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Dihydropyridine medicine nano suspension and preparation method thereof

A dihydropyridine, nanosuspension technology, applied in the directions of drug combination, nanotechnology, pharmaceutical formulations, etc., can solve the problems of improving the solubility of dihydropyridines without nanosuspension technology, and achieve good physical stability. , the effect of increasing the specific surface area and increasing the dissolution rate

Pending Publication Date: 2021-11-09
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no disclosure of using nanosuspension technology to improve the solubility of dihydropyridines.

Method used

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  • Dihydropyridine medicine nano suspension and preparation method thereof
  • Dihydropyridine medicine nano suspension and preparation method thereof
  • Dihydropyridine medicine nano suspension and preparation method thereof

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preparation example Construction

[0063] The embodiment of the present invention also discloses a preparation method of the above-mentioned dihydropyridine drug nanosuspension, which specifically includes the following steps:

[0064] (1) Add the stabilizer to the water for 15-60 minutes to form a stabilizer solution;

[0065] (2) Add dihydropyridines to the above stabilizer solution, and magnetically stir for 30-90 minutes to obtain a coarse suspension;

[0066] (3) Add the coarse suspension into the grinding chamber of the ultrafine grinder, and add grinding beads at the same time, and grind to obtain the dihydropyridine drug nanosuspension;

[0067] Among them, the grinding beads are yttrium-stabilized zirconium beads, zirconium silicate grinding beads or polystyrene grinding beads, the particle size of the grinding beads is 0.3-0.8mm, and the volume of the grinding beads is 140ml; the grinding time is 15-60min, and the grinding speed It is 1500-4500rpm, and the grinding temperature is controlled at 10-30°...

Embodiment 1

[0071] Embodiment 1 of the present invention also discloses a preparation method of a dihydropyridine drug nanosuspension, specifically comprising the following steps:

[0072] (1) Take 0.1g of Soluplus, add it to 50ml of distilled water, stir with a magnetic stirrer for 30min, and the stirring speed is 600r / min to obtain a stabilizer solution;

[0073] (2) Add 0.25g nitrendipine to the stabilizer solution, stir with a magnetic stirrer for 60min, and the stirring speed is 450r / min to obtain a coarse suspension;

[0074] (3) Add the coarse suspension to the grinding chamber of the circulating nano-grinding machine, then add 140 ml of zirconia grinding beads with a particle size of 0.6-0.8 mm, and grind for 30 min at 3000 rpm to obtain the nitrendipine nano-suspension .

[0075] The prepared nitrendipine nanosuspension was diluted 3 times with purified water, and the measured particle size was 478.6nm, and the potential was -28.62mV.

Embodiment 2

[0077] Embodiment 2 of the present invention also discloses a preparation method of a dihydropyridine drug nanosuspension, specifically comprising the following steps:

[0078] (1) Take chitosan 0.1g, add in 50ml distilled water, stir with a magnetic stirrer for 30min, and the stirring speed is 600r / min to obtain a stabilizer solution;

[0079] (2) Add 0.25g nitrendipine to the stabilizer solution, stir with a magnetic stirrer for 60min, and the stirring speed is 450r / min to obtain a coarse suspension;

[0080] (3) Add the coarse suspension to the grinding chamber of the circulating nano-grinding machine, then add 140 ml of zirconia grinding beads with a particle size of 0.6-0.8 mm, and grind for 30 min at 3000 rpm to obtain the nitrendipine nano-suspension .

[0081] The prepared nitrendipine nanosuspension was diluted 3 times with purified water, and the measured particle size was 277.1 nm, and the potential was -6.55 mV.

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Abstract

The invention discloses a dihydropyridine medicine nano suspension which is prepared by performing nanocrystallization treatment on a dihydropyridine medicine and a stabilizer, the dihydropyridine medicine is prepared from any one of nifedipine, nitrendipine, nisoldipine and felodipine; the stabilizing agent is any one of Soluplus, chitosan, TPGS, povidone K30, lecithin and poloxamer 407; the invention further discloses a preparation method of the dihydropyridine medicine nano suspension, and any one or combination of more of a medium grinding method, a high-pressure homogenization method, a solvent precipitation method and a high-pressure homogenization method is adopted. The dihydropyridine drug nano suspension prepared by the method has the characteristics of high preparation efficiency and high dissolution rate, and can ensure quick absorption and stable drug effect of the drug when being used as a preparation intermediate or a drug preparation finished product; the mechanism is clear, the process technology is feasible, stable and reliable, and a technical means easy to industrialize is provided for development of the nano suspension.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a dihydropyridine drug nanosuspension and a preparation method thereof. Background technique [0002] Dihydropyridine drugs are common drugs for the clinical treatment of arrhythmia, hypertension, angina pectoris and other diseases. They can inhibit the influx of extracellular calcium ions, relax vascular smooth muscle, reduce peripheral vascular resistance, and lower blood pressure. Nifedipine, nitrendipine, felodipine, and nisoldipine are classified as dihydropyridine drugs on average, belonging to class II of the biopharmaceutical classification system (BCS), that is, low solubility and high permeability. [0003] At present, in view of the problem of poor solubility of dihydropyridine drugs, domestic and foreign researchers have improved it by using new drug preparation methods. For example, Chinese invention patent CN109730967A discloses "a solid dispersi...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4422A61K47/26A61K47/24A61K47/32A61K47/34A61K47/36A61P9/06A61P9/10A61P9/12B82Y5/00B82Y40/00
CPCA61K31/4422A61K9/10A61K47/26A61K47/34A61K47/32A61K47/36A61K47/24A61P9/06A61P9/12A61P9/10B82Y5/00B82Y40/00
Inventor 杨建宏马世杰田宗花买亚萍李治芳侯延辉
Owner NINGXIA MEDICAL UNIV
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