Ritschel W A, Ritschel-Beurlin G, Grummich K
Arzneimittelforschung. 1980;30(3):432-5.
The rate of percutaneous absorption of nitroglycerin from different ointment preparations was studied in the rabbit using an indirect method which suffices bioavailability requirements. Ointment bases of different lipophilic character were compared with a commercially available preparation. Rate of absorption was fastest from the least lipophilic base. A hypothesis is presented regarding the clinical observation that topical use of nitroglycerin may not show enzyme induction as was found in peroral use. According to this hypothesis while achieving therapeutically effective levels the rate of percutaneous absorption should be slow enough not to result in a systemic drug concentration critical to enzyme induction. One experimental preparation (A) resulted in practically identical rate of absorption as obtained with the standard preparation.
采用一种满足生物利用度要求的间接方法,在兔身上研究了不同软膏制剂中硝酸甘油的经皮吸收速率。将不同亲脂性的软膏基质与一种市售制剂进行了比较。从亲脂性最低的基质中吸收速率最快。针对局部使用硝酸甘油可能不会像口服使用那样出现酶诱导这一临床观察结果,提出了一个假设。根据这一假设,在达到治疗有效水平时,经皮吸收速率应足够慢,以免导致对酶诱导至关重要的全身药物浓度。一种实验制剂(A)的吸收速率与标准制剂几乎相同。