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作为非离子表面活性剂类别的模型辅料,Croda型羊毛脂催化乙氧基化产物的水溶液对亲脂性治疗剂的平衡增溶作用。

Equilibrium solubilization of lipophilic therapeutic agents by aqueous solutions of products of catalytic oxyethylation of Croda-type lanolin as model excipients of the class of non-ionic surface active agents.

作者信息

Zgoda Marian Mikołaj, Lukosek Marek, Nachajski Michał Jakub

机构信息

Drug Form Technology Unit, Department of Applied Pharmacy, Medical University, Lodz.

出版信息

Polim Med. 2007;37(2):33-50.

Abstract

Research was conducted into the properties and identity of the products of Croda-type hypoallergenic lanolin, which were obtained with the use of a selective catalyst (K-4) and a standard alkaline catalyst (Na/NaOH). The 1HNMR method was employed to assess the content of oxyethylated segments and the analytic level of hydrophilic-lipophilic balance (HLB). Surface activity of products soluble in water with n(TE) > or = 40 was examined and the thermodynamic potential for micelle formation deltaGm(o) was calculated. Basic viscosity and hydrodynamic values were determined for the solubilizers and their micellar adduct with ibuprofen, ketoprofen and naproxen. In addition, the amount of solubilized therapeutic agents c/s/ was examined by means of the spectroscopic method and the micellar partition coefficient--Kw(m) was estimated. The results obtained in the course of research served as a basis for determining the solubilization mechanism and the stability of the micellar adduct for the purpose of application. This enabled the commencement of technological work on the design and manufacture of a model dosage form administered to the skin and containing the products of lanolin oxyethylation.

摘要

对使用选择性催化剂(K - 4)和标准碱性催化剂(Na/NaOH)制得的Croda型低敏羊毛脂产品的性质和特性进行了研究。采用1HNMR方法评估氧乙基化链段的含量和亲水亲油平衡(HLB)的分析水平。检测了n(TE)≥40的水溶性产品的表面活性,并计算了胶束形成的热力学势ΔGm(o)。测定了增溶剂及其与布洛芬、酮洛芬和萘普生的胶束加合物的基本粘度和流体力学值。此外,通过光谱法检测了增溶治疗剂的量c/s/,并估算了胶束分配系数——Kw(m)。研究过程中获得的结果为确定增溶机制和胶束加合物的稳定性以用于应用提供了依据。这使得能够开始进行关于设计和制造一种施用于皮肤且含有羊毛脂氧乙基化产物的模型剂型的技术工作。

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