Taguchi H
J Nutr Sci Vitaminol (Tokyo). 1981;27(4):283-90. doi: 10.3177/jnsv.27.283.
Serum and urinary distributions of following oral and parenteral administration of leucovorin (3-15 mg) were examined in normal adult volunteers microbiologically using lactobacillus casei, Streptococcus faecalis and Pediococcus cerevisiae as test organisms. By the parenteral route, nearly one-third of the folate in the serum and urine was in the form of folinic acid and the remainder as 5-methyltetrahydrofolic acid. Almost all the folate in serum and urine was in the form of 5-methyltetrahydrofolic acid after oral administration. Peak serum folate was observed 3 hr after oral administration, later than that seen after parenteral administration (30 min). Elevation of serum folate was achieved by the increase of the methyl form of folate following repeated administration of leucovorin orally and parenterally. As the form of folate actually rescuing normal cells in a high-dose methotrexate regimen was thought to be methyl, use of the oral route as a principal means of administration of leucovorin in a rescue program was looked into.
在正常成年志愿者中，采用干酪乳杆菌、粪肠球菌和酿酒片球菌作为测试微生物，通过微生物学方法研究了口服和肠胃外给予亚叶酸（3 - 15毫克）后的血清和尿液分布情况。通过肠胃外途径给药，血清和尿液中近三分之一的叶酸呈亚叶酸形式，其余为5 - 甲基四氢叶酸。口服给药后，血清和尿液中几乎所有的叶酸均呈5 - 甲基四氢叶酸形式。口服给药后3小时观察到血清叶酸峰值，晚于肠胃外给药后的峰值（30分钟）。通过口服和肠胃外重复给予亚叶酸后，叶酸甲基形式的增加实现了血清叶酸的升高。由于在高剂量甲氨蝶呤治疗方案中实际拯救正常细胞的叶酸形式被认为是甲基形式，因此研究了在救援方案中使用口服途径作为亚叶酸主要给药方式的情况。
