家兔口服司帕沙星后眼内组织分布及其药动学研究_药学论文.doc免费

家兔口服司帕沙星后眼内组织分布及其药动学研究_药学论文 家兔口服司帕沙星后眼内组织分布及其药动学研究_药学论文 【摘要】 目的 研究司帕沙星家兔口服后在其眼组织的分布及药动学。方法 给家兔灌服司帕沙星，不同时间点采集眼内各组织标本。以高效液相色谱法测定眼内各组织中的药物浓度，用3p97程序计算药动学参数。结果 给药后泪液、角膜、房水、虹膜睫状体、晶状体4.0h达峰，玻璃体6.0h达峰。司帕沙星在泪液、角膜、房水、虹膜睫状体、晶状体、玻璃体组织中cmax分别为(13.75±1.36)、(3.25±0.32)、(2.06±0.14)、(3.41±0.26)、(1.62±0.13)和(2.18±0.18)μg/ml；各眼组织中t1/2β分别为(8.18±0.70)、(9.94±3.90)、(5.05±0.66)、(13.54±6.37)、(5.67±1.15)和(3.60±1.23)h；AUC0～t分别为(118.68±5.64)、(28.18±5.42)、(17.52±2.09)、(36.77±10.47)、(16.12±0.59)和(16.57±0.47)(μg·h)/ml。结论 司帕沙星家兔口服后在眼内各组织中分布广，浓度较高，可替代治疗眼病时肠外给药。 【关键词】 司帕沙星； 兔； 组织分布； 药动学； HPLC ABSTRACT Objective To study distribution and pharmacokinetics of sparfloxacin in ocular tissues after oral administration in rabbits. Methods Ocular tissues samples were taken in different times after oral administration inrabbits. The concentrations of sparfloxacin in ocular tissues were determined by HPLC. The pharmacokinetics parameters were calculated by 3p97 soft ware. Results The peak time of lacrimal fluid, cornea, aqueous humor, irisciliary body and lens was 4.0h after oral administration, and that of vitreous body was 6.0h. The peak concentration in lacrimal fluid, cornea, aqueous humor, irisciliary body, lens and vitreous body was (13.75±1.36)μg/ml, (3.25±0.32)μg/g, (2.06±0.14)μg/ml, (3.41±0.26)μg/g, (1.62±0.13)μg/g and (2.18±0.18)μg/ml respectively; halflife time in various tissues was (8.18±0.70)h, (9.94±3.90)h, (5.05±0.66)h, (13.54±6.37)h, (5.67±1.15)h and (3.60±1.23)h respectively; AUC0～t in various tissues was (118.68±5.64)(μg·h)/ml, (28.18±5.42)(μg·h)/g, (17.52±2.09)(μg·h)/ml, (36.77±10.47)(μg·h)/g, (16.12±0.59)(μg·h)/g and (16.57±0.47)(μg·h)/ml respectively. Conlusion Sparfloxacin has a good distribution and high concentration in various intraocular tissues of rabbit after oarl administration. It can replace parenteral sparfloxacin for ophthalmic diseases. KEY WORDS Sparfloxacin; Rabbit; Distribution; Pharmacokinetics; HPLC 司帕沙星(sparfloxacin，SPLX)是一种对葡萄球菌和包括肺炎球菌在内的链球菌等革兰阳性菌有效的新型广谱氟喹诺酮类抗