| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Animal models | Seven adult female cynomolgus monkeys, each weighing 3 to 5 kg with normotensive IOP |
Preparation Method | 50 μL (25 μL×2) of 0.04% AR-13324 was topically applied to 1 eye of each monkey. An equal volume of vehicle was applied to the contralateral control eye. IOP was measured before drug administration and 6 hours after dosing with a calibrated neumatonometer in the sit ting position. IOP reading was taken 2 times on each eye and the average of 2 values was used to perform statistical analysis. |
Dosage form | 50 μL (25 μL×2) of 0.04% AR-13324 |
Applications | Six hours after a single dose of 0.04% AR-13324 to 7 normal monkey eyes, the IOP measured by pneumatonometer in treated eyes was reduced (P< 0.005) by 25% when compared with baseline measurements and by 24% when compared with contralateral vehicle-treated eyes |
Animal models | Male DB rabbits (n=11, 2.15-0.09 kg) |
Preparation Method | The protocol entailed once per day—topical application of 1 drop of 0.04% AR-13324 for 2 days. Then, on the morning of the third day，the animals were anesthetized and surgically prepared, and then, measurements were obtained before dosing with AR-13324 or vehicle (baseline measurements) and for 3 h after dosing. |
Dosage form | 1 drop of 0.04% AR-13324 for 2 days |
Applications | At 3 h postdosing, the reduction in EVP caused by AR-13324 treatment accounted for 42% of the measured reduction in IOP. |
| 产品描述 | AR-13324 is a potent inhibitor of ROCK I and ROCK II that has been shown to induce morphologic changes in cultured human and porcine TM cells at low concentration. AR-13324, a rho kinase inhibitor, and an inhibitor of the norepinephrine transporter, reduces intraocular pressure (IOP) in normotensive monkey eyes[1]. AR-13324 produces statistically significant lowering of EVP in DB rabbits[2]. The fixed-dose combination of AR-13324 0.02% and latanoprost 0.005% in PG324 Ophthalmic Solution provides clinically and statistically superior ocular hypotensive efficacy relative to its individual active components at the same concentrations[3]. AR-13324 0.02% was less effective than latanoprost by approximately 1 mmHg in patients with unmedicated IOPs in the range of 22 to 35 mmHg[4] Six hours after a single dose of 0.04% AR-13324 to 7 normal monkey eyes, the IOP measured by pneumatonometer in treated eyes was reduced (P< 0.005) by 25% when compared with baseline measurements and by 24% when compared with contralateral vehicle-treated eyes[1]. At 3 h postdosing, the reduction in EVP caused by AR-13324 treatment accounted for 42% of the measured reduction in IOP[2]. References: |
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