[Pharmacokinetics of recombinant pro-urokinase ocular dosage form]

Thrombolytic enzymes are widely used in the treatment of vascular diseases of the eyes and of intraocular hemorrhages. We studied the pharmacokinetics of recombinant prourokinase (proRUK) in ocular structures after its intravitreal administration and subtenon's implantation of collagen infusion system (SICIS). Kinetic parameters of accumulation of labeled proRUK in ocular structures were obtained. After intravitreal administration, the proRUK half-life (T1/2) was 7.9 +/- 1.44 h, with proRUK losing none of its enzymatic activity while in the vitreous body. The maximum accumulation of proRUK in the vitreous administered by the SICIS is observed after 4-5 h and is 1.5-2.0% of the dose administered. In the sclera the maximum accumulation of proRUK is 10-15% (4-6 h after administration), in the vascular membrane 0.8% (4 h after administration). We believe that combination of intravitreal and SICIS-aided administration of proRUK to patients with extensive hemorrhages (subtotal and total hemopthalmia) will improve the efficacy of therapy.