Bucolo C, Mangiafico P
Fidia Oftal Research Laboratories, Catania, Italy.
J Ocul Pharmacol Ther. 1999 Dec;15(6):567-73. doi: 10.1089/jop.1999.15.567.
A new formulation based on pilocarpine hyaluronate salt has been shown to improve the bioavailability of the drug and to extend the duration of activity. We evaluated the extent of intraocular pressure reduction, the duration of action and the kinetics of miotic response of this formulation in comparison with a commercial preparation with the same drug concentration. Ocular hypertension in the rabbit was induced by alpha-chymotrypsin or by water loading. The hypotensive effect of the new formulation 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 in normotensive rabbits showing a greater miotic response and an extended duration when the eyes were treated with the new formulation. The pharmacological profile of the new formulation described in this study indicates an increase of efficacy and duration of action compared to the commercial preparation.
一种基于毛果芸香碱透明质酸盐的新制剂已被证明可提高药物的生物利用度并延长活性持续时间。我们评估了该制剂与具有相同药物浓度的市售制剂相比,降低眼压的程度、作用持续时间和缩瞳反应动力学。通过α-糜蛋白酶或水负荷诱导家兔眼压升高。在正常血压和高血压动物中,新制剂治疗的降压效果均显著大于且长于用市售制剂治疗的兔眼。此外,我们评估了正常血压兔的缩瞳反应,结果显示用新制剂治疗眼睛时,缩瞳反应更大且持续时间更长。本研究中描述的新制剂的药理学特征表明,与市售制剂相比,其疗效和作用持续时间有所增加。