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小肠移植受者中环孢素微乳剂和他克莫司的低生物利用度:与肠道P-糖蛋白活性的可能关系。

Low bioavailability of cyclosporine microemulsion and tacrolimus in a small bowel transplant recipient: possible relationship to intestinal P-glycoprotein activity.

作者信息

Kaplan B, Lown K, Craig R, Abecassis M, Kaufman D, Leventhal J, Stuart F, Meier-Kriesche H U, Fryer J

机构信息

Department of Medicine, St. Barnabas Medical Center, Livingston, New Jersey, USA.

出版信息

Transplantation. 1999 Jan 27;67(2):333-5. doi: 10.1097/00007890-199901270-00026.

DOI:10.1097/00007890-199901270-00026
PMID:10075604
Abstract

With intestine transplants the allograft is dependent on itself for maintenance of adequate immunosuppression. We evaluated an intestinal transplant recipient who required very large doses of either tacrolimus or cyclosporine emulsion to achieve acceptable blood concentrations. Pharmacokinetic studies revealed bioavailabilities of 2% and 6% respectively, while D-xylose and B12 absorption were found to be within normal limits and fecal fat was only slightly increased, suggesting that there was a selective absorptive defect for these drugs. Biopsies of the allograft ileum revealed a high P-glycoprotein activity compared to the jejunum or to intestinal biopsies from other normal subjects. This may be a contributing factor to poor immunosuppressive drug absorption in this patient and others.

摘要

对于肠道移植,同种异体移植物自身依赖维持足够的免疫抑制。我们评估了一名肠道移植受者,他需要非常大剂量的他克莫司或环孢素乳剂才能达到可接受的血药浓度。药代动力学研究分别显示生物利用度为2%和6%,而D-木糖和维生素B12吸收在正常范围内,粪便脂肪仅略有增加,提示这些药物存在选择性吸收缺陷。同种异体移植回肠活检显示,与空肠或其他正常受试者的肠道活检相比,P-糖蛋白活性较高。这可能是该患者及其他患者免疫抑制药物吸收不良的一个促成因素。

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Low bioavailability of cyclosporine microemulsion and tacrolimus in a small bowel transplant recipient: possible relationship to intestinal P-glycoprotein activity.小肠移植受者中环孢素微乳剂和他克莫司的低生物利用度:与肠道P-糖蛋白活性的可能关系。
Transplantation. 1999 Jan 27;67(2):333-5. doi: 10.1097/00007890-199901270-00026.
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