滴眼剂中防腐剂成分分析及选用

Analysis and selection of preservatives in eye drops

:90-94
 

目的:分析目前滴眼剂中防腐剂的添加情况,为眼科临床针对不同疾病选择合适的滴眼剂提供参考,倡导合理用药。方法:对临床使用的 194 种滴眼剂说明书中防腐剂成分标注进行统计分析,并对防腐剂的种类、新型防腐剂、眼表毒性研究情况进行归纳综述。结果:滴眼剂中防腐剂大致可分为 5 类,如季铵盐类、醇类、羟苯酯类、有机汞、纯氯氧复合物等。进口滴眼剂的防腐剂以苯扎氯铵为主。国产滴眼剂中新药多以苯扎氯铵为防腐剂,老药则以羟苯乙酯防腐为主;国产药说明书中,有 20.83% 未注明所含防腐剂种类。目前防腐剂中苯扎氯铵抗菌活性虽强,但引起眼表损害的报道也最多,新型防腐剂的研发及无防腐剂滴眼剂可减少眼表的损害。结论:滴眼剂中防腐剂种类繁多、标准不统一,临床医生应熟悉每种眼用制剂防腐剂成分和含量,尤其对青光眼及中重度干眼症使用含防腐剂的滴眼剂时,应关注其对眼表的损害,尽量选择新型防腐剂或不含防腐剂的滴眼剂以减少不良反应的发生。

Objective: To provide guidance for ophthalmologist to choose suitable eye drops for different eye diseases and promote rational drug use by analyzing present situation of preservatives in eye drops. Methods: According to the instructions of 194 kinds of eye drops, statistical analysis was retrospectively carried out on the types, new type, and ocular surface toxicity of preservatives in eye drops. Results: The preservatives of eye drops could be basically divided into 5 categories, such as quaternary ammonium salts, alcohols, hydroxyphenyl esters, organic mercury compounds, pure chlorine oxygen complexes, etc. Besides, most of the preservatives in imported eye drops were benzalkonium chloride, and the new categories of domestic eye drops also utilized benzalkonium chloride as the preservative. However, ethylparaben was used to be considered as preservatives in old-brand domestic eye drops.Moreover, 20.83% domestic drugs’ instructions failed to describe its preservatives. In addition, benzalkonium chloride yielded stronger antibacterial activities compared with other preservatives, but a huge number of animal and in vitro studies demonstrated that benzalkonium chloride may cause or enhance harmful consequences on the eye structures of the anterior segment. Fortunately, preservative-free formulations and new categories would provide clinically benefits. Conclusion: Owing to the various kinds of preservatives and lacking of unified standard of application, clinicians should master the types and content of each preservative in ophthalmic drugs, especially in glaucoma, moderate, and severe dry eyes. Besides, considering ocular surface damage, ophthalmologists should choose new types or preservative-free eye drops to reduce the occurrence of adverse reactions.

论著

激光诱导的脉络膜新生血管模型构建中的麻醉剂和激光能量选择

Selection of anesthetic agent and laser parameter in laserinduced choroid neovascularization models

:222-228
 
目的:比较水合氯醛和阿佛丁两种药物对小鼠的麻醉作用以及不同激光能量对脉络膜新生血管造模成功率的影响。方法:24只C57/BL6小鼠随机分为3组,分别予以200,300和400 mW的532 nm激光进行视网膜光凝;每组再按1:1分为2个亚组,随机使用4.3%水合氯醛或1.2%阿佛丁进行小鼠腹腔注射麻醉。在激光光凝后第4,7,1 0和1 4天进行视网膜荧光素造影(Fundus Fluorescein Angiography,FFA)、SD-OCT检查,在第1 4天时对脉络膜行IB4染色检查。结果:阿佛丁和水合氯醛诱导小鼠进入麻醉时间长分别为(120±30) s和(150±45) s,持续时间分别为(30±15) min和(50±20) min,差异均有统计学意义(均P=0.0001);发生不可逆性白内障的比率分别为2/24和1/24,麻醉导致的死亡数分别为1和0只,差异均无统计学意义(P =0.551,P =0.300)。200,300和400 mW三个激光能量组的造模成功率分别为9.38%,37.5%和93.75%,差异有统计学意义(P=0.0001)。FFA显示:造模成功的小鼠在4 d时荧光素渗漏达到高峰,随后荧光素溢漏的面积逐渐减小。结论:与阿佛丁相比,水合氯醛对小鼠的麻醉维持时间长且不会增加病死率和不可逆性白内障的发生率;400 mW的532 nm激光能量是诱发CNV的较好设置。
Objective: To compare the narcotic effects of chloral hydrate and avertin in mouse models and the success rate of choroidal neovascularization (CNV) mouse model establishment with different energy hierarchy of laser. Methods: Twenty-four mice were randomized into 3 groups, the 532 nm laser was used with different power levels of 200, 300 and 400 mW for each group. In each group, the chloral hydrate was used for 4 mice and avertin for the other 4 mice at random. On day 4, 7, 10 and 14, all mice were tested by the fundus fluorescein angiography (FFA), SD-OCT, and the choroid was stained with the isolectin B4 conjugated AF488 on day 14. Results: The anesthesia induction time of avertin and chloral hydrate was (120±30) s and (150±45) s, and the duration of anesthesia was (30±15) min and (50±20) min, the differences were statistically significant (all P=0.0001); the incidence of irreversible cataract of avertin models and chloral hydrate models was 2/24 and 1/24, the number of death in two models was 1 and without statistical significance (P=0.551, P=0.300). With the increase of laser energy, the success rate of experiments was also gradually increased, from 9.38%, 37.5% to 93.75% (P=0.0001) in 200, 300 and 400 mW group, respectively. According to the results of FFA, the peak of fluorescence leaking was at day 4 after the laser burning, and was gradually reduced. Conclusion: Compared with avertin chloral hydrate can improve the duration of anesthesia without increasing the risk of cataract and mortality. As for the 532 nm laser, the 400 mW energy could be an optimal parameter for the laser-induced CNV.
其他期刊
  • 眼科学报

    主管:中华人民共和国教育部
    主办:中山大学
    承办:中山大学中山眼科中心
    主编:林浩添
    主管:中华人民共和国教育部
    主办:中山大学
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  • Eye Science

    主管:中华人民共和国教育部
    主办:中山大学
    承办:中山大学中山眼科中心
    主编:林浩添
    主管:中华人民共和国教育部
    主办:中山大学
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