Roflumilast dispersible tablet composition and preparation method thereof

Abstract

The invention provides a roflumilast dispersible tablet composition, which is characterized by being composed of: roflumilast, copovidone, sodium stearyl fumarate and pharmaceutically-acceptable auxiliary materials. The roflumilast dispersible tablet composition prepared through the method in the invention is good in dispersion uniformity. A common tablet needs more than 5 min to disintegrate completely, while the roflumilast dispersible tablet can be disintegrated completely only within 70 s and can pass through a 2# sieve, wherein the time is far less than 3 min specified in Chinese pharmacopoeia. The roflumilast dispersible tablet is greatly increased in disintegration speed and meanwhile is greatly increased in dissolution rate compared with the common tablets in the prior art. The dissolution rate can reach 85% at 5 min and furthermore can reach 95% at 15 min. The roflumilast dispersible tablet composition is greatly increased in bio-utilization rate.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a roflumilast dispersible tablet composition and a preparation method thereof. Background technique [0002] Roflumilast, English name: Roflumilast, chemical name: 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy ) benzamide, the molecular formula is: C 17 h 14 Cl 2 f 2 N 2 o 3 , the molecular weight is 403.21, and the chemical structural formula is: [0003] [0004] Chronic obstructive pulmonary disease (COPD) is a preventable and treatable disease characterized by airflow limitation that is not fully reversible and progressive. COPD mainly involves the lungs. As a chronic inflammatory disease of the airways and lungs, COPD has become one of the common diseases and leading causes of death worldwide. As an anti-inflammatory drug, roflumilast can effectively improve the lung function of patients with moderate to severe COPD, reduce the f...

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Problems solved by technology

[0005] Chinese patent CN102743353A discloses a roflumilast tablet preparation and its preparation method. The patent uses povidone K90 as a binder. However, due to the high viscosity of povidone K90 and its strong hygroscopicity, it is easy to cause the sample to be damaged for a long time. Dissolution is affected to a greater extent after standing

[0007] The inventor developed Roflumilast Dispersible Tablets through a large number of experiments and explorations, which overcomes the shortcomings of slow onset of action and low bioavailability of traditional dosage forms, and improves its clinical application value

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