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LU Yan, CONG Feng, QIAN Shuai, WEI Yuanfeng, ZHANG Jianjun, LIN Yining, GAO Yuan. Enhanced dissolution and eliminated gelation of lenvatinib mesylate by coamorphous system[J]. Journal of China Pharmaceutical University, 2021, 52(1): 44-51. DOI: 10.11665/j.issn.1000-5048.20210106
Citation: LU Yan, CONG Feng, QIAN Shuai, WEI Yuanfeng, ZHANG Jianjun, LIN Yining, GAO Yuan. Enhanced dissolution and eliminated gelation of lenvatinib mesylate by coamorphous system[J]. Journal of China Pharmaceutical University, 2021, 52(1): 44-51. DOI: 10.11665/j.issn.1000-5048.20210106
shu

Enhanced dissolution and eliminated gelation of lenvatinib mesylate by coamorphous system

  • 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.81703712, No.81773675, No.81873012) and the Double First-Class Project of China Pharmaceutical University (No.CPU2018GY11, No.CPU2018GY27)
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  • Received Date: August 09, 2020
  • Revised Date: December 07, 2020
    Graphical Abstract
    • Abstract
  • Lenvatinib mesylate (LF), a multi-target tyrosinase inhibitor mainly used in the treatment of a variety of cancers, has low oral bioavailability mainly due to its gelation during the dissolution process. In the current study, in order to enhance dissolution and eliminate gelation of LF, a supramolecular coamorphous system of LF-baicalein (BAI) (molar ratio, 1∶1) was prepared by rotary evaporation and characterized by PLM, PXRD, DSC and FTIR. Results indicated the formation of coamorphous system with a single Tg of 118 °C. Different from original LF crystal, no gelation phenomenon was observed during the dissolution of coamorphous LF-BAI. In addition, the dissolution rate of LF was increased by 2.2-fold after coamorphization. Meanwhile, the dissolution rate of the co-former BAI was also enhanced by more than 25.4-fold. Stability test showed that the prepared coamorphous system had a good physical stability for at least 90 days under 25 °C/ 60%RH and 40 °C /75%RH conditions.
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    • References (21)
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