Nimodipine solid dispersoid and preparation method thereof

A nimodipine solid, nimodipine technology, applied in the field of medicine, can solve the problems of aging, slow drug dissolution, insoluble tablets and the like

Inactive Publication Date: 2009-07-08
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Nimodipine is insoluble in water and its aqueous medium, so it is made into tablets because of its poor solubility, the drug dissolves slowly in water in vitro, and the bioavailability is low
Solid dispersion technology is one of the effective methods to improve the in vitro dissolution rate of insoluble drugs, but the large amount of carrier and serious aging phenomenon are difficult problems for solid dispersions

Method used

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  • Nimodipine solid dispersoid and preparation method thereof
  • Nimodipine solid dispersoid and preparation method thereof
  • Nimodipine solid dispersoid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Take 10g of PEG4000 and 0.5g of micro-powdered silica gel and mix well, heat to melt PEG4000, add 1g of nimodipine, mix well, quickly pour the molten material on the steel plate and spread it flat, put it in a -20°C refrigerator, freeze for 8 hours, and then transfer to a vacuum Continue to dry in the drying oven for 24-48h (at room temperature), take it out, grind it, and pass it through an 80-mesh sieve. The solid dispersion of the invention has an in vitro cumulative dissolution percentage of 101.12±2.45% (n=6) within 45 minutes.

Embodiment 2

[0043] Take 5g of PEG4000 and 5g of micro-powder silica gel and mix well, heat to melt PEG4000, add 5g of nimodipine, mix well, quickly pour the molten material on the steel plate, place in -20°C refrigerator, freeze for 8 hours, and then transfer to vacuum drying Continue to dry in the box for 24-48h (at room temperature), take it out, grind it, and pass it through an 80-mesh sieve. The solid dispersion of the invention has an in vitro cumulative dissolution percentage of 100.16±1.30% (n=6) within 45 minutes.

Embodiment 3

[0045] Take 10g of PEG4000 and 0.5g of talcum powder and mix well, heat to melt PEG4000, add 1g of nimodipine, mix well, quickly pour the molten material on the steel plate and spread it, put it in -20℃ refrigerator, freeze for 8 hours, and then transfer to vacuum Continue to dry in the drying oven for 24-48h (at room temperature), take it out, grind it, and pass it through an 80-mesh sieve. The solid dispersion of the invention has an in vitro cumulative dissolution rate of 99.22±2.05% (n=6) within 45 minutes.

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Abstract

The invention relates to the field of medical technology, more particularly to a nimodipine solid dispersoid and a preparation method thereof. The invention employs the nimodipine as an active ingredient and adds a macromolecular carrier material and an antisticking agent to prepare the nimodipine solid dispersoid; and the feeding ratio of the nimodipine, the macromolecular carrier material and the antisticking agent is 1:0.2-10:0.2-10. The nimodipine solid dispersoid is prepared by a melting method, a coprecipitation method, a solvent dispersion method, a solvent melting method or a grinding method respectively. The invention, by preparing the solid dispersoid with the nimodipine and a small amount of carrier material, significantly increases the equilibrium solubility and the degree of in vitro dissolution thereof and prominently enhances bioavailability, thus solving the problems of large dosage of the carrier of the solid dispersoid and severe aging; in addition the invention has the characteristics of small dosage of the carrier, rapid dissolution, high bioavailability and simple preparation method without the aging phenomenon.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nimodipine solid dispersion and a preparation method thereof. Background technique [0002] Nimodipine (Nimodipine, NMD) is the second generation of dihydropyridine calcium antagonists, the chemical name is (±) isopropyl-2-methoxyethyl-1,4-dihydro-2,6-dimethyl Base-4(3-nitrophenyl)-3,5-pyridinedicarboxylate. This product is light yellow crystal or crystalline powder, odorless and tasteless. [0003] The pharmacological property of nimodipine is to effectively regulate the level of intracellular calcium to maintain normal physiological functions. The effect on cerebral blood vessels is particularly prominent, and it can be combined with specific receptors of the central nervous system. This specificity enables this product to effectively prevent and treat brain tissue ischemia caused by cerebral vasospasm caused by subarachnoid hemorrhage. Sexual damage, inhibit ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/435A61P9/12
Inventor 逄秀娟马英杰
Owner SHENYANG PHARMA UNIVERSITY
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