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本文报道第二代血卟啉光敏剂PSD=007的制备及其理化待性和对肿瘤组织的选择性摄入作用及对小鼠S180肉瘤的实验性光敏诊治效果。作者用色谱法由血卟啉光敏剂分离除去70％左右的无关或低效组分,并保留其已知PRT效应较强的低极性组分而制备得组成稳定,光敏效应强的新光敏剂PSD-007。与血卟啉衍生物(HPD)对比测定结果表明,PDS-007于不同时间内在肿瘤组织中的滞留量均高于HPD约1倍,显示其具有较好的肿瘤选择性PRT效应的基础。静脉注射5～10mg/kg体重剂量的PSD-007于S180肉瘤带瘤小鼠后24及48小时,分别用体腔紫外线机及氩离子激光5145波段诊察,均见肿瘤显示鲜明桔红色荧光,后者与周围正常组织有清晰的边缘,在同一条件下用5145光连续进行辐照治疗20分钟,照光后24小时在肿瘤区出现淤血样青紫、瘤体变平坦、其中心区发生凹陷、硬结、个别的成块脱落,显示了明确的实验性肿瘤光敏诊治效果。本文还报道了家兔静脉注射PSD-007后的主要药物动力学参数,为临床合理用药提供了参考依据。
This article reports the second generation of hematoporphyrin photosensitizer PSD = 007 preparation and physico-chemical properties and selectivity of tumor tissue uptake of S180 sarcoma mice experimental photopic diagnosis and treatment. The authors used chromatographic separation of hematoporphyrin photosensitizer to remove about 70% unrelated or inefficient components, and retain its known PRT strong low-polarity components and prepared a stable composition, strong photosensitivity of the new photosensitive Agent PSD-007. Compared with hematoporphyrin derivative (HPD), the results of PDS-007 showed that the retention of PDS-007 in tumor tissue was about 1 time higher than that of HPD, indicating that PDS-007 had a good foundation for tumor-selective PRT. Intravenous injection of 5 mg / kg body weight dose of PSD-007 in S180 sarcoma with mice 24 and 48 hours after the lesion, respectively, with the body cavity UV and 5145 band argon laser diagnostics were found in the tumor showed clear orange fluorescence, the latter And the surrounding normal tissue has a clear edge, under the same conditions with 5145 light irradiation for 20 minutes, 24 hours after light in the tumor area bruising-like purple, flat tumor, the central area of depression, induration, individual Of the block off, showing a clear experimental diagnosis of tumor photosensitivity. This paper also reports the main pharmacokinetic parameters of rabbits after intravenous injection of PSD-007, which provides a reference for clinical rational drug use.