ABSTRACT
The pharmacokinetics and content of 3H11-8H-HPD in tumor, liver, skin and muscular of tumor-bearing nude mice were reported and compared with free 3H-H'PD. The conjugated molar ratio of 3Hll-3H-HPD was 1 : 27. The 97% antibody activity of conjugate was retained. After 3Hll-3H-HPD or 3H-HPD iv into tumor-bearing nude mice, the pharmacokinetics parameter of blood-drug concentration indicated that the T1/2 of conjugate group was longer than that of 3H-HPD, the elimination rate constant ( Kel ) of conjugat group was larger than that of 3H-HPD group, but the aparent volume of distribution ( Vd ) of the former was less than that of the latter. Tissue distribution study reveald that the radioactivity in tumor tissue of conjugate was increased average 0.9 fold than that of 3H-HPD group. Tumor/liver ratio in both 3Hll-3H-HPD group and 3H-HPD group were 0.66 ? 0.24 and 0.42?0.20, respectively. Contents of 3Hll-3H-HPD in skin or muscular were decreased average 1 fold than that of free 3H-HPD, respectively. The study result was shown the pharmacokinetics characteristic of large molecule conjugate and the targeting action of monoclonal antibody.
ABSTRACT
? carotene could decrease significantly the ear index and the quantity of Evan' s blue exudation that were skin photosensitive side actions in mice treated by photodynimic therapy ( PDT ) . The PGE 1 content in skin and the histamine content in skin and blood of mice were remarkably raised by raised by PDT. For example, the PGE 1 content in hematoporphyrin derivative group was 6.4 fold greater than that of control group. The PGE1 and histamine cotents were obviously decreased to nearly normal level by pretreatment with ? carotene. The results indicated that ? carotene can antagonise the skin photosensitive side action induced by PDT and the action was related to the decrease of PGE1 and histamine content in skin of mice. The cyclo-oxidase inhibitor indomethacin and the H1 receptor blocker benadryl could also decrease ear index and the quantity of Evan' s blue exudation