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肽与蛋白质类药物静脉注射往往受到一定限制,经鼻腔给药可以作为一种替代方法。这种给药方法虽然避免了肝脏首过效应,但经对包括人类在内的不同种属生物鼻上皮异体代谢活性研究表明:鼻粘膜的酶屏障同样能产生一种“伪首过效应”。它包括:第1相,细胞色素P—450酶,经对其多方面的毒理学研究表明,这些酶能够使吸入的污染物变成活性代谢物而诱发鼻肿瘤。它的活性比肝脏还要高,因其NAOPH—细胞色素P—450还原酶的含量要高出3—4倍。第Ⅱ相酶的活性也在鼻腔上皮发现。肽和蛋白质类药物可由于鼻粘膜的肽酶和蛋白酶活性作
Peptides and protein drugs are often subject to some restrictions on intravenous administration, which can be used as an alternative. Although this method of administration avoids the first-pass effect of the liver, studies on the biological activity of nasal epithelial allogeneic metabolites in different species, including humans, have shown that the nasal mucosal enzyme barrier can also produce a “pseudo-first pass effect”. It includes: Phase 1, a cytochrome P-450 enzyme, and its multifaceted toxicology studies show that these enzymes can cause inhaled contaminants to become active metabolites and induce nasal tumors. It is also more active than the liver because it contains 3-4 times more NAOPH-cytochrome P-450 reductase. Phase II enzyme activity is also found in the nasal epithelium. Peptides and proteinaceous drugs can be due to the nasal mucosal peptidase and protease activity