Overview of the BAK-free travoprost/timolol BAK-free fixed combination

Introduction: Glaucoma is the second leading cause of blindness globally, representing a significant public health concern. More than 60 million people are affected by glaucoma worldwide; as this population ages, the number is expected to increase. Glaucoma is a collection of heterogeneous diseases sharing common clinical characteristics. The goal of treatment is to prevent significant visual dysfunction through reduction of intraocular pressure (IOP).

Areas covered: This is a review of the current literature about combination therapeutic regimens for the reduction of IOP, focusing on the risk : benefit profile of a fixed-combination therapy using travoprost and timolol.

Expert opinion: Since the debut of prostaglandin analogues in the 1990s, only modest innovation has occurred in glaucoma pharmacology. A growing body of research has established that the preservative benzalkonium chloride (BAK) might not be the benign contributor expected of excipient ingredients. Thus, BAK-free treatments were developed, with the goal of IOP reduction without furthering ocular surface disease symptoms. The BAK-free travoprost/timolol combination represents an important addition to glaucoma medication options and may fill an unmet need in this therapeutic arena.     

The effects of topical nasal steroids on rat respiratory mucosa in vivo, with special reference to benzalkonium chloride

Fifty rats were treated with topical nasal steroids with and without the preservative benzalkonium chloride in their right nostril twice daily for 21 days, while the left nostrils were exposed to 0.9% NaCl. By cutting the noses serially in frontal sections, the structure of the mucosal lining of all parts of the nose could be investigated. Areas with squamous cell metaplasia were observed in all nostrils exposed to topical steroids containing benzalkonium chloride. Such alterations were not observed in any nasal cavities exposed to the topical nasal steroid without the preservative or to 0.9% NaCl. In conclusion, benzalkonium chloride appears to be potentially toxic to the mucosa in vivo.     

Benzalkonium Chloride: A Bronchoconstricting Preservative in Continuous Albuterol Nebulizer Solutions

For convenience, many pediatric hospitals are preparing solutions for continuous nebulized albuterol using the 0.5% 20‐ml multidose albuterol dropper bottle. This product contains benzalkonium chloride (BAC) that, by itself, produces bronchospasm that is dose dependent and cumulative. The bronchoconstrictive effects of BAC are greater in patients with more severe airway obstruction and increased airway responsiveness. Use of BAC‐containing albuterol during severe acute asthma exacerbations may antagonize the bronchodilator response to albuterol, prolong treatment, and increase the risk of albuterol‐related systemic adverse effects. Such a deleterious effect of BAC is difficult to detect because some patients improve slowly or may even worsen during treatment. We recommend that only preservative‐free albuterol products be used.     

不含苯扎氯铵的抗青光眼滴眼液疗效及安全性的Meta分析

目的通过荟萃分析评价不含苯扎氯铵(BAK)的滴眼液治疗青光眼和高眼压症的有效性及安全性。设计荟萃分析。研究对象Medline(1966-2011年)、EMbase(1966-2010年)、Cochrane图书馆(2010年)及中国生物医学文献数据库CBM(1979-2010年)有关含与不含BAK的滴眼液治疗青光眼和高眼压症的临床对照研究文献资料。方法采用Cochrane系统评价的方法检索文献,按照纳入和排除标准限定研究对象,通过Jadad评分量表进行文献质量评估后,使用Cochrane协作网提供的RevMan 4.2统计软件进行Meta分析,以获得两者治疗青光眼和高眼压症的疗效及安全性是否有差异的相关证据。主要指标眼压,药物不良反应。结果纳入含与不含BAK的滴眼液治疗青光眼和高眼压症的临床对照研究6项(2313眼)。Meta分析结果显示,两类滴眼液均能有效降低眼压,两类滴眼液的降眼压幅度差异为0.08 mm Hg(95%CI,-0.10~0.27)(P=0.38)。随访期内发生相对较多的三种药物不良反应为结膜充血(10.98%)、过敏性结膜炎(4.84%)和干眼(3.11%)。采用固定效应模型进行Mete分析,用两类滴眼液者发生结膜充血、过敏性结膜炎和眼干的合并比值比分别为1.37(95%CI,1.05~1.80)、2.1(95%CI,1.26~3.48)和1.69(95%CI,1.13~2.53)(P<0.05)。结论不含BAK的滴眼液降眼压效果与含有BAK的滴眼液的差异无统计学意义且安全性更高,但尚需更多高质量的前瞻性临床对照研究进一步证实。     

胶原润眼液对新洁尔灭所致兔干眼症的治疗

目的评价胶原润眼液对防腐剂新洁尔灭所致兔干眼症的治疗效果。方法通过摘除兔眼泪腺,使用新洁尔灭制备干眼模型并应用胶原润眼液对其进行治疗。SchirmerI试验检测泪液分泌情况,并行虎红角膜染色、眼睑组织病理检查。结果与模型组相比,治疗组兔眼充血、水肿等术后症状较轻;虎红着色评分值第10天、第14天模型组均高于治疗组:模型组分别为(5.5±2.5)分、(5.9±1.8)分,治疗组分别为(2.6±1.5)分、(2.3±1.8)分,差异均有统计学意义(P<0.05,P<0.01);治疗组给予胶原润眼液后第5天、第10天、第14天,模型组与治疗组SchirmerI试验滤纸湿长值差异均无统计学意义(均为P>0.05);治疗组较模型组兔眼角膜上皮细胞层次增多,内皮层细胞空泡变性减少;眼睑内皮下血管扩张充血程度和腺体增生程度均较轻。结论胶原润眼液对防腐剂新洁尔灭所致的兔干眼症具有一定的缓解和治疗作用。     

HPLC法测定稀苯扎溴铵溶液中苯扎溴铵含量

目的 建立HPLC测定稀苯扎溴铵溶液中苯扎溴铵含量的方法.方法样品：自制0.1%稀苯扎溴铵溶液;色谱柱：以Agilent C18（5 μm,4.6 mm×250 mm）为色谱柱,流动相：0.02 mol/L庚烷磺酸钠溶液（含0.1%三乙胺,用磷酸调pH至3.45±0.10）-乙腈（35：65）;流速1.0 ml/min,检测波长210 nm,进样量10 μl.结果苯扎溴铵在39.8~238.6 μg/ml范围内时,与峰面积呈良好的线性关系（r=1.0000）,平均回收率为97.44%.结论 HPLC测定苯扎溴铵含量的方法简便,灵敏度高,重复性好,可用于稀苯扎溴铵溶液中苯扎溴铵的含量测定.     

羊膜凝胶对大鼠干眼的治疗作用及其作用机制

目的 通过局部应用苯扎氯铵(benzalkonium chloride,BAC)建立大鼠干眼模型,观察羊膜凝胶对大鼠干眼的治疗作用。方法 随机选取25只健康Wistar大鼠制作干眼动物模型后,随机分为干眼对照组(A组)、溶剂治疗组(B组)、羊膜提取液组(C组)、羊膜凝胶组(D组)和人工泪液治疗组(E组),另取5只大鼠作为正常对照组。每组治疗前后分别检测大鼠干眼指标,包括泪液分泌试验、泪膜破裂时间及角膜荧光染色评分。治疗4周后收集大鼠眼组织标本行病理及生化检测,包括角膜HE染色、PAS染色、免疫组化染色及TUNEL试验。结果 随着治疗时间的延长,羊膜匀浆提取液及羊膜凝胶均可改善大鼠干眼状况。治疗4周后D组大鼠的各项干眼指标相对于B组均有明显好转,干眼治疗效果明显优于E组(P<0.05)。另外,羊膜凝胶可使干眼大鼠的角膜上皮平整规则,角膜上皮K10表达下调,增加角膜MUC1 的表达,有助于维持泪膜稳定性。结论 羊膜凝胶可通过维持角膜上皮完整性,抑制角结膜鳞状上皮化生,促进结膜杯状细胞增殖、黏蛋白分泌而减轻干眼的病理损伤,从而缓解干眼的症状,具有治疗大鼠干眼的效果。     

Revisiting Ocular Allergy: Evaluating Symptoms,Benzalkonium Chloride and Efficacy of Topical Ketotifen 0.025%

ABSTRACT

This interesting study raises a scientific issue for revisiting three important elements on diagnosis, use of preservatives and selection of the appropriate topical treatment. Itchy feeling can be encountered in other ophthalmic conditions misdiagnosed as allergy, benzalkonium chloride is responsible for surface toxicity resulting in reduced efficacy and tolerability of topical allergy medications and it should be avoided on the management of ocular allergy. Unpreserved ketotifen 0,025% has been shown to be the least toxic formulation being the optimum option for efficacy and tolerability on the management of ocular allergy.     

Antistatic treatment for reducing airborne contamination of insulating materials in intensive care

In an effort to reduce airborne contamination by Staphylococcus epidermidis harboured on emitted skin scales, items used in patient care were studied as regards bacterial contamination and electrical resistance. An alcoholic benzalkonium chloride sodium was used to coat stopcocks, latex drains, silicon drains and plastic covering. Static electricity did not accumulate when the insulating resistance was less than 10(9) to 10(10) ohms. Study items not treated with the antistatic solution had resistances of greater than 2 x 10(12) ohms, which decreased to 2 x 10(6) to 8 x 10(10) ohms following antistatic treatment. The resistance of the silicon drain before and after antistatic exposure remained unchanged; an increase in its weight after treatment suggests absorption rather than the solution adhering to its surface. Statistically significantly lowered aerobic bacterial colony counts occurred from study items antistatistically treated as compared to those items left untreated. The coating of an entire room and its metal contents failed to decrease bacterial contamination. The results suggest that coating of insulating objects with an antistatic solution will reduce electrical resistance and thereby airborne bacterial contamination.