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不同途径给药后豚鼠外淋巴液中甲泼尼龙琥珀酸钠的代谢动力学特征

发布时间:2019-07-09 06:55
【摘要】:目的:探讨鼓室内灌注、明胶海绵经圆窗给药后豚鼠外淋巴液中甲泼尼龙琥珀酸钠(methylprednisolone,MTH)的代谢动力学特征,为临床选择经鼓室给药方式提供实验依据。 方法:采用鼓室内灌注MTH (62.5mg/ml)及将浸满MTH(62.5mg/ml)的明胶海绵放置于圆窗上两种方式给药,采集2种途径给药后1~12h鼓阶外淋巴液,应用高效液相色谱仪分别检测其中的甲泼尼龙浓度。 结果:鼓室内灌注或明胶海绵经圆窗给药后外淋巴液中MTH的最高浓度均出现在给药后1.5h;在取材的每个时间点,鼓室内灌注给药后外淋巴液中的MTH浓度均高于明胶海绵经圆窗给药者,除5、6及12h外,两者相比差异均有统计学意义。鼓室内灌注给药后外淋巴液中MTH的生物半衰期t1/2=1.84h,明胶海绵圆窗给药后甲泼尼龙t1/2=1.87h。鼓室内灌注、明胶海绵经圆窗给药后12h取材时间点的豚鼠较给药前与取外淋巴前ABR波形Ⅲ波阈值比较差异均无统计学意义(P值均0.05)。 结论:局部给药后MTH能够有效地经圆窗膜渗透进入外淋巴液。鼓室内灌注给药后外淋巴液中的甲泼尼龙浓度较高。该浓度的MTH对内耳功能未见明显影响。
文内图片:甲泼尼龙琥珀酸钠HPLC色谱图A:空白淋巴液,B:空白淋巴液+对照品,,C:样品
图片说明:甲泼尼龙琥珀酸钠HPLC色谱图A:空白淋巴液,B:空白淋巴液+对照品,C:样品
[Abstract]:Objective: to investigate the metabolic kinetic characteristics of sodium methylprednisolone succinate (methylprednisolone,MTH) in perilymph of guinea pigs after indoor infusion of gelatin sponge and administration of gelatin sponge through round window, and to provide experimental basis for clinical selection of drug administration through tympanic cavity. Methods: MTH (62.5mg/ml) was infused in tympanic cavity and gelatin sponge soaked with MTH (62.5mg/ml) was placed on a round window. The perilymph of the tympanic stage was collected 1 h after administration, and the concentration of methylprednisolone was detected by high performance liquid chromatography (HPLC). Results: the highest concentration of MTH in perilymph was 1.5 hours after administration of gelatin sponge through round window, and the concentration of MTH in perilymph after intratympanic infusion was higher than that of gelatin sponge through round window at each time point, except for 5, 6 and 12 hours, there was significant difference between the two groups. The biological half-life of MTH in perilymph after intratympanic infusion was T1 鈮

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