Patton T F, Robinson J R
J Pharm Sci. 1975 Aug;64(8):1312-6. doi: 10.1002/jps.2600640811.
The flow properties and viscosity of the vehicle into which drugs are incorporated can be determining factors in the bioavailability of topically applied ophthalmic drugs. It is shown, in rabbits, that when polyvinyl alcohol and methylcellulose are compared on a viscosity basis, there is essentially no difference in the two vehicles with regard to their influence on ocular drug bioavailability. Moreover, the rate of drainage loss for polyvinyl alcohol solutions, as determined by the radioactive technetium technique, compares favorably to methylcellulose solutions of similar viscosity. The relationship between viscosity and contact time or drainage loss of a drug is not a direct one, but an optimum viscosity range exists for polyvinyl alcohol solutions. This optimum range of 12-15 cps in rabbits is identical to that found for methylcellulose and differs considerably from the commonly employed viscosity in commercial preparations. Based on the methylcellulose-polyvinyl alcohol comparison, it appears that vehicles exhibiting or approximating Newtonian flow properties show comparable effects as ophthalmic vehicles. Finally, a discussion of non-Newtonian vehicles and their expected behavior in the eye is presented.
药物所掺入的载体的流动性质和粘度可能是局部应用的眼科药物生物利用度的决定因素。在兔子身上的研究表明,当以粘度为基础比较聚乙烯醇和甲基纤维素时,就它们对眼部药物生物利用度的影响而言,这两种载体基本没有差异。此外,通过放射性锝技术测定,聚乙烯醇溶液的引流损失率与粘度相似的甲基纤维素溶液相比具有优势。药物的粘度与接触时间或引流损失之间的关系并非直接相关,但聚乙烯醇溶液存在一个最佳粘度范围。兔子身上这个12 - 15厘泊的最佳范围与甲基纤维素的相同,且与商业制剂中常用的粘度有很大差异。基于甲基纤维素 - 聚乙烯醇的比较,似乎表现出或近似牛顿流动性质的载体作为眼科载体显示出可比的效果。最后,对非牛顿载体及其在眼中的预期行为进行了讨论。