China Animal Husbandry and Veterinary Medicine ›› 2024, Vol. 51 ›› Issue (1): 417-426.doi: 10.16431/j.cnki.1671-7236.2024.01.042

• Basic Veterinary Medicine • Previous Articles     Next Articles

Preparation and Pharmacodynamic Evaluation of Rifaximin Transdermal Preparation

ZHANG Jianxu1, WANG Yufei1,2, XU Shiyao3, ZHANG Jiabin1,2, HUO Yurou1,4, ZHAO Qi1,4, LI Bo1,2, YANG Yujie1,4, WANG Kai1, LI Qianxue1   

  1. 1. Changchun Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Changchun 130122, China;
    2. College of Veterinary Medicine, Jilin Agricultural University, Changchun 130118, China;
    3. College of Life Science, Tonghua Normal University, Tonghua 134002, China;
    4. College of Life Science and Technology, Changchun University of Science and Technology, Changchun 130022, China
  • Received:2023-06-29 Online:2024-01-05 Published:2023-12-27

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Abstract: 【Objective】 The aim of this study was to develop a transdermal formulation of rifaximin with convenient administration and good skin penetration for the treatment of intestinal diseases in livestock and poultry, and preliminarily evaluate its formulation and efficacy.【Method】 The concentration of rifaximin was detected by ultraviolet spectrophotometer.The orthogonal design method was used in the transdermal preparation test.The in vitro transdermal ability of the preparation was investigated by isolated pig skin, and the prescription components were screened by the cumulative permeation amount (Q) per unit area of 12 h.The storage stability test was carried out at 40 and 60 ℃.A mouse model of Salmonella Typhimurium infection was established, and the prepared transdermal or gavage preparation were used to treat the infection model and evaluate the therapeutic effect by comparing the survival rate, organ bacterial load and histopathological changes.【Result】 Rifaximin transdermal preparation was as follows:The system contained rifaximin 2%, azone 4%, menthol 2%, acetone glycerol 20%, dimethyl sulfoxide 30%, and anhydrous ethanol to 100%.The average cumulative permeation amount per unit area of the formulation for 12 h was 132.82 μg/cm2.After placing the preparation at 60 and 40 ℃ for 10 d, the drug content was kept at 89.78% and 93.53% of the initial value respectively, which indicated its good stability.Compared with infection without treatment group, the organ bacterial load in each organ of transdermal group and gavage group were significantly reduced (P<0.05).After 3 d of administration, the survival rate of rifaximin transdermal treatment group (91.67%) was higher than that of gavage treatment group (83.33%).The pathological changes of cecum were obvious before and after treatment.Compared with infection without treatment group, the edema of the intestinal submucosa, the infiltration of inflammatory cells in the submucosa, intestinal crypts and intestinal epithelium were reduced, the number of goblet cells in the intestinal villi was increased, the integrity of the intestinal epithelium was significantly restored, and the lesions were alleviated in the two treatment groups.【Conclusion】 The transdermal preparation of rifaximin had the advantages of simple preparation process, good stability and better therapeutic effect through skin.

Key words: rifaximin; transdermal preparation; pharmacodynamic evaluation

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