背景:血泊芬是一种基于卟啉的光敏剂,在中国已用于葡萄酒色斑胎记的光动力疗法。本研究评估了血氧素在健康志愿者中的药代动力学和皮肤光敏作用。
方法:16名健康受试者接受单次静脉输注注射血氧素(5mg/kg)。血氧素(MHD)及其代谢产物血氧卟啉(HP)在血浆中的浓度,测定尿液和粪便。计算药代动力学参数。此外,在太阳模拟器的照射下评估皮肤的光敏化,532nm激光,和阳光。
结果:MHD和HP的Cmax分别为46.7±8.41和1.04±0.265μg/ml,分别。MHD和HP的t1/2分别为5.09±0.945和5.71±2.65h,分别。MHD和HP的AUC0-24h分别为29.8±6.19和0.757±0.285h·μg/ml,分别。MHD和HP的AUC0-∞分别为29.8±6.2和0.792±0.308h·μg/ml,分别。96h时MHD和HP的累积粪便排泄率分别为45.3%和1.05%,分别。然而,96h时MHD的累积尿排泄率仅为0.132%。尿液中HP的浓度低于MHD的10%。给药52小时后,与暴露于各种光源相关的皮肤光敏化作用最小.
结论:MHD和HP在静脉输注后主要通过粪便排出。血泊芬相关的皮肤光敏化作用不明显。
BACKGROUND: Hemoporfin is a porphyrin-based photosensitizer and has been used for photodynamic therapy of port wine stain birthmarks in China. This
study assessed the pharmacokinetics and cutaneous
photosensitization of Hemoporfin in healthy volunteers.
METHODS: Sixteen healthy subjects received a single intravenous infusion injection of Hemoporfin (5 mg/kg). The concentrations of Hemoporfin (MHD) and its metabolite Haematoporphyrin (HP) in plasma, urine and faeces were determined. The pharmacokinetic parameters were calculated. In addition, the cutaneous
photosensitization was evaluated under the irradiation of solar simulator, 532 nm laser, and sunlight.
RESULTS: The Cmax of MHD and HP were 46.7 ± 8.41 and 1.04 ± 0.265 μg/ml, respectively. The t1/2 of MHD and HP were 5.09 ± 0.945 and 5.71 ± 2.65 h, respectively. The AUC0-24h of MHD and HP were 29.8 ± 6.19 and 0.757 ± 0.285 h·μg/ml, respectively. The AUC0-∞ of MHD and HP were 29.8 ± 6.2 and 0.792 ± 0.308 h·μg/ml, respectively. The cumulative fecal excretion rate of MHD and HP were 45.3% and 1.05% at 96 h, respectively. Whereas, the cumulative urinary excretion rate of MHD was only 0.132% at 96 h. The concentration of HP in urine was less than 10% of MHD. After 52 h of administration, the cutaneous
photosensitization associated with the exposure to various light sources was minimal.
CONCLUSIONS: MHD and HP were excreted mainly through the faeces after intravenous infusion. Hemoporfin associated cutaneous
photosensitization was insignificant.