Galanthamine hydrobromide dispersible tablet and preparation method thereof

A technology of galantamine hydrobromide and dispersible tablets, which is applied in the directions of non-active ingredients, such as medical preparations, pharmaceutical formulations, and active ingredients of heterocyclic compounds, can solve the problem of reduced permeability, galantamine hydrobromide, etc. problems such as low permeability and complexity, to achieve the effect of improving bioavailability and improving bioavailability

Inactive Publication Date: 2014-06-25
张绪伟
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The permeability of galantamine hydrobromide is very low and also depends on the pH environment. In the gastrointestinal tract, the permeability of galantamine hydrobromide decreases when the pH of the environment increases fr

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Galantamine Hydrobromide 4g

[0035] Hydroxypropyl-β-cyclodextrin 20g

[0036] Mannitol 50g

[0037] Compressible starch 50g

[0038] Microcrystalline cellulose 15g

[0039] Low-substituted hydroxypropyl cellulose 15g

[0040] 2% polyvinylpyrrolidone aqueous solution 60g

[0041] Talc 2g

[0042] Make 1000 pieces.

[0043] Preparation Process:

[0044] Take the prescription amount of hydroxypropyl-β-cyclodextrin and dissolve it in a proper amount of water to make a saturated aqueous solution. Pass the 120-mesh sieve of galanthamine hydrobromide and dissolve in a proper amount of ethanol. Add the hydrobromic acid under magnetic stirring. The ethanol solution of lantamine was slowly added to the saturated aqueous solution of hydroxypropyl cyclodextrin, and after all was added, the stirring was continued at room temperature for 3 hours, and most of the ethanol was removed by rotary evaporation at 45°C. Put it into the shallow dish, put it in the freezer compartment of the refrigerator,...

Embodiment 2

[0048] Galantamine Hydrobromide 4g

[0049] Hydroxypropyl-β-cyclodextrin 20g

[0050] Mannitol 50g

[0051] Compressible starch 25g

[0052] Microcrystalline cellulose 25g

[0053] Low-substituted hydroxypropyl cellulose 25g

[0054] 2% polyvinylpyrrolidone aqueous solution 100g

[0055] Magnesium stearate 2g

[0056] Magnesium Lauryl Sulfate 3g

[0057] Make 1000 pieces.

[0058] Preparation Process:

[0059] Take the prescription amount of hydroxypropyl-β-cyclodextrin and dissolve it in a proper amount of water to make a saturated aqueous solution. Pass the 120-mesh sieve of galanthamine hydrobromide and dissolve in a proper amount of ethanol. Add the hydrobromic acid under magnetic stirring. The ethanol solution of lantamine was slowly added to the saturated aqueous solution of hydroxypropyl-β-cyclodextrin, and after all was added, stirring was continued at room temperature for 4 hours, and most of the ethanol was removed by rotary evaporation at 45°C. Put it into the shallow dish, put i...

Embodiment 3

[0063] Galantamine Hydrobromide 4g

[0064] Hydroxypropyl-β-cyclodextrin 20g

[0065] Mannitol 50g

[0066] Compressible starch 50g

[0067] Microcrystalline cellulose 25g

[0068] Croscarmellose Sodium 10g

[0069] 2% polyvinylpyrrolidone aqueous solution 60g

[0070] Magnesium stearate 2g

[0071] Make 1000 pieces.

[0072] Preparation Process:

[0073] Take the prescription amount of hydroxypropyl-β-cyclodextrin and dissolve it in a proper amount of water to make a saturated aqueous solution. Pass the 120-mesh sieve of galanthamine hydrobromide and dissolve in a proper amount of ethanol. Add the hydrobromic acid under magnetic stirring. The ethanol solution of rantamine was slowly added to the saturated aqueous solution of hydroxypropyl cyclodextrin, and after all was added, the stirring was continued at room temperature for 2 hours, and most of the ethanol was removed by rotary evaporation at 40°C. Put it into the shallow dish, put it in the freezer compartment of the refrigerator, the...

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PUM

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Abstract

The invention belongs to the field of medicinal preparations, and in particular relates to a dalanthamine hydrobromide dispersible tablet and a preparation method thereof. Due to low bioavailability of dalanthamine hydrobromide in oral absorption and large difference among administration individuals, the dalanthamine hydrobromide dispersible tablet comprises dalanthamine hydrobromide, hydroxypropyl-beta-cyclodextrin, packing, a disintegrating agent, an adhesive and a lubricant. Dalanthamine hydrobromide is easily dissolved in water after being included by hydroxypropyl-beta-cyclodextrin (HP-beta-CD), so that the medicinal stability can be improved, in-vivo release of the medicament can be accelerated, absorption can be improved, bioavailability can be improved, and difference among administration individuals can be reduced.

Description

Invention field [0001] The present invention relates to the field of chemical pharmacy, in particular to the field of senile diseases, namely, a dispersible tablet of galanthamine hydrobromide and a preparation method thereof, which are used for the treatment of senile dementia. Background of the invention [0002] With the aging of the population, the mental health problems of the elderly have become increasingly prominent. Epidemiological surveys abroad show that the prevalence of dementia among people aged 65 years and over is 5-7%, of which 50-70% are senile dementia (AD ). The prevalence of dementia reported in my country in the past is much lower than that in foreign countries, but in recent years, domestic surveys show that the prevalence of dementia among people over 65 years old is about 4.61%, of which AD accounts for about 2.9%, which is close to foreign reports. . It is especially worth noting that the prevalence of AD increases rapidly with age. At present, the pop...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/48A61K31/55
Inventor 张绪伟代先慧
Owner 张绪伟
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