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Method for preparing roflumilast tablets

A technology for roflumilast tablets and tableting, which is applied in the field of preparing roflumilast tablets, can solve problems such as being unfavorable to large-scale production, cumbersome process, easy consumption and the like

Inactive Publication Date: 2016-12-07
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method does not use micronization, the raw materials are dissolved in ethanol, mixed with auxiliary materials and dried evenly, crushed and then granulated with a binder, and dried; two-step mixing and two-step drying, the process is cumbersome and not conducive to large-scale production, and it is easy to consume energy increased cost

Method used

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  • Method for preparing roflumilast tablets
  • Method for preparing roflumilast tablets
  • Method for preparing roflumilast tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The selection test of embodiment 1 principal agent dissolving solvent

[0033] Take about 0.5 g of the raw materials and put them in a beaker, gradually add ethanol solutions of different concentrations (50%, 75%, 95%), observe while shaking until the solution is clear, and weigh the amount of added solvent. According to the amount of different ethanol concentrations, 250g of mixed auxiliary materials were used to make soft materials, and the humidity of the soft materials was observed, and sieved with a 20-mesh sieve. The results are shown in Table 1.

[0034] Table 1 The selection and investigation results of the main ingredient dissolving solvent

[0035]

[0036] Result: The above-mentioned ethanol solutions with different concentrations can dissolve 500mg of raw materials (1000 prescriptions) well under a certain amount, and the amount of solvent has a good wetting effect on 1000 prescriptions (about 250g) To determine the formability of this product, use 50-95...

Embodiment 2

[0037] Embodiment 2 The screening test of roflumilast tablet binder of the present invention

[0038] Because this product is a small-scale drug, the proportion of the raw material in the preparation is very small, and the content uniformity is one of the main quality control indicators. In order to ensure the content uniformity, the raw and auxiliary materials need to be directly mixed with the raw material. The process is complex and difficult to control Therefore, it is planned to uniformly disperse the raw material drug in the solvent for granulation, and select different types of binders such as hydroxypropyl cellulose (HPC), hypromellose (HPMC), povidone K30 (PVPK30) , povidone K90 (PVPK90), carboxymethyl cellulose sodium (CMC-Na) and starch, were prepared with water and 50% ethanol respectively into the binder solution of conventional concentration, then added the same amount (0.5g) of the main drug , Observe the dissolution situation and phenomenon. The results are sh...

Embodiment 3

[0044] Embodiment 3 The proportioning test of principal ingredient and binder in the roflumilast tablet of the present invention

[0045] The raw materials and PVPK90 were added to appropriate amount of 50% ethanol in different proportions, stirred to disperse and dissolve, and the dispersion and dissolution conditions were observed.

[0046] Table 4 Dissolution investigation results of different ratios of main drug and PVPK90

[0047]

[0048] Results: When the ratio of raw material to PVPK90 is 1:3 or above, the raw material drug can be completely dissolved into a solution, and the ratio of API to PVPk90 in the prescription of this product is determined to be 1:3 or above.

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Abstract

The invention provides a method for preparing roflumilast tablets. The method includes steps of a, weighing raw materials and excipients including, by weight, 1 part of roflumilast, 20-450 parts of lactose, 10-250 parts of corn starch, 3-25 parts of povidone K90 and 0.5-25 parts of magnesium stearate; b, dissolving the roflumilast and the povidone K90 in 50-95% ethyl alcohol to prepare medicine-containing adhesive; c, sieving the lactose and the corn starch and mixing the lactose and the corn starch with each other to obtain mixtures; d, adding the medicine-containing adhesive obtained at the step b into the mixtures of the lactose and the corn starch and carrying out granulation, drying, shaping, total blending and tabletting to obtain the tablets. The method for preparing the roflumilast tablets has the advantages that the medicine content uniformity can be guaranteed, raw material micronization for controlling the particle sizes can be omitted, and dissolution of indissolvable medicines can be improved; the indissolvable medicines can be jointly dissolved, accordingly, technological operation steps can be reduced, energy can be saved, and the cost can be lowered.

Description

technical field [0001] The invention relates to a method for preparing roflumilast tablets, belonging to the field of pharmaceutical preparations. Background technique [0002] Roflumilast was researched and developed by Anda Company of Germany in 1993. In 2009, Nycomyn Company of Switzerland completed the Phase III clinical trial. It was approved for marketing by the European Union in July 2010. It is the first new type of COPD approved by the European Union in more than ten years. Therapeutic drugs have been marketed in Germany, Britain, Denmark and other countries. In December 2010, it was approved for marketing in Canada, and in March 2011, it was approved for clinical use by the U.S. FDA (trade name: "Daliresp TM ", specification: 0.5mg, dosage form: tablet) has thus become the first new oral drug approved for the treatment of chronic obstructive pulmonary disease worldwide in more than ten years. [0003] Patent application number CN201210261940.7, invention name: ro...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/44A61K47/36A61K47/32A61P11/00
Inventor 陈龙江赵栋沈利兰西刘真君王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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