Dept. of Anesthesiology and Intensive Care Medicine, University Medical Center, Mannheim, Germany.
Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):1310-6. doi: 10.1016/j.ejpb.2013.06.013. Epub 2013 Jul 10.
The purpose of this study was to evaluate whether propofol could be absorbed buccally when administered in semifluorinated alkanes (SFAs), here specifically perfluorobutylpentane (F4H5). This was evaluated in anesthetised and conscious rats and mini-pigs, to measure the relative bioavailability of propofol following buccal administration, but also partly to evaluate the animal models used for this investigation. The absolute bioavailability in the conscious animals was approximately 10% for both species and approximately 50% and 30% in the anesthetised rats and mini-pigs, respectively. This clearly demonstrates that propofol can be absorbed buccally, and F4H5 appears to be a relevant excipient for buccal administration of lipophilic drugs like propofol. The lower absorption in the conscious animals clearly indicates the need for an optimisation of the formulation.
本研究旨在评估在半氟化烷烃（SFAs）中，具体为全氟丁基戊烷（F4H5）给药时，丙泊酚能否经颊黏膜吸收。为此，在麻醉和清醒大鼠和小型猪中进行了评估，以测量颊黏膜给予丙泊酚后的相对生物利用度，但部分也是为了评估用于该研究的动物模型。在清醒动物中，两种物种的绝对生物利用度约为 10%，麻醉大鼠和小型猪分别约为 50%和 30%。这清楚地表明丙泊酚可以经颊黏膜吸收，并且 F4H5 似乎是亲脂性药物如丙泊酚颊黏膜给药的一种合适赋形剂。在清醒动物中较低的吸收显然表明需要对制剂进行优化。
