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題 名 | 碳酸酐酶抑制劑6-Hydroxyethoxyzolamide局部點眼後之兔眼藥物動力學=The Ocular Pharmacokinetics of a Topical Carbonic Anhydrase Inhibitor: 6-Hydroxyethoxy-2-benzothiazole Sulfonamide in Rabbits after Topical Instillation |
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作 者 | 呂大文; 江樵熹; 張澶榮; 林秋燕; | 書刊名 | 中華民國眼科醫學會雜誌 |
卷 期 | 38:1 1999.03[民88.03] |
頁 次 | 頁41-49 |
分類號 | 418.2323 |
關鍵詞 | 碳酸酐酶抑制劑; 藥物動力學; 青光眼; Canbonic anhydrase inhibitor; Glaucoma; Topical; 6-Hydroxyethoxy-2-benzothlazole Sulfonamide; Ocular pharmacokinetics; |
語 文 | 中文(Chinese) |
中文摘要 | 磺胺類碳酸酐�t抑制劑臨床上常用來治療高血壓與青光眼。最初許多學者認為此 類藥物只有系統性給予才能見效,近來許多學者對局部點用之碳酸酐�t抑制劑重新評估,證 明了碳酸酐�t抑制劑並非只有系統性給藥才有降眼壓的功能,局部點用亦具良好之療效。但 因文獻上有關於局部點用碳酸酐�t抑制劑藥物之眼部藥物動力學報導較為缺乏,故在本研 究中我們以 6-Hydroxyethoxy-2-benzothlazole Sulfonamide (6-HS) 作為局部點用碳酸酐 �t抑制劑模式藥物,研究其於 Alpha-chymotrypsin 導致青光眼之兔眼與正常兔眼局部點眼 後於眼部組織之藥物動力學變化,結果發現 6-HS 於房水液中青光眼兔眼要比正常兔眼排除 速率大 (Ke:0.005 vs. 0.003),在虹膜 - 睫狀體複合體則青光眼兔眼要較正常兔眼先達到 最高濃度 (45 minutes vs.90 minutes),在水晶體之藥物濃度兩者無差異, 在玻璃體中則 青光眼兔眼之 6-HS 濃度為正常眼兩倍以上 (4.1ug/g vs. 1.8 ug/g)。 |
英文摘要 | Carbonic anhydrase inhibitors (CAIs) are very fulness was limited to as second line antiglaucoma medications or acute glaucoma due to a variety of systemic side effects. Recently, after reevaluation of CAIs, it was found that CAIs could be applied topically as well as systemically to decrease intraocular pressure (IOP) . However, there were very few reports on the ocular pharmacokinetics of CAIs. In this study, we used 6-hydroxythoxy-2-benzothiazole sulfonamide (6-HS) as a model drug to evaluate its pharmacokinetics in the rabbit ocular tissue after topical instillation. We found that the elimination rate constant of 6-HS in the aqueous humor of alpha-chymotrypsin induced rabbit glaucoma eyes was greater than that of normal eyes (Ke: 0.005 vs. 0.003). In the irisciliary body complex, 6-HS reached peak concentrations in the glaucoma eyes were earlier than those in normal eyes (45 minutes vs. 90 minutes). In the vitreous, the concentrations of 6-HS were twice higher in the glaucoma eyes than those in the normal eyes (4.1ug/g vs. 1.8ug/g). |
本系統中英文摘要資訊取自各篇刊載內容。