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[表面活性剂与模型膜和生物膜的相互作用。第二十二部分。分光光度法测定局部麻醉药庚卡因在磷脂脂质体与水相之间的分配系数]

[Interactions of surfactants with model and biological membranes. XXII. Spectrophotometric determination of partition coefficient of heptacaine, a local anesthetic, between the phospholipid liposome and water phase].

作者信息

Hammel M, Uhríková D, Balgavý P

机构信息

Katedra fyzikálnej chémie lieciv Farmaceutical fakulty University Komenského, Bratislava.

出版信息

Ceska Slov Farm. 1996 Mar;45(2):58-66.

PMID:8653276
Abstract

The partition coefficient of the local anaesthetic heptacaine (monohydrochloride of [2-(heptaloxy)phenyl]-2-(1-piperidinyl)ethyl ester of carbamic acid) between unilamellar liposomes prepared from chromatographically pure egg yolk phosphatidylcholine and the aqueous phase (NaCl solution, ionic strength I = 0,1,pH 4,5, temperature t = 20 degrees C) was determined using UV-VIS spectrophotometry. The contribution to the anaesthetic spectra due to light scattering on liposomes was eliminated numerically using the scattering function. This procedure gave more precise results than the subtraction of liposomes spectra. The values of the partition coefficient defined with the use of molar concentrations, weight concentrations and molar fractions estimated at a wavelength of lambda = 292 nm were Kp = 1116 +/- 49, Kp(m) = 1098 +/- 48 and Kp(x) = 47575 +/- 2089, respectively.

摘要

采用紫外可见分光光度法测定了局部麻醉药庚卡因(氨基甲酸[2-(庚氧基)苯基]-2-(1-哌啶基)乙酯的盐酸盐)在由色谱纯蛋黄卵磷脂制备的单层脂质体与水相(NaCl溶液,离子强度I = 0.1,pH 4.5,温度t = 20℃)之间的分配系数。利用散射函数通过数值方法消除了脂质体上光散射对麻醉光谱的影响。该方法比减去脂质体光谱能得到更精确的结果。在波长λ = 292 nm处,使用摩尔浓度、重量浓度和摩尔分数定义的分配系数值分别为Kp = 1116 ± 49、Kp(m) = 1098 ± 48和Kp(x) = 47575 ± 2089。

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