Benzyl nicotinate
(Synonyms: 烟酸苄酯) 目录号 : GC63815
Benzyl nicotinate 是一种血管扩张剂，用作引起充血的活性成分。
Cas No.:94-44-0
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
Benzyl nicotinate, a vasodilator, is used as an active ingredient that causes hyperemia[1][2].
[1]. Erjavec V, et al. In vivo study of liposomes as drug carriers to oral mucosa using EPR oximetry. Int J Pharm. 2006;307(1):1-8. [2]. Petelin M, et al. In vivo study of different ointments for drug delivery into oral mucosa by EPR oximetry. Int J Pharm. 2004;270(1-2):83-91.
| Cas No. | 94-44-0 | SDF | Download SDF |
| 别名 | 烟酸苄酯 | ||
| 分子式 | C13H11NO2 | 分子量 | 213.23 |
| 溶解度 | 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 | 4.6898 mL | 23.4489 mL | 46.8977 mL |
| 5 mM | 0.938 mL | 4.6898 mL | 9.3795 mL |
| 10 mM | 0.469 mL | 2.3449 mL | 4.6898 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。
Degradation kinetics of Benzyl nicotinate in aqueous solution
Indian J Pharm Sci 2010 Jan;72(1):46-9.PMID:20582189DOI:10.4103/0250-474X.62238.
The degradation of Benzyl nicotinate in aqueous solution over a pH range of 2.0-10.0 at 50+/-0.2 degrees was studied. The degradation was determined by high performance liquid chromatography. The degradation was observed to follow apparent first-order rate kinetics and the rate constant for the decomposition at 25 degrees was estimated by extrapolation. The reaction was shown to be hydroxide ion catalyzed and the Arrhenius plots showed the temperature dependence of Benzyl nicotinate degradation. A significant increase in the stability of Benzyl nicotinate was observed when glycerol or polyethylene glycol 400 was incorporated into the aqueous solution.
Kinetics of blood flow after topical application of Benzyl nicotinate on different anatomic sites
Arch Dermatol Res 2006 Nov;298(6):291-300.PMID:16967307DOI:10.1007/s00403-006-0692-y.
Cutaneous characteristics, e.g., thickness of the SC and density of follicles, affect the penetration of topically applied substances. In the present study, the penetration of Benzyl nicotinate, causing a vasodilation, was studied on three anatomic sites (forearm, forehead and calf) differing in their skin characteristics. Therefore, the blood flow of the superficial dermal plexus and that of the larger capillaries in the deeper skin layers was simultaneously measured using a laser Doppler flowmeter. In addition, the cutaneous temperature and redness were determined as a function of time. These four biological reactions were measured in turn on a skin area treated with a gel containing Benzyl nicotinate and on an untreated control area. The highest basal levels were observed on the forehead. Topical application of Benzyl nicotinate resulted in an increase in each biological response. Compared to the other sites, the maximal values were reached earliest on the forehead, which also showed the fastest decrease. No significant differences were obtained comparing the kinetic data of the calf with that of the forearm. The results indicate an additional contribution by the numerous vellus hair follicles of the forehead to the penetration and exposure of the drug.
Influence of nanosized delivery systems with Benzyl nicotinate and penetration enhancers on skin oxygenation
Int J Pharm 2008 Jul 9;359(1-2):220-7.PMID:18472233DOI:10.1016/j.ijpharm.2008.03.014.
Many novel nanosized delivery systems have been designed for topical application of drugs since they can overcome the skin barrier and improve drug bioavailability. The increased absorption is often a consequence of a reversibly disrupted barrier function of the skin by the vehicle itself or by specific ingredients that act as penetration enhancers. This paper reports the effects of two nanosized systems (microemulsion and liposomes), in the presence and absence of penetration enhancers (PE), on the topical delivery of a lipophilic drug in vivo and compares that to classical hydrogel formulation. A vasodilator Benzyl nicotinate (BN), which increases the blood flow of the skin, was incorporated into the formulations, and skin oxygenation was followed by electron paramagnetic resonance oximetry. It was found that microemulsions and liposomes (with or without PE) accelerate the rate of BN action when compared to hydrogel. However, incorporation of PE in microemulsion also improves the effectiveness of BN action. To understand why PE enhances the action of BN, its effect on the structure of the stratum corneum was investigated in vitro. The increased fluidity of the stratum corneum lipids provides an explanation for the greater penetration of BN into the skin when the drug and PE are together incorporated into the appropriate formulation.
Comparison of blood flow to the cutaneous temperature and redness after topical application of Benzyl nicotinate
J Biomed Opt 2006 Jan-Feb;11(1):014025.PMID:16526902DOI:10.1117/1.2166370.
The topical application of drugs, such as nicotinates, affects cutaneous blood flow. Such a biological response, which is dependent on the drug and the individual, can be measured noninvasively using laser Doppler flowmetry. We illustrate the kinetics of vasodilation caused by topically applied Benzyl nicotinate using a new frequency-selective laser Doppler flowmeter. This flowmeter measures the blood flow in the superficial dermal plexus and the deeper lying larger capillaries simultaneously and indirectly by determining the flow velocity. Both sets of data are compared with the skin temperature and redness. Four biological parameters are measured consecutively on a skin area treated with gel containing Benzyl nicotinate and on an untreated control area. A linear relationship between both blood flows is observed. However, no correlation is obtained between the microcirculation with either the cutaneous temperature or the redness. These results indicate the transport of the drug in the blood from the upper to the deeper capillaries. Cutaneous temperature and redness are unsuitable parameters to measure the kinetics of the blood flow after topical application of drugs.
Improved skin oxygenation after Benzyl nicotinate application in different carriers as measured by EPR oximetry in vivo
J Control Release 2001 Jan 29;70(1-2):203-11.PMID:11166420DOI:10.1016/s0168-3659(00)00351-5.
The development of formulations, which increase skin oxygenation and of methods for measuring oxygen levels in skin are important for dealing with processes affected by the level of oxygen, e.g., rate of healing and efficiency of radiation oncology. In this study we have investigated the role of carriers on the efficacy of Benzyl nicotinate (BN) action in skin after dermal application in different formulations by EPR oximetry in vivo. The time course of pO2 in the skin after application of rubefacient is followed directly for the first time. The results obtained proved the applicability of in vivo EPR oximetry as a sensitive method by which small alterations in pO2 can be detected. We have found that the type of vehicle significantly influences the time when BN starts to act, the duration of its action, and the maximal increase in pO2. The ranking of vehicle efficiency was: lipid nanoparticles in hydrophilic gel>liposomes in hydrophilic gel>hydrophilic gel>hydrophobic ointment>hydrophobic cream. Primarily the semi-solid vehicle determines the lag-time of action, but the maximal oxygen level is influenced decisively by the particulate carrier systems. BN effectiveness was dose dependent. 2.5% w/w concentration of BN appears to be the most appropriate for therapeutic application. After repeated application a successive increase of pO2 base line in skin and of the maximal pO2 was noticed.