Gawande V T, Bothara K G, Singh A, Mahajan A A
Department of Pharmaceutical Chemistry, STES's Sinhgad Institute of Pharmacy, Narhe Road, Narhe, Pune-411 041, India.
Indian J Pharm Sci. 2015 Jan-Feb;77(1):75-82. doi: 10.4103/0250-474x.151607.
The present research work was carried out to determine stability of cefditoren pivoxil, an orally absorbed prodrug that is rapidly hydrolysed by intestinal esterases to the active cephalosporin cefditoren. Cefditoren was subjected to stress conditions recommended by the International Conference on Harmonization of Technical Requirements for Registration of Pharmaceuticals for Human Use guideline Q1A (R2). Cefditoren pivoxil was susceptible for degradation under acidic, alkaline and neutral hydrolytic conditions while it was stable under photolytic and thermal stress conditions. Separation of cefditoren and degradation products were carried out by using HPLC. The unknown degradation products were characterized by liquid chromatography-mass spectrometry/time of flight studies. Structures were proposed for each fragment based on best possible molecular formula and complete degradation pathways were reported for cefditoren and its degradants.
本研究旨在确定头孢妥仑匹酯的稳定性，头孢妥仑匹酯是一种口服吸收的前药，可被肠道酯酶迅速水解为活性头孢菌素头孢妥仑。头孢妥仑按照人用药品注册技术要求国际协调会指南Q1A（R2）推荐的条件进行强制降解试验。头孢妥仑匹酯在酸性、碱性和中性水解条件下易降解，而在光解和热应激条件下稳定。采用高效液相色谱法分离头孢妥仑及其降解产物。通过液相色谱-质谱/飞行时间研究对未知降解产物进行表征。根据最佳可能的分子式为每个碎片提出结构，并报道了头孢妥仑及其降解产物的完整降解途径。
