Picloxydine
(Synonyms: 哌氯定) 目录号 : GC32369
Picloxydine是抗细菌(antibacterial)和牙菌斑活性的杂环双胍。
Cas No.:5636-92-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity.
0.4% Picloxydine produces a highly significant drop in the number of aerobic organisms. 0.4% Picloxydine is far more effective than 0.2% Picloxydine or chlorhexidine in reducing the total viable count of oral aerobic and anaerobic organisms[1]. Picloxydine is also used in eye drops in the topical therapy of trachoma[2].
[1]. Newcomb GM, et al. An in vivo comparison of chlorhexidine and picloxydine mouthrinses: a possible association between chemical structure and antiplaque activity. J Periodontol. 1977 May;48(5):282-4. [2]. Obikili AG, et al. A double-blind comparison of picloxydine dihydrochloride (Vitabact eye drops) and sulfacetamide eye drops in the topical therapy of trachoma. Rev Int Trach Pathol Ocul Trop Subtrop Sante Publique. 1988;65(3-4):119-32.
| Cas No. | 5636-92-0 | SDF | |
| 别名 | 哌氯定 | ||
| Canonical SMILES | N=C(N1CCN(C(NC(NC2=CC=C(Cl)C=C2)=N)=N)CC1)NC(NC3=CC=C(Cl)C=C3)=N | ||
| 分子式 | C20H24Cl2N10 | 分子量 | 475.38 |
| 溶解度 | DMSO : 11.36 mg/mL (23.90 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1036 mL | 10.5179 mL | 21.0358 mL |
| 5 mM | 0.4207 mL | 2.1036 mL | 4.2072 mL |
| 10 mM | 0.2104 mL | 1.0518 mL | 2.1036 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[Antibacterial effect of the antiseptic Picloxydine dihydrochloride on conjunctival isolates of gram-negative bacteria]
Vestn Oftalmol 2021;137(5. Vyp. 2):238-247.PMID:34669333DOI:10.17116/oftalma2021137052238.
The preoperative and postoperative use of antiseptics can be an alternative to antibiotics in repeated courses of anti-VEGF therapy for reducing the risk of developing antibiotic resistance in eye microflora. Among gram-negative bacteria, the most frequently isolated pathogen that causes eye infections is Pseudomonas aeruginosa, which is characterized by reduced sensitivity to antibiotics and disinfectants. Purpose: To study the effect of the antiseptic Picloxydine dihydrochloride on the gram-negative bacteria Escherichia coli, Pseudomonas luteola and P. aeruginosa isolated from the conjunctiva. Material and methods: The identification of bacterial isolates and study of their sensitivity to antibiotics were carried out using the automated bacteriological analyzer BD Phoenix 100. To determine the bactericidal concentration, the method of serial dilutions of the antiseptic in a liquid nutrient medium was used. The binding of cationic molecules of Picloxydine dihydrochloride to bacterial cells was detected by neutralizing the bacterial surface with increasing amounts of antiseptic, and measuring the zeta potential on the Zetasizer Nano ZS analyzer. The ultrastructure of bacterial cells was studied using the two-beam scanning ion-electron microscope Quanta 200 3D. Results: The most resistant was P. aeruginosa. The interaction mechanism of Picloxydine dihydrochloride with bacterial cells includes electrostatic binding of positively charged antiseptic molecules to negatively charged cell walls. Picloxydine dihydrochloride has a destructive effect on the bacterial cell wall and plasma membrane, which leads to cell lysis and release of intracellular components. Conclusion: Picloxydine dihydrochloride exhibits bactericidal activity against gram-negative conjunctival isolates and is promising for preventive use during repeated courses of intravitreal injections.
Ocular flora in patients undergoing intravitreal injections: antibiotic resistance patterns and susceptibility to antiseptic Picloxydine
Int J Ophthalmol 2020 Jan 18;13(1):85-92.PMID:31956575DOI:10.18240/ijo.2020.01.13.
Aim: To study antibiotic resistance patterns and susceptibility to eye antiseptic Picloxydine of conjunctival flora in patients undergoing intravitreal injections (IVIs). Methods: Conjunctival swabs were taken in 4 groups of patients, 20 patients in each group (n=80): without IVIs and ophthalmic operations in history (group N1; control group); with the first IVI and antibiotic eye drops Tobrex applied 3d before IVI and 5d after it (group N2); with 20 or more IVIs and repeated courses of antibiotic eye drops (group N3); with the first IVI and antiseptic eye drops Vitabact (Picloxydine) applied 3d before IVI and 5d after it (group N4). In groups N2 and N4 swabs were taken at baseline and after the treatment. Efficacy of Picloxydine in inhibition of growth of conjunctival isolates susceptible and resistant to antibiotic was studied in vitro. Minimal inhibition concentrations (MIC) were determined with microdilution test. Results: Two of the three patients who had to undergo the IVI procedure showed conjunctiva bacterial contamination. Along with few Staphylococcus aureus and Gram-negative isolates susceptible to most antibiotics, the majority (71%-77%) of causative agents were coagulase-negative Staphylococci (CoNS), 40%-50% of which were multidrug resistant (MDR). Eye disinfection in the operating room and peri-injection courses of Tobrex or Vitabact resulted in total elimination of isolates found at baseline. However, in 10% and 20% of patients, respectively, recolonization of the conjunctiva with differing strains occurred. In patients with repeated IVI and Tobrex/Maxitrol treatment, the conjunctival flora showed high resistance rates: 90% of CoNS were MDR. In the in vitro study, Picloxydine showed bactericidal effect against Staphylococci isolates both antibiotic resistant and susceptible with MIC鈮?3.56 碌g/mL. Incubation of bacteria for 15min in Vitabact eye drops, commercially available form of Picloxydine, 434 碌g/mL, showed total loss of colony forming units of all tested isolates including Pseudomonas aeruginosa. Conclusion: The confirmed efficacy of eye antiseptic Picloxydine against conjunctival bacterial isolates and the presence of its commercial form, 0.05% eye drops, convenient for use by patients before and after injection, make this eye antiseptic promising for prophylaxis of IVI-associated infectious complications.
Chlorhexidine and other alternatives for povidone-iodine in ophthalmic surgery: review of comparative studies
J Cataract Refract Surg 2022 Mar 1;48(3):363-369.PMID:34538779DOI:10.1097/j.jcrs.0000000000000754.
Povidone-iodine (PVI) is a universally accepted antiseptic agent used in ophthalmic surgery. Insufficient antisepsis in patients with self-reported allergies to iodine has led to devastating complications. The aim of this study was to review the current evidence for alternatives to PVI in ocular surgery. Aqueous chlorhexidine has been used as a primary antiseptic agent in Sweden for several years and has proven efficiency and safety; in a study of a large series of intravitreal injections in Australia, the endophthalmitis rates were similar to those after the use of PVI. The evidence related to using other disinfectants such as Picloxydine, hypochlorous acid solution, and polyhexanide is scarce. Single studies have shown lower patient discomfort after conjunctival lavage with chlorhexidine or hypochlorous acid than with PVI. No evidence was found to suggest changing from PVI to other antiseptic agents. Disinfectant solutions other than PVI or chlorhexidine will require further investigations to show their utility in ocular surgery.
An in vivo comparison of chlorhexidine and Picloxydine mouthrinses: a possible association between chemical structure and antiplaque activity
J Periodontol 1977 May;48(5):282-4.PMID:323454DOI:10.1902/jop.1977.48.5.282.
A double blind clinical trial was conducted in which both the plaque-inhibiting ability and the in vivo effects on the oral flora of chlorhexidine and Picloxydine mouthwashes was compared. While Picloxydine in higher concentration suppressed the oral flora more effectively than chlorhexidine, the latter agent inhibited plaque development to a much greater extent. This lack of correlation between antibacterial and antiplaque activity can be related to structural differences between these two bis-biguanides.
Disproportionate effect of cationic antiseptics on the quantum yield and fluorescence lifetime of bacteriochlorophyll molecules in the LH1-RC complex of R. rubrum chromatophores
Photosynth Res 2022 Aug;153(1-2):103-112.PMID:35277801DOI:10.1007/s11120-022-00909-8.
Photosynthetic membrane complexes of purple bacteria are convenient and informative macromolecular systems for studying the mechanisms of action of various physicochemical factors on the functioning of catalytic proteins both in an isolated state and as part of functional membranes. In this work, we studied the effect of cationic antiseptics (chlorhexidine, Picloxydine, miramistin, and octenidine) on the fluorescence intensity and the efficiency of energy transfer from the light-harvesting LH1 complex to the reaction center (RC) of Rhodospirillum rubrum chromatophores. The effect of antiseptics on the fluorescence intensity and the energy transfer increased in the following order: chlorhexidine, Picloxydine, miramistin, octenidine. The most pronounced changes in the intensity and lifetime of fluorescence were observed with the addition of miramistin and octenidine. At the same concentration of antiseptics, the increase in fluorescence intensity was 2-3 times higher than the increase in its lifetime. It is concluded that the addition of antiseptics decreases the efficiency of the energy migration LH1 鈫?RC and increases the fluorescence rate constant kfl. We associate the latter with a change in the polarization of the microenvironment of bacteriochlorophyll molecules upon the addition of charged antiseptic molecules. A possible mechanism of antiseptic action on R. rubrum chromatophores is considered. This work is a continuation of the study of the effect of antiseptics on the energy transfer and fluorescence intensity in chromatophores of purple bacteria published earlier in Photosynthesis Research (Strakhovskaya et al. in Photosyn Res 147:197-209, 2021).