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Preparation methods of nimodipine hot-melt extruded solid dispersion and nimodipine tablet

A technology of hot-melt extrusion and solid dispersion, which is applied in the field of medicine, can solve problems such as pollution, solvent residue, and poor dissolution in hydrochloric acid medium, and achieve the effects of strong operability, fast dissolution speed, and high dissolution rate

Active Publication Date: 2019-03-19
YABAO PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In order to solve the problems of solvent residue, pollution and poor dissolution in hydrochloric acid medium in the existing production process of nimodipine tablets, the invention provides a method for preparing a hot-melt extrusion solid dispersion of nimodipine, which comprises the following step:

Method used

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  • Preparation methods of nimodipine hot-melt extruded solid dispersion and nimodipine tablet
  • Preparation methods of nimodipine hot-melt extruded solid dispersion and nimodipine tablet
  • Preparation methods of nimodipine hot-melt extruded solid dispersion and nimodipine tablet

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Effect test

Embodiment 1

[0070] Raw drug nimodipine 30g, povidone K25 65g, povidone K12 5g were mixed for 10 minutes, and the extrusion parameters of the hot melt extruder were set: the temperature from the feeding port to the die was 50-80-130-170- 170-170-170-170-160-150°C, speed 50rpm, the material is extruded into transparent yellow strips, after cooling, cut off by a granulator, and then crushed with a high-speed universal grinder, and the mixed powder (equivalent to Nimodipine 30mg), measure the stripping curve under the pH1.2 according to the dissolution assay paddle method, after the solid dispersion powder meets the quality requirements, add crospovidone 30g in the 100g nimodipine solid dispersion powder, Mix 146g of microcrystalline cellulose, 53g of lactose, and 1g of magnesium stearate for 10 minutes, press the tablet according to the tablet weight of 330mg, use 12% coating premix for film coating, and the coating weight gain is 3-5%; according to the dissolution rate Assay The dissolution...

Embodiment 2

[0072] Nimodipine 30g, povidone K25 240g, povidone K17 30g mixed for 10 minutes, set the extrusion parameters of the hot melt extruder: the temperature from the feeding port to the die is 50-80-130-160-165- 165-165-160-160-150°C, speed 300rpm, the material is extruded into transparent yellow strips, after cooling, cut off by a granulator, pulverized with a Fitzmill pulverizer, and accurately weighed the mixed powder (equivalent to nimodipine 30mg), measure the dissolution curve at pH1.2 according to the dissolution method paddle method, after the solid dispersion powder meets the quality requirements, take by weighing 300g nimodipine solid dispersion powder, add croscarmellose sodium 30g , 84g of microcrystalline cellulose, 35g of starch, and 1g of magnesium stearate were mixed for 10 minutes, pressed according to the tablet weight of 450mg, and film-coated with 12% coating premix, and the coating weight increased by 3-5%; The dissolution profile at pH 1.2 was determined by pa...

Embodiment 3

[0074] Nimodipine 30g was mixed with povidone K25 150g for 10 minutes, and the extrusion parameters of the hot melt extruder were set: the temperature from the feeding port to the die was 50-80-110-150-160-160-160-160- 155-155°C, speed 500rpm, the material is extruded into transparent yellow strips, after cooling, cut off by a granulator, and then crushed with a high-speed universal pulverizer, and the mixed powder (equivalent to 30mg of nimodipine) is accurately weighed, according to Dissolution assay Paddle method measures the dissolution curve under pH1.2, after the solid dispersion powder meets the quality requirements, take by weighing 180g nimodipine solid dispersion powder, add crospovidone 30g, microcrystalline cellulose 150g, 39g of lactose and 1g of magnesium stearate were mixed for 10 minutes, and pressed according to the tablet weight of 400mg. Finally, the coating premix solution with a solid content of 15% is used for film coating, and the weight gain of the coat...

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Abstract

The invention belongs to the field of pharmacy and relates to preparation method of a nimodipine hot-melt extruded solid dispersion and a nimodipine tablet. The preparation methods are characterized by taking povidone as the main carrier material, and adding in plasticizers as needed to reduce extrusion temperature and facilitate extrusion; finally, mixing the dispersion with auxiliary materials such as disintegrants, fillers and lubricant, pressing the mixture into the tablet directly, and then coating the tablet with a thin film to keep the tablet dry and out of the sun. The nimodipine hot-melt extruded solid dispersion and the nimodipine tablet have the advantages of high dissolving-out speed and high dissolution rate.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a nimodipine hot-melt extruded solid dispersion and a method for preparing a tablet thereof. Background technique [0002] The original research of Nimodipine Tablets was produced by Bayer AG in Germany Belonging to BCS class II drugs, it has low solubility in water and poor bioavailability. The original research uses acetone as a solvent to dissolve the nimodipine raw material and povidone k25 (PVP-K25), and then prepares a solid dispersion by solvent method, thereby improving the bioavailability of the drug. Domestic generic drugs are mostly prepared by simple raw material micronization and wet granulation processes. The drug exists in a crystalline state, with low dissolution rate and poor bioavailability. In addition, some manufacturers use a large amount of ethanol solvent to prepare solid dispersions. [0003] Nimodipine hot-melt extrusion technology uses acetone granulation to p...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/4422A61K47/32
CPCA61K9/2027A61K9/2095A61K9/28A61K31/4422
Inventor 戚永明田瑞琼何英翠徐从飞
Owner YABAO PHARMA GRP CO LTD