Bucolo C, Spadaro A, Mangiafico S
Fidia Oftal Research Laboratories, Catania, Italy.
Ophthalmic Res. 1998;30(2):101-6. doi: 10.1159/000055461.
A new formulation (HYA) based on timolol hyaluronate and pilocarpine hyaluronate salts has been shown to improve the bioavailability of the drugs and to extend the duration of their action. Extent of the intraocular pressure lowering effect, duration of action and aqueous bioavailability of timolol and pilocarpine of HYA were compared with a commercial preparation. Ocular hypertension in the rabbit was induced by alpha-chymotrypsin or by water loading. The hypotensive effect of HYA treatment was significantly greater and longer than that observed in rabbit eyes treated with the commercial preparation both in the normotensive and in the hypertensive animals. Furthermore, we evaluated the miotic response; due to pilocarpine, normotensive rabbits showed a greater miotic response and an extended duration when the eyes were treated with HYA. The new formulation increased the aqueous availability of timolol and pilocarpine compared to the commercial preparation as determined by HPLC. The pharmacodynamic and pharmacokinetic profiles of HYA indicate an increase in efficacy and duration of action along with an increase in bioavailability of timolol and pilocarpine in comparison with the commercial preparation.
一种基于噻吗洛尔透明质酸盐和毛果芸香碱透明质酸盐的新制剂（HYA）已被证明可提高药物的生物利用度并延长其作用持续时间。将HYA中噻吗洛尔和毛果芸香碱的眼内压降低效果程度、作用持续时间和房水生物利用度与一种商业制剂进行了比较。通过α-糜蛋白酶或水负荷诱导兔眼高血压。在正常血压和高血压动物中，HYA治疗的降压效果均显著大于且长于用商业制剂治疗的兔眼。此外，我们评估了缩瞳反应；由于毛果芸香碱的作用，正常血压的兔在用HYA治疗眼睛时表现出更大的缩瞳反应和更长的持续时间。通过高效液相色谱法测定，与商业制剂相比，新制剂提高了噻吗洛尔和毛果芸香碱的房水可用性。与商业制剂相比，HYA的药效学和药代动力学特征表明其疗效和作用持续时间增加，同时噻吗洛尔和毛果芸香碱的生物利用度也增加。
