Description

Procaine powder can be used as a raw material, chemical material in the laboratory. These physical properties help characterize its purity and solid-state structure. The electrical charge is neutral, so it does not have the advantages of electrostatic force and repulsive force. This limits its potential in technological applications. It is a chiral compound with both left-handed and right-handed properties. This optical activity is due to the chiral center in its molecule. The rotation of left rotation is -14.3 °, and the rotation of right rotation is+13.9 °. It has low toxicity. When used at the correct dosage, it is usually a safe anesthetic. However, excessive or misuse can lead to toxic reactions, including death. Overall, as an anesthetic drug, the study of its physical properties is crucial for its application and production, and these characteristics will also play an important role in the fields of technology and medicine.

Chemical Formula
C13H20N2O2
M.W
236.31
Melting point     61°
Boiling point       378.78°C (rough estimate)
Density 1.0604 (rough estimate)
Refractive index 1.5430 (estimate)

Procaine powder, chemical name is 4-aminobenzoic acid 2-(diethylamino)ethyl ester hydrochloride. The synthesis of Procaine typically involves several steps, primarily using p-nitrobenzoic acid as the starting material. Below is a detailed synthesis route:

Raw Materials: p-nitrobenzoic acid, diethylaminoethanol, xylene (as solvent and catalyst), and an antifoaming agent.

Procedure:

1. In a three-necked flask equipped with a thermometer, water separator, and reflux condenser, add p-nitrobenzoic acid, diethylaminoethanol, xylene, and the antifoaming agent.

2. Heat the mixture under reflux conditions (oil bath temperature around 180°C, internal temperature around 145°C) for a period of time (typically 6 hours) to allow for the esterification reaction to occur.

3. Continuously remove the water formed during the esterification (a reversible reaction) by azeotropic distillation with xylene.4. After the reaction, cool the mixture and pour into a conical flask to allow for solid separation.

5. Distill off the excess xylene under reduced pressure, dissolve the residue in 3% hydrochloric acid, and filter to remove unreacted p-nitrobenzoic acid. The filtrate containing nitrocaine is retained for further use.

Step 2: Reduction of Nitrocaine to Aminoester

Raw Materials: Nitrocaine solution, iron powder, sodium hydroxide, and hydrochloric acid.

Procedure:

1. Transfer the nitrocaine solution to a three-necked flask with stirring and temperature control.

2. Adjust the pH to 4.0-4.2 with 20% sodium hydroxide solution.

3. Gradually add iron powder in small portions while maintaining the temperature below 70°C (cooling may be required).

4. Allow the reduction reaction to proceed for 2 hours at 40-45°C.

5. Acidify the solution with hydrochloric acid to pH 5, then adjust the pH to 7.8-8.0 with saturated sodium sulfide solution to precipitate iron salts.

6. Filter the mixture, wash the precipitate, and acidify the filtrate again to pH 6.

7. Treat the solution with activated carbon, filter, and alkalize with 20% sodium hydroxide to pH 9.5-10.5 to precipitate the aminoester (Procaine base).

Step 3: Formation of Procaine Hydrochloride

Raw Materials: Procaine base, concentrated hydrochloric acid, and optional recrystallization solvents.

Procedure:

1. Dissolve the Procaine base in water and add concentrated hydrochloric acid dropwise until the pH reaches 5.5.
2. Heat the solution to 60°C and add saturated salt. Optionally, add an antioxidant such as sodium hydrosulfite and heat to 65-70°C for hot filtration.
3. Cool the filtrate to crystallization temperature, filter the crystals, and wash with cold ethanol.
4. Dry the crystals to obtain Procaine Hydrochloride.
5. For further purification, dissolve the crude product in distilled water, add activated carbon, filter hot, and cool to allow crystallization. Wash the crystals and dry to obtain the final product.

Pure API (Active pharmaceutical ingredient) for science researching only, Standard substance for analysis, Pharmacokinetic study, receptor resistance test etc. Also known as “novocaine”, is commonly used in clinical practice. White crystalline or crystalline powder, soluble in water. The use of procaine is procaine injection, procaine therapy, etc. Adding a small amount of epinephrine into the injection can prolong the action time.

Procaine is not only a local anesthetic, but also widely used in the treatment of many diseases in clinical departments. Clinical application in pediatrics: treatment of whooping cough. Clinical application in dermatology: the treatment of herpes zoster, the treatment of allergic purpura, pruritus, neurodermatitis. Clinical application in obstetrics and gynecology: treatment of cervical dystocia, treatment of cervical edema, oxytocin effect. Clinical application in gastroenterology (treatment of pancreatitis). Clinical application in respiratory department: treatment of hemoptysis.

Quality & Analysis

thermal stability

The thermal stability is relatively average, with a thermal decomposition temperature of around 350 ° C. This can lead to easy degradation and release of toxic gases during the heating process.

1. Thermal degradation mechanism

Thermal degradation refers to the chemical reaction of drugs under high temperature conditions due to the action of thermal energy, which decomposes into monomers or other substances, resulting in a decrease in drug quality. The thermal degradation mechanism is mainly the decarboxylation of carboxyl groups and the fracture of epoxy rings.

The carboxyl group in Procaine is very prone to decarboxylation, which is caused by acidic environment. Under high temperature conditions, the epoxy ring will also break and two end groups will escape, while a single methyl group reacts with a hydroxyl group, resulting in molecular impurities.

2. Determination and evaluation of thermal stability

The determination of thermal stability can be carried out using thermogravimetric analysis. This method is suitable for determining the thermal stability of drugs and can determine the parameters such as decomposition temperature, weight loss rate, and decomposition kinetics parameters of drugs. Usually, the drug sample is placed in a weighed aluminum measuring plate, and then heated with a constant heating rate, constant flow rate, and a stable flow rate of inert gas. The decomposition temperature is measured by recording the mass loss generated during the process.

In addition, thermal stability can also be evaluated by affecting its efficacy. Generally speaking, drugs with good thermal stability have much better efficacy. Therefore, the thermal stability of a drug can be evaluated by examining its pharmacological changes after high-temperature treatment.

. Factors affecting the thermal stability of Procaine

The thermal stability is influenced by various factors. For example, it is easy to undergo decarboxylation under acidic conditions; At high temperatures, the epoxy ring can also break, leading to the pyrolysis of drugs. In addition, factors such as oxygen, water, and sunlight can also affect the thermal stability during long-term storage.

4. Methods to improve the thermal stability of Procaine

There are several methods to improve the thermal stability:
(1) Avoid using excessively high temperatures.
(2) Use some additives, such as calcium hydroxide, to increase thermal stability.
(3) Strengthen protection during storage, such as keeping drugs in cool and dry conditions.
(4) Use formulations containing stabilizers to improve the stability of drug quality.

Solubility

Procaine is easily soluble in water and methanol, slightly soluble in ethanol and chloroform, but not in benzene or dichloromethane. The solubility of this drug in water is 1g and can be dissolved in 100mL of water.

The solubility is crucial in studying the chemical and physical properties of the substance. It is a weakly acidic drug with a pKa value of 8.9. The solubility in water is temperature dependent, and the higher the temperature, the higher its solubility. The water solubility is 1 g/mL at 20 ℃, but it is about 7 g/mL at 40 ℃, which can be described by a solubility curve.

Procaine’s solubility is also affected by other factors, such as pH value of solvent, ionic strength and concentration. Under acidic conditions, procaine is more easily soluble. Therefore, when preparing Procaine hydrochloride, Procaine can be dissolved in hydrochloric acid aqueous solution first, and then the hydrochloride can be precipitated.

In addition to water, it can also be dissolved in other common solvents. Organic solvents such as acetone, methanol, and chloroform can also be used to dissolve procaine. Nevertheless, the solubility in different solvents varies. For example, it has a higher solubility in acetone and a lower solubility in water. In certain situations, different solvents can be selected as needed for ease of use.

Because procaine powder is a drug, its solubility is also crucial in the pharmaceutical industry and clinical applications. During the production process, it is necessary to dissolve the drug in a suitable carrier in order to prepare various dosage forms, such as injections, oral formulations, sugar coated formulations, etc. At the same time, the factors that affect the solubility of Procaine also include particle size, morphology, and crystal defects. These factors also need to consider production factors such as solubility and yield to ensure the effectiveness of production and use.

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