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Journal of Chinese Pharmaceutical Sciences ›› 2020, Vol. 29 ›› Issue (1): 55-65.DOI: 10.5246/jcps.2020.01.005

• Original articles • Previous Articles     Next Articles

Study on solubility improvement of lidocaine by ternary solid dispersion

Wenling Fan1,2*, Yan Xu1,2, Xinyi Zhang1,2, Liuqing Di1,2, Lei Li3   

  1. 1. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
    2. Institute of Jiangsu Engineering Research Center for Efficient Delivery System of Traditional Chinese Medicine, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
    3. Department of Chemical Engineering, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China
  • Received:2019-09-14 Revised:2019-10-23 Online:2020-01-21 Published:2019-11-15
  • Contact: Tel.: +86-025-85811317, E-mail: fanwl.happy@163.com
  • Supported by:
    National Natural Science Fund of China (Grant No. 30801552 & 81274095), the third key project funded by Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization (Grant No. 012092002006-10), the 55th postdoctoral project (Grant No. 021062001001).

Abstract:

In the present study, we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion (SD) that facilitated solubility and dissolution rate of the poorly water soluble drug and compare with binary SD with single poloxamer. Lidocaine (LIC) was selected as a model drug, and poloxamer 188 (P188) and poloxamer 407 (P407) were utilized as single and mixed carriers. Depending on DSC and the dissolution testing, the appropriate ratio of SD prepared by melting method was optimized. Ternary and binary SD was characterized by DSC, XRD, SEM and FTIR. In vitro dissolution study, phase solubility study and saturated solubility study were performed to clarify solubilization from apparent phenomena and inherent reason. Moreover, stability study under different relative humidity (RH) was investigated. Physical characterizations of binary and ternary SD exhibited the formation of eutectic mixture and the presence of molecular interaction. Compared with the pure LIC, the dissolution rate and solubility of LIC in binary and ternary SDs were enhanced. The phase solubility study revealed an AL-type curve. Furthermore, the stability test indicated that ternary and binary SD was stable. The results of this study demonstrated that SD with mixed poloxamers could improve dissolution rate and solubility of poorly water-soluble drug.

Key words: Solubility, Lidocaine, Poloxamer, Solid dispersion

CLC Number: 

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