Thoma K, Kübler N
Institut für Pharmazie und Lebensmittelchemie Ludwig-Maximilians-Universität, München, Germany.
Pharmazie. 1997 Apr;52(4):294-302.
The polyene antibiotics amphotericin B, natamycin and nystatin are rapidly degraded under the influence of light. Amphotericin B as a heptaene has a markedly higher photostability than the tetraenes natamycin and nystatin. With a new HPLC method for the separation of the different polyene components we could perform a quantitative analysis of the photodegradation process. Initially degradation products with unchanged spectrophotometric absorption spectra are formed from each of the three polyene antibiotics. Longer light exposure leads to the subsequent degradation of the polyene structures. This photochemical instability was also detected in various drug products with polyene antibiotics as active ingredient. On direct sun exposure of topically applied polyene antibiotics a pronounced photodeactivation of the drug substances is expected.
多烯抗生素两性霉素B、游霉素和制霉菌素在光照影响下会迅速降解。作为七烯类抗生素,两性霉素B的光稳定性明显高于四烯类的游霉素和制霉菌素。通过一种用于分离不同多烯成分的新型高效液相色谱法,我们能够对光降解过程进行定量分析。最初,这三种多烯抗生素各自都会形成具有不变分光光度吸收光谱的降解产物。光照时间延长会导致多烯结构随后发生降解。在以多烯抗生素为活性成分的各种药品中也检测到了这种光化学不稳定性。局部应用的多烯抗生素直接暴露在阳光下时,预计药物会发生明显的光失活。