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Roflumilast pharmaceutical composition with high bioavailability and preparation method thereof

A technology for roflumilast and a composition, which is applied in the field of roflumilast pharmaceutical compositions and their preparation, can solve the problems of extremely high production equipment requirements, small specifications, and difficulty in industrialized implementation, and achieves solutions to differences in content uniformity. larger effect

Active Publication Date: 2011-12-14
天津汉嘉医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The second generation of selective PDE-4 inhibitors, such as cilomilast and roflumilast, but the results of some trials of cilomilast are different from expectations in terms of drug efficacy and safety. As a result, further development of the drug has been discontinued
[0020] Due to its small size, the roflumilast pharmaceutical composition produced by the prior art has extremely high requirements on production equipment, and most of them use imported equipment from abroad, which is expensive and difficult to implement the project industrially

Method used

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  • Roflumilast pharmaceutical composition with high bioavailability and preparation method thereof
  • Roflumilast pharmaceutical composition with high bioavailability and preparation method thereof
  • Roflumilast pharmaceutical composition with high bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] The described roflumilast pharmaceutical composition of every 1000, its formula consists of:

[0093] Roflumilast 0.5g

[0094] Beta cyclodextrin 1g

[0095] Lactose 10g

[0096] Microcrystalline Cellulose 12 70 g

[0097] Magnesium Stearate 2g

[0098] Preparation Process:

[0099] 1) Preparation: dry microcrystalline cellulose 12, lactose, and magnesium stearate at 80°C for 4 hours, and set aside;

[0100] 2) Put the prescribed amount of beta-cyclodextrin and roflumilast in a container, mix well, grind until the particle size is 80±10um, and set aside;

[0101] 3) Mix item 2) with the prescribed amount of microcrystalline cellulose 12 and magnesium stearate;

[0102] 4) Tablet compression: adjust the appropriate hardness and tablet weight, and perform tablet compression;

[0103] 5) Packing: packed by aluminum-plastic blister packaging machine;

[0104] 6) Storage.

Embodiment 2

[0106] The described roflumilast pharmaceutical composition of every 1000, its formula consists of:

[0107] Roflumilast 0.25g

[0108] Beta cyclodextrin 0.5g

[0109] Lactose 5g

[0110] Microcrystalline Cellulose 12 70 g

[0111] Magnesium Stearate 2g

[0112] Preparation process: with embodiment 1.

Embodiment 3

[0114] The described roflumilast pharmaceutical composition of every 1000, its formula consists of:

[0115] Roflumilast 1g

[0116] Beta Cyclodextrin 2g

[0117] Lactose 20g

[0118] Microcrystalline Cellulose 12 140 g

[0119] Magnesium Stearate 2g

[0120] Preparation process: with embodiment 1.

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Abstract

The invention discloses a high-bioavailability roflumilast medicinal composition, which consists of roflumilast, betacyclodextrin, lactobiose, microcrystalline cellulose and magnesium stearate. The medicinal composition is characterized in that: a weight ratio of the roflumilast to the betacyclodextrin to the lactobiose is 1:2:20; the roflumilast medicinal composition has the advantages of improving yield, reducing cost, realizing industrialization, along with high stability; and the composition is better applied clinically, and the dissolution rate and bioavailability can be improved effectively; and the high-bioavailability roflumilast medicinal composition can be used for treating chronic obstructive pulmonary diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a roflumilast pharmaceutical composition and a preparation method thereof. Background technique [0002] There are approximately 42 million asthmatics and 28 million COPD (chronic obstructive pulmonary disease) patients worldwide. In the past ten years, with the global air pollution and environmental deterioration, the morbidity and mortality of asthma are on the rise, and more than 180,000 people die from asthma every year. Another analysis shows that by 2020, COPD will climb from the current sixth place in the global cause of death to the third place. It is conservatively estimated that the number of deaths due to COPD will reach more than 3.5 million worldwide by then. In China, an epidemiological survey conducted by Academician Zhong Nanshan showed that the overall prevalence of COPD in China is 8.2%, of which 12.4% are male and 5.1% are female. There are more...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61K47/40A61P11/00
Inventor 严洁黄欣
Owner 天津汉嘉医药科技有限公司
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