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许多研究已证实了人体或动物鼻腔内给药的功效。因为鼻粘膜表面积大,又充满血管,所以有些药物鼻腔内给药的绝对生物利用度可高达100%。这种给药途径特别适用于发生严重首过代谢或在胃肠道中易分解的药物。本研究的目的是考察药物疏水性对鼻腔内吸收的影响。研究中采用两个β阻滞剂美托洛尔(Ⅰ)及烯丙洛尔(Ⅱ)。两者的疏水性显著不同。用锥瓶振摇法得到的辛酸缓冲液表观分配系数(K_(sf)),烯丙洛尔为9.5;美托洛尔为0.5;用反相HPLC法求得的表观分配系数(K_(HPLC)),烯丙洛尔为12.4,美托洛尔为1.45。其它的物理
Numerous studies have demonstrated the efficacy of intranasal administration in humans or animals. Because of the large surface area of the nasal mucosa, which is also full of blood vessels, the absolute bioavailability of some drugs for intranasal administration can be as high as 100%. This route of administration is particularly suitable for those who have experienced severe first-pass metabolism or are prone to break down in the gastrointestinal tract. The purpose of this study was to investigate the effect of drug hydrophobicity on nasal absorption. Two beta blockers metoprolol (I) and allylpolore (II) were used in the study. The hydrophobicity of both is significantly different. The octanoate buffer apparent partition coefficient (K sf) obtained by shaking flask method was 9.5 and that of metoprolol was 0.5. The apparent partition coefficient (K_ (HPLC)), alprenolol 12.4 and metoprolol 1.45. Other physics