中外健康文摘
中外健康文摘
중외건강문적
WORLD HEALTH DIGEST
2012年
47期
38-39
,共2页
加替沙星%兔%组织分布%药动学%高效液相色谱法
加替沙星%兔%組織分佈%藥動學%高效液相色譜法
가체사성%토%조직분포%약동학%고효액상색보법
Gatifloxacin%Rabbit%Distribution%Pharmacokinetics%HPLC
目的加替沙星在兔眼内的药动学研究.方法兔眼局部给加替沙星，以高效液相色谱法测定眼内各组织中药物浓度，用3p97程序计算药动学参数.结果加替沙星在角膜、房水、虹膜-睫状体、晶状体和玻璃体组织中Cmax分别为(16.49±1.78)μg?g-1、(1.94±0.14)μg?mL-1、(8.57±0.29)μg?g-1、(0.89±0.09)μg?g-1和(0.73±0.03)μg?g-1；各组织中Tmax分别为(0.47±0.05)h、(0.66±0.08)h、(0.61±0.08)h、(1.10±0.09)h和(0.83±0.06)h；AUC0~t分别为(51.31±3.04)μg?h?g-1、(6.55±0.45)μg?h?mL-1、(51.99±25.66)μg?h?g-1、(4.91±0.41)μg?h?g-1、(3.25±0.13)μg?h?g-1.结论加替沙星在眼内各组织中渗透性好，浓度较高，具有较强的抗菌作用.
目的加替沙星在兔眼內的藥動學研究.方法兔眼跼部給加替沙星，以高效液相色譜法測定眼內各組織中藥物濃度，用3p97程序計算藥動學參數.結果加替沙星在角膜、房水、虹膜-睫狀體、晶狀體和玻璃體組織中Cmax分彆為(16.49±1.78)μg?g-1、(1.94±0.14)μg?mL-1、(8.57±0.29)μg?g-1、(0.89±0.09)μg?g-1和(0.73±0.03)μg?g-1；各組織中Tmax分彆為(0.47±0.05)h、(0.66±0.08)h、(0.61±0.08)h、(1.10±0.09)h和(0.83±0.06)h；AUC0~t分彆為(51.31±3.04)μg?h?g-1、(6.55±0.45)μg?h?mL-1、(51.99±25.66)μg?h?g-1、(4.91±0.41)μg?h?g-1、(3.25±0.13)μg?h?g-1.結論加替沙星在眼內各組織中滲透性好，濃度較高，具有較彊的抗菌作用.
목적가체사성재토안내적약동학연구.방법토안국부급가체사성，이고효액상색보법측정안내각조직중약물농도，용3p97정서계산약동학삼수.결과가체사성재각막、방수、홍막-첩상체、정상체화파리체조직중Cmax분별위(16.49±1.78)μg?g-1、(1.94±0.14)μg?mL-1、(8.57±0.29)μg?g-1、(0.89±0.09)μg?g-1화(0.73±0.03)μg?g-1；각조직중Tmax분별위(0.47±0.05)h、(0.66±0.08)h、(0.61±0.08)h、(1.10±0.09)h화(0.83±0.06)h；AUC0~t분별위(51.31±3.04)μg?h?g-1、(6.55±0.45)μg?h?mL-1、(51.99±25.66)μg?h?g-1、(4.91±0.41)μg?h?g-1、(3.25±0.13)μg?h?g-1.결론가체사성재안내각조직중삼투성호，농도교고，구유교강적항균작용.
OBJECTIVE: To study pharmacokinetics of gatifloxacin in ocular tissues of rabbit after ocular instillation. METHODS : The drug concentrations in ocular tissues were determined by HPLC after topical ocular instillation in rabbits;the pharmacokinetics parameters were figured out by 3p97 process. RESULTS: The Cmax of gatifloxacin in lacrimal fluid cornea,aqueous humor,iris — ciliary body,lens and vitreous body were(16.49±1.78)μg?g-1、(1.94±0.14)μg?mL-1、(8.57±0.29)μg?g-1、(0.89±0.09)μg?g-1 and(0.73±0.03)μg?g-1; Tmax in various tissues wer(0.47±0.05) h、(0.66±0.08)h、(0.61±0.08)h、(1.10±0.09)h and(0.83±0.06)h respectively; AUC0~t in various tissues were (51.31±3.04)μg?h?g-1 、(6.55±0.45)μg?h?mL-1、(51.99±25.66)μg?h?g-1、(4.91±0.41)μg?h?g-1、(3.25± 0.13)μg?h?g-1. respectively. CONCLUSION : Gatifloxacin with strong antibacterial effect has a good permeability and high concentration in various intraocular tissues of rabbit after ocular instillation .
