Bergrem H, Opedal I
Scand J Gastroenterol. 1983 May;18(4):545-9. doi: 10.3109/00365528309181635.
The effect of intestinal malabsorption on the oral bioavailability of prednisolone has been studied in six patients with celiac disease and in six patients with malabsorption of various etiologies, five of whom had undergone gut resections. The serum protein-binding of prednisolone was measured in five patients with celiac disease and hypoalbuminemia and in eight healthy controls. Compared with the controls, patients with celiac disease had a 22% lower peak serum prednisolone concentration (p less than 0.05) and a 16% smaller area under the time-concentration curve of total prednisolone (NS). The proportion of free prednisolone was 79% greater in patients with celiac disease (p less than 0.01), and the area under the time-concentration curve of free, biologically active prednisolone 53% larger (p less than 0.05). There were no significant differences in peak prednisolone concentration or area under the time-concentration curve between the controls and the other patients with malabsorption, who all had normal serum albumin concentrations. These results indicate that the absorption of prednisolone in patients with malabsorption is normal and that the apparently reduced bioavailability in celiac disease patients is more likely to be due to an increased volume of distribution secondary to hypoalbuminemia and reduced protein-binding.
研究了肠道吸收不良对泼尼松龙口服生物利用度的影响，研究对象为6例乳糜泻患者和6例各种病因导致吸收不良的患者，其中5例曾接受肠道切除术。测定了5例乳糜泻伴低白蛋白血症患者和8名健康对照者中泼尼松龙的血清蛋白结合情况。与对照组相比，乳糜泻患者的泼尼松龙血清峰值浓度低22%（p<0.05），总泼尼松龙时间-浓度曲线下面积小16%（无统计学意义）。乳糜泻患者中游离泼尼松龙的比例高79%（p<0.01），游离的、具有生物活性的泼尼松龙时间-浓度曲线下面积大53%（p<0.05）。对照组与其他吸收不良患者（血清白蛋白浓度均正常）之间的泼尼松龙峰值浓度或时间-浓度曲线下面积无显著差异。这些结果表明，吸收不良患者对泼尼松龙的吸收正常，乳糜泻患者中生物利用度明显降低更可能是由于低白蛋白血症继发的分布容积增加和蛋白结合减少所致。
