Departments of Pharmacy & Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco, San Francisco, California, 94143.
Pharm Res. 1986 Oct;3(5):253-62. doi: 10.1023/A:1016303216873.
The literature addressing determination of the bioavailability of dermatological and other topically administered drugs has been reviewed. The various methods employed, their advantages and drawbacks, have been identified and evaluated. The state of the art and the success of topical bioavailability assessment are discussed in the light of the information presented. It is concluded that, although current methodology ensures the responsible use of topical medicaments, the techniques are, on the whole, quantitatively inadequate. A number of recommendations are proposed as possible improvements to the approaches now undertaken, and specific measurements for drugs in different therapeutic categories are suggested. The ultimate objective of this survey is to catalyze the establishment of straightforward, objective, quantitative, and reproducible methods to evaluate topical bioavailability and to reduce significantly, thereby, the incidence of bioinequivalence and pharmacological inactivity observed following drug dosing to the skin.
已对皮肤科和其他局部用药物生物利用度测定的文献进行了综述。确定并评估了所采用的各种方法、其优缺点。根据所提供的信息,讨论了局部生物利用度评估的现状和成功。结论是,尽管目前的方法学确保了局部药物的合理使用,但这些技术在整体上在定量方面是不足的。提出了一些建议,作为对目前采用的方法的可能改进,并为不同治疗类别的药物提出了具体的测量方法。本研究的最终目标是促进建立简单、客观、定量和可重复的方法来评估局部生物利用度,并显著减少经皮给药后观察到的生物等效性和药理活性不足的发生率。