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Optically sensitive pure S-(-)-arotinolol acid salt, preparation method and applications thereof

A technology of acid salt and hydrochloride, which is applied in the field of medicine and can solve the problems of not providing a preparation method

Inactive Publication Date: 2014-03-05
北京博爱旺康医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although S-(-)-alolol is disclosed in the patent EP0105996, its preparation method is not provided

Method used

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  • Optically sensitive pure S-(-)-arotinolol acid salt, preparation method and applications thereof
  • Optically sensitive pure S-(-)-arotinolol acid salt, preparation method and applications thereof
  • Optically sensitive pure S-(-)-arotinolol acid salt, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Inorganic acid salt S-(-)-alolol syrup of the present invention

[0046] Dissolve 30 g of sucrose and 1 g of sucralose in 60 ml of warm water, add 1 g of inorganic acid salt S-(-)-alolol after cooling, and add 0.05 g of orange flavoring agent, and dilute the mixture with water to obtain 100 ml of syrup.

Embodiment 2

[0047] Example 2 Organic acid salt S-(-)-alolol syrup of the present invention

[0048] Dissolve 30 g of sucrose and 1 g of sucralose in 60 ml of warm water, add 1 g of organic acid salt S-(-)-alolol after cooling, and add 0.05 g of orange flavoring agent, and dilute the mixture with water to obtain 100 ml of syrup.

Embodiment 3

[0049] Example 3 Inorganic acid salt S-(-)-arololol enteric-coated tablet of the present invention

[0050] Take 100g of inorganic acid salt S-(-)-alolol, mix with 500g of lactose monohydrate, 200g of microcrystalline cellulose, and 50g of hydroxypropyl cellulose, add an appropriate amount of aqueous solution to granulate, and use a swinging granulator to pass 18 mesh screen and dried in an oven. After drying, use a 20-mesh sieve to sieve the granules and mix with 8 g of magnesium stearate. Compress the dry mixture into tablet cores with a punch of 5 mm diameter in a tablet machine, and in a coating device, 200 g of cellulose acetate phthalate and 15 g of cetyl alcohol in 2000 g of isopropanol and 2000 g of dichloromethane Spray the mixed solution on the tablet core to make enteric-coated tablet.

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PUM

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Abstract

The invention belongs to the technical field of medicine, specifically discloses an optically sensitive pure S-(-)-arotinolol acid salt, and researches a preparation method and applications of the arotinolol acid salt at the same time. Through a large amount of research and experimental results, the technicians found that the prepared S-(-)-arotinolol acid salt is a crystal product, and can be used for preparation of drugs or heath care product for treating essential hypertension, angina pectoris, tachycardia induced arrhythmia, and essential tremor.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an optically pure S-(-)-alolol acid salt and a preparation method and application thereof. Background technique [0002] S-(-)-alolol, the chemical name is S-(-)-5-[2-[(3-tert-butylamino-2-hydroxypropyl)mercapto]-4-thiazolyl]-2-thiophene Formamide is a drug with β-receptor blocker and weak α-receptor blocker effect, used for the treatment of essential hypertension, angina pectoris, tachycardia arrhythmia and essential tremor. The radioligand binding studies have proved that there are differences in the affinity between arololol and β and α receptors. In the human body, β-receptor blockade is dominant, and α-receptor blocker activity is weak. The ratio of alpha-receptor blockade and beta-receptor blockade is 1:8. However, α-blockers can cause adverse reactions such as orthostatic hypotension, dizziness, fainting, palpitations, and water and sodium retention. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/04A61K31/427A61P9/12A61P9/10A61P9/06A61P25/14A23L1/29A23L33/00
CPCC07D417/04
Inventor 黄华
Owner 北京博爱旺康医药科技有限公司
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