Lidocaine hydrochloride (Lignocaine hydrochloride)
(Synonyms: 盐酸利多卡因; Lignocaine hydrochloride) 目录号 : GC33831
An Analytical Reference Standard
Cas No.:73-78-9
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
Lidocaine is an analytical reference standard that is categorized as an adulterant. It is commonly used as a topical anesthetic.1 Lidocaine is also found as an adulterant in cocaine .2,3,4,5 This product is intended for research and forensic applications.
1.Kumar, M., Chawla, R., and Goyal, M.Topical anesthesiaJ. Anaesthesiol. Clin. Pharmacol.31(4)450-456(2015) 2.DeCarvalho, T.C., Tosato, F., Souza, L.M., et al.Thin layer chromatography coupled to paper spray ionization mass spectrometry for cocaine and its adulterants analysisForensic Sci. Int.26256-65(2016) 3.Floriani, G., Gasparetto, J.C., Pontarolo, R., et al.Development and validation of an HPLC-DAD method for simultaneous determination of cocaine, benzoic acid, benzoylecgonine and the main adulterants found in products based on cocaineForensic Sci. Int.23532-39(2014) 4.Grobério, T.S., Zacca, J.J., Botelho, ?.D., et al.Discrimination and quantification of cocaine and adulterants in seized drug samples by infrared spectroscopy and PLSRForensic Sci. Int.257297-306(2015) 5.Phillips, K.A., Hirsch, G.A., Epstein, D.H., et al.Cardiac complications of unwitting co-injection of quinine/quinidine with heroin in an intravenous drug userJ. Gen. Intern. Med.27(12)1722-1725(2012)
| Cas No. | 73-78-9 | SDF | |
| 别名 | 盐酸利多卡因; Lignocaine hydrochloride | ||
| Canonical SMILES | O=C(NC1=C(C)C=CC=C1C)CN(CC)CC.[H]Cl | ||
| 分子式 | C14H23ClN2O | 分子量 | 270.8 |
| 溶解度 | Water : ≥ 36 mg/mL (132.94 mM) | 储存条件 | 4°C, protect from light |
| 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 | 3.6928 mL | 18.4638 mL | 36.9276 mL |
| 5 mM | 0.7386 mL | 3.6928 mL | 7.3855 mL |
| 10 mM | 0.3693 mL | 1.8464 mL | 3.6928 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。
Immediate Use After Reconstitution of a Biostimulatory Poly-L-Lactic Acid Injectable Implant
J Drugs Dermatol 2020 Dec 1;19(12):1199-1203.PMID:33346524DOI:10.36849/JDD.2020.5228.
Background: Poly-L-lactic acid (PLLA) is a biodegradable, synthetic polymer that stimulates collagen production and can improve skin quality, volume, and thickness. The current reconstitution procedure for Sculptra, a PLLA-containing injectable device involves 2 hours standing time before use. Objective: To evaluate and validate an immediate-use procedure for reconstituting a PLLA-containing injectable device. Methods and materials: Three batches of the product were shaken for 1 minute immediately after reconstitution with 8 mL of sterile water. Different physicochemical tests including viscosity, concentration of excipients (sodium carboxymethylcellulose and mannitol), pH, and particle size distribution were performed for standing times 0, 2, 24, and 72 hours after immediate shaking, and compared with the standard 2 hours standing time before shaking. The recovery and stability of optional addition of 1 mL of 2% Lidocaine hydrochloride was also assessed. Results: All physiochemical parameters evaluated were equivalent, regardless of reconstitution procedure, showing that shaking vigorously for 1 minute dissolves the excipients of the product properly without a required standing time and with no impact to the PLLA particles. There were no differences in Lidocaine hydrochloride content of suspensions after 0 and 72 hours. Conclusion: The PLLA-containing product can be used immediately after reconstitution including vigorous shaking, as shown from physicochemical analyses. Optional addition of Lidocaine hydrochloride is feasible. J Drugs Dermatol. 2020;19(12): doi:10.36849/JDD.2020.5228.
Lidocaine hydrochloride Gel for Ocular Surface Anesthesia: Pharmacokinetic Evaluation and Randomized Placebo-Controlled Trial in China
J Ocul Pharmacol Ther 2022 Oct;38(8):567-575.PMID:36288558DOI:10.1089/jop.2022.0080.
Backgrounds: A new generic formulation of 3.5% Lidocaine hydrochloride ophthalmic gel has been developed in China. This study aimed to evaluate the pharmacokinetics and effectiveness of this Lidocaine hydrochloride gel for ocular surface anesthesia. Methods: In the pharmacokinetics study, the new form of 3.5% Lidocaine hydrochloride gel or Akten™ 3.5% Lidocaine hydrochloride gel was applied in eyes of 70 rabbits. The ocular tissues and plasma samples were collected after the application of 3.5% Lidocaine hydrochloride gel or Akten lidocaine gel and analyzed using the liquid chromatography with tandem mass spectrometry (LC-MS/MS) method to determine the concentration of lidocaine. A multicenter, randomized, double-blind prospective clinical trial was conducted in Chinese adults. Two hundred twenty participants were 1:1 randomized into the sham gel group or the Lidocaine hydrochloride group. The primary efficacy endpoint was defined as the percentage of subjects achieving anesthesia by 5 min. Results: The animal pharmacokinetics study showed the lidocaine level was significantly higher in the choroid at 15 min and the vitreous body at 15 and 30 min; it was lower in tears at 8 h for 3.5% Lidocaine hydrochloride gel than Akten (P ≤ 0.05). Our clinical trial showed that the percentage of subjects achieving anesthesia within 5 min in the Lidocaine hydrochloride gel group was significantly higher than the sham gel group (86.92%-18.18%, P < 0.0001). The incidence of adverse events was relatively low and favorable for both groups. Conclusion: This new formulation of Lidocaine hydrochloride gel, with pharmacokinetics similar to Akten, may exert a sustained, effective, and safe anesthetic effect. The clinical trial for this new generic formulation of Lidocaine hydrochloride has been registered with the Drug Clinical Trial Registration and Information Publicity Platform established by State Food and Drug Administration of China (Registration No. CTR20160593).
Lidocaine hydrochloride Compared with MS222 for the Euthanasia of Zebrafish (Danio rerio)
J Am Assoc Lab Anim Sci 2016 Nov;55(6):816-820.PMID:27931323doi
Despite several shortcomings, MS222 is the most commonly used chemical agent for euthanasia of zebrafish. Although Lidocaine hydrochloride has some advantages over MS222, its effectiveness as a euthanasia agent for zebrafish is unknown. Larvae at 9 to 16 d postfertilization were exposed to 250 mg/L MS222 or 400, 500, 600, 700, 800, 900, or 1000 mg/L lidocaine and observed for cessation of heartbeat. Adult zebrafish were exposed to 250 mg/L MS222 or 400, 500, or 600 mg/L lidocaine; times to loss of righting reflex, cessation of opercular movement, and complete recovery; body length; aversive behavior; and gross and microscopic evidence of acute toxicity were evaluated. The heartbeat was not lost from any larvae in any group, regardless of drug or dosage. For adults, time to loss of righting reflex was greatest in the 500-mg/L lidocaine group. Opercular movement ceased earlier in all lidocaine groups compared with the MS222 group. Fish in the 500-mg/L lidocaine group were smaller than those in other groups. Fewer fish in the lidocaine groups displayed aversive behavior (erratic swimming and piping) compared with the MS222 group. No fish in the Lidocaine hydrochloride groups (n = 30) recovered from euthanasia, whereas one fish in the MS222 group did (n = 10). Neither the MS222 nor lidocaine groups showed any gross or histologic changes suggestive of acute toxicity. Our results suggest that Lidocaine hydrochloride may be an effective alternative chemical euthanasia agent for adult zebrafish but should not be used in larval fish.
Chromatographic Determination of Aminoacridine Hydrochloride, Lidocaine hydrochloride and Lidocaine Toxic Impurity in Oral Gel
J Chromatogr Sci 2016 Apr;54(4):492-9.PMID:26671412DOI:10.1093/chromsci/bmv170.
Two sensitive and selective analytical methods were developed for simultaneous determination of aminoacridine hydrochloride and Lidocaine hydrochloride in bulk powder and pharmaceutical formulation. Method A was based on HPLC separation of the cited drugs with determination of the toxic lidocaine-related impurity 2,6-dimethylaniline. The separation was achieved using reversed-phase column C18, 250 × 4.6 mm, 5 µm particle size and mobile phase consisting of 0.05 M disodium hydrogen phosphate dihydrate (pH 6.0 ± 0.2 adjusted with phosphoric acid) and acetonitrile (55 : 45, v/v). Quantitation was achieved with UV detection at 240 nm. Linear calibration curve was in the range of 1.00-10.00, 13.20-132.00 and 1.32-13.20 µg mL(-1) for aminoacridine hydrochloride, Lidocaine hydrochloride and 2,6-dimethylaniline, respectively. Method B was based on TLC separation of the cited drugs followed by densitometric measurement at 365 nm on the fluorescent mode for aminoacridine hydrochloride and 220 nm on the absorption mode for Lidocaine hydrochloride. The separation was carried out using ethyl acetate-methanol-acetic acid (65 : 30 : 5 by volume) as a developing system. The calibration curve was in the range of 25.00-250.00 ng spot(-1) and 0.99-9.90 µg spot(-1) for aminoacridine hydrochloride and Lidocaine hydrochloride, respectively. The results obtained were statistically analyzed and compared with those obtained by applying the manufacturer's method.
Iontophoretic delivery of Lidocaine hydrochloride through ex-vivo human skin
J Dermatolog Treat 2020 Mar;31(2):191-199.PMID:30843444DOI:10.1080/09546634.2019.1589640.
Background: Iontophoresis is one of the widely used noninvasive and painless transdermal drug delivery technique.Objective: Transdermal delivery of Lidocaine hydrochloride using continuous and modulated iontophoresis were evaluated across human skin ex-vivo and further assessed for skin tolerance in-vivo in the Swiss albino mice.Methods: Continuous DC was modified into modulated DC by introducing ON-OFF time in continuous DC. Iontophoresis studies were conducted on human skin samples for 60 min.Results: Drug permeation of 2% lidocaine HCl was enhanced in current density-, duty cycle- and time-dependent manner across human skin. The lidocaine HCl concentration obtained with modulated DC and continuous DC iontophoresis were about three-fold and four-fold higher than passive group respectively for all current densities across human skin. Continuous DC iontophoresis was found to be more effective than modulated DC. However, no significant difference was observed in transport of lidocaine HCl between 75% and 100% (continuous) duty cycle at all current density. Further, in-vivo reversibility studies with mice confirmed that modulated iontophoresis was well tolerated by the tissue and the injury caused is transient and reversible.Conclusion: For clinical application, modulated DC iontophoresis with 75% duty cycle at 0.5 mA/cm2 current density would be recommended.