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Roflumilast oral preparation and preparation method thereof

A technology for roflumilast and oral preparations, applied in the field of medicine, can solve the problems of unfavorable industrialization, increased drug cost for patients, and high input cost

Inactive Publication Date: 2014-02-12
JIANGSU CAREFREE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since this technology requires special micronization equipment in industrial production, the input cost is high, so it is not conducive to industrialization and virtually increases the cost of medication for patients

Method used

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  • Roflumilast oral preparation and preparation method thereof
  • Roflumilast oral preparation and preparation method thereof
  • Roflumilast oral preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Weigh 0.5 g of roflumilast raw material, dissolve it in 80 ml of methanol, and use it as a raw material solution; weigh about 12 g of starch, and prepare 10% starch slurry by boiling paddle method, as a binder. Weigh 160g of lactose and 30g of microcrystalline cellulose after passing through an 80-mesh sieve, add them to a tank mixer, stir to mix evenly, then add roflumilast solution, stir to moisten evenly, dry at 85°C, and evaporate methanol to dryness. Take the mixture after evaporating methanol, put it in a trough mixer, add 55g of 15% starch slurry, mix to make soft materials, and granulate with a swinging granulator. Dry at 80°C, add 2 g of croscarmellose sodium and 1.5 g of magnesium stearate after sizing, and mix. Check the granule content, determine the weight of the tablet, compress the tablet, coat it with a film, pack it, and get the Roflumilast tablet.

Embodiment 2

[0025] Weigh 0.5g of roflumilast raw material and dissolve it in 70ml of 95% ethanol as a raw material solution; weigh about 15g of starch, and make 15% starch slurry by boiling paddle method as a binder. Weigh 130g of lactose and 60g of starch after passing through an 80-mesh sieve, add them to a tank mixer, stir to mix evenly, then add roflumilast solution, stir to moisten evenly, dry at 70°C, and evaporate ethanol to dryness. Take the mixture after evaporating ethanol, put it in a trough mixer, add 70 g of 15% starch slurry, mix to make soft materials, and granulate with a swinging granulator. Dry at 70°C, add 2g of magnesium stearate after granulation, and mix. Check the granule content, determine the weight of the tablet, compress the tablet, coat it with a film, pack it, and get the Roflumilast tablet.

[0026] According to the method of Example 2, roflumilast tablets were prepared, the specification was 0.5 mg, and the batch number was 110501. Carried out the comparis...

Embodiment 3

[0032] Weigh 1.0 g of roflumilast raw material and dissolve it in 95 ml of 95% ethanol as a raw material solution; weigh about 6 g of PVPK30 to make a 6% PVPK30 solution as a binder. Weigh 185g of mannitol and 15g of hydroxypropyl cellulose after passing through a 100-mesh sieve, add them to a tank mixer, stir to mix evenly, then add roflumilast solution, stir to moisten evenly, dry at 70°C, and evaporate ethanol to dryness . Take the mixture after evaporating ethanol, put it in a trough mixer, add 65g of 6% starch slurry, mix to make soft materials, and granulate with a swinging granulator. Dry at 75°C, add 2g of micro-powder silica gel after sizing, and mix. Check the granule content, determine the weight of the tablet, compress the tablet, coat it with a film, pack it, and get the Roflumilast tablet.

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PUM

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Abstract

The invention provides a roflumilast oral preparation and a preparation method thereof. According to the invention, solvent solid dispersion technology is adopted, and the solid oral preparation is prepared by 0.1-50 wt% of roflumilast and 50-99.9 wt% of pharmaceutically acceptable auxiliary materials. Roflumilast tablets with stable and controllable quality can be produced by using common pharmaceutical equipment, which is helpful for vast patients to obtain cheap and good medicine products.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of roflumilast, in particular to an oral preparation of roflumilast and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Chronic Obstructive Pulmonary Disease (COPD) is a serious lung disease that can cause difficulty breathing. The main symptoms include wheezing, chronic cough, phlegm, etc. An attack can last up to several weeks and can lead to reduced lung function, severe anxiety, and even an increased risk of death. According to a study by the National Heart, Lung and Blood Institute, COPD is the fourth leading cause of death in the United States, and smoking is the main cause of COPD. [0003] Roflumilast is an oral, selective phosphodiesterase 4 (PDE4) inhibitor that has been shown to inhibit COPD-associated inflammation with a novel mode of action. It is the first drug for a new type of treatment for severe COPD. It is also the first...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61P11/00A61P29/00
Inventor 秦引林谢吉元
Owner JIANGSU CAREFREE PHARM CO LTD
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