鼻腔作为全身给药途径的研究

目的：以安乃近、对乙酰氨基酚、双氯灭痛、吲哚美辛、吡罗昔康和普罗帕酮为模型药，进行药物的鼻腔吸收研究，完善和发展鼻腔吸收的系统研究方法。方法：采用Ｖ－Ｃ扩散池进行离体透膜试验；采用大鼠鼻腔循环装置进行在体内吸收试验；鼻腔全身吸收实验在志愿者体内进行，同时还采用示踪元素标记化合物法进行了药物的鼻腔吸收研究。此外，对药物的鼻粘膜纤毛毒性也进行了研究。结果：安乃近、对乙酰氨基酚鼻腔吸收良好，有望开发为鼻腔给药制剂；普罗帕酮鼻纤毛毒性较大，不适合鼻腔给药；另三种药物初步结果表明鼻腔吸收良好，值得进一步研究。结论：本文提出并采用的一系列研究方法适合作药物鼻腔吸收研究

Study on nasal cavity as drug systemic administration route

Aim:Analgin,acetaminophen,diclofenac,indomethacin,piroxicam and propafenone were selected as model drugs to carry out drug nasal absorption study as well as to consummate and develope the systemic methodology of drug nasal absorption study.Method:V C diffusion cell was used to make the in vitro nasal mucosa permeation test;a recirculation equippment through rat nasal cavity was used to do in situ nasal recirculation test,drug systemic nasal absorption test was done in volunteers,drug labelling and labelled drug nasal absorption and drug nasal cilitoxicity tests were also made in the study.Results:Analgin and acetaminophen were absorbed through nasal route easily and suitable to be developed as nasal preparations;propafenone was much cilitoxic and unsuitable to be administered nasally.Other three drugs permeated through nasal mucosa fairly easily in the preliminary test and deserve to be studied further.Conclusion:The series of methodology put forward in this paper is suitable for drug nasal absorption study.