四种卟啉类光敏药物理化性质的比较

对四种卟啉类光敏药物包括三种国产血卟啉衍生物扬州光卟啉(YHPD原名“激光三号”)、HPS和LF 019]和美国光富林Ⅱ(photofrin Ⅱ,简称PF Ⅱ)进行了高效液相色谱分析,表明四种产品中都有血卟啉、3(8)-(1-羟乙基)-8(3)-乙烯基次卟啉、原卟啉和双血卟啉醚存在,后者在PF Ⅱ中含量最高。血卟啉的含量在HPS中最高,YHPD和LF 019中较低,两者所含双血卟啉醚相近。LF 019中原卟啉含量最高。比较了四种样品在生物凝胶柱上的行为。对四种样品及其甲酯化衍生物进行了薄层分析。测定了四种产品的紫外、红外光谱和核磁共振氢谱。对样品进行的聚集态研究表明,样品浓度、酸碱度、有机溶剂、光照射和温度与卟啉类化合物的聚集状态有影响。不同样品聚集态的稳定性有差别。

COMPARATIVE STUDIES ON PHYSICO-CHEMICAL PROPERTIES OF FOUR PORPHYRIN PHOTOSENSITIZERS

The HPLC analysis of four porphyrin photosensitizers including three China-made products (YHPD-Jiguan #3, HPS and LFO19) and photofrin Ⅱ indicated that they contained different amounts of hematoporphyrin, 3(8)-(1-hydroxyethyl)-8(3)-vinyldeuteroporphyrin, protoporphyrin as well as dihematoporphyrin ethers (DHE). Photofrin Ⅱ contained the highest content of DHE. The content of hematoporphyrin was highest in HPS, but relatively low in YHPD and LF019. The content of dihematoporphyrin ethers in LF019 was very close to that in YHPD. LFO19 was found to contain the highest percentage of protoporphyrin. The behaviors of the four porphyrin photosensitizers on the Bio-gel p-10 column were different, indicating differences in their aggregation states. The TLC of the four photosensitizers themselves or their methyl esters suggested the complexity of their composition. The UV, IR and ¹HNMR spectra were measured. The results of the survey of different effects on the aggregation state showed that the concentration, pH, organic solvents, irradiation and temperature may cause changes of the aggregetion slate of the products in solution. YHPD and LFO19 could form relatively more stable aggregates than HPS. But the aggregate of photofrin Ⅱ was much more stable.