Division of Pharmaceutical Technology, Defence Research Laboratory, Tezpur 784 001, Assam, India; Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, 835 215 Ranchi, Jharkhand, India.
Division of Pharmaceutical Technology, Defence Research Laboratory, Tezpur 784 001, Assam, India.
Eur J Pharm Sci. 2014 Jun 2;56:28-36. doi: 10.1016/j.ejps.2014.01.013. Epub 2014 Feb 14.
The prophylactic and neuroprotective impact of a transdermal patch containing eserine and pralidoxime chloride (2-PAM) against (±)-Anatoxin A poisoning was investigated using Wistar strain albino rats. Rats were smooth-shaved on the dorsal side, attached with a drug-in-adhesive matrix type prophylactic transdermal patch for 72 h and challenged with subcutaneous injection of three doses (1.0, 1.5 and 2.0×LD50) of (±)-Anatoxin A. The LD50 value of (±)-Anatoxin A was determined to be 1.25mg/kg, and at this particular dose (1.0×LD50) of toxin induced severe clinical symptom including extreme seizures in rats, resulting acute brain injuries in discrete brain regions, leading to 100% mortality within 5 min. The anticonvulsant effect, antiarrythmic effect, nerve conduction study, clinical observations and mortality, neuroprotective effect as well as skin histopathology of the prophylactic transdermal patch against (±)-Anatoxin A poisoning were investigated systematically. It was found that seizures, tachycardia, nerve damage, clinical symptoms, brain injuries and mortality induced by such lethal toxin were effectively prevented by the prophylactic patch treatment up to certain LD50 level. Hence, it could be a choice of potential therapeutic regimen against such lethal poisoning.
用含有毒扁豆碱和氯解磷定（2-PAM）的透皮贴剂对（±）-石房蛤毒素中毒的预防和神经保护作用进行了研究，实验对象为 Wistar 品系白化大鼠。将大鼠背部光滑剃毛，贴上含有药物的黏附基质型预防用透皮贴剂 72 小时，然后皮下注射（±）-石房蛤毒素 3 个剂量（1.0、1.5 和 2.0×LD50）。（±）-石房蛤毒素的 LD50 值为 1.25mg/kg，在这个特定的毒素剂量（1.0×LD50）下，会引起大鼠严重的临床症状，包括极度惊厥，导致大脑离散区域的急性损伤，5 分钟内导致 100%的死亡率。本文系统研究了预防用透皮贴剂对（±）-石房蛤毒素中毒的抗惊厥作用、抗心律失常作用、神经传导研究、临床观察和死亡率、神经保护作用以及皮肤组织病理学。结果表明，在一定 LD50 水平下，这种致命毒素引起的惊厥、心动过速、神经损伤、临床症状、脑损伤和死亡率可被预防贴剂治疗有效预防。因此，它可能是针对这种致命中毒的潜在治疗方案的选择。
