Pharmaceuticals Dimenhydrinate Raw Materials powder

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Dimenhydrinate powder Usage and Synthesis.

It is a double salt of diphenhydramine and 8-clofylline. It has the same effect as diphenhydramine hydrochloride, but its antihistamine effect is weaker than the latter. It can inhibit the emetic chemical receptive area of the brain, and has general central inhibition and anticholinergic effects, thus having sedative and antiemetic effects. The absorption is rapid and complete after oral administration, the effect takes 15 to 60 minutes, the effect lasts 3 to 6 hours, the elimination phase half-life (t1/2β) 4-6 hours, and the plasma protein binding rate is high. It is metabolized primarily in the liver and excreted in the urine as metabolites. Patients with liver dysfunction who take this product can produce accumulation in the body and should be reduced.

Drug interaction of Dimenhydrinate powder.

1. Do not drink alcohol after taking the drug, and do not take it with other central nervous depressants.

2. This product can make ethanol, central nervous system inhibitors, tricyclic antidepressants and other synergies. It can briefly affect the absorption of barbiturates and sodium sulfanilate. When used with sodium p-aminosalicylate, the blood concentration of the latter was reduced.

3. Take it with food or milk to reduce the irritation of the stomach.

Pharmacological action of Dimenhydrinate.

1. H1 receptor blocking effect
As a histamine H1 receptor antagonist, it inhibits histamine-mediated allergic reactions, reduces vascular exudation and tissue edema

2. Central anticholinergic effect
Blocks cholinergic receptors in the central nervous system (CNS), reduces the excitability of the vestibular nuclei, and relieves vertigo and vomiting

3. Vestibular function regulation
Directly inhibits the excessive excitement of the labyrinth (inner ear vestibular system), and improves nausea and vomiting caused by motion sickness (such as motion sickness and seasickness)

4. Medulla oblongata emetic chemoreceptor inhibition
Acts on the emetic chemoreceptor zone (CTZ) of the medulla oblongata to reduce vomiting reflexes caused by radiotherapy, surgery or drugs

5. Sedative effect
Produces mild central inhibition through the blood-brain barrier, which may cause side effects such as drowsiness and decreased attention

Product method of Bulk Dimenhydrinate powder.

1. Synthesis of core raw materials
‌8-chlorotheophylline preparation‌
Using theophylline as raw material, chlorination reaction generates 8-chlorotheophylline (1,3-dimethyl-8-chloro-3,7-dihydro-1H-purine-2,6-dione)

‌Benzhydryloxyethylamine synthesis‌
By reacting benzhydryl alcohol with 2-chloroethyldimethylamine, N,N-dimethyl-2-(benzhydryloxy)ethylamine is generated

2. Salt formation reaction
8-chlorotheophylline and benzhydryloxyethylamine are combined in a solvent to form dimenhydrinate (C24H28ClN5O3)

3. Process optimization direction
‌Catalyst selection‌: Some processes use palladium catalyst oxidation method, but there are problems of high cost and difficult recovery
‌Alternative oxidant‌: Potassium persulfate can replace oxygen oxidation method to increase the yield to more than 90%

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