Comparative clinical trial to study the efficacy of Yashtimadhu Ghrita Application with Zytee mouth gel (Cholinsalicyclate and Benzalkonium chloride) in management of Mukhpaka in Children with special reference to Apthous stomatitis.

开始日期2022-04-04

申办/合作机构-

NCT03686904 / Completed临床4期IIT

Investigating the Effect of an Anti-Biofilm Solution to Reduce Bacterial Burden and Accelerate Healing in Chronic Wounds.

This is a prospective, randomized, double-blinded, single site study examining the impact of a biofilm-based treatment of chronic wounds of the lower extremity. 200 subjects will be enrolled in this study. Benzalkonium solution wound irrigation and Benzalkonium wound gel will be compared to standard of care wound preparation and dressing (NS wound irrigation and hydrocolloid gel) following local debridement. Wounds will be assessed maximum of 12 weeks with a minimum of 4 follow up visits. Patients will be recruited from the general wound clinic population. No enticement will be offered and participation will be completely voluntary. At enrollment and at each follow up visit the wound will be assessed for size (length, width, and depth), signs of infection or irritation, qualitative and quantitative cultures will be taken before and after debridement, patients will be assessed for compliance to the treatment protocol, satisfaction with their treatment, any adverse effects of the treatment, and hospitalizations since last assessment. It is anticipated that enrollment and completion of the study will take 1 year.

开始日期2018-11-19

申办/合作机构

Georgetown University

[+1]

EUCTR2016-004188-38-FR / Not yet recruiting临床4期

Contraceptive Efficacy, Tolerance and Acceptability of A Benzalkonium Chloride Spermicide Cream In Women Aged Over 40 Years of Age - PHASE IV, INTERNATIONAL, OPEN-LABEL, MULTICENTRE, PROSPECTIVE STUDY - BZK40+

开始日期2017-12-14

申办/合作机构

Laboratoire Innotech International SAS

100 项与苯扎氯铵相关的临床结果

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100 项与苯扎氯铵相关的转化医学

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100 项与苯扎氯铵相关的专利（医药）

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项与苯扎氯铵相关的文献（医药）

2024-06-01·Biofilm

Multi-species biofilms of environmental microbiota isolated from fruit packing facilities promoted tolerance of Listeria monocytogenes to benzalkonium chloride

Article

作者: LaBorde, Luke F ; Kovac, Jasna ; Voloshchuk, Olena ; Rolon, M Laura ; Bartlett, Katelyn V

Listeria monocytogenes may survive and persist in food processing environments due to formation of complex multi-species biofilms of environmental microbiota that co-exists in these environments. This study aimed to determine the effect of selected environmental microbiota on biofilm formation and tolerance of L. monocytogenes to benzalkonium chloride in formed biofilms. The studied microbiota included bacterial families previously shown to co-occur with L. monocytogenes in tree fruit packing facilities, including Pseudomonadaceae, Xanthomonadaceae, Microbacteriaceae, and Flavobacteriaceae. Biofilm formation ability and the effect of formed biofilms on the tolerance of L. monocytogenes to benzalkonium chloride was measured in single- and multi-family assemblages. Biofilms were grown statically on polystyrene pegs submerged in a R2A broth. Biofilm formation was quantified using a crystal violet assay, spread-plating, confocal laser scanning microscopy, and its composition was assessed using amplicon sequencing. The concentration of L. monocytogenes in biofilms was determined using the most probable number method. Biofilms were exposed to the sanitizer benzalkonium chloride, and the death kinetics of L. monocytogenes were quantified using a most probable number method. A total of 8, 8, 6, and 3 strains of Pseudomonadaceae, Xanthomonadaceae, Microbacteriaceae, and Flavobacteriaceae, respectively, were isolated from the environmental microbiota of tree fruit packing facilities and were used in this study. Biofilms formed by Pseudomonadaceae, Xanthomonadaceae, and all multi-family assemblages had significantly higher concentration of bacteria, as well as L. monocytogenes, compared to biofilms formed by L. monocytogenes alone. Furthermore, multi-family assemblage biofilms increased the tolerance of L. monocytogenes to benzalkonium chloride compared to L. monocytogenes mono-species biofilms and planktonic multi-family assemblages. These findings suggest that L. monocytogenes control strategies should focus not only on assessing the efficacy of sanitizers against L. monocytogenes, but also against biofilm-forming microorganisms that reside in the food processing built environment, such as Pseudomonadaceae or Xanthomonadaceae.

2024-03-01·Journal of ethnopharmacology

Modified Danzhi Xiaoyao Powder (MDXP) improves the corneal damage in dry eye disease (DED) mice through phagocytosis

Article

作者: Yu, Yunfeng ; Jiang, Pengfei ; Tian, Sainan ; Qin, Gen-Yan ; Tan, Kang ; Peng, Jun ; Liu, Tingting ; Liu, Pei ; Peng, Qinghua

ETHNOPHARMACOLOGICAL RELEVANCE:

Modified Danzhi Xiaoyao Powder (MDXP) is a traditional Chinese medicine formula remedy for treating Dry Eye Disease (DED). It showed the function of dispersing stagnated liver Qi for relieving Qi stagnation and clearing heat, which can be effective in treating conditions such as Dry Eye Disease (DED) and irregular menstruation due to liver depression and fire transformation.

AIM OF THE STUDY:

This study investigated the mechanism of the effect of MDXP in mice with DED.

MATERIALS AND METHODS:

A DED model was induced in mice using chronic painful stimulation (tail clamping) in combination with Benzalkonium Chloride Solution drops administered in a dry box for 28 days. After modeling, the MDXP groups were given Chinese medicine with different dosages by gavage for 14 days. The following parameters were recorded in each group: body mass, anal temperature, tear secretion, tear film rupture time, and corneal fluorescein staining. Behavioral changes were evaluated by elevating cross-maze and open-field experiments. The levels of inflammatory factors serum tumor necrosis factor-α (TNF-α), interleukin 1β (IL-1β), fcγR-mediated phagocytosis pathway cell division control protein 42 homolog (CDC42), actin-related protein 2/3 complex subunit 2 (ARPC2), and actin-related protein 3 (ACTR3) were measured by using Enzyme-linked immunoassay (ELISA), immunohistochemical staining, and real-time fluorescent qualitative polymerase chain reaction (RT-qPCR).

RESULTS:

MDXP increased body mass and lowered body temperature, prolonged tear film break-up time, promoted tear secretion, repaired corneal damage, decreased horizontal and vertical scores, elevated percentage of open arm times and boom opening time percentage, and reduced the expression levels of inflammatory factors of TNF-α, IL-1β and pathway-related proteins CDC42, ARPC2, and ACTR3 in mice. MDXP also reduced the expression levels of inflammatory factors of TNF-α and IL-1β in human corneal endothelial cells (HCECs), mouse mononuclear macrophage cells (RAW264.7), and human myeloid leukemia mononuclear cells (THP-1).

CONCLUSIONS:

MDXP can relieve tension and anxiety, inhibit apoptosis, reduce phagocytosis, reduce the expression of pro-inflammatory factors, repair corneal damage, and improve the symptoms in DED mice. The mechanism of action may be through the fcγR-mediated phagocytosis pathway.

2024-03-01·Experimental eye research

Sialylated IVIg promotes clinical improvements in a rabbit dry eye model by regulating inflammatory cytokines

Article

作者: Choi, Hyeongjwa ; Yang, Seung-Woo ; Hwang, Han-Sung ; Lee, Sung-Vin ; Lee, Ha-Eun ; Baek, Hayeon ; Joo, Jin-Soo ; Kim, Seulki ; Kim, Joon-Young ; Kang, Young-Sun ; Lee, Sang-Won ; Park, Min

Dry eye disease (DED) is caused by a loss of homeostasis of the tear film, which results in visual disturbance, ocular surface inflammation and damage, and neurosensory abnormalities. Although it is prevalent in 5-50% of the global population, there are limited clinical options for its treatment. This study explored the potential use of human intravenous immunoglobulin (IVIg) and its enriched fractions of sialylation, sialylated IVIg (sIVIg), as a treatment for DED. Fifteen female New Zealand white rabbits were topically instilled with 0.2% benzalkonium chloride (BAC) twice daily for five consecutive days to induce experimental dry eye. Saline, 0.4% IVIg, or 0.04% sIVIg eye drops were instilled twice daily for 20 consecutive days. Clinical evaluations, such as non-invasive tear break-up time (NIBUT) and corneal fluorescein staining (CFS), were conducted. mRNA levels of mucin 4, mucin 16, TNF-α, IL-1β, MMP9, IL-10, TGF-β, and CD209 in rabbit conjunctival tissues were examined using reverse transcription polymerase chain reaction (RT-PCR) or quantitative RT-PCR (qRT-PCR). The relationships between CD209 family members in rabbits and various mammalian species were analyzed using a phylogenetic tree. IVIg or sIVIg treatment resulted in clinical improvements in the rabbit DED model. The inflammatory cytokines, TNF-α and IL-1β, were increased and mucin 4 and mucin 16, cell surface-associated mucins, were decreased in BAC-induced dry eye. Following IVIg or sIVIg treatment, inflammatory cytokines decreased, whereas the anti-inflammatory cytokine, IL-10, increased substantially. Moreover, a 10-fold lower sIVIg treatment dose resulted in prolonged IL-10 production, representing a significantly improved DED compared to IVIg. Furthermore, the expression of rabbit CD209 mRNA in the rabbit conjunctiva and its close relationship with primate homologs suggest that it may interact with IVIg or sIVIg to promote IL-10 expression, as previously described in humans. At a lower dosage, sIVIg showed a more efficient improvement in DED, making it a promising new candidate medication for DED.

项与苯扎氯铵相关的新闻（医药）

2024-05-30

·赛柏蓝

药大麦破局积雪草营销乱象，入局淡化痘印蓝海市场

当下，快节奏的生活方式，不规律的生活作息，使得痘肌人群日益增多，这在推动淡化痘印市场规模快速扩大的同时，也助推了淡化痘印市场竞争越发白热化，同质化问题凸显，行业乱象层出不穷。对此，药大麦携芙宁®积雪苷霜软膏与芙效宁®积雪苷片入局淡化痘印蓝海市场，旨在破局积雪草营销乱象，满足市场需求，提升消费者体验。祛痘市场迈向千亿淡化痘印精细化需求日益凸显当前，祛痘也已从众多消费者青春期的“苦恼”，转变为长期面临的肌肤问题。据青眼情报调研数据显示，在社交平台，“祛痘”关键词的热度增长迅速。由近半年关键词“祛痘”在抖音平台的搜索热度可以看出，消费者对“祛痘”关键词内容关注度呈波动上升趋势，且对比去年同期，热度同比增长404.39%。截至去年10月底，小红书平台的“怎样祛痘”话题总浏览量达11.51亿次。由此，给祛痘市场带来强劲的增长动力，2023年中国祛痘护肤品市场规模为864亿元，2017-2023年市场规模年均同比增速为7.3%，预计2025年中国护肤祛痘市场规模将突破950亿元。图源自《2024年祛痘产品市场趋势洞察报告》（以下简称“《报告》”）与此同时，消费者对于祛痘产品功效的需求也愈发多元化。调研显示，消费者并不满足于祛痘产品仅具有祛痘功效。据《报告》显示，近七成消费者不仅停留于当下的祛痘效果，也希望能够实现淡化痘印效果。由此可见，淡化痘印市场可见存在巨大潜力。专业淡化痘印品牌较少积雪草类目乱象层出不穷5月10日，由北京市药品监督管理局发布的北京市2023年第五期化妆品质量安全公告中的4批次不合格产品，有2批次为祛痘类产品。实际上，淡化痘印是祛痘赛道类产品一个老生常谈的话题，一直以来都存在假冒伪劣产品难以控制、产品五花八门、消费者难以选择合适的产品、行业竞争不规范等问题，这些问题都是行业内亟须解决的顽疾。从以往国家和各省市药监局发布的关于祛痘产品不合格的通告中来看，不乏存在水杨酸超标、添加禁用组分等情况，其中出现违禁添加是最为常见的现象之一。据了解，这是由于部分禁用组分具有一定的功效，例如抗生素（如上述黄体酮）的抑菌、抗微生物效果可以快速起到改善炎症、祛除红肿的作用，使消费者觉得产品“真实有效”。因此，一些商家为了追逐利益，常将其添加在祛痘类产品中使用。但实际上，违禁添加导致的淡化痘印类产品暴雷只是冰山一角，而因积雪草核心成分虚假宣传则是造成淡化痘印类产品不合格则成为企业上黑榜的又一原因。近年来，随着国民健康意识的增强，国内淡化痘印类产品朝着绿色、天然、无污染方向不断转型升级，消费者越来越青睐以植物活性成分为主的产品，植物提取物热度高涨，积雪草作为各大淡化痘印类产品的宠儿，是护肤界植物原料中当之无愧的“顶流”。据美业颜究院数据显示，在2021年-2023年9月近3年期间含积雪草提取物的备案产品数高达13万+件。据美丽修行大数据《2023年爆款功效成分榜单及趋势预测》显示，积雪草提取物入选2023年爆款功效成分榜单TOP3，热度持续上升。与此带来的行业乱象也层出不穷。在阿里巴巴和百度爱采购等商品批发平台，不同的积雪草成分，价格也是天壤之别。如含量10：1的积雪草提取物，1千克批发价格普遍低于100元；90%含量的积雪草苷或羟基积雪草甙，1千克的报价普遍高于10000元。这也不难理解，为何积雪草类产品大多添加的是积雪草提取物。不过，这并不意味着添加积雪草提取物的产品就更廉价。比如，有一些品牌出于商业机密的考虑，只会在成分表中标注“积雪草提取物”。但这也让行业的顽疾“概念性添加”有了较大生存空间。在部分积雪草类产品的成分表中，如果有效成分的含量小于1%，按规定可以不按添加量的顺序排列。所以，产品如果添加了多种含量均小于1%的积雪草相关成分，便无法通过排序推测各种成分含量的高低。比如，在某品牌的积雪草睡眠面膜中，尽管添加了多达5种积雪草核心成分——积雪草提取物、积雪草苷、积雪草酸、羟基积雪草酸和羟基积雪草甙。然而，在该产品备案成分表全部45种成分中，这几大积雪草相关成分分别排在第21、41、43、44及第45位。不过，诚如上述研发工程师所说，“不论产品添加了什么成分，添加了多少含量，但如果抛开起效浓度、成分间的协同效应或生产工艺等谈产品价值，都是耍流氓。至于怎么加、加多少，很多时候只能取决于品牌厂家的良心。”药大麦携高质积雪草修复系列产品入局品类市场在当下这个竞争激烈的市场，引领行业潮流、能够真正打动消费者的产品，无疑需要拥有卓越的品质和创新的理念。近日，药大麦凭借其高质积雪草修复系列产品（芙宁®积雪苷霜软膏与芙效宁®积雪苷片），吸引了市场的广泛关注，成为品类市场的一股清流。药大麦的芙宁®积雪苷霜软膏，以其独特的配方、高质量的原材料和高效的修复效果，逐渐赢得了消费者的广泛好评。其中，芙宁®积雪苷霜软膏的原料含有24%的积雪草苷，这一数字不仅远超同类产品，更是高于国家标准10%。这样的高含量，保证了其卓越品质，同时也为消费者带来了更好的使用体验。积雪草作为一种传统中草药，在中医理论中被誉为“生肌散”，具有促进肌肤再生、淡化痘印等多种功效。药大麦充分利用积雪草的这一特性，将其融入到芙宁®积雪苷霜软膏和芙效宁®积雪苷片产品中，使得产品不仅具备了高效的修复效果，更能够满足消费者对于肌肤护理的多元化需求。除了软膏产品外，药大麦还推出了口服的芙效宁®积雪苷片。口服药物+外用软膏这种创新的全方位修复产品组合，既能够充分发挥积雪草的内服效果，又能够通过外用软膏直接作用于肌肤，达到更好的修复效果。这种全方位的修复方案，无疑为消费者提供了更加便捷、高效的护肤。尽管淡化痘印市场呈一片蓝海之态，但目前在这场千亿赛道中，仍存在市场集中度不高的情况，尚未具有足够影响力的龙头企业。总的来说，该市场机遇与挑战并存，药大麦实力不容小觑。另外，值得一提的是，药大麦针对皮肤科用药问题，不仅仅局限于淡化痘印（芙宁®积雪苷霜软膏与芙效宁®积雪苷片）的产品，其旗下的以祛疣+提高免疫力为主的咪喹莫特乳膏和转移因子胶囊、以杀菌为主的苯扎氯铵溶液、以治疗灰指甲为主的盐酸阿莫罗芬搽剂、以治疗脱发为主的非那雄胺片、以治疗特异性皮炎为主的他克莫司软膏等产品，全方位布局“她经济”。药大麦作为行业新兴力量，已经形成了规模化的一站式、全渠道、全链路的需求挖掘、市场推广服务体系，这将助力其开拓皮肤科用药市场。未来，药大麦将投入大量精力参与到人才培养、品牌建设与市场拓展中，致力于成为中国最专业的药品线上推广商、运营商、大包商，期待与更多的高精尖人才、医药企业及其品牌在未来数字化经济环境下共建同进，继续为广大消费者提供更多优质的医药健康产品和服务，积极推动中国医药健康产业高质量前行，共话医药健康产业新格局。如您对以上业务感兴趣，欢迎您联系我们！合作联系：

临床研究

2024-03-25

·FiercePharma

Novo Nordisk, Actylis ink pact to supply antiseptic in parts of Europe

Novo Nordisk and U.S.-based Actylis made a pact to provide the antiseptic and disinfectant benzalkonium chloride to a number of countries in Europe. Novo Nordisk’s Pharmatech unit and U.S.-based Actylis, which manufactures and supplies raw materials for pharmaceuticals, inked a deal to provide the antiseptic and disinfectant benzalkonium chloride to a number of countries in Europe. Pharmaceutical grade benzalkonium chloride will be distributed by the two companies in Germany, Spain, Portugal, the U.K. and Ireland, according to a March 25 press release. The product is often used before surgeries or for wound care, according to the Cleveland Clinic. It can also be used as an antimicrobial preservative for pharma products. Financial terms of the deal weren’t disclosed. “This new agreement, built on our existing partnership in North America, represents a major opportunity for Actylis Europe to complete our pharmaceutical product portfolio while supporting the development of Novo Nordisk Pharmatech BKC for new applications,” Ian Jenning, an Actylis senior vice president, said in the release. The name Actylis is fairly new to the manufacturing game, having been cobbled together by chemical supplier Aceto and 10 other companies in 2022. Prior to the launch two years ago that was initiated by CEO Gilles Cottier, Aceto spent more than 70 years as a source and supplier in the industry. Last September, Novo Nordisk, which is known for its blockbuster drugs Ozempic and Wegovy, signed a production agreement with South Africa’s Aspen Pharmacare to expand insulin supplies with a goal of reaching more than 500,000 diabetes patients in sub-Saharan Africa. More recently, Novo Holdings, which operates under Novo Nordisk’s owner the Novo Nordisk Foundation, agreed to pay $16.5 billion to snap up contract manufacturing giant Catalent. The deal is one of the driving forces behind the seismic changes in the CDMO industry right now. As part of that deal, Novo Nordisk plans to buy three large Catalent facilities for $11 billion.

引进/卖出

2024-03-03

·药渡

鼻腔药物递送全揭秘，优势与挑战知多少？

来源：药渡撰文：哥哈骎编辑：维他命鼻腔喷雾可用于鼻腔局部或全身给药。它们在局部用于治疗鼻塞和过敏性鼻炎等疾病。在某些情况下，鼻腔给药途径也可以是全身治疗的首选，因为它提供了一种可以替代注射给药的有效方法。药物活性物质可以非常迅速地直接通过鼻子吸收。许多全身给药的药物以鼻喷雾剂的形式存在，常用于镇痛剂、偏头痛、骨质疏松症和恶心等适应症的治疗。其他应用于包括激素替代疗法、阿尔茨海默病和帕金森病的治疗。鼻腔喷雾剂被视为一种更有效的药物运输方式，有可能穿过血脑屏障（Blood Brian Barrier）给药。图1. 鼻腔结构示意图，来源：NanoPharma1鼻腔给药的优势及受重视原因鼻腔给药对于某些适应症来说具有其它给药途径不具备的优势，例如对于COVID-19病毒，鼻腔给药可以将药物活性分子递送到感染/作用的主要部位。鼻腔的脉管系统通常有利于全身递送，尤其有利于粘膜抗体的递送。除此之外，鼻腔给药是非侵入性的，相对于注射给药可以享有更高的患者接受度和依从性，同时同样避免了胃肠道中的首过代谢。由于多种因素的共同作用，鼻腔给药领域成为了制剂领域重要的给药途径。首先，COVID-19产生了重大影响。鼻腔途径是病毒的主要进入点，因此人们对开发经鼻递送的预防剂和疫苗产生了相当大的兴趣。这使得研发者将注意力集中在缓释配方上，以确保更持久的保护，以及抗体和其他生物制剂的递送，而不单单是关注药物活性中间体。鼻用疫苗提供了粘膜免疫的可能，以补充肌肉注射疫苗提供的全身免疫。第二个重要的驱动因素是“鼻子到大脑”递送途径，对于解决大脑和中枢神经系统（CNS，central nervous system）疾病的有效性。鼻腔给药具有对中枢神经系统较高的生物利用度，以及较低的全身血液浓度方面的优势。这些优势可以保障最小的副作用，以及良好的药效。血脑屏障（BBB, blood brain barrier）在阻止大多数药物和几乎所有生物制剂通过方面非常有效，然而鼻腔给药可以克服这种限制，从而实现许多新的疗法。第三个因素是快速救援，鼻腔药物递送充分利用鼻腔丰富的脉管系统，相对于静脉注射实现快速起效的优势，而且使用方法更为简易，利于紧急情况下的快速救援。综合以上优势，鼻用药物开发项目快速增加。研究者对于如何最好地传递蛋白质、抗体、疫苗甚至mRNA的理解，在广度和深度两个维度都得到了拓展。纳米颗粒的制剂技术在制药行业正变得越来越普遍，该技术的进步同时也在推动鼻腔给药的发展。然而，对于鼻用药物产品，学术界和工业界还没有建立起完美的体外体内相关性，并且在赋形剂方面仍然相对受限。2鼻腔给药的关键质量特性鼻腔给药的关键挑战包括：靶向最佳治疗区域、防止渗透到肺部、避免刺激鼻粘膜、确保足够的保留时间、粘液纤毛清除等。鼻用药物产品是“组合”产品，其性能由设备和制剂之间的相互作用决定。设备的选择通常受以下因素的影响：应用（例如疫苗）、目标患者群体、无防腐剂给药的要求以及商业限制。喷雾设备在结构材料、内部几何形状和防止微生物污染的特征方面需要着重考虑。从制剂的角度考虑，关键质量特性（CQA，Critical Quality Attributes）包括pH、渗透压和流变特性。递送的颗粒或液滴尺寸是关键，因为它对体内行为产生重要影响。对于液体制剂来说，需要控制的一个关键质量属性是总体渗透压，它通常需要保持在290~500 mosm/kg范围内，以避免鼻粘膜刺激，但对于紧急情况或一次性应用等特殊情况，渗透压的最高限值可以适当放宽。除此之外，液体制剂的pH值也需要严格控制，因为它会影响局部耐受性，并且可能对药物稳定性来说至关重要。通常情况下，微酸性的pH值是最佳的。鼻用药液体制剂的流变学特性，尤其是粘度，对于雾化性能和鼻腔中的沉积起着极为关键的影响作用，它能够直接影响喷雾液滴大小，对于药物保留也可能至关重要。因为，鼻腔黏膜纤毛清除机制在清除异物方面发挥重要作用，因此药物化学家可能需要通过流变学角度，以及使用黏膜粘合剂的手段来抵消它们的影响。递送液滴的大小会影响体内沉积，因此在制剂过程中需要并对其进行严格控制，以促使液滴在目标部位沉积，并最大限度地减少可引起毒性作用的肺部递送。3鼻腔给药面临的问题与挑战在递送生物制剂时，粘液纤毛清除是一项主要挑战，它可以在生物药物被吸收之前就将其粗暴地清除。所谓的生物药物，指的是蛋白质、肽、抗体和核酸分子等，它们比传统的小分子药物大得多，并且膜通透率很低，因此较难实现有效吸收或延长治疗效果。此外，粘液由较长的疏水性多肽分子组成，通常与含亲水性蛋白质不相容。这些生物大分子固有的不稳定性，也是制剂中不可忽略的重要因素。生物制剂可能会因静电、酶促作用和雾化过程中的剪切作用而分解、聚集从而失去活性。塑料表面容器对于蛋白质的吸收，也是一个公认的问题。鼻腔给药制剂面对的第一个选择是粉末还是液体制剂？鼻用粉末不太常见，但这种制剂方法却具有一些明显的优势，特别是在用递送高剂量的药物和药品运输方面优势明显。另一方面，液体制剂往往起效更快，因为其省略了体内溶解的环节，通常是生物制剂更容易选的解决方案。省略了具有挑战的冻干或喷雾干燥工艺环节，因此能够更快地实现生产工艺的开发。对于液体制剂来说，可以通过添加诸如粘度调节剂、粘膜粘附聚合物、缓冲剂和防腐剂等赋形剂，来控制制剂的性能。粉末制剂除了活性药物之外，通常含有载体物质，例如乳糖、甘露醇或羟丙基甲基纤维素 (HPMC) （载体的选择相对较少），载体物质与活性药物成分混合或共喷雾干燥。在某些情况下，额外的赋形剂可用于不同用途，例如优化喷雾干燥过程，以控制极小颗粒的比例，从而减少药物在肺部的沉积可能。粉末颗粒的大小和形状是至关重要的，因为这些参数将高度影响剂量分散。需要注意的是，在配制生物制剂时，防腐剂经常会起到反作用。比如苯扎氯铵（图1）是最广泛使用的鼻腔喷雾防腐剂，但它可能会导致蛋白质从溶液中沉淀出来。图2. 苯扎氯胺化学结构式药物吸收当然是关系到鼻腔喷雾制剂成败的重中之重。药物的有效吸收是药效的关键，但目前的技术发展尚难确定，药物到底是直接输送到大脑还是通过全身系统循环。将这两种体内途径区别分析是一项困难的研究内容。相比之下，赋形剂直接被大脑吸收是需要避免的情况，防止非活性成分不必要的吸收对于鼻腔喷雾制剂的开发同样重要。4鼻腔喷雾未来发展的技术重点面对首当其冲的黏液纤毛清除挑战，以及持续释放和药物保留的要求，鼻腔喷雾药的发展方向首先指向了更先进和复杂的制剂配方。另一方面，通过控制液滴的大小来促进药物输送，以及开发无防腐剂的喷雾产品同样取决于制剂配方与喷雾剂的设备。扩展赋形剂的选择范围，尤其是选择更好的黏膜粘合剂和渗透增强剂，将对鼻腔喷雾药的药效产生深远影响。但在实现这些愿景之前，研究者需要首先建立更强大的体外工具，特别是评估黏液和制剂之间的体内相互作用。在实现这些基本的要求之前，很难跨越性地深刻理解赋形剂的真正作用机理。可以说，目前在开发赋形剂方面的工作，在很大程度上是一种试错法的策略，如何将其引入QbD的模式也是研究者们未来需要努力的目标。除此之外，纳米技术的发展与鼻腔喷雾药物的进步也息息相关。纳米乳液、纳米颗粒和纳米胶束的应用，可以更有效地实现鼻腔药物递送的目标，但同时也要警惕这一技术可能带来的副作用，比如透增强剂等赋形剂的递送抵达脑部。5展望鼻腔喷雾未来的应用领域鼻腔疫苗未来可能会变得更加普遍，不仅适用于呼吸道病毒，还可能适用于艾滋病毒等其他疾病。此外，鼻对脑递送的制剂或许能够对帕金森氏疾病取得一定成果。生物制剂的兴起，对鼻腔给药的促进作用将越来越明显。未来更多的生物制剂将有可能通过这条递送路线实现其药用价值，有望提高人们应对包括慢性鼻炎、呼吸系统和中枢神经系统疾病在内的多种疾病的能力。参考文献：1. NanoPharma, Focusing on current trends and technical challenges associated with formulation, Apr. 20222. Lea-Adriana Keller et al. Intranasal drug delivery: opportunities and toxicologic challenges during drug development. Drug Deliv. Transl. Res. 2022, 12, 735-757.3. Wisam Al Bakri et al. Overview of intranasally delivered peptides: key considerations for pharmaceutical development. Expert Opin. Drug. Deliv.2018, 15, 991-1005.专栏作者哥哈骎南开大学本科、硕士，德国比勒菲尔德大学博士。多肽化学、多肽API GMP生产专家、欧洲制药公司首席科学家；拥有Lean Six Sigma黑带认证；著有专著《Side Reactions in Peptide Synthesis》。*声明：本文仅是介绍医药疾病领域研究进展或简述研究概况或分享医药相关讯息，并非也不会进行治疗或诊断方案推荐，也不对相关投资构成任何建议。内容如有疏漏，欢迎沟通指出！当多肽遇上抗体：抗体多肽偶联物Peptibody研发进展及前景展望盘点：2023年CDE发布药品注册指导原则及法规全景图国内首个「十亿美元分子」诞生记：从零到一→同类最佳→年销售额破十亿美元……

疫苗

100 项与苯扎氯铵相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00857	苯扎氯铵	D09AA11 R02AA16 D08AJ01	-

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
感染	日本	Fuji Yakuhin Co., Ltd.	1994-11-24
消毒剂	日本	Maruishi Pharmaceutical Co., Ltd.	1985-02-14

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ARVO2023	N/A	-	-	Benzalkonium chloride	淵範鹽鬱網夢鹹鏇簾鬱(築餘獵夢遞廠鹹鏇壓顧) = Topical administration of BAC following corneal abrasion in mice delayed corneal epithelial wound healing and impairs corneal stromal nerves, representing a model of neurotrophic persistent corneal epithelial defect. 鏇繭願簾製選築夢襯窪 (繭艱鹽鏇夢積製醖蓋壓 )	-	2023-04-23
ARVO Annual Meeting 2019 (ARVO2019)	N/A	干眼综合征	60	Topical BAC at concentrations ranging 0.05-0.2%	願範遞遞膚鹽襯構繭鑰(夢鹹餘餘艱夢衊襯壓顧) = 簾襯憲顧簾鹹觸繭廠襯鑰製積醖網鬱衊構襯齋 (窪選繭顧構鏇糧憲膚醖 )	-	2019-07-01
				benzalkonium chloride	製蓋蓋衊鹽觸艱顧鑰醖(憲願壓壓夢築顧簾鹹鬱) = 餘淵網遞選築齋構選獵憲範憲淵夢網獵膚築膚 (餘襯構鬱築壓餘蓋膚顧 ) 更多
ARVO Annual Meeting 2019 (ARVO2019)	N/A	-	-	0.1% RF + 0.01% BAK + 1% methylcellulose	醖膚鑰齋憲淵廠鏇壓蓋(鹹鏇築蓋遞願願糧窪齋) = 網範壓餘鏇製範築範襯鹹鑰糧簾醖範築願製觸 (顧鑰壓範廠網顧淵選鏇, ±3.4)	-	2019-07-01
				0.5% RF + 0.01% BAK + 1% methylcellulose	醖膚鑰齋憲淵廠鏇壓蓋(鹹鏇築蓋遞願願糧窪齋) = 糧襯鹽壓衊襯醖窪簾憲鹹鑰糧簾醖範築願製觸 (顧鑰壓範廠網顧淵選鏇, ±45.8)
ARVO2012	N/A	-	-	Benzalkonium Chloride 0.002%	壓襯範鑰襯獵衊淵積鏇(衊簾艱憲範積夢構製鹽) = 衊襯鏇範壓鹽廠選糧鹹鑰選糧獵壓構築觸憲糧 (鹹簾憲願選夢糧築憲憲 )	-	2012-03-01
				Benzalkonium Chloride 0.003%	壓襯範鑰襯獵衊淵積鏇(衊簾艱憲範積夢構製鹽) = 廠衊淵遞鏇齋齋鹽餘糧鑰選糧獵壓構築觸憲糧 (鹹簾憲願選夢糧築憲憲 )
ARVO2009	N/A	-	3	0.02% benzalkonium chloride	獵選觸繭衊築鏇獵獵遞(觸艱觸鑰繭積艱齋糧糧) = After benzalkonium chloride exposure, superficial punctate keratopathy was observed; this epithelial change disappeared within 24 hours. 顧壓窪窪糧糧製餘醖餘 (蓋鑰淵獵顧壓齋鹹鬱醖 )	积极	2009-04-01
ARVO2008	N/A	C-reactive protein \| interleukins (IL)-1 \| IL-10 ... 更多	-	Benzalkonium Chloride	蓋積築窪鏇蓋觸積壓衊(壓築艱願糧鬱觸餘膚艱) = 積鑰糧憲壓簾襯簾憲餘獵衊範衊窪積衊衊觸觸 (蓋醖淵築鹽襯餘觸壓糧 ) 更多	-	2008-05-01
				H2O2	觸鑰願糧鹹壓蓋觸獵鬱(襯鏇蓋壓艱衊鬱構淵遞) = 製鹹壓鬱衊繭鏇鬱襯餘簾鏇積膚獵鏇鹽願壓構 (齋窪觸獵鹽襯齋範齋壓 )
AAO2007	N/A	青光眼	-	Topical glaucoma medications with BAK	糧觸選鹹鏇繭遞艱構鬱(選鑰構壓獵艱築膚壓願) = 鹹蓋憲範憲願糧壓構艱鑰築觸顧廠餘襯夢獵淵 (糧網壓齋獵齋製鑰糧鹽 )	-	2007-11-11
				Topical glaucoma medications without BAK	糧觸選鹹鏇繭遞艱構鬱(選鑰構壓獵艱築膚壓願) = 繭襯積遞製顧蓋願襯網鑰築觸顧廠餘襯夢獵淵 (糧網壓齋獵齋製鑰糧鹽 )
AAAAI2006	N/A	-	34	Saline spray with 0.01% BKC	憲鏇積鹹淵積壓積鏇繭(蓋衊範襯顧憲觸繭鑰鏇) = 範襯獵構蓋鹽廠築築膚鏇選觸膚糧範衊鏇鑰鹹 (構鑰鑰淵製獵鑰繭顧構 )	-	2006-02-01
				Saline spray without BKC	憲鏇積鹹淵積壓積鏇繭(蓋衊範襯顧憲觸繭鑰鏇) = 糧獵鹹鹹醖襯觸製窪選鏇選觸膚糧範衊鏇鑰鹹 (構鑰鑰淵製獵鑰繭顧構 )
ARVO2005	N/A	细菌性眼感染	-	Gatifloxacin	遞鹹築獵淵齋築艱餘構(願網餘糧網窪鹽鏇築壓) = 繭鏇範糧網顧憲鑰獵構壓壓淵繭積範範鏇鑰襯 (齋願鏇願積鬱齋築淵窪 )	-	2005-05-01
				Gatifloxacin with Benzalkonium Chloride	遞鹹築獵淵齋築艱餘構(願網餘糧網窪鹽鏇築壓) = 簾壓鑰顧壓願窪艱鏇網壓壓淵繭積範範鏇鑰襯 (齋願鏇願積鬱齋築淵窪 )
ARVO2002	N/A	-	11	0.5% Timolol Maleate with Preservative (0.005% Benzalkonium Chloride)	蓋積簾築鹽襯鏇艱壓築(築艱糧觸淵糧糧築艱艱) = 觸鹹顧繭網醖窪願淵憲鬱選觸糧鹽繭鏇構壓鏇 (顧衊積觸範製顧顧蓋憲 ) 更多	-	2002-12-01
				0.5% Timolol Maleate without Preservative	蓋積簾築鹽襯鏇艱壓築(築艱糧觸淵糧糧築艱艱) = 壓鹽網選廠鑰壓簾壓鑰鬱選觸糧鹽繭鏇構壓鏇 (顧衊積觸範製顧顧蓋憲 ) 更多