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Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat

by Bihong Hong 1,2,*,†, Jianlin He 1,2,†, Jipeng Sun 1,2, Qingqing Le 1,2, Kaikai Bai 1,2, Yanhua Mou 3, Yiping Zhang 1,2, Weizhu Chen 1,2 and Wenwen Huang 1,2
1
Third Institute of Oceanography, Ministry of Natural Resources, Xiamen 361005, China
2
Technical Innovation Center for Utilization of Marine Biological Resources, Ministry of Natural Resources, Xiamen 361005, China
3
Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2020, 12(1), 32; https://doi.org/10.3390/pharmaceutics12010032
Received: 27 November 2019 / Revised: 26 December 2019 / Accepted: 29 December 2019 / Published: 1 January 2020
Tetrodotoxin (TTX) was identified as a latent neurotoxin that has a significant analgesia effect. It was rapidly absorbed and excreted in rat after intramuscular (i.m.) injection. To maintain the effect, frequent injections were required. The enteric sustained-release TTX pellets with sucrose pellets as a drug carrier was prepared by fluidized bed spray irrigation, coated in sequence with Eudragit NE30D as a sustained-release layer, hydroxypropyl methylcellulose (HPMC) as a barrier layer and Eudragit L30D-55 as an enteric coating. TTX in the pellets could be sustained released for 12 h in dissolution test. In vivo, TTX pellets reached Cmax at 5 h, and t1/2 was 14.52 ± 2.37 h after intragastrically (i.g.) administration in rat. In acetic acid induced writhing test in rat, the pellets at the dosages of 20, 40, 60 and 80 μg·kg−1 produced analgesic effect at about 1.5 h to 9 h and the strongest effect was at about 3 h to 6 h. Simultaneously, the LD50 of the enteric sustained-release TTX pellets was 840.13 μg·kg−1, and the ED50 was about 30 μg·kg−1. Thus, the therapeutic index was about 25. The enteric sustained-release TTX pellets with absolute analgesia effect and greatly enhanced safety was prepared. View Full-Text
Keywords: tetrodotoxin; pharmacokinetic study; sustained-release; enteric pellets; analgesia tetrodotoxin; pharmacokinetic study; sustained-release; enteric pellets; analgesia
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Hong, B.; He, J.; Sun, J.; Le, Q.; Bai, K.; Mou, Y.; Zhang, Y.; Chen, W.; Huang, W. Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat. Pharmaceutics 2020, 12, 32.

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