Camber O, Edman P
Department of Pharmaceutics, University of Uppsala, Sweden.
Curr Eye Res. 1989 Jun;8(6):563-7. doi: 10.3109/02713688908995755.
Sodium hyaluronate, as an additive to aqueous ophthalmic formulations, has been claimed to increase the ocular contact time and, thereby, the drug bioavailability. In the present study, the effect of sodium hyaluronate on corneal residence time and drug absorption in rabbits was investigated. Addition of sodium hyaluronate (0.125%) to a 3H-pilocarpine HCl solution resulted in increased retention of radioactivity in tear fluid and a 2-fold increase in drug concentration in the cornea and aqueous humor. Further, the effects of concentration and molecular weight of sodium hyaluronate on the miosis induced by pilocarpine in rabbits were studied. A significant increase of miotic response was seen at concentrations just less than 0.1% sodium hyaluronate. Pilocarpine solutions prepared from high mol.wt. sodium hyaluronate exhibited a greater miotic response than those prepared from lower mol.wt. samples. This might indicate that other physicochemical properties of sodium hyaluronate influence drug bioavailability.
透明质酸钠作为眼科水性制剂的添加剂,据称可延长眼部接触时间,从而提高药物生物利用度。在本研究中,研究了透明质酸钠对家兔角膜停留时间和药物吸收的影响。向3H-毛果芸香碱盐酸盐溶液中添加0.125%的透明质酸钠,可使泪液中的放射性保留增加,角膜和房水中的药物浓度增加两倍。此外,还研究了透明质酸钠的浓度和分子量对毛果芸香碱诱导家兔瞳孔缩小的影响。在透明质酸钠浓度略低于0.1%时,缩瞳反应显著增强。由高分子量透明质酸钠制备的毛果芸香碱溶液比由低分子量样品制备的溶液表现出更大的缩瞳反应。这可能表明透明质酸钠的其他物理化学性质会影响药物生物利用度。