Oxcarbazepine dry suspension and preparation method thereof

A technology of dry suspension and suspending agent, which is applied in nervous system diseases, powder delivery, active ingredients of heterocyclic compounds, etc. It can solve problems such as easy layering, long drying time of granules, and easy agglomeration of granules, achieving Storage stable effect

Inactive Publication Date: 2015-01-21
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation method of existing dry suspension mainly contains two kinds: one is to mix medicine and adjuvant evenly and subpackage, this method is simple to prepare, but powder fluidity is poor and easy to layer; the other is wet granulation method, At present, most of the preparation methods of dry suspension disclosed in China are wet granulation method, but the granulation of this method has problems such as easy agglomeration, long drying time of granules, brittle granules and more powder.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Oxcarbazepine and Mannitol, Micronized (Oxcarbazepine:Mannitol=3:7) 50g microcrystalline cellulose 10g xanthan gum 34g Polyethylene castor oil 1g sucrose 3.5g Sweet Orange Flavor 0.5g silica 1g

[0035] Add 10g of microcrystalline fiber, 34g of xanthan gum, 3.5g of sucrose, and 1g of polyethylene castor oil into pure water at 40-55°C, stir well, and prepare a blank suspension with uniform dispersion; Add 50 g of oxcarbazepine and mannitol to the above blank suspension, stir quickly to form a uniformly dispersed drug-containing suspension; spray-dry the drug-containing suspension (inlet air temperature 135°C, liquid inlet speed 40ml / min, atomization pressure 150kpa), to obtain dry granules; pass the dry granules through a 60-mesh sieve for granulation, add 0.5g of sweet orange essence and 1g of silicon dioxide and mix evenly to obtain. The viscosity of a single dose of the resulting dry suspension in 100 ml of an aqueous...

Embodiment 2

[0038] Oxcarbazepine and Mannitol, Micronized (Oxcarbazepine:Mannitol=3:7) 50g microcrystalline cellulose 10g xanthan gum 34g Polyethylene castor oil 1g aspartame 3.5g Sweet Orange Flavor 0.5g Silicon Dimethide 1g

[0039] Add 10g of microcrystalline fiber, 34g of xanthan gum, 3.5g of aspartame, and 1g of polyethylene castor oil into pure water at 40-55°C, stir well, and prepare a uniformly dispersed blank suspension; Add 50 g of the co-micronized drug oxcarbazepine and mannitol to the above blank suspension, and stir quickly to form a uniformly dispersed drug-containing suspension; spray-dry the drug-containing suspension (inlet air temperature 135°C , feed speed 40ml / min, atomization pressure 150kpa), to obtain dry granules; pass dry granules through a 60-mesh sieve for granulation, add sweet orange essence 0.5g, silicon dioxide 1g and mix evenly to obtain final product. The viscosity of a single dose of the resulting dry su...

Embodiment 3

[0042] Oxcarbazepine and Mannitol, Micronized (Oxcarbazepine:Mannitol=3:7) 50g microcrystalline cellulose 10g xanthan gum 34g polyoxyethylene castor oil 1g sucrose 3.75g Sweet Orange Flavor 0.25g silica 1g

[0043] Add 10g of microcrystalline fiber, 34g of xanthan gum, 3.75g of sucrose, and 1g of polyethylene castor oil into water at 40-55°C, stir well, and prepare a uniformly dispersed blank suspension; Add 50 g of carzepine and mannitol to the above blank suspension, stir quickly to form a uniformly dispersed drug-containing suspension; spray-dry the drug-containing suspension (inlet air temperature 135°C, liquid inlet speed 40ml / min, atomization pressure 150kpa), to obtain dry granules; pass the dry granules through a 60-mesh sieve for granulation, add 0.5g of sweet orange essence and 1g of silicon dioxide and mix evenly to obtain. The viscosity of a single dose of the resulting dry suspension in 100 ml of an aqueous solut...

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Abstract

The invention discloses an oxcarbazepine dry suspension and a preparation method thereof. The oxcarbazepine dry suspension is prepared from oxcarbazepine, microcrystalline cellulose, xanthan gum, solubilizer, filler, a conventional amount of flavoring agent and aromatizer. According to the oxcarbazepine dry suspension prepared by adopting a spray drying method, time can be saved, the defects of agglomeration, high particle cracking rate, non-uniform shape and grain diameters and the like of a wet-process granulation method can be overcome, and the prepared granules are uniform, high in dissolving speed, relatively excellent in liquidity and excellent in taste, the production efficiency can be improved, and the cost for the dry suspension can be reduced. The oxcarbazepine dry suspension is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a dry suspension of oxcarbazepine and a preparation method thereof. Background technique [0002] Oxcarbazepine (10,11-dihydro-10-oxo-5 H -Dibenzo[ b, f ] aza-5-carboxamide) is a known anticonvulsant drug used to treat convulsions caused by epileptic seizures. [0003] Oxcarbazepine is mainly exerted by its 10-monohydroxy metabolite (MHD), and the mechanism of action is still unclear, but in vitro electrophysiological studies have shown that oxcarbazepine and MHD can block voltage-sensitive sodium ion channels and stabilize them in a highly excited state. Nerve cell membrane inhibits repeated firing of neurons and reduces synaptic transmission of nerve impulses. In addition, the anticonvulsant effect of oxcarbazepine is also related to increasing the conductance of potassium ions and regulating the calcium ion channels activated by high voltage. The drug can be ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/55A61K47/38A61K47/36A61K47/26A61P25/08
Inventor 王晓蕾刁媛媛郭夏
Owner AVENTIS PHARMA HAINAN
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