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通过季铵化提高二乙氨基乙基纤维素的体外胆汁酸结合能力。

Increasing the in vitro bile acid binding capacity of diethylaminoethylcellulose by quaternization.

作者信息

Clas S D

机构信息

Department of Chemistry, McGill University, Montreal, Quebec, Canada.

出版信息

J Pharm Sci. 1991 Sep;80(9):891-4. doi: 10.1002/jps.2600800918.

Abstract

Diethylaminoethylcellulose (DEAE-cellulose) was quaternized with methyl iodide (DEAE-cellulose-CH3I), and its in vitro binding capacity for sodium glycocholate, at room temperature, in water, Tris-HCl buffer (0.0015-0.0050 M, pH 7.0), and aqueous NaCl (0.0025 M) was determined by reversed-phase HPLC. Quaternization increased the in vitro bile salt binding capacity of DEAE-cellulose. On a molar basis, the binding capacity was greater than that of cholestyramine, a cholesterol-lowering agent. Increasing the ionic strength of the medium decreased the binding capacities, as expected if ionic interactions are important. However, conversion of DEAE-cellulose-CH3I to its chloride form did not change the binding capacity. The bile salt binding capacity of DEAE-cellulose-CH3I was similar for both sodium cholate and sodium glycocholate.

摘要

用碘甲烷将二乙氨基乙基纤维素(DEAE - 纤维素)季铵化(DEAE - 纤维素 - CH3I),并通过反相高效液相色谱法测定其在室温下于水、Tris - HCl缓冲液(0.0015 - 0.0050 M,pH 7.0)和NaCl水溶液(0.0025 M)中对甘氨胆酸钠的体外结合能力。季铵化提高了DEAE - 纤维素的体外胆汁盐结合能力。以摩尔为基础,其结合能力大于降胆固醇药物消胆胺。正如预期的那样,如果离子相互作用很重要,那么增加介质的离子强度会降低结合能力。然而,将DEAE - 纤维素 - CH3I转化为其氯化物形式并没有改变结合能力。DEAE - 纤维素 - CH3I对胆酸钠和甘氨胆酸钠的胆汁盐结合能力相似。

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