Esbelin B, Beyssac E, Aiache J M, Shiu G K, Skelly J P
Biopharmaceutics Department, Faculty of Pharmacy, Clermont-Ferrand, France.
J Pharm Sci. 1991 Oct;80(10):991-4. doi: 10.1002/jps.2600801017.
The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with peanut oil in order to simulate high fat meals and to correlate the in vitro percent dissolved with the in vivo results obtained. The in vivo study was carried out on three groups of healthy volunteers receiving each dosage form in a randomized order just before a high fat breakfast or in the fasting state. The in vitro percent dissolved obtained was compared with those published results obtained with rotating bottles. A linear relationship was established between these results. From the in vivo absorbed percentages calculated according to the Wagner-Nelson method, a linear relation was found between the in vivo percent absorbed and the in vitro percent dissolved in the different conditions. The relationships observed are similar for all the forms under both conditions. The "Bio-Dis" offers advantages over the rotating bottle method. The study reported allows this dissolution apparatus to be proposed as an alternative to the rotating bottle apparatus.
目的是研究一种新的体外溶出方法——“Bio-Dis”装置，并将其与经典的转瓶法进行比较。研究了几种茶碱控释剂型。在标准条件下，在pH值递增时以及用花生油处理后进行溶出试验，以模拟高脂餐，并将体外溶出百分比与所获得的体内结果相关联。体内研究针对三组健康志愿者进行，他们在高脂早餐前或禁食状态下以随机顺序接受每种剂型。将获得的体外溶出百分比与用转瓶法得到的已发表结果进行比较。在这些结果之间建立了线性关系。根据Wagner-Nelson方法计算体内吸收百分比，发现在不同条件下体内吸收百分比与体外溶出百分比之间存在线性关系。在两种条件下，所有剂型观察到的关系相似。“Bio-Dis”比转瓶法具有优势。所报道的研究使得这种溶出装置可以作为转瓶装置的替代方法被推荐。
