Wassef R, Cohen Z, Nordgren S, Langer B
Transplantation. 1985 May;39(5):496-9. doi: 10.1097/00007890-198505000-00007.
The absorption of oral cyclosporine (CsA) was studied in a canine small intestinal transplantation model. Absorption of CsA was almost absent in bowel-resected dogs. Autotransplanted dogs showed a persisting malabsorption of CsA (mean peak of 687 +/- 348 ng/ml vs. 1683 +/- 154 ng/ml in control dogs). Allotransplanted dogs with normal graft histology showed a similar malabsorption (mean increase in CsA level: 833 ng/ml), whereas allotransplanted dogs with rejection of the graft showed a markedly decreased absorption (mean increase: 368 +/- 31 ng/ml). In two autotransplanted dogs pretreated with olive oil alone, CsA absorption increased over four weeks to a mean peak of 2215 +/- 5 ng/ml. We conclude that oral CsA is absorbed through the small intestine. Absorption of CsA is decreased after autotransplantation and allotransplantation, and rejection of the graft impedes it further. Regular administration of olive oil alone enhances absorption of oral CsA in a canine model.
在犬小肠移植模型中研究了口服环孢素(CsA)的吸收情况。在肠切除的犬中,CsA几乎不被吸收。自体移植的犬表现出持续的CsA吸收不良(平均峰值为687±348 ng/ml,而对照犬为1683±154 ng/ml)。移植组织学正常的同种异体移植犬表现出类似的吸收不良(CsA水平平均升高:833 ng/ml),而移植组织发生排斥反应的同种异体移植犬吸收明显减少(平均升高:368±31 ng/ml)。在两只仅用橄榄油预处理的自体移植犬中,CsA吸收在四周内增加至平均峰值2215±5 ng/ml。我们得出结论,口服CsA通过小肠吸收。自体移植和同种异体移植后CsA吸收减少,移植组织的排斥反应进一步阻碍其吸收。在犬模型中,单独定期给予橄榄油可增强口服CsA的吸收。