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首页> 外文期刊>Journal of ocular pharmacology and therapeutics: The official journal of the Association for Ocular Pharmacology and Therapeutics >Aqueous humor concentrations of bimatoprost free acid, bimatoprost and travoprost free acid in cataract surgical patients administered multiple topical ocular doses of LUMIGAN or TRAVATAN.
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Aqueous humor concentrations of bimatoprost free acid, bimatoprost and travoprost free acid in cataract surgical patients administered multiple topical ocular doses of LUMIGAN or TRAVATAN.

机译：白内障手术患者的LUMAGAN或TRAVATAN多次局部眼用剂量的白内障手术患者的房水中Bimatoprost游离酸，Bimatoprost和travoprost游离酸的浓度。

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PURPOSE: To quantify the aqueous humor (AH) concentrations of bimatoprost (amide), travoprost (isopropyl ester), and their hydrolysis products, bimatoprost free acid (BFA) and travoprost free acid (TFA), after multiple topical ocular doses of LUMIGAN and TRAVATAN, respectively, in patients awaiting cataract surgery. METHODS: In 2 separate open-label, sparse-sampling trials, glaucoma patients with cataracts received LUMIGAN (bimatoprost ophthalmic solution, 0.03%) or TRAVATAN (travoprost ophthalmic solution, 0.004%) bilaterally once daily for at least 21 days prior to cataract surgery. Anterior chamber paracentesis was performed at selected times up to 5 h after the last dose and an AH sample was collected. AH samples were assayed by an independent bioanalytical laboratory using a sensitive and validated tandem LC-MS/MS method. The assay lower limits of quantitation were 0.59 nM for bimatoprost, 0.29 nM for BFA, and 0.44 nM for TFA. RESULTS: AH concentrations of BFA (17-phenyl-trinor PGF(2alpha)) were quantifiable in all but one sample at 0.5 h. The maximum concentration achieved (C(max)) of BFA was 30.9 + or - 16.41 nM (n =5), observed at 2 h postdose. AH concentrations of bimatoprost amide were lower than BFA at all time points, with a C(max) of 6.81 + or - 1.36 nM (n = 7) at 1 h postdose. For TFA, measurable AH concentrations were obtained at all time points with a TFA C(max) of 3.91 + or - 2.27 nM (n = 5), which was observed at 3 h after the dose (all data are mean + or - SEM). CONCLUSIONS: Once daily topical ocular administration of LUMIGAN or TRAVATAN for 3 weeks resulted in significant concentrations of BFA and TFA in the AH. Quantifiable levels of bimatoprost amide were also measured. Maximum concentrations of BFA (30.9 nM) and TFA (3.91 nM) in the anterior chamber are sufficient to fully activate the FP prostanoid receptors in the target cells of the ciliary muscle and trabecular meshwork. Both bimatoprost in LUMIGAN and travoprost in TRAVATAN are essentially prodrugs that are rapidly hydrolyzed to their respective free acids that induce the IOP-lowering effect observed with both drugs in vivo.
机译：目的：在多次局部眼用LUMIGAN和TRAVATAN分别用于等待白内障手术的患者。方法：在2个单独的，开放标签，稀疏抽样试验中，患有白内障的青光眼患者在白内障手术前至少21天每天每天一次接受双侧LUMIGAN（比马前列素眼用溶液，0.03％）或TRAVATAN（特拉沃前列素眼用溶液，0.004％）。 。在最后一次给药后直至5小时的选定时间进行前房穿刺术，并收集AH样本。 AH样品由独立的生物分析实验室使用敏感且经过验证的串联LC-MS / MS方法进行分析。该测定的定量下限为比马前列素为0.59 nM，BFA为0.29 nM和TFA为0.44 nM。结果：在0.5 h时，除一个样品外，所有样品中AH的BFA（17-苯基-trinor PGF（2alpha））浓度均可定量。给药后2小时观察到的BFA的最大浓度（C（max））为30.9 +或-16.41 nM（n = 5）。 Bimatoprost酰胺的AH浓度在所有时间点均低于BFA，给药后1 h C（max）为6.81 +或-1.36 nM（n = 7）。对于TFA，在所有时间点均获得可测量的AH浓度，其TFA C（max）为3.91 +或-2.27 nM（n = 5），在给药后3小时观察到（所有数据均为平均值±SEM） ）。结论：LUMIGAN或TRAVATAN的每日局部眼部给药3周导致AH中BFA和TFA的浓度显着升高。还测量了比马前列素酰胺的定量水平。前房中BFA（30.9 nM）和TFA（3.91 nM）的最大浓度足以完全激活睫状肌和小梁网靶细胞中的FP类前列腺素受体。 LUMIGAN中的比马前列素和TRAVATAN中的曲伏前列素本质上都是前药，它们会迅速水解成各自的游离酸，从而诱导两种药物在体内观察到的降低IOP的作用。

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