Nimodipine solid dispersant and tablet and their preparation methods

A nimodipine solid and dispersant technology, applied in the field of medicine, can solve the problems of uneven particle size, complicated process, small particle size, etc., and achieve the effects of high bioavailability, simple preparation steps, and high dissolution rate

Active Publication Date: 2015-07-01
SHANGHAI CHEMPARTNER CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is to overcome the fact that the solid dispersion produced by the solid dispersion technology in the prior art is powdery, with small particle size and uneven particle size, and must be granulated, or crushed and granulated. Only after compression can be carried out, and the preparation of solid dispersion and granulation are separate processes, making the process complicated and other defects, a kind of nimodipine solid dispersion, tablet and preparation method thereof are provided

Method used

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  • Nimodipine solid dispersant and tablet and their preparation methods
  • Nimodipine solid dispersant and tablet and their preparation methods
  • Nimodipine solid dispersant and tablet and their preparation methods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] (1) Add 300g of microcrystalline cellulose (MCC), 100g of starch and 50g of crospovidone (PVPP) into the fluidized bed as a filler;

[0066] (2) Add 30g of nimodipine and 30g of povidone K25 (PVP K25) into 800g of ethanol and dissolve completely;

[0067] (3) Spray the above solution evenly on the filler in the fluidized bed, the atomization pressure of the fluidized bed is 1.8bar, the spraying speed of the fluidized bed is 6g / min, and the air intake volume during granulation is 30m 3 / h, the inlet air temperature is 60°C during granulation, and the drying time is 30 minutes after granulation, and the air inlet volume during drying is 40m 3 / h, the air inlet temperature is 70°C, the particles are dried and discharged to obtain the composition;

[0068] (4) Add 8 g of micropowder silica gel, 20 g of croscarmellose sodium and 4 g of magnesium stearate to 660 g of the prepared composition, mix well, press into tablets, and coat.

[0069] The marked amount per tablet is 3...

Embodiment 2

[0071] (1) Add 50g of microcrystalline cellulose (MCC) and 10g of starch into the fluidized bed as filler;

[0072] (2) Add 30g of nimodipine and 180g of povidone K30 (PVP K30) into a mixed solvent composed of 300g of chloroform and 10g of methanol to dissolve completely;

[0073] (3) Spray the above solution evenly on the filler in the fluidized bed, the atomization pressure of the fluidized bed is 1.5bar, the spraying speed of the fluidized bed is 5g / min, and the air intake volume during granulation is 25m 3 / h, the air inlet temperature is 40°C during granulation, and it is dried for 40 minutes after granulation, and the air inlet volume during drying is 30m 3 / h, the air inlet temperature is 65°C, the particles are dried and discharged, and the composition is obtained;

[0074] (4) Add 10 g of talc powder, 35 g of crospovidone (PVPP) and 5 g of stearic acid to 270 g of the prepared composition, mix well, press into tablets, and coat.

[0075] The marked amount per tablet...

Embodiment 3

[0077] (1) Add 100g of microcrystalline cellulose (MCC), 50g of lactose and 60g of mannitol into the fluidized bed as filler;

[0078] (2) Add 30g of nimodipine and 105g of povidone K25 (PVP K25) into a mixed solvent composed of 250g of ethyl acetate and 50g of acetone to completely dissolve;

[0079] (3) Spray the above solution evenly onto the filler in the fluidized bed, the atomization pressure of the fluidized bed is 1.5bar, the spraying speed of the fluidized bed is 7g / min, and the air intake volume during granulation is 35m 3 / h, the inlet air temperature is 30°C during granulation, and the drying time is 30 minutes after granulation, and the air inlet volume during drying is 35m 3 / h, the air inlet temperature is 40°C, the granules are dried in the fluidized bed, and then transferred to an oven for 5 hours to continue drying, the drying temperature is 50°C, and the material is discharged after drying to obtain the composition;

[0080] (4) Add 2 g of talc powder, 16 g...

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Abstract

The invention discloses a nimodipine solid dispersant and tablet and their preparation methods. The preparation method of the nimodipine solid dispersant comprises the following steps of blending nimodipine, polyvinylpyrrolidone and a volatile organic solvent to obtain a uniform mixed solution, uniformly spraying the mixed solution to a filler by a fluidized bed under the conditions of atomization pressure of 1.2-3.0bar, a liquid spraying rate of 3-12g/min, an inlet air temperature of 20-80 DEG C and an inlet air amount of 20-80m<3>/h, and carrying out granulation and drying, wherein a mass ratio of nimodipine to polyvinylpyrrolidone is 1: (1-6) and a mass ratio of nimodipine to the filler is 1: (2-15). The preparation method of the nimodipine solid tablet comprises carrying out raw material drying, adding accessory materials into the dried raw materials and carrying out tabletting. The preparation methods have simple processes. Preparation processes of the solid dispersant and tablet can be carried out simultaneously. The nimodipine solid dispersant particles have uniform particle size distribution, high solubility, good stability and high bioavailability.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a nimodipine solid dispersion, a tablet and a preparation method thereof. Background technique [0002] Nimodipine, the English name is Nimodipine, the chemical name is 1-methylethyl-2-methoxyethyl, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl )-3,5-pyridinedicarboxylate, the structural formula is as follows: [0003] [0004] Molecular formula: C 21 h 26 N 2 o 7 , molecular weight: 418.45. [0005] Nimodipine is a dihydropyridine calcium antagonist, clinically used for the prevention and treatment of cerebral vasospasm after subarachnoid hemorrhage, and the improvement of blood circulation in the recovery period of acute cerebrovascular disease. Neuronal protection and treatment of vascular dementia. [0006] Nimodipine raw material is light yellow crystalline powder, odorless, tasteless, almost insoluble in water, belongs to the second class drug with low solubility and high perm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/28A61K31/4422A61K47/32A61P9/10A61P25/28A61J3/00
Inventor 施斌高敏刘岐焦艳任宏伟
Owner SHANGHAI CHEMPARTNER CO LTD
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