两种方法检测汰可分手消毒液杀菌效果的比较

为比较两种不同方法检测汰可分手消毒液的杀菌效果,采用悬液定量杀菌试验和载体浸泡定量杀菌试验对汰可分手消毒液进行了杀菌效果观察。结果,用含苯扎氯铵250 mg/L的汰可分手消毒液作用1 m in,对悬液中金黄色葡萄球菌、大肠杆菌杀灭率达到100%,对白色念珠菌的平均杀灭率为99.90%;对布片上金黄色葡萄球菌、大肠杆菌和白色念珠菌的平均杀灭率分别为99.89%、99.85%和99.65%。结论,两种检测方法对汰可分手消毒液杀菌效果检测存在差异,用悬液定量法检测的杀菌效果比载体定量法检测结果好。     

Ranking of surfactant skin irritancy in vivo in man using the plastic occlusion stress test (POST)

Irritant effects and disturbance of water-holding capacity induced by surfactants were investigated using the plastic occlusion stress test (POST) technique. 4 surfactants (sodium lauryl sulphate (SLS), sorbitan monolaurate, cocoamidopropyl betaine and benzalkonium chloride) and an amphoteric/nonionic (A/N) mix were investigated. 1 x daily for 3 days, test surfactants were applied to marked sites (open) on the volar forearm. After 24 h occlusion with a plastic chamber on the 4th day, skin surface water loss (SSWL) (g/m2h) was recorded continuously for 25 min with an evaporimeter. The differences between the surfactants were statistically significant (Friedman's test p less than 0.01). SLS and the A/N mix revealed significant differences compared to the other compounds (p less than 0.05), both in decay constants and in values recorded at the beginning and at the end of the decay curve. The study suggests a mechanism for the high irritant potential of sodium lauryl sulphate compared to other surfactants: sorbitan monolaurate and benzalkonium chloride seem to influence (at the concentrations tested) to a lesser extent the water-holding capacity of the stratum corneum. The clinical and biological relevance of these observations requires long-term clinical correlations with final product use tests.     

Development and characterization of different low methoxy pectin microcapsules by an emulsion–interface reaction technique

In the controlled release area, biodegradable microcapsules are one of the most useful devices to deliver materials in an effective, prolonged and safe manner. A new charged film microcapsular carrier system, using three different pectins, is described. The study utilized pectin microcapsules prepared by two encapsulation mechanisms of interfacial reaction explored through interaction of charged droplet–oil-anionic surfactant-calcium or oil-cationic surfactant with negatively charged pectin. A method for drug encapsulation was developed based on the type of pectin, surfactants and emulsification technique. Both types of surfactant, anionic sodium dodecyl sulphate (SDS) and cationic benzalkonium chloride (BzACl) promoted polymer film formation on the oil droplet surfaces, probably through cross-linking and electrostatic interaction, respectively. Microcapsules consisting of pectin as shell and hydrophobic oil as core were characterized. The resulting microcapsules were relatively small particles (d<3?µm), had high total particle number, specific surface area and drug encapsulation efficiency. They also demonstrated good stability with minimum particle aggregation. Correlation between physicochemical and drug release kinetic parameters were investigated with regard to the effect of pectin macromolecular structure and nature of surfactant used as a counterion in the manufacturing of microcapsules. The release rate of the encapsulated material (prednisolone) in three microcapsules can be controlled by manipulating the conformational flexibility of pectins in the presence of different counterions. As a result, biodegradable pectin microcapsules offer a novel approach for developing sustained release drug delivery systems that have potential for colonic drug delivery.     

Ophthalmic preservatives: focus on polyquaternium-1

Introduction: Ophthalmic preservatives, such as polyquaternium-1 (PQ-1), are critical for the inhibition of growth of microbial contaminants in multi-dose bottles of topical medications. These antimicrobial agents must have a high efficacy against pathogenic organisms, while maintaining a favorable tolerability and safety profile.

Areas covered: This review focuses on the ophthalmic preservative PQ-1. For comparison purposes, the most commonly used preservative, benzalkonium chloride (BAK), is also discussed. This survey focuses primarily on data collected during the past 10 years.

Expert opinion: Effective drug delivery requires more than just an active ingredient that achieves its desired biological effect on end-target tissues. In addition, drugs must be stable in the containers that they are stored in, and must possess minimal undesired local and systemic side effects that can cause patients to decrease their adherence. In addressing these concerns, specifically in topical ophthalmic drops, one must take into account the active ingredients, vehicle components and preservatives. Medications with fewer adverse effects may lead to enhanced adherence to therapy; therefore, the induction of such adverse outcomes must be considered by physicians when treating patients with chronic ocular disease. Although BAK will continue to be used in ophthalmic medications, due to its familiarity and compatibility with a broad range of topical ocular formulations, PQ-1 is certainly a viable alternative in the preservative formulary armamentarium.     

Is the irritant benzalkonium chloride a contact allergen? A contribution to the ongoing debate from a clinical perspective

Background:  Benzalkonium chloride (BAC) is a well-recognized irritant. However, doubts exist that it is also a contact allergen.
Objective:  Analysis of clinical patch test data addressing the reaction profile and synchronous reproducibility of BAC 0.1% in petrolatum (pet.) and possible increases in risk of BAC contact allergy in certain (occupationally exposed) subgroups.
Patients /Methods:  Data of 42 898 patients tested with BAC 0.1% in pet. in 3 different series (topical drugs, ophthalmics, and disinfectants) in the departments of the Information Network of Departments of Dermatology ( http://www.ivdk.org ) between 1996 and 2006 was analysed.
Results:  Overall, morphologically 'positive' reactions were rare, 0.6–1.5%, with a total of 41 stronger positive reactions. Concordance, assessed in 3322 patients tested in duplicate, was low (kappa coefficient 0.15, 95% CI: 0–0.31). Positive test reactions were observed significantly more often in the disinfectants series compared with the 2 other series, indicating that suspected exposure to disinfectants may be associated with sensitization. However, variation of stronger BAC test positivity across potentially relevant (occupational) groups was non-significant.
Conclusion:  This analysis of routine clinical data and a number of previous reports add further, if weak, evidence to the notion that BAC is a contact allergen, albeit a very rare one.     

Comparative efficacy of topical antihistamines in an animal model of early phase allergic conjunctivitis

In order to compare the relative efficacy of topical antihistamines with balanced saline solution (BSS) and benzalkonium chloride (BC) in the early phase of allergic conjunctivitis in an animal model of ocular anaphylaxis, 96 male guinea pigs were sensitized with intraperitoneal egg albumin (EA) and aluminum hydroxide. Seventy-six animals were used for determination of Evans blue (EB) extravasation and 20 for clinical evaluation of the allergic response (redness, edema, discharge and itch-scratch response). Eighteen days after sensitization the animals were topically challenged by conjunctival instillation of EA and treated 15 min before and 15 min after challenge with commercially available drugs (ketotifen, ketotifen single dose units [SDU], olopatadine, azelastine, spaglumic acid and emedastine) and controls (BSS and BC). The animals used for EB quantification were anesthetized and received an intravenous injection of EB simultaneously to the topical challenge. The ocular extravasation of the colorant was determined by 620 nm absorbance spectrophotometry. The animals used for clinical evaluation were observed for clinical signs of the allergic reaction. EB ocular extravasation was significantly lower in the eyes treated by spaglumic acid and emedastine. The clinical scoring was consistent with EB extravasation, though the difference was not statistically significant. Spaglumic acid and emedastine seem to be the most useful drugs to reduce EB extravasation and allergic signs in an animal model of early phase allergic conjunctivitis.     

Topical effect of benzalkonium bromide on wound healing and potential cellular and molecular mechanisms

Benzalkonium bromide (BB) has been widely used as a skin antiseptic for wound management. However, BB had proinflammation and reactive oxygen species (ROS) induction effect, making its role in wound healing complex and unclear. A rat full‐thickness skin defect wound model was established. The effects of BB, povidone iodine (PVP‐I), chlorhexidine gluconate (CHG), and normal saline (NS) on wound healing and infection control were then evaluated based on wound healing rate (WHr) and bacterial killing. The wound tissues were sectioned for histopathological evaluation and nuclear factor E2 related factor 2 (Nrf2) expression determination. The ROS production, Nrf2 activation, and heme oxygenase 1 (HO‐1) expression of the HaCat cells and the cytotoxicity treated with BB were further explored. Compared with NS, PVP‐I, and CHG, BB showed the best wound infection control efficiency while delayed wound healing with the WHr of 91.42 ± 5.12% at day 20. The wound tissue of the BB group showed many inflammatory cells but few granulation tissue and capillaries and no obvious collagen deposition, resulting in the lowest histopathological scores of 4.17 ± 0.75 for BB group. BB showed higher cytotoxicity on HaCat cells with the lowest IC25, IC50, and IC75 of 1.90, 4.16, and 9.09 g/mL compared with PVP‐I and CHG. TUNEL staining evaluated the cytotoxicity of BB on wound tissue, which indicates the high apoptosis index BB group (5.05 ± 1.77). Compared with PVP‐I and CHG, BB induced much more cell apoptosis. The results of flow cytometry and fluorescence staining showed that PVP‐I, CHG, and BB induced ROS production in a concentration‐dependent manner and cells treated with BB had the highest ROS production at the same inhibition concentration. The cells and the wound tissues treated with BB showed highest Nrf2 activation and HO‐1 expression than PVP‐I and CHG. BB was highly efficient in wound infection control while delayed wound healing. The prolonged and strengthened inflammation and the raised ROS production originating from BB administration may contribute to delayed wound healing.     

不同浓度人血清滴眼液治疗重症干眼大鼠的实验研究

目的 探讨不同浓度人血清滴眼液在重症干眼大鼠中的治疗效果.设计实验研究.研究对象 Sprague-Dawley （SD）大鼠28只.方法 28只健康成年雄性SD大鼠,随机分为正常对照组（n=4）,重症干眼组（n=24）,使用0.2%苯扎氯铵溶液点眼1周制作重症干眼模型.然后将重症干眼大鼠随机分为阴性对照组（n=6）,20%血清组（n=6）,50%血清组（n=6）,100%血清组（n=6）,使用相应浓度的血清滴眼液治疗28天,观察各组大鼠在制模后第0、7、14、21、28天的泪液分泌情况和眼表的改变.主要指标应用Schirmer试验、角膜荧光素染色、结膜印迹细胞学检查干眼程度.结果 重症干眼组与正常组大鼠各观察指标的差异有统计学意义,其中Schirmer试验（2.12±1.50 mm vs 8.67±2.36 mm,P=0.000）,角膜荧光素染色分级（4.0 vs 0.33±0.58,P=0.008）.结膜印迹细胞学分级（1.76±0.52 vs 0.33±0.58,P=0.000）.20%血清组大鼠较阴性对照组在第7、21天泪液分泌增ta（P=0.003,0.035）;第7、14、21、28天角膜荧光素染色减轻（P=0.001,0.006,0.021,0.001）;第14、21、28天印迹细胞学分级减轻（P=0.015,0.002,0.01）. 50%血清组较阴性对照组在第7、14、28天角膜荧光素染色减轻（P=0.025,0.023,0.004）;第14天印迹细胞学分级减轻（P=0.046）. 100%血清组较阴性对照组在第28天角膜荧光素染色减轻（P=0.021）,余差异无统计学意义（P〉0.05）.结论 不同浓度人血清滴眼液均有助于重症干眼大鼠角膜上皮的修复,其中20%的人血清滴眼液效果最理想,可以增加泪液分泌,减轻结膜和角膜上皮的损害.     

omega-3治疗大鼠干眼的实验研究

目的　探讨ｏｍｅｇａ-３治疗苯扎氯铵诱导的大鼠干眼的疗效及其可能机制。方法　４５只６～８周龄ＳＤ大鼠,随机分为３组,每组１５只。生理盐水组用生理盐水灌胃,橄榄油组用橄榄油灌胃,ｏｍｅｇａ-３组用ｏｍｅｇａ-３灌胃,连续２个月。２个月后,３组分别接受１５ｄ的苯扎氯铵诱导干眼,干眼诱导期间大鼠灌胃同前。在干眼诱导当天、第５天、第１０天、第１５天观察泪液分泌量、泪膜破裂时间（ｔｅａｒｂｒｅａｋ-ｕｐｔｉｍｅ,ＢＵＴ）和角膜荧光素染色评分,干眼诱导第１５天行大鼠角膜和结膜组织的ＨＥ染色。结果　干眼诱导第１５天ｏｍｅｇａ-３组泪液分泌量比橄榄油组和生理盐水组明显增多,差异均有统计学意义（Ｐ＝０．０２３、０．０２７）。干眼诱导第１０天、第１５天ｏｍｅｇａ-３组ＢＵＴ较橄榄油组和生理盐水组明显变长,差异均有统计学意义（均为Ｐ＜０．０５）。干眼诱导第１５天ｏｍｅｇａ-３组角膜荧光素染色评分比橄榄油组和生理盐水组明显减少,差异均有统计学意义（Ｐ＝０．０１２、０．０１５）。干眼诱导第１５天ｏｍｅｇａ-３组角膜、结膜组织与正常角膜、结膜组织相似。橄榄油组和生理盐水组角膜上皮细胞层次明显增加,表层细胞不规则缺失,基底细胞排列紊乱,基质层少许水肿;结膜上皮结构不完整,排列不规则,结膜上皮细胞增生,基底层细胞排列不整齐,可见炎性细胞浸润。结论　ｏｍｅｇａ-３能有效抑制泪液分泌量,增强泪膜稳定性,保护角膜和结膜组织。