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盐酸多塞平微球对大鼠带状疱疹后神经痛模型的影响。

Effect of Tetrodotoxin Pellets in a Rat Model of Postherpetic Neuralgia.

机构信息

Department of Materials Science and Engineering, College of Materials, Xiamen University, Xiamen 361005, China.

Engineering Research Center of Marine Biological Resource Comprehensive Utilization, Third Institute of Oceanography, State Oceanic Administration, Xiamen 361005, China.

出版信息

Mar Drugs. 2018 Jun 5;16(6):195. doi: 10.3390/md16060195.

DOI:10.3390/md16060195
PMID:29874779
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6025269/
Abstract

Postherpetic neuralgia (PHN) is nerve pain caused by a reactivation of the varicella zoster virus. Medications are used to reduce PHN but their use is limited by serious side effects. Tetrodotoxin (TTX) is a latent neurotoxin that can block neuropathic pain, but its therapeutic index is only 3⁻5 times with intravenous or intramuscular injection. Therefore, we prepared oral TTX pellets and examined their effect in a rat model of PHN induced by resiniferatoxin (RTX). Oral TTX pellets were significantly effective at preventing RTX-induced mechanical and thermal allodynia, and similar to pregabalin. Moreover, oral administration of TTX pellets dose-dependently inhibited RTX-induced PHN compared with intramuscular administration of TTX injection. We also studied the pharmacokinetic profile of TTX pellets. Our results showed that the blood concentration of TTX reached a maximum plasma concentration (C) at around 2 h, with an elimination half-life time (t) of 3.23 ± 1.74 h after intragastric administration. The median lethal dose (LD) of TTX pellets was 517.43 μg/kg via oral administration to rats, while the median effective dose (ED50) was approximately 5.85 μg/kg, and the therapeutic index was 88.45. Altogether, this has indicated that oral TTX pellets greatly enhance safety when compared with TTX injection.

摘要

带状疱疹后神经痛 (PHN) 是由水痘带状疱疹病毒再激活引起的神经痛。药物被用于减轻 PHN，但由于严重的副作用，其应用受到限制。河豚毒素 (TTX) 是一种潜伏的神经毒素，可阻断神经病理性疼痛，但静脉或肌肉注射的治疗指数仅为 3-5 倍。因此，我们制备了口服 TTX 微丸，并在树脂毒素 (RTX) 诱导的 PHN 大鼠模型中研究了其疗效。口服 TTX 微丸在预防 RTX 诱导的机械性和热感觉异常方面非常有效，与普瑞巴林相当。此外，与肌肉注射 TTX 注射液相比，口服 TTX 微丸可剂量依赖性地抑制 RTX 诱导的 PHN。我们还研究了 TTX 微丸的药代动力学特征。结果表明，口服 TTX 微丸后，TTX 的血药浓度在大约 2 小时达到最大血浆浓度 (C)，消除半衰期 (t) 为 3.23±1.74 小时。TTX 微丸经口给予大鼠的半数致死剂量 (LD) 为 517.43μg/kg，半数有效剂量 (ED50) 约为 5.85μg/kg，治疗指数为 88.45。总之，这表明与 TTX 注射液相比，口服 TTX 微丸大大提高了安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/6769803357af/marinedrugs-16-00195-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/a3702562578b/marinedrugs-16-00195-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/359e5247b63e/marinedrugs-16-00195-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/0d9600cb4296/marinedrugs-16-00195-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/0bb9ad175106/marinedrugs-16-00195-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/798850aa5aa0/marinedrugs-16-00195-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/99a409d0164e/marinedrugs-16-00195-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/6769803357af/marinedrugs-16-00195-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/a3702562578b/marinedrugs-16-00195-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/359e5247b63e/marinedrugs-16-00195-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/0d9600cb4296/marinedrugs-16-00195-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/0bb9ad175106/marinedrugs-16-00195-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/798850aa5aa0/marinedrugs-16-00195-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/99a409d0164e/marinedrugs-16-00195-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c537/6025269/6769803357af/marinedrugs-16-00195-g007.jpg

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