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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
OBJECTIVE: To study the nasal absorption of acetaminophen, diclofenac, indomethacin, piroxicam and propafenone, and to improve and develop the nasal absorption system. Methods: V-C diffusion cell was used for in vitro transmembrane membrane permeation test; rat nasal circulation device was used for in vivo absorption test; systemic nasal absorption test was carried out in volunteers; tracer element labeling compound method Nasal absorption studies. In addition, the nasal mucociliary toxicity of the drug was also studied. Results: Analgin, acetaminophen nasal absorption well, is expected to develop nasal preparations; propafenone nasal cilia toxicity is not suitable for nasal administration; the other three drugs preliminary results show that nasal absorption well, it is worth further the study. Conclusion: A series of research methods proposed and adopted in this paper are suitable for nasal absorption studies