| 引用本文: | 陈光宇,何群,颜学军,王适,吕毅,张湘晖.新目安眼用即型凝胶与普通凝胶兔眼内药动学特性比较研究[J].中国现代应用药学,2019,36(9):1050-1054. |
| CHEN Guangyu,HE Qun,YAN Xuejun,WANG Shi,LYU Yi,ZHANG Xianghui.Comparative Research Between the New Mu-an In-situ Forming Eye Gel and the Common Gel on the Transit Pharmacokinetics Character in Rabbit Aqueous Humor[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(9):1050-1054. |
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| 新目安眼用即型凝胶与普通凝胶兔眼内药动学特性比较研究 |
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陈光宇1, 何群1,2, 颜学军1, 王适3, 吕毅4, 张湘晖5
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1.湖南省药食同源功能性食品工程技术研究中心, 长沙 410208;2.湖南省药学"十二五"重点学科, 长沙 410208;3.湖南食品药品职业学院, 长沙 410208;4.湖南中医药大学第一临床医学院, 长沙 410007;5.湖南中医药大学第二临床医学院, 长沙 410005
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| 摘要: |
| 目的 探索新目安眼用即型凝胶相变过程对兔眼内房水中药物药动学特性的影响，并与普通凝胶比较，评价该即型凝胶的剂型特征。方法 以新西兰家兔为试验对象，采用眼部给予新目安眼用即型凝胶（存在相变过程）和普通凝胶后，按时间点取房水，测定更昔洛韦含量，建立药物在房水中的药动学方程，计算体内药动学参数，比较两者的差别。结果 新目安眼用即型凝胶房水中更昔洛韦药动学方程为C=18.94×e-0.015 4 t-18.94×e-0.079 85 t，普通凝胶房水中更昔洛韦药动学方程为C=15.42×e-0.015 3 t-15.42×e-0.048 8 t，说明两者在兔眼内的药动学机制相同。从各药动学参数比较分析，新目安眼用即型凝胶由于相变过程使达峰时间仅为25.51 min，达峰浓度高达10.31 μg·mL-1，吸收半衰期缩短为8.679 min，AUC提高到992.4 μg·mL-1·min，而普通凝胶达峰时间为34.63 min，达峰浓度仅为6.232 μg·mL-1，吸收半衰期为14.20 min，AUC仅为691.4 μg·mL-1·min。结论 即型凝胶相转变过程能将相变潜能（△H）转变成药物角膜渗透的动能，可最大限度发挥药效。 |
| 关键词: 新目安眼用即型凝胶 更昔洛韦 泊洛萨姆188 泊洛萨姆407 房水 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.09.004 |
| 分类号:R969.1 |
| 基金项目:湖南省自然科学基金项目（11JJ3107） |
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| Comparative Research Between the New Mu-an In-situ Forming Eye Gel and the Common Gel on the Transit Pharmacokinetics Character in Rabbit Aqueous Humor |
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CHEN Guangyu1, HE Qun1,2, YAN Xuejun1, WANG Shi3, LYU Yi4, ZHANG Xianghui5
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1.Engineering Center of Medicinal and Edible Functional Food, Hunan University of Chinese Medicine, Changsha 410208, China;2.Key Disciplinary Areas of "the Twelfth Five-year Plan" in Hunan Province, Changsha 410208, China;3.Hunan Food and Drug Professional College, Changsha 410208, China;4.First Clinical Medical College of Hunan University of Chinese Medicine, Changsha 410007, China;5.Second Clinical Medical College of Hunan University of Chinese Medicine, Changsha 410005, China
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| Abstract: |
| OBJECTIVE To evaluate the characteristic of the dosage form of the new Mu-an in-situ forming eye gel by compare the effect of the drug transit pharmacokinetics character in rabbit aqueous humor of the phase transition process with common gel. METHODS Taken New Zealand rabbits as research objects, after giving new Mu-an in-situ forming eye gel(had phase transition process) and common gel in ocular, obtained aqueous humor in different time points, detected the content of ganciclovir, established the transit pharmacokinetics equations of drug in aqueous humor, calculated the transit pharmacokinetics parameters of drugs in vivo, made a comparison between the new Mu-an in-situ forming eye gel and the common gel. RESULTS The transit pharmacokinetics equations of ganciclovir in aqueous humor of new Mu-an in-situ forming eye gel was C=18.94×e-0.015 4 t-18.94×e-0.079 85 t, the transit pharmacokinetics equations of ganciclovir in aqueous humor of common gel was C=15.42×e-0.015 3 t-15.42×e-0.048 8 t. It could explain that both two gel had the same transit mechanism in aqueous humor of rabbits. Through the comparative analysis of different pharmacokinetic parameters, it showed that time to peak of new Mu-an in-situ forming eye gel was 25.51 min, the concentration to peak was 10.31 μg·mL-1, t1/2 was 8.679 min and the AUC was 992.4 μg·mL-1·min, while for common gel, the time to peak was 34.63 min, the concentration to peak was 6.232 μg·mL-1, t1/2 was 14.20 min and the AUC was 691.4 μg·mL-1·min. CONCLUSION Phase transition energy(△H) turns into kinetic energy of drug permeate cornea in the phase transition process of in-situ gel, which can take pesticide effect for it to be as effective as possible. |
| Key words: new Mu-an in-situ forming eye gel ganciclovir poloxamer 188 poloxamer 407 aqueous humor |
