Description

The chemical name of lidocaine is n-diethylaminoacetyl-2,6-xylidine. N-(2,6-2 methylphenyl)-2-(diethylamino) acetamide hydrochloride monohydrate is commonly used. 99.9% Pure Lidocaine Powde is a local anesthetic with extensive applications. In addition to its chemical reaction properties, Lidocaine also has various physical properties, which are also very important and have a significant impact on the performance and effectiveness of Lidocaine in the preparation and application process. The solubility in water is relatively high, reaching 6g/L. However, in organic solvents such as ethanol, methanol, and acetone, Lidocaine has relatively poor solubility. This characteristic affects the solubility and stability of Lidocaine in different carriers, and also determines the appropriate solvent type selected during the preparation process of the formulation. It is a local anesthetic widely used to relieve pain during surgical procedures, dentistry, skin surgery, and other processes. In addition to being used as an anesthetic, Lidocaine has also been found to have a range of other medical and non medical uses.

Morphological

powder

Acidity coefficient (PKA)

PKA 7.88 (H2O) (approximate)

Solubility ethanol

4 mg / ml

Storage condition

store at RT

Flash point

9 ℃

Color

white to slightly yellow

1. Synthesis of 99.9% Pure Lidocaine Powder by Acetylamine Method:

Acetylamine method is one of the most common methods for synthesizing Lidocaine. The steps of this method are as follows:

1.1 Firstly, 4-aminobenzoic acid (PABA) is acylated with acetic anhydride in the presence of sulfuric acid to obtain N-acetyl-4-aminobenzoic acid ethyl ester (AAPE). The reaction equation is:

PABA + (CH3CO)2O + H2SO4 → AAPE + CH3COOH + H2O

1.2 Then, AAPE and acetone were subjected to suspension condensation reaction in the presence of sodium iodide to obtain N – (2,6-dimethylphenyl)-N’-acetyl-4-aminobenzamide (DAPA), with the reaction equation as follows:

AAPE + 2,6-(CH3)2C6H3NH2 + NaI → DAPA + CH3COOH + NaI

1.3 Finally, reduce DAPA to obtain Lidocaine, and the reaction equation is:

DAPA + NaBH4 → Lidocaine + NaOH + BH3(CH3)2O

Acetylamine method is an efficient and simple method for synthesizing Lidocaine, but attention needs to be paid to controlling reaction conditions and the dosage of reactants to improve the synthesis yield and purity.

2. Synthesis of Lidocaine using aniline method:

The aniline method is also a commonly used method for preparing Lidocaine, with the following steps:

2.1 Perform acylation reaction between p-aminobenzoic acid (PAPA) and aniline in the presence of sulfuric acid to obtain N-phenyl-4-aminobenzoic acid benzoamide (BAPA). The reaction equation is:

PAPA + C6H5NH2 + H2SO4 → BAPA + H2O

2.2 Then, BAPA and 2,6-dimethylphenol were subjected to a condensation reaction in the presence of alkali to obtain N – (2,6-dimethylphenyl) – N ‘- phenyl-4-aminobenzamide (DPPA), with the reaction equation as follows:

BAPA + 2,6-(CH3)2C6H3OH + NaOH → DPPA + H2O + Na2SO4

2.3 Finally, reduce DPPA and sodium hydroxide in the presence of ethanol to obtain Lidocaine, with the reaction equation as follows:

DPPA + NaOH + 2H2 → Lidocaine + H2O + Na2SO4

It is important to control the molar ratio of reactants, reaction temperature, time, and other conditions in the preparation of Lidocaine using the aniline method to ensure high yield and purity.

When using Lidocaine, we need to consider all its reaction properties, which will help us better understand and use it. The following is a detailed description of all reaction properties of Lidocaine.

1. Acid-base properties:

99.9% Pure Lidocaine Powder belongs to amine compounds and therefore appears alkaline in solution. Lidocaine molecules contain two basic nitrogen atoms that can accept protons to form salts. In water, Lidocaine salts are easily soluble and have strong electrolysis properties. When Lidocaine combines with strong acids, it can form hydrochloride, which is a commonly used method for preparing Lidocaine anesthetics.

2. Oxidation-reduction properties:

Lidocaine molecules contain resonance structures of methylene and benzene rings, and the charge transfer between them gives Lidocaine good reducibility. In the body, Lidocaine is often reduced to its metabolites such as monoethylglycinxlide (MEGX) and glycinxlide (GX). These metabolites have different pharmacological activities and can affect the bioavailability and efficacy of Lidocaine in vivo.

3. Thermal stability:

Lidocaine has good thermal stability. After several months of storage at room temperature, there will be no significant decomposition reaction. In high temperature and humidity environments, Lidocaine may decompose, leading to a decrease in its anesthetic effect. Therefore, we need to pay attention to maintaining good conditions when storing and using Lidocaine.

4. Allergic reactions:

Allergic reactions to Lidocaine are a very rare phenomenon, but they cannot be completely ruled out. If any allergic symptoms occur, such as swelling, shortness of breath, rash, gastrointestinal discomfort, etc., Lidocaine should be immediately stopped and seek medical assistance.

5. Transformation effect:

Lidocaine undergoes metabolism and transformation in the body, with the most important metabolic pathways including N-demethylation and hydroxylation reactions in the liver. The conversion products MEGX and GX have different pharmacological activities and can be used as indicators for evaluating Lidocaine metabolism. The conversion effect has a significant impact on the efficacy and tolerance of Lidocaine.

The molecular structure of lidocaine contains amide bonds, and there are two methyl groups at the adjacent position. The steric hindrance makes the product stable to acids and bases, and it is difficult to hydrolyze under general conditions. It had tertiary amine structure and alkaloid-like properties, and formed white precipitate with trinitrophenol test solution. After the test sample was dissolved with glacial acetic acid, mercury acetate test solution and crystal violet indicator solution were added, and titrated with perchloric acid titration solution ( 0.1 mol / L ) until the solution was green. The usage amount of perchloric acid titration solution was recorded and calculated to obtain. Sample preparation has two methods : 1. Perchloric acid titration solution 2. Crystal violet indicator solution.

Anesthetics:

The main use of Lidocaine is as an anesthetic. It can alleviate pain by inhibiting the Na+channels of individual neurons. Lidocaine is commonly used for local anesthesia in surgical, dental, and skin surgeries. In addition, Lidocaine can also be used as a sedative in situations where general anesthesia is required for cardiac surgery.

Treatment of arrhythmia:

Lidocaine is also commonly used to treat arrhythmia. Due to Lidocaine’s ability to inhibit Na+channels within heart cells, it can weaken or eliminate discomfort caused by arrhythmia. Because Lidocaine has the characteristics of rapid and transient effects, it has a better effect in the treatment of acute arrhythmia.

Treatment of epilepsy:

Lidocaine can also be used as one of the drugs for treating epilepsy, especially for those with difficult to control epilepsy. The anti epileptic effect of Lidocaine is believed to be related to its ability to block sodium ion channels in neurons. The advantages of Lidocaine are its fast onset, easy dosage adjustment, and minimal side effects.

Treating pain:

In addition to acting as an anesthetic, Lidocaine can also be used to treat pain from different sources. For example, local injection of Lidocaine can alleviate neuropathic pain, muscle pain and other symptoms, and can also reduce pain and other discomfort caused by infection or trauma.

Inhibiting withdrawal symptoms of psychological substance abuse:

99.9% Pure Lidocaine Powder has also been found to help suppress withdrawal symptoms among drug users, alcoholics, cigarette users, and others. Lidocaine is believed to alleviate withdrawal symptoms by inhibiting neuronal activity, while also reducing discomfort such as visual and auditory hallucinations.

Treatment of other diseases:

Lidocaine can also be used as a medication to treat other diseases, such as muscle spasms, tremors, etc. Meanwhile, in clinical practice, Lidocaine is also widely used for pain control before, during, and after surgery, as well as for the treatment of diseases in the heart, nervous system, respiratory system, and other areas.

Lidocaine is a local anesthetic commonly used to alleviate pain in local tissues. Its molecular structure is relatively simple. Below is a detailed analysis of the molecular structure of lidocaine:

1. Chemical name and formula:

The chemical name of lidocaine is 2-(diethylamine)-N-(2,6-dimethylphenylene) acetamide, commonly referred to as lidocaine. Its chemical formula is C14H22N2O, with a molecular weight of approximately 234.34 g/mol.

2. Aromatic ring:

Lidocaine molecules contain an aromatic ring composed of a methyl substituted benzene ring, which is connected to an acyl group. This aromatic ring is commonly referred to as the benzene ring.

3. Amide group:

The core structure of lidocaine is an acylamide group (-CONH-), which is attached to the position of the benzene ring. The amide group plays a crucial role in the molecule of lidocaine, affecting its local anesthetic effect.

4. Diethylamino group:

Lidocaine molecules contain a diethylamino group (-N(C2H5)2), which is connected to a carbon atom of the amide group. This group is a side chain in the lidocaine molecule, and together with the acyl group, it affects its biological activity.

5. Methyl substituent:

On the benzene ring of lidocaine, in addition to the acylamine group, there are two methyl groups (-CH3) substituted at positions 2 and 6, respectively. These methyl substituents are also important components of lidocaine molecules.

6. Stereoscopic configuration:

The diethylamino group in the molecule of lidocaine has a chiral center, but in general, it is a racemate, a mixture containing two enantiomers.

In summary, the molecular structure of lidocaine is relatively simple, mainly composed of benzene ring, amide group, diethylamino group, and methyl substituent. These structural features collectively endow lidocaine with its local anesthetic effect.

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