J]. Journal of Chinese Pharmaceutical Sciences, 2025, 34(2): 109-125.

Figures/Tables 29

Table 1. Factors for the synthesis of PS-DVB microspheres.

Table 2. Saturated swelling degree and apparent density of PS-DVB.

Table 3. Effect of different catalysts on chlorine content.

Table 4. Saturated swelling degree and apparent density of PS-DVB-Cl.

Table 5. Saturated swelling degree and apparent density of anion exchange resin.

Table 6. Loss on drying of imported resin and self-made resin.

Table 7. Residue of ignition of imported resin and self-made resin.

References 31

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Synthesis of a novel pharmaceutical excipient: An anion exchange resin

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