Vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation

A technology for trifluoromethanesulfonic acid and pharmaceutical preparations, which is applied in the field of pharmaceutical preparations containing vilanterol trifluoromethanesulfonate, can solve problems such as long action time, improve health status, reduce the number of acute exacerbations, clinical efficacy and good safety effect

Inactive Publication Date: 2014-07-23
SHANGHAI NEW ASIA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its pair M 3 Cholinergic receptors are highly selective and can interact with M after entering the body 2 and M 3 receptor binding, but its interaction with M 3 The receptor binds more strongly, and the half-life is M 2 6 times that of the receptor, therefore, its action time is long, it is a long-acting cholinergic receptor antagonist, and its anti-M 2 Adverse reactions of receptors, such as tachycardia, etc., are relatively rare

Method used

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  • Vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation
  • Vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation
  • Vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Vilanterol triflate / fluticasone furoate aclidinium bromide granules / tablets / capsules Prescription:

[0033]

[0034] Preparation steps: mix the main ingredient, lactose, and croscarmellose sodium uniformly in equal amounts, prepare a soft material with 3% PVP k30 as a binder, granulate with a 20-mesh sieve, dry at 60°C, and dry at 20-mesh The granules are obtained by sieving and granulating. Add the prescribed amount of magnesium stearate after granulation, mix uniformly and compress to obtain tablets or fill capsules to obtain capsules.

Embodiment 2

[0036] Vilanterol triflate / fluticasone furoate aclidinium bromide orally disintegrating tablets:

[0037]

[0038] Preparation steps: mix the main ingredient and auxiliary materials uniformly by the equal-volume incremental method, pass through a 100-mesh sieve, and directly compress into tablets.

Embodiment 3

[0040] Vilanterol triflate / fluticasone furoate aclidinium bromide extended-release tablets prescription:

[0041]

[0042] Preparation steps: mix the main ingredient, microcrystalline cellulose, and hypromellose evenly in equal amounts, use 0.5% hydroxypropyl cellulose as a binder to prepare a soft material, granulate with a 20-mesh sieve, and dry at 60°C , 20-mesh sieve, adding magnesium stearate in prescribed amount, mixing evenly, and compressing into tablets to obtain sustained-release tablets.

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Abstract

The invention discloses a vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation, which comprises the following main active ingredients: long-acting beta2 receptor agonist vilanterol trifluoromethanesulfonate, glucocorticoid drug fluticasone furoate and long-acting anticholinergic drug aclidinium bromide, or physiologically acceptable salts of the fluticasone furoate and aclidinium bromide, thus composing a compound preparation. The vilanterol trifluoromethanesulfonate has the effect of continuously dilating blood vessels for 24 hours; the fluticasone furoate is fast-acting potent glucocorticoid, and the duration time of the drug is longer than that of other glucocorticoids; the aclidinium bromide is long-acting cholinergic receptor antagonist, and combines with beta2 receptor agonist so as to play roles of synergism and reduction of adverse drug reaction. The vilanterol trifluoromethanesulfonate, the fluticasone furoate and the aclidinium bromide are combined for use to prepare an inhalable compound preparation which can be taken once daily due to 24-hour acting. The vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation can enhance the curative effect, solves the compliance problem of patients with coexisting chronic obstructive pulmonary disease and asthma, thus being appreciable in application prospects.

Description

technical field [0001] The present invention relates to a pharmaceutical preparation containing vilanterol trifluoromethanesulfonate and a preparation method thereof, that is, containing long-acting β 2 A compound preparation of the receptor agonist vilanterol trifluoromethanesulfonate, the long-acting anticholinergic drug aclidinium bromide and the glucocorticoid fluticasone furoate, which is used to effectively treat the respiratory system such as asthma and chronic obstructive pulmonary disease disease. Background technique [0002] Chronic obstructive pulmonary disease (COPD) is a common chronic respiratory disease. COPD has a large number of patients and a high mortality rate, which affects the health of the public and brings a heavy economic burden to the society. COPD is currently the fourth leading cause of death in the world, and it is estimated that by 2020, COPD may become the third leading cause of death in the world. COPD is mainly manifested as airflow limita...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P11/06A61P11/00A61P29/00A61K31/439A61K31/137
Inventor 苏恩云袁凌霄乔晋林
Owner SHANGHAI NEW ASIA PHARMA
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