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Bilastine compound

A bilastine and compound technology, applied in the field of bilastine compounds and their preparation, can solve the problems of no anticholinergic effect, a large number of bilastine impurities, difficult to pass through the blood-brain barrier and the like

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The first generation H 1 Receptor antagonists, such as chlorpheniramine, diphenhydramine, etc., are fat-soluble, can pass through the blood-brain barrier, often have a sedative effect, and also have anticholinergic effects, manifested as dry mouth, blurred vision, urinary Retention, etc., are more obvious in the elderly. Because of its central sedative effect and / or anticholinergic effect, it seriously affects the daily life, study and work of the drug users, and it is increasingly unsuitable for the doctor-patient population.
The second generation H 1 Among the receptor antagonists, such as cetirizine, loratadine, azelastine, ketotifen, terfenadine, and astemizole, most of them have long half-lives and long duration of action. Second, it absorbs quickly, does not have fat solubility, does not easily pass through the blood-brain barrier, has little impact on the central nervous system, and has no anticholinergic effect. It is widely welcomed by both doctors and patients, but cardiotoxicity is an adverse reaction that cannot be ignored. Moreover, most of these drugs are metabolized by cytochrome P450 isoenzymes in the liver, and they are easy to interact with drugs, and the safety and therapeutic effect of administration in different populations are also different.
[0016] In the research process, repeating the method of the prior art, the obtained bilastine has a large number of impurities, a high total amount of impurities, and low optical purity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] In a 500ml reaction flask equipped with stirring, thermometer and condenser, add 60 grams of bilastine and 240 milliliters of water, add 0.05 grams of dimethylformamide (DMF) to the above aqueous solution, stir for 40 minutes, filter, and the filtrate Cool to 8°C and set aside.

[0050] Cool 900ml of acetonitrile-methyl ethyl ketone = 7:5 mixture to 8°C, add the above standby solution while stirring, keep warm for 18 hours, crystals precipitate, filter, and dry to obtain 53.3 grams of white crystals. Purity 99.9% (HPLC normalization method), optical purity 99.96% ee (chiral HPLC).

[0051] This crystal was subjected to X-ray diffraction measurement. Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50 ° . The result is as follows:

[0052]

Embodiment 2

[0054] Capsules containing bilastine compound

[0055] Prescription: 20 grams of bilastine compound, 100 grams of mannitol, 140 grams of lactose, 50 grams of calcium carbonate, 5 grams of magnesium stearate, appropriate amount of 8% ethyl cellulose solution, 1000 enteric-coated capsules, made into 1000 capsules .

[0056] Process: Mix bilastine compound, mannitol, lactose, and calcium carbonate evenly; add an appropriate amount of binder 8% ethyl cellulose solution to make a soft material, granulate with a 20-mesh screen, and dry at 40°C±2°C. Whole grains, add externally mixed magnesium stearate, mix evenly, pack into capsules, and obtain.

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Abstract

Belonging to the medical technology field, the invention in particular relates to a Bilastine compound and a preparation method thereof. The Bilastine obtained by the invention has the advantages of: chemical purity of 99.9%, maximum impurity of less than 1 per thousand, optical purity up to 99.96 percent enantiomeric excess, and good stability. The compound provided by the invention has the characteristics of low production cost and stable quality, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a bilastine compound and a preparation method thereof. Background technique [0002] Allergic rhinitis (AR), also known as allergic rhinitis, refers to a non-infectious inflammatory disease of the nasal mucosa mainly mediated by IgE (immunoglobulin) after the body is exposed to allergens. According to whether the patient has seasonal characteristics, it can be divided into perennial allergic rhinitis (PAR) and seasonal allergic rhinitis (SAR). Urticaria is a localized edema reaction caused by dilation and increased permeability of small blood vessels in the skin and mucous membrane. The main clinical manifestations are wheals and erythema, which may also be accompanied by abdominal pain and diarrhea. In severe cases, laryngeal edema or even shock may occur. Easy to relapse, increasing the suffering of patients. According to the duration of the disease, urticaria ca...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/454A61P11/02A61P37/08A61P17/00
CPCC07D401/04
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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