Nimrod A, Ezra E, Ezov N, Nachum G, Parisada B
BioTechnology General Ltd., Kiryat Weizmann, Rehovot, Israel.
J Ocul Pharmacol. 1992 Summer;8(2):161-72. doi: 10.1089/jop.1992.8.161.
The feasibility of using bacteria-derived hyaluronate solution as a viscous aid for anterior chamber surgery was examined by studying the pharmacokinetic behavior and metabolic fate of 14C-labelled material, following administration to rats and rabbits. Intravenously-administered HA disappeared rapidly from the blood of rabbits and rats with a mean t1/2 of 5.3 and 3.7 min, respectively. The labelled material has concomittantly accumulated in the liver, where it was digested to oligomeric sugar subunits; these were further utilized metabolically either for energy generation or for incorporation into new high molecular weight species. Metabolic cage studies has indicated that most of the 14C-HA label administered intravenously to rats was excreted as CO2 via the respiration within 24h, while a smaller portion was excreted in the urine. The disposition of viscous 14C-HA administered into the anterior eye chamber of rabbits was slow and followed first-order kinetics with a t1/2 of 10.5h. No degradation occurred in the aqueous humour. Low blood levels of 14C-labeled material were found during 72h after intra-ocular administration. The results indicate that the absorption, distribution, metabolism and excretion of bacteria-derived HA is similar to those of the currently used ophthalmic surgery HA aids extracted from rooster combs.
通过研究给大鼠和兔子注射14C标记物质后的药代动力学行为和代谢归宿,考察了使用细菌衍生的透明质酸盐溶液作为前房手术粘性辅助剂的可行性。静脉注射的透明质酸(HA)在兔子和大鼠血液中迅速消失,平均半衰期分别为5.3分钟和3.7分钟。标记物质同时在肝脏中积累,并在肝脏中被消化成寡聚糖亚基;这些亚基进一步用于代谢产生能量或并入新的高分子量物质中。代谢笼研究表明,静脉注射给大鼠的大部分14C-HA标记物在24小时内通过呼吸以二氧化碳形式排出,而一小部分则通过尿液排出。注入兔子眼前房的粘性14C-HA的处置缓慢,遵循一级动力学,半衰期为10.5小时。房水中未发生降解。眼内给药后72小时内,血液中14C标记物质的水平较低。结果表明,细菌衍生的透明质酸的吸收、分布、代谢和排泄与目前用于眼科手术的从公鸡鸡冠中提取的透明质酸辅助剂相似。