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Preparation technology of roflumilast film-coated tablets

A technology of roflumilast and film coating, which is applied in the field of tablet preparation, can solve the problem of difficulty in realizing tablet production quickly and efficiently, and achieves good batch-to-batch reproducibility, less fine powder, and smooth plain tablets. Effect

Inactive Publication Date: 2020-09-11
山东希尔康泰药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Roflumilast Biopharmaceutical Classification (BCS) belongs to the second class (low solubility-high permeability drug), which belongs to the drug that is poorly soluble in water, and the bioavailability of the drug in the process of preparing the drug basically depends on the drug from Release in pharmaceutical dosage forms, the current roflumilast film-coated tablets are difficult to quickly and efficiently realize the production of tablets by using the traditional preparation process during the preparation process

Method used

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  • Preparation technology of roflumilast film-coated tablets
  • Preparation technology of roflumilast film-coated tablets
  • Preparation technology of roflumilast film-coated tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation of the first batch of samples (batch number 120301) and the study of the main process parameters were carried out in small scale scale-up.

[0039] Equipment: SHK-6 laboratory fast wet granulator, YK60 swing granulator, DHG-9203A electric blast drying oven, ZP5 rotary tablet press, GBB-38 laboratory high-efficiency coating machine.

[0040] (1) Screening and mixing of raw and auxiliary materials: take roflumilast raw materials and micronize them (particle size range: D(90)=13.498, D(50)=5.398, D(10)=1.086), and set aside; lactose, starch, Magnesium stearate is passed through an 80-mesh sieve respectively, and is set aside. Mix the prescription amount of roflumilast with about 13% of the prescription amount of starch in equal increments; set aside (the weight after mixing accounts for about 3.1% of the total prescription amount). The roflumilast starch mixture was mixed with the prescription amount of lactose and remaining starch in a laboratory rapid we...

Embodiment 2

[0058] The preparation of the second batch of samples (batch number 120302) and the study of the main process parameters were carried out in small scale scale-up.

[0059] (1) Screening and mixing of raw and auxiliary materials: micronize the raw materials of roflumilast (particle size range: D(90)=13.498, D(50)=5.398, D(10)=1.086), and set aside; lactose, starch, Magnesium stearate is passed through an 80-mesh sieve respectively, and is set aside. Mix the prescription amount of roflumilast with about 13% of the prescription amount of starch in equal increments; set aside (the weight after mixing accounts for about 3.1% of the total prescription amount). The roflumilast starch mixture was mixed with the prescribed amount of lactose and remaining starch in a laboratory rapid wet granulator (stirrer speed 400 rpm, cutter speed 600 rpm, 4 minutes). Samples were taken at the upper, middle and lower positions to determine the content, and the RSD was calculated. The results are sh...

Embodiment 3

[0074] The preparation of the third batch of samples (batch number 120303) and the study of the main process parameters were carried out in small scale scale-up.

[0075] (1) Screening and mixing of raw and auxiliary materials: micronize the raw materials of roflumilast (particle size range: D(90)=13.498, D(50)=5.398, D(10)=1.086), and set aside; lactose, starch, Magnesium stearate, pass through 80 mesh sieves respectively, and set aside. Mix the prescription amount of roflumilast with about 13% of the prescription amount of starch in equal increments; set aside (the weight after mixing accounts for about 3.1% of the total prescription amount). The roflumilast starch mixture was mixed with the prescribed amount of lactose and remaining starch in a laboratory rapid wet granulator (stirrer speed 400 rpm, cutter speed 600 rpm, 4 minutes). Samples were taken at the upper, middle and lower positions to determine the content, and the RSD was calculated. The results are shown in Tab...

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Abstract

The invention relates to the technical field of tablet preparation, in particular to a preparation technology of roflumilast film-coated tablets. The preparation technology comprises the following steps of S1, micronizing roflumilast, and filtering starch, lactose and magnesium stearate through an 80-mesh sieve for later use; S2, dissolving hydroxypropyl methylcellulose into water to prepare aqueous solutions of different concentrations for later use; S3, mixing a mixture obtained by multiple equal incremental blending of 1 g of roflumilast and 15 g of starch with 398 g of lactose and remaining starch in the step S1; S4, adding an adhesive for granulation after mixing is ended; S5, preparing wet granules from prepared soft materials; S6, drying the wet granules obtained in the step S5; S7,carrying out granulation on the dried granules through a 20-mesh sieve; and S8, carrying out tableting by using a shallow concave mold with the diameter of 9 mm. When granulation is carried out by using the method, the granulation condition is good, the granules are uniform, the tablets are bright and clean, and the friability of tablet cores meets the requirements. Samples meeting the standard can be prepared through the method, the interbatch reproducibility is good, the samples are equivalent to originally commercially available products in quality, and production can be smoothly implemented through the preparation technology of a prescription.

Description

technical field [0001] The invention relates to the technical field of tablet preparation, in particular to the preparation process of roflumilast film-coated tablets. Background technique [0002] Roflumilast is an oral selective phosphodiesterase-4 (PDE4) inhibitor, a new type of chronic obstructive pulmonary disease (COPD) therapeutic drug for the treatment of asthma and chronic obstructive pulmonary disease. The first new oral drug that has been approved for the treatment of chronic obstructive pulmonary disease worldwide in more than ten years, the dosage form of roflumilast is tablet. Roflumilast Biopharmaceutical Classification (BCS) belongs to the second class (low solubility-high permeability drug), which belongs to the drug that is poorly soluble in water, and the bioavailability of the drug in the process of preparing the drug basically depends on the drug from Release in the pharmaceutical dosage form, the current roflumilast film-coated tablets are difficult to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K47/36A61K47/38A61K47/26A61K47/12A61K31/44A61P11/00
CPCA61K9/2013A61K9/2018A61K9/2054A61K9/2059A61K9/2095A61K9/2806A61K31/44A61P11/00
Inventor 张存国广国良王贺
Owner 山东希尔康泰药业有限公司
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