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目的观察眼内可植入性聚乳酸氧氟沙星缓释药栓在兔眼玻璃体腔内的药物缓释过程。方法将相对分子质量各为 ６ １２０和 ２ ５５０的聚乳酸分别混载 ５％，１０％氧氟沙星制成药栓，并作体外药物释放。相对分子质量为 １２ ５５０含１５％氧氟沙星药栓植入兔眼玻璃体腔内，以高效液相色谱法在不同时间点作药物浓度测定。结果３０天内氧氟沙星释放率为 ７０％～９０％，释药时间与聚合物相对分子质量呈正相关。兔眼玻璃体４２天药物浓度变化范围 ０．４９６～１０． ８８５μｇ／ｍｌ，维持高于最小抑菌浓度时间平均为 ３０天。结论相对分子质量为１２ ５５０的聚乳酸含 １５％氧氟沙星缓释药栓在兔眼内药代动力学特点符合眼内炎抗菌药物治疗的基本要求。
Objective To observe the drug release process of intraocular implantable ofloxacin poly-lactate sustained release suppositories in vitreous cavity of rabbit eyes. Methods Polylactic acid with relative molecular mass of 6 120 and 2 550 respectively was mixed with 5% and ofloxacin 10% to make suppository, and the medicine was released in vitro. The relative molecular mass of 12 550 containing 15% ofloxacin was implanted into the vitreous chamber of rabbits, and the drug concentration was determined by HPLC at different time points. Results The release rate of ofloxacin was 70% -90% within 30 days. The release time was positively correlated with the relative molecular mass of the polymer. The 42-day rabbit vitreous body drug concentration range 0.496 ~ 10. 885μg / ml, to maintain above the minimum inhibitory concentration of an average of 30 days. Conclusion The relative molecular mass of 12 550 polylactic acid containing 15% ofloxacin sustained release drug suppository in rabbit intraocular pharmacokinetic characteristics in line with endophthalmitis antibacterial drug treatment of the basic requirements.