Pharmacokinetics of linezolid in rabbit eyes / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the pharmacokinetics of linezolid eye drops in rabbit eyes after a single dose administration. METHODS: Forty New Zealand rabbits are topically applied 50 μL of linezolid eye drops. Ocular tears, aqueous humour, cornea and conjunctiva are sampled at different intervals after drug instillation, and the drug levels are assayed by HPLC. The pharmacokinetic parameters are calculated by DAS 2.1.1 process. RESULTS: The peak concentrations of linezolid in tears, aqueous humour, cornea and conjunctiva are (2861.15±669.43) μg · g-1, (165.71±115.04) μg · mL-1, (58.62±15.48) μLg · g-1, and (305.02±287.64) μg · g-1, respectively. The half-lives of elimination are (60.67±25.59), (36.81±37.39), (38.09±11.59), and (19.85±7.06) h and AUC0-∞ are (4211.92±806.09) μg · h · g-1, (1634.65±1174.85) μg · h · mL-1, (2834.13±578.96) μg · h · g-1, and (3883.84±1846.13) μg · h · g-1, respectively. Blank tears, aqueous humour, cornea and conjunctiva didn't interfere with the determination of linezolid. CONCLUSION: Linezolid has a good pharmacokinetic character and permeability in rabbit eyes.