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Memantine hydrochloride sustained-release capsule and preparation method thereof

A technology of memantine hydrochloride and sustained-release capsules, applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve problems such as adverse events, poor compressibility of lipid substances, and reduced patient compliance, so as to improve curative effect, uniform and slow The effect of simple and easy release and production method

Active Publication Date: 2013-07-03
SHANGHAI FOSUN PHARMA DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lipid substances are notoriously poorly compressible and can be problematic for compression of the final composition if used in large amounts in the formulation
Using a twice-daily memantine dosing regimen with immediate-release tablets may be undesirable as patient compliance decreases with more frequent dosing
Also, administration of immediate release tablets may result in a greater frequency of adverse events due to the faster rate of absorption

Method used

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  • Memantine hydrochloride sustained-release capsule and preparation method thereof
  • Memantine hydrochloride sustained-release capsule and preparation method thereof
  • Memantine hydrochloride sustained-release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] First crush memantine hydrochloride to particle size D with a jet mill 90 Less than 10 μm, micronized memantine hydrochloride was obtained.

[0046] (1) Dosing: Dissolve 50g of micronized memantine hydrochloride and 50g of ethyl cellulose in 400g of ethanol, and use Glatt's fluidized bed to spray the drug-containing solution to the On the core of 400g sucrose balls, obtain memantine hydrochloride drug-containing pellets.

[0047] (2) Coating: Evenly disperse 50g of talcum powder in 183g of water to form a uniform suspension of talc powder, and mix it with 167g of Eudragit NE30D (copolymer of ethyl acrylate and methyl methacrylate (2:1), Solid content is 30% water dispersion) water dispersion is stirred and mixed uniformly, gets 400g from the medicine-containing pellet that step (1) makes, uses the fluidized bed of Glatt to spray coating with this coating liquid at 25 ℃ of temperature to obtain coated sustained-release pellets.

[0048] (3) Aging: Mix the slow-release...

Embodiment 2

[0053] (1) drug application: 50g memantine hydrochloride and binder 75g ethyl cellulose are dissolved in 500g of ethanol, and the solvent spray is applied to the 375g sucrose ball core at a temperature of 28°C with the fluidized bed of Glatt, Dry at 28°C for 5-10 minutes to obtain the drug-coated pellets.

[0054] (2) Coating: Evenly disperse 36g of talc powder and 7.2g of triethyl citrate in 237g of water to form a uniform suspension of talc powder, with 108g of polyacrylic acid resin polymer - Eudragit RS 30D and 12g of Eudragit RL30D (both are water dispersions with a solid content of 30%) stirring and mixing evenly, spray the coating solution onto 420g drug-loaded pellets with the fluidized bed of Glatt at a temperature of 25°C-30°C, to obtain sustained-release pellets.

[0055] (3) Preparation of capsules: mix the slow-release pellets and talcum powder evenly in a weight ratio of 50:1, sieve, sieve off excess talcum powder, and pack about 167 mg of pellets into hard gelat...

Embodiment 3

[0058] First crush memantine hydrochloride to particle size D with a jet mill 90 Less than 10 μm, micronized memantine hydrochloride was obtained.

[0059] (1) Suspension dosing: 50g of micronized memantine hydrochloride and 100g of binder polyvinylpyrrolidone, 25g of anti-sticking agent talcum powder are evenly dispersed in 800g of water, and the fluidized bed of Glatt is used at a temperature of 40°C The solvent is sprayed onto the core of 325g sucrose pellets to obtain the pellets.

[0060] (2) Coating: the ethyl cellulose (10cps) of 60g and the hydroxypropyl methylcellulose of 15g are dissolved in ethanol, spray on the 425g medicine pellet with this coating liquid at the temperature of 28 ℃, obtain Slow-release pellets.

[0061] (3) Preparation of capsules: the sustained-release pellets were packed into hard gelatin capsules in a conventional manner.

[0062] Content of Memantine Hydrochloride in Shangyao Pellets

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Abstract

The invention provides a preparation method of a memantine hydrochloride sustained-release preparation. According to the present invention, sustained-release pellets are obtained by sustained-release coating of drug-containing pellets containing memantine hydrochloride. The drug-containing pellets are obtained by extrusion spheronization or solution medicine-feeding or suspension medicine-feeding, and are nearly circular in shape. The shape and granularity-controllable drug-containing pellets are subjected to sustained-release coating and the thickness of the film formed by coating can also be controlled. The invention realizes the controllability of the coating film and the spherical pellets, and reproducibility of stability of releasing the memantine hydrochloride is controlled under the circumstance of guaranteeing nonoccurrence of crystal form of memantine hydrochloride. The preparation of the invention can provide sustained release in the form of a single dose within 24 hours. The drug penetrates and diffuses to the release medium through the film pores. Because the size is small, the medicine taking is less susceptible to foods and the efficacy is improved. The production method of the present invention is simple, is suitable for industrial production, and has a great application value.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to memantine hydrochloride sustained-release capsules and a preparation method thereof. Background technique [0002] Memantine HCl is used in the treatment of moderate to severe Alzheimer's dementia. Alzheimer's disease (AD) is an irreversible progressive disorder of brain cell (neuron) deterioration, which leads to loss of cognitive function, primary memory, judgment and reasoning, motor coordination and pattern recognition. In advanced stages of the disease, all memory and intellectual function may be lost. People with Alzheimer's have problems with memory, judgment, and thinking, making it difficult to work or participate in daily life. It is associated with senile dementia, the mental decline (loss of intelligence) associated with old age. Senile dementia is defined as two main types: Alzheimer's type caused by generalized wasting disease and caused by vascular problems, mainly...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/13A61K47/32A61K47/38A61P25/28
Inventor 何平钱晓明谭萍莉
Owner SHANGHAI FOSUN PHARMA DEV CO LTD
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