大鼠局部和口服给予他克莫司后房水和血清的渗透：一项吸收研究。
Aqueous humor and serum penetration of tacrolimus after topical and oral administration in rats: an absorption study.
作者信息
Yalçindağ F Nilüfer, Batioğlu Figen, Ari Nuray, Ozdemir Ozden
机构信息
Ankara University Faculty of Medicine Ophthalmology Department, Ankara, Turkey.
出版信息
Clin Ophthalmol. 2007 Mar;1(1):61-4.
PURPOSE
To investigate the penetration of tacrolimus to the aqueous and serum after topical and oral administration.
METHODS
Thirty Wistar rats were divided into three groups. In the first group (n = 12), a single dose of 0.3 % isotonic tacrolimus solution was applied topically to the rat eyes. The second group (n = 12), received 0.1 mg/kg/day tacrolimus for three days. In control group (n = 6), the rats were administered a single drop of 0.3% salin solution topically. Following collection of samples, the amounts of tacrolimus in aqueous and serum samples were compared with each other.
RESULTS
In group I, the mean concentration of tacrolimus was 35.16 ng/ml in aqueous and 2.22 ng/ml in serum. In group II, the mean concentration of tacrolimus was 13.08 ng/ml in aqueous and 13.45 ng/ml in serum. There was no significant difference in the serum concentration levels of tacrolimus between group I and control group. However there was a significant difference of the drug concentrations in aqueous between the groups (p < 0.001). The mean aqueous and serum concentrations of tacrolimus in group II, differed significantly from the mean concentrations in group I (p < 0.001) and the control group (p < 0.001).
CONCLUSION
Tacrolimus may be a promising treatment modality in intraocular inflammation by topical application besides systemic administration.
目的
研究局部和口服给予他克莫司后其在房水和血清中的渗透情况。
方法
30只Wistar大鼠分为三组。第一组（n = 12），将单剂量0.3%的等渗他克莫司溶液局部应用于大鼠眼部。第二组（n = 12），给予0.1mg/kg/天的他克莫司，持续三天。对照组（n = 6），大鼠局部给予一滴0.3%的盐溶液。采集样本后，比较房水和血清样本中他克莫司的含量。
结果
在第一组中，他克莫司在房水中的平均浓度为35.16ng/ml，在血清中为2.22ng/ml。在第二组中，他克莫司在房水中的平均浓度为13.08ng/ml，在血清中为13.45ng/ml。第一组和对照组之间他克莫司的血清浓度水平无显著差异。然而，各组之间房水中药物浓度存在显著差异（p < 0.001）。第二组中他克莫司的房水和血清平均浓度与第一组（p < 0.001）和对照组（p < 0.001）的平均浓度有显著差异。
结论
除全身给药外，他克莫司局部应用可能是治疗眼内炎症的一种有前景的治疗方式。
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