盐酸纳洛酮鼻腔喷雾剂的制备及评价

发布时间：2018-04-28 03:29

本文选题：盐酸纳洛酮 + 鼻腔喷雾剂　；参考：《国际药学研究杂志》2017年06期

【摘要】：目的制备盐酸纳洛酮鼻腔喷雾剂并考察制剂的纤毛毒性和体内药代动力学行为。方法考察盐酸纳洛酮在不同pH溶液中的稳定性,不同吸收促进剂对盐酸纳洛酮的促渗透效果,筛选出适宜的处方;以离体蟾蜍上颚黏膜表面纤毛的相对运动百分率评价盐酸纳洛酮鼻腔喷雾剂的纤毛毒性;考察盐酸纳洛酮鼻腔喷雾剂在大鼠体内的药代动力学行为。结果盐酸纳洛酮溶液在pH3.5~5.5范围内稳定,0.2%乙二胺四乙酸二钠(EDTA-2Na)促渗透效果最好;盐酸纳洛酮鼻腔喷雾剂的纤毛毒性小且可恢复;盐酸纳洛酮鼻腔喷雾剂起效快,在大鼠体内的生物利用度与肌肉注射相当。结论本文制备的鼻腔喷雾剂体外性质稳定可控,纤毛毒性小,起效快,生物利用度高,具有较好的应用前景。
[Abstract]:Objective to prepare naloxone hydrochloride nasal spray and investigate its cilia toxicity and pharmacokinetics in vivo. Methods the stability of naloxone hydrochloride in different pH solution and the effect of different absorption accelerator on the permeation of naloxone hydrochloride were investigated. The ciliated toxicity of naloxone hydrochloride nasal spray was evaluated by the relative movement percentage of the cilium on the maxillary surface of toad in vitro, and the pharmacokinetic behavior of naloxone hydrochloride nasal spray in rats was investigated. Results Naloxone hydrochloride solution stabilized 0.2% ethylenediamine tetraacetic acid disodium EDTA-2Na) in the range of pH3.5~5.5 to promote permeation, naloxone hydrochloride nasal spray had little toxicity and could be recovered, and naloxone hydrochloride nasal spray had a quick effect. Bioavailability in rats was comparable to intramuscular injection. Conclusion the nasal spray prepared in this paper has stable and controllable properties in vitro, low cilia toxicity, high bioavailability, and has a good prospect of application.
【作者单位】：徐州医科大学;军事医学科学院毒物药物研究所药物制剂室抗毒药物与毒理学国家重点实验室;北京中医药大学基础医学院;
【基金】：国家自然科学基金资助项目(81573357) 北京市自然科学基金资助项目(7162148)
【分类号】：R943

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