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Method for preparing nimodipine dispersible tablet with high dissolution

A technology of nimodipine and nimodipine, applied in the field of preparation of high-dissolution nimodipine dispersible tablets, can solve the problems of decreased bioavailability, complicated preparation process, low inclusion rate, etc., and achieves the improvement of oral biological Effects of availability, avoidance of drug metabolic inactivation, and ease of industrial production

Active Publication Date: 2007-04-25
徐竹青
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The low inclusion rate and small drug loading in clathrate technology have been unsolved problems for a long time. In recent years, many scholars have found that after the drug is encapsulated in cyclodextrin, although the solubility is improved, However, it is difficult for the drug to be released from the cyclodextrin cavity, and the complex of cyclodextrin and drug cannot be absorbed across the membrane, so the bioavailability decreases instead.
[0006] Solid dispersion technology plays a very significant role in improving the dissolution rate of insoluble drugs, but its preparation method has problems such as complex process, many equipments required, difficulty in scaling up, low reproducibility, residual organic solvents, and poor product stability , it is easy to age after being placed for a period of time, which limits its industrialization

Method used

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  • Method for preparing nimodipine dispersible tablet with high dissolution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] (1) Preparation of nimodipine solid solution: take copovidone S630 as the carrier, premix with nimodipine according to the ratio of 9:1 and 5 minutes, and the temperature of the melt extruder from the first section to the machine head is respectively Set to 90°C-130°C-130°C-130°C-130°C (specifically, the temperature of the first section is set to 90°C, the second section is set to 130°C, the third section is set to 130°C, and the fourth section is set to 130°C. The section is set to 130°C, the head temperature is set to 130°C), the premix of drug and carrier is added, and at a speed of 36 rpm, the melt extruder shears and disperses it, and melts and extrudes it at room temperature After cooling or quenching, a golden yellow transparent solid solution is obtained.

[0019] (2) The preparation of nimodipine solid solution dispersible tablets: get 200 grams of nimodipine solid solution, 73 grams of microcrystalline cellulose, 15 grams of crospovidone, 3 grams of sodium lau...

Embodiment 2

[0022] (1) Preparation of nimodipine solid solution: take polyethylene glycol as the carrier, premix with nimodipine according to the ratio of 9:1 and 5 minutes, and the temperature of the melt extruder from the first section to the machine head is respectively Set at 90°C-130°C-130°C-130°C-130°C, add the premix of drug and carrier, and at a speed of 36 rpm, the melt extruder shears and disperses it, and melts and extrudes it. After cooling at room temperature or quenching, a golden yellow transparent solid solution is obtained.

[0023] (2) Preparation of nimodipine solid solution dispersible tablets: get 300 grams of nimodipine solid solution, 108 grams of starch, 27 grams of croscarmellose sodium, 4.5 grams of poloxamer and 10.5 grams of magnesium stearate, Nimodipine solid solution is pulverized, 60-80 mesh particles are collected, starch is made into soft material with 8% starch slurry, granulated with a 60 mesh sieve, granulated with a 60 mesh sieve after drying, mixed w...

Embodiment 3

[0026] (1) Preparation of nimodipine solid solution: take Acrylic Resin No. 4 as the carrier, premix with nimodipine according to the ratio of 5:1 and 5 minutes, and melt the extrusion machine from the first section to the temperature of the head Set at 90°C-130°C-130°C-130°C-130°C respectively, add the premix of drug and carrier, and at a speed of 36 rpm, the melt extruder shears and disperses it, and melts and extrudes it , After cooling at room temperature or quenching, a golden yellow transparent solid solution is obtained.

[0027] (2) The preparation of nimodipine solid solution dispersible tablets: get 180 grams of nimodipine solid solution, 65 grams of dextrin, 30 grams of low-substituted hydroxypropyl cellulose, 15 grams of sodium lauryl sulfate and 10 grams of micropowder silica gel, Nimodipine solid solution is pulverized, 60-80 mesh particles are collected, 8% starch slurry is used as soft material for dextrin, granulated with 60 mesh sieve, granulated with 60 mesh...

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Abstract

The invention relates to a method for preparing soluble Dunimodi disperser. Wherein, it comprises that using the Dunimodi material and hydrophilic carrier, via fusion protrusion technique, to prepare their sosoloid; breaking the sosoloid, to be mixed with stuff, lubricant and surface activator into tablet. The invention has simple process while the product has high dissolve speed, the drug can be released as molecule, to improve its utilization.

Description

technical field [0001] The invention relates to a preparation method of high-dissolution nimodipine dispersible tablets, which belongs to the improvement of the dosage form of nimodipine oral preparations. Background technique [0002] Nimodipine is a second-generation dihydropyridine calcium antagonist, which has good activity in the treatment of hypertension and migraine. Nimodipine was first developed and introduced to the market by Bayer, Germany. Utilization is low. [0003] Nimodipine is a hydrophobic drug with a saturated solubility in water of only 4 μg / ml. Since it is insoluble in water, a large part of the drug is always dispersed in the gastrointestinal fluid in the form of aggregates after entering the body, and cannot reach the molecular state. Therefore can not realize transmembrane absorption, has had a strong impact on its therapeutic effect. According to the commonly used drug biopharmaceutics classification system in the world, nimodipine belongs to the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/435A61P9/12A61P25/06
Inventor 唐星杨睿孙蕴哲徐竹青
Owner 徐竹青
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