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新型表面活性剂(胆酸催化氧乙基化产物)的增溶特性

Solubilizing properties of new surface-active agents, products of catalytic oxyethylation of cholic acid.

作者信息

Kołodziejczyk Michał Krzysztof, Nachajski Michal Jakub, Lukosek Marek, Zgoda Marian Mikołaj

机构信息

Chair of Applied Pharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151 Łódź, Poland.

2Surface-Active Agent Plant "ICSO Blachownia", ul. Energetyków 9, 47-225 Kedzierzyn-Koźle, Poland.

出版信息

Acta Pol Pharm. 2013 Nov-Dec;70(6):1065-77.

Abstract

Solubilizing properties of aqueous solutions of a series of surface-active agents, products of oxyethylation of cholic acid, were examined in the present study. The content of oxyethylated segments determined by means of the 1H NMR method enabled the verification of the molecular mass of surfactants along with the calculation of the structural hydrophilic-lipophilic balance (HLB), the solubility parameter delta1/2, and the required solubility level of balance HLB(R). Viscosimetric measurements enabled the calculation of the limiting viscosity number, the content-average molecular mass, the effective volume, the hydrodynamic radius of the surfactant micelle and their equilibrium adducts with rutin, diclofenac and loratadine (BCS Class II and III). By means of the spectrophotometric method (UV) the amount of the solubilized diclofenac, loratadine and rutin (rutoside) was determined in the equilibrium system (saturated solution) in the environment of aqueous solutions of cholic acid derivatives of n(TE) = 20-70. The obtained results serve as a basis for determining the solubilization mechanism of lipophilic therapeutic products and indirectly for estimating the influence of the above process on pharmaceutical as well as biological availability of a micellar adduct from model drug forms (Lindbladt lithogenolitic index).

摘要

本研究考察了一系列表面活性剂(胆酸乙氧基化产物)水溶液的增溶性能。通过¹H NMR方法测定的乙氧基化链段含量,能够验证表面活性剂的分子量,并计算结构亲水亲油平衡(HLB)、溶解度参数δ¹/₂以及所需的平衡HLB溶解度水平(R)。粘度测量能够计算极限粘度值、数均分子量、有效体积、表面活性剂胶束及其与芦丁、双氯芬酸和氯雷他定(BCS II类和III类)的平衡加合物的流体力学半径。通过分光光度法(UV)测定了在n(TE) = 20 - 70的胆酸衍生物水溶液环境中平衡体系(饱和溶液)中增溶的双氯芬酸、氯雷他定和芦丁(芦丁糖苷)的量。所得结果为确定亲脂性治疗产品的增溶机制提供了依据,并间接用于评估上述过程对模型药物形式的胶束加合物的药物及生物利用度的影响(Lindbladt结石形成指数)。

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