Loratadine Raw Material Powder

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Loratadine Powder Usage and Synthesis:

Loratadine Raw Material is a commonly used raw material for anti-allergic drugs. It is a second-generation long-acting tricyclic antihistamine drug. It has a fast onset, strong effect, and does not contain hormones. Hedine inhibits the allergic symptoms caused by histamine by competitively inhibiting histamine H1 receptors, and has no obvious anticholinergic and central inhibitory effects. Loratadine Powder is clinically used to relieve symptoms associated with allergic rhinitis such as sneezing, runny nose and itchy nose as well as itching and burning of the eyes. It is also used to relieve the symptoms of chronic urticaria and other allergic skin diseases. Loratadine (SCH29851) is a selective histamine H1 receptor antagonist used for the treatment of allergy. It is also a selective B(0)AT2 inhibitor with IC50 of 4 μM. Compound (I) (0.05mol) was dissolved in toluene (450ml), and ethyl chloroformate (0.15mol) was added dropwise. After addition, heat on a steam bath for 2h, then stir overnight at room temperature. Add 800ml of water. The benzene layer was separated, washed with water and dried. Concentrate under reduced pressure to obtain an oil, which is impregnated with petroleum ether and then recrystallized with acetonitrile to obtain loratadine with a yield of 64%.

Pharmacokinetics of Loratadine Powder:

Drugs that inhibit the function of liver drug-metabolizing enzymes can slow down the metabolism of this product, such as itraconazole and ketoconazole, taking 400 mg of ketoconazole together every day can make this product and its active metabolite descarboxyethyl clorazine Plasma concentrations of hedidine increased, but no ECG changes were observed. Combination with macrolide antibiotics, cimetidine, theophylline and other drugs can also inhibit the metabolism of loratadine. The main ingredient is loratadine, and the excipients are lactose, starch, dextrin, magnesium stearate, and low-substituted carboxypropyl cellulose. Loratadine relieves related symptoms of allergic rhinitis, such as sneezing, runny nose, nasal itching, eye Itching and burning sensation. This product is an H1 receptor blocker with high selectivity to peripheral H1 receptors and weak affinity to central H1 receptors, which can inhibit the release of leukotrienes and histamine from mast cells.

Pharmacology This product is a long-acting tricyclic antihistamine, competitively inhibits histamine H1 receptors, and inhibits allergic symptoms caused by histamine. This product has no obvious anticholinergic and central inhibitory effects. No obvious teratogenic effect was found in toxicology animal experiments. This product is an H1 receptor blocker with high selectivity to peripheral H1 receptors and weak affinity to central H1 receptors, which can inhibit the release of leukotrienes and histamine from mast cells. This product has quick onset and long-lasting effect. Its antihistamine effect is stronger than that of astemizole and terfenadine, and its antiallergic effect is better. Oral absorption is rapid and good, and the blood concentration reaches the peak within 1.5 hours. Most of it is metabolized by the liver, and its metabolites are still active. The original drug and metabolites are excreted from urine and feces.

Clinical Application of Loratadine Powder:

Antihistamines are highly selective to peripheral nerve H1 receptors, with strong and long-lasting effects. For allergic arthritis, allergic rhinitis. Use It is a national second-class anti-allergic new drug, used to relieve nasal and non-nasal symptoms of seasonal allergic rhinitis and relieve chronic urticaria. Loratadine Loratadine is the zwitterionic feature in the molecular structure of the second-generation antihistamine drug, so that it has no obvious central inhibitory effect. It is mainly used in the prevention and treatment of allergic rhinitis, chronic idiopathic urticaria, allergic Diseases such as asthma and atopic dermatitis. For the relief of symptoms associated with allergic rhinitis such as sneezing, runny nose and itchy nose, nasal congestion, and itching and burning of the eyes. It is also suitable for the relief of symptoms and signs of chronic urticaria, pruritic skin diseases and other allergic skin diseases.

Properties White crystalline powder, odorless and tasteless. Soluble in methanol, ethanol, acetone, dissolved in ether. Slightly soluble in 0.1mol/L hydrochloric acid, insoluble in 0.1mol/L sodium hydroxide. Identification of melting point 133～137℃

1. This product and mercuric chloride test solution form white precipitate.

2. The absorption wavelength of the ethanol solution of this product is 247nm.

3. The retention time of the HPLC peak of this product should be consistent with that of the reference product

4. The infrared absorption spectrum of this product is consistent with that of the reference substance. Content 98.5～101.0% Solution color and clarity 1mg/ml ethanol Clear colorless toluene ≤0.05% n-hexane ≤0.029% moisture ≤0.5% ignition residue ≤0.2% cyanide.

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