Wurster D E, Weng H L, Flanagan D R
J Pharm Sci. 1986 Nov;75(11):1104-6. doi: 10.1002/jps.2600751117.
The mechanisms that control the dissolution rates of chemical compounds in liquids have long been of interest to pharmaceutical scientists. Generally, control of the dissolution rate can be classified as being by interfacial reaction rate or by the rate of mass transport. Little work has been done in the area of sparingly soluble compounds dissolving in nonpolar organic solvents. In this study the dissolution of three isomers of methylacetanilide was investigated in three nonpolar organic solvents (hexane, heptane, and cyclohexane). The dissolution apparatus used a flat plate into which the nondisintegrating tablet could be placed so that dissolution occurred only from one face of the tablet. Agitation was provided by a four-bladed stirrer whose outer edge was 2 cm from the tablet surface. Dissolution data were collected only for concentrations less than 5% of the saturation solubility of the given compound in the given solvent. All dissolution profiles were linear. Dissolution rates were obtained from the slopes of these plots. Plots of In (dissolution rate) versus In (stirring speed) were also linear and yielded slopes that were close to the value of 0.50 predicted by the convective diffusion model employed.
长期以来,控制化合物在液体中溶解速率的机制一直是制药科学家感兴趣的课题。一般来说,溶解速率的控制可分为界面反应速率控制或传质速率控制。在微溶性化合物溶解于非极性有机溶剂领域所做的工作很少。在本研究中,对三种甲基乙酰苯胺异构体在三种非极性有机溶剂(己烷、庚烷和环己烷)中的溶解情况进行了研究。溶解装置使用一块平板,可将不崩解的片剂放置其中,使溶解仅从片剂的一个表面发生。搅拌由一个四叶搅拌器提供,其外缘距片剂表面2厘米。仅在给定化合物在给定溶剂中的饱和溶解度的5%以下的浓度下收集溶解数据。所有溶解曲线都是线性的。溶解速率由这些曲线的斜率得出。In(溶解速率)对In(搅拌速度)的曲线也是线性的,其斜率接近所采用的对流扩散模型预测的0.50值。