阿司匹林 ADME
中文名称
通路描述
在水中，阿司匹林（乙酰水杨酸，ASA）溶解并解离为乙酰水杨酸离子（ASA-）。ASA-是一种抗凝血剂和非甾体抗炎药（NSAID）；其治疗作用通过与 PTGS 酶相互作用介导。在摩尔基础上，ASA-（a）作为镇痛剂和抗炎剂更有效，(b) 具有更大的胃溃疡生成活性，(c) 作为前列腺素生物合成和血小板聚集的抑制剂比水杨酸盐（ST）更有效（Flower 1974；Mills 等，1974；Rainsford 1975；Rainsford 1977）。乙酰水杨酸在胃黏膜中发现的条件中仅轻微溶解，主要是因为溶剂的可用性不足。吸收面积和吸收量在小肠中增加。通过溶解片剂或使用 ASA 盐类进一步增加吸收。实际上，100% 的治疗剂量阿司匹林被吸收，主要由肠黏膜细胞吸收（Artursson & Karlsson, 1991；Yee 1997）。只有少数百分比的 ASA-保持不变，其余被水解为水杨酸盐（ST）。ST 的主要代谢途径是与甘氨酸结合形成水杨酸。这占产品的 20-65%。与葡萄糖醛酸结合（酯和醚）去除多达 42% 的 ST。最后，一小部分也被细胞色素羟基化（Hutt 等，1986）。
英文描述
Aspirin ADME In water aspirin (acetylsalicylic acid, ASA) dissolves, dissociating into the acetylsalicylate ion (ASA-). ASA- is an anti-clotting agent and nonsteroidal anti-inflammatory drug (NSAID); the therapeutic effects are mediated through its interaction with PTGS enzymes. On a molar basis ASA- (a) is more potent as an analgesic/anti-inflammatory agent, (b) has greater gastric ulcerogenic activity, and (c) is much more effective as an inhibitor of prostaglandin biosynthesis and platelet aggregation than salicylate (ST) (Flower 1974; Mills et al, 1974; Rainsford 1975; Rainsford 1977).
Acetylsalicylic acid is only slightly soluble in conditions being found in the stomach mucosa, mostly because of unavailability of sufficient amount of solvent. The absorption, as well as the absorbing area, increases in the small intestine. Further increased absorption is achieved by dissolving tablets before ingestion or usage of ASA salts (Dressman et al, 2012). Practically 100% of therapeutic aspirin doses are taken up, mostly by intestinal mucosal cells (Artursson & Karlsson, 1991; Yee 1997).
Only a few percent of ASA- remain unchanged, the rest is hydrolyzed to salicylate (ST). The major route of ST catabolism is conjugation with glycine to form salicyluric acid. This accounts for 20â65% of the products. Conjugation to glucuronides (ester and ether) removes up to 42% of ST. Finally, a minor part also gets hydroxylated by cytochromes (Hutt et al, 1986).
Acetylsalicylic acid is only slightly soluble in conditions being found in the stomach mucosa, mostly because of unavailability of sufficient amount of solvent. The absorption, as well as the absorbing area, increases in the small intestine. Further increased absorption is achieved by dissolving tablets before ingestion or usage of ASA salts (Dressman et al, 2012). Practically 100% of therapeutic aspirin doses are taken up, mostly by intestinal mucosal cells (Artursson & Karlsson, 1991; Yee 1997).
Only a few percent of ASA- remain unchanged, the rest is hydrolyzed to salicylate (ST). The major route of ST catabolism is conjugation with glycine to form salicyluric acid. This accounts for 20â65% of the products. Conjugation to glucuronides (ester and ether) removes up to 42% of ST. Finally, a minor part also gets hydroxylated by cytochromes (Hutt et al, 1986).
所含基因
42 个基因