| 他克莫司阳离子微乳凝胶的兔眼刺激性研究及房水药动学研究 |
| 投稿时间：2021-04-13 修订日期：2021-06-08 点此下载全文 |
| 引用本文：林昕,张佳良,周欣,宋洪涛.他克莫司阳离子微乳凝胶的兔眼刺激性研究及房水药动学研究[J].药学实践杂志,2023,41(3):177~181 |
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| 中文摘要:目的 研究他克莫司阳离子微乳凝胶对兔眼的刺激性及房水药动学。方法 通过HE染色处理的兔眼组织病理切片观察该制剂的眼部刺激性。采用角膜穿刺术抽取兔眼房水，通过液相色谱-质谱联用仪进行房水药动学研究。结果 他克莫司阳离子微乳凝胶对兔眼无明显刺激性，其房水药动学参数AUC为（128.34±13.09）ng·h /ml，是他克莫司阳离子纳米乳AUC（113.61±12.36）ng·h /ml的1.13倍，是市售他克莫司滴眼液Talymus®AUC（68.25±10.82） ng·h/ml的1.88倍。结论 他克莫司阳离子微乳凝胶眼部刺激性小、滞留时间长且生物利用度高，具有较好的临床应用前景。 |
| 中文关键词:他克莫司 阳离子微乳凝胶 眼部刺激性 药动学 |
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| The eye irritation test and pharmacokinetic study of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits |
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| Abstract:Objective To study the eye irritation and the pharmacokinetics of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits. Methods The eye irritation of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits was observed by histological cross-sections of external ocular tissues stained with HE. The aqueous humor of rabbit eyes was extracted by corneal puncture and analyzed by HPLC-MS for pharmacokinetic study. Results Tacrolimus-loaded cationic nanoemulsion-based in-situ gel had no significant irritation on rabbit eyes. The pharmacokinetic parameter showed that the AUC of tacrolimus-loaded cationic nanoemulsion-based in-situ gel was (128.34±13.09) ng·h/ml, which was 1.13 times of tacrolimus-loaded cationic nanoemulsion (113.61±12.36) ng·h/ml and 1.88 times of Talymus® (68.25±10.82) ng·h /ml. Conclusion Tacrolimus-loaded cationic nanoemulsion-based in-situ gel had the advantages of low irritation, long retention time and high bioavailability in rabbit eyes. It has a good potential for clinical application. |
| keywords:tacrolimus cationic nanoemulsion-based in-situ gel eye irritation pharmacokinetics |
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