Description

Diphenhydramine Hydrochloride powder is a diphenhydramine-like drug, and its chemical name is 2-(Diphenylmethoxy)-N,N-dimethylethylamine hydrochloride. It is white crystalline powder or flake crystal, tasteless, odorless, non-flammable, with low saturated vapor pressure, easily soluble in water and ethanol, slightly soluble in chloroform and benzene, almost insoluble in ether. It is a compound that is very soluble in water. At normal temperature, it can form a transparent solution with water, and its solubility will increase as the temperature rises. The pH value is between 4.0-5.5, which means that it is a weak acidic substance. It can be used as an ingredient in medicines such as allergies. It is a diphenhydramine drug, which can be used to treat allergic diseases such as allergic rhinitis, hay fever, food allergy, etc. It can also be used to relieve symptoms such as cough, sedative sleep, anticholinergic effect, and prevention of motion sickness.

Diphenhydramine Hydrochloride powder is a diphenhydramine drug, which has various pharmacological effects and can be used to treat various diseases and symptoms.

1. Treatment of allergic symptoms: Diphenhydramine Hydrochloride is an antihistamine drug that can prevent the release and action of histamine, thereby reducing symptoms caused by allergic reactions, such as sneezing, nasal congestion, runny nose, itchy skin, etc. Therefore, Diphenhydramine Hydrochloride is widely used in the treatment of allergic rhinitis, hay fever, food allergy and other allergic diseases.
2. Relieve cough: Diphenhydramine Hydrochloride has antitussive effect, it can suppress the excitement of the central nervous system and relieve cough. Therefore, Diphenhydramine Hydrochloride can also be used to treat dry cough, acute bronchitis and other diseases.
3. Sedation and sleep: Diphenhydramine Hydrochloride has a sedative effect, which can affect the central nervous system and reduce the excitability of neurons, thereby producing a sedative effect. Therefore, Diphenhydramine Hydrochloride is also used to treat insomnia, anxiety and other diseases.
4. Anticholinergic effect: Diphenhydramine Hydrochloride has an anticholinergic effect, which can prevent the action of acetylcholine and bind to histamine receptors, thereby producing an antiallergic effect. This pharmacological effect makes Diphenhydramine Hydrochloride also be used to treat diseases such as motion sickness and ship motion sickness.
5. Analgesic: Diphenhydramine Hydrochloride has a slight analgesic effect and can be used to relieve mild pain. However, due to its weak analgesic effect, it is generally not used alone as an analgesic, but in combination with other drugs.
6. Prevention of motion sickness: Diphenhydramine Hydrochloride can also be used to prevent motion sickness, such as seasickness and airsickness. Its sedative and antiallergic effects can reduce symptoms such as nausea and vomiting caused by motion sickness.
7. Antidepressant: Some studies in recent years have also found that Diphenhydramine Hydrochloride has a certain antidepressant effect and can relieve depression symptoms to a certain extent. However, the drug is not the main antidepressant drug and is often used as an adjuvant treatment.

Diphenhydramine Hydrochloride powder is a diphenhydramine drug also known as HCl-DPH. It can be used to treat allergic rhinitis, hay fever, food allergies and other allergic diseases, and it can also be used to relieve cough, sedative sleep, anticholinergic effect, and prevent motion sickness. This article will introduce all the synthesis methods of Diphenhydramine Hydrochloride.

1. Benzoyl peroxide-sodium nitrite method: This method is a traditional method for preparing Diphenhydramine Hydrochloride. First, benzoyl peroxide (C6H5COOC6H5) is reacted with sodium nitrite to produce 2,2-diphenylethane-1-nitrogen dioxide (C6H5CH2)2N2O). Then, this intermediate is added into HCl solution, and sodium sulfite is further added for reduction to obtain Diphenhydramine Hydrochloride. The mechanism of this reaction is as follows.

2C6H5COOC6H5 + 2NaNO2 + 4HCl → 2(C6H5CH2)2N2·2HCl + 4NaCl + 2H2O

2(C6H5CH2)2N2O·2HCl + Na2SO3 → 2C17H21NO·HCl + Na2SO4 + H2O

2. Aniline-phenylacetonitrile method: This method has low raw material cost and relatively simple reaction, and is an economical and practical synthesis method. First, aniline and phenylacetonitrile are heated and reacted to generate α-phenyl-N-phenylacetonitrile methylacetamide. The intermediate is then subjected to hydrogenation reduction to obtain Diphenhydramine Hydrochloride. The mechanism of this reaction is as follows:

C6H5NH2 + C6H5CH2CN → HC(C6H5)2CH2NHCOCH3

HC(C6H5)2CH2NHCOCH3 + H2 → C17H21NO·HCl

3. Methylene blue-aniline method: This method uses methylene blue and aniline as raw materials, and prepares Diphenhydramine Hydrochloride through heating reaction, acidolysis and other steps. The mechanism of this reaction is as follows:

C10H8N2S·2HCl + 2C6H5NH2 → HC(C6H5)2CH2NHCSNHC6H5 + 2H2O

HC(C6H5)2CH2NHCSNHC6H5 + 2HCl → C17H21NO·HCl + C6H5NH2 + C10H8N2S

4. 1-phenyl-2-(dimethylamino) ethylene-aniline method: this method uses 1-phenyl-2-(dimethylamino)ethylene and aniline as raw materials, and obtains Diphenhydramine Hydrochloride by heating and reacting. The mechanism of this reaction is as follows:

C6H5NH2 + CH2=C(C6H5) N(CH3)2 → HC(C6H5)2CH2NHCH(CH3)2

HC(C6H5)2CH2NHCH(CH3)2 + HCl → C17H21NO·HCl

In summary, Diphenhydramine Hydrochloride has a variety of synthesis methods, among which the benzoyl peroxide-sodium nitrite method, aniline-phenylacetonitrile method and methylene blue-aniline method are the most commonly used. In the preparation process, it is necessary to pay attention to the control of factors such as reaction conditions and catalysts to ensure the smooth progress of the reaction and obtain high-quality Diphenhydramine Hydrochloride powder products.

Chemical Formula

C15H10O5

Exact Mass

270

Molecular Weight

270

m/z

270 (100.0%), 271 (16.2%), 272 (1.2%), 272 (1.0%)

Elemental Analysis

C, 66.67; H, 3.73; O, 29.60

Common analysis methods:

High performance liquid chromatography:

High-performance liquid chromatography (HPLC) is a commonly used quality control method, which has the advantages of high sensitivity, good resolution, and simple operation. Usually, a C18 reversed-phase chromatographic column is used, with methanol-water-ferric chloride (30:70:1) as the mobile phase, and the detection wavelength is 254 nm.

Electrochemical method:

Electrochemical method is a fast and sensitive drug analysis method, which has advantages in rapid detection. The commonly used electrochemical methods include cyclic voltammetry, square wave voltammetry, constant potential step method, etc. Taking square wave voltammetry as an example, this method can quickly measure the concentration range of Diphenhydramine Hydrochloride and shows a good linear relationship.

Infrared spectroscopy:

Infrared spectroscopy is a physical and chemical analysis method with simple principle and convenient operation. The sample was pressed into a thin sheet using a KBr pellet, and the infrared absorption spectrum was scanned to detect the characteristic peak position and spectral image of Diphenhydramine Hydrochloride.

Atomic absorption spectrometry:

Atomic absorption spectrometry is a method to accurately measure iron, zinc and other trace elements in Diphenhydramine Hydrochloride. Firstly, HNO3 is used to dissolve the drug sample, and convert it into ionic state, perform spectral measurement in the atomic absorption instrument, and determine the content of trace elements in the sample by comparing the difference between the sample spectrum and the standard spectrum.

Capillary gas chromatography:

Capillary gas chromatography is a method of drug analysis with high sensitivity and good separation effect. Diphenhydramine Hydrochloride is usually separated and detected using a Capillary GC column with N2 as the carrier gas at a separation temperature range of 10°C to 300°.

stability:

The stability of Diphenhydramine Hydrochloride powder is affected by environmental factors, such as temperature, humidity, light, etc. Diphenhydramine Hydrochloride crystals are stable at room temperature, but are susceptible to moisture absorption and should be stored in a dry place. Avoid high temperature, direct sunlight and other light conditions, Diphenhydramine Hydrochloride is easy to decompose and become invalid. During the production, storage and use of the preparation, attention should be paid to the stability of Diphenhydramine Hydrochloride to ensure the quality and effectiveness of the drug.

Diphenhydramine Hydrochloride has certain toxicity, excessive use or misuse may lead to a series of adverse reactions and toxic reactions.

The following will introduce from two aspects of acute poisoning and chronic poisoning.

Acute poisoning:

The acute poisoning of Diphenhydramine Hydrochloride mainly manifests as nervous system and cardiovascular system symptoms. Common nervous system symptoms include drowsiness, dizziness, confusion, convulsions, etc.; cardiovascular system symptoms include bradycardia, hypotension, arrhythmia, etc., and may be accompanied by symptoms such as dyspnea, dry mouth, and insomnia. When the dose is too high, patients will experience severe symptoms such as coma, convulsions, apnea, and even life-threatening.

Chronic poisoning:

Long-term use of Diphenhydramine Hydrochloride may also cause chronic poisoning. Common symptoms of chronic poisoning include drowsiness, dizziness, constipation, loss of appetite, and blurred vision. In addition, chronic use may lead to drug dependence and withdrawal symptoms. When patients have these symptoms, they should stop using the drug as soon as possible and seek the guidance and treatment of a doctor.

 

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