配方变量对盐酸奈福泮鼻内原位凝胶凝胶化温度的影响(会议论文)#

Ammar A. Alabdly, Hanan J. Kassab
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引用次数: 2

摘要

Nefopam (N.F.)盐酸是一种非麻醉性中枢作用非阿片类苯并恶唑镇痛药,用于缓解急性和慢性疼痛。由于其在肝脏中的首次降解,其生物利用度较低(约36%)。鼻内给药已被作为一种新的途径,用于靶向脑活动部位,并通过肝脏代谢提高盐酸n.f.h cl的生物利用度。采用不同浓度的poloxam407、poloxam188、HPMC K4M、Carbapol 934和透明质酸聚合物,采用冷法制备N.F. HCl原位凝胶。结果表明,鉴定试验与参考文献重叠,溶解度研究表明,nf.hcl适合鼻内给药;配伍研究发现盐酸奈福泮与HPMC K4M和卡波波尔934不配伍;同时,与甲基纤维素和透明质酸无相互作用。总之,所获得的结果显示,所生产的盐酸N.F.鼻内原位凝胶具有令人难以置信的能力,旨在提高药物的生物利用度,绕过口服盐酸N.F.所面临的肝脏代谢作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation Variables Effect on Gelation Temperature of Nefopam Hydrochloride intranasal in Situ Gel (Conference Paper) #
Nefopam (N.F.) HCl is a non-narcotic centrally-acting, non-opioid benzoxazocine analgesic to relieve acute and chronic pain. It exhibits low bioavailability (about 36%) due to its first-pass degradation in the liver. Intranasal administration has been used as a new route for targeting active brain sites and enhancing the bioavailability of N.F. HCl bypassing hepatic metabolism. In situ gel of N.F. HCl was prepared by the cold method using different concentrations of Poloxamer 407, Poloxamer 188, HPMC K4M, Carbapol 934, and Hyaluronic acid polymers. The results show that identification tests are superimposed with references, solubility study shows that N.F. HCl is suitable to be administered intranasally; Compatibility studies reveal incompatibility of Nefopam HCl with HPMC K4M and Carbapol 934; meanwhile, no interaction with Methylcellulose and Hyaluronic acid. In conclusion, the obtained results revealed the incredible ability of the produced N.F. HCl intranasal in situ gel is intended to enhance drug bioavailability bypassing the metabolizing effect of the liver that N.F. HCl is facing when given orally.
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