Memantine hydrochloride and donepezil hydrochloride composite preparation

A technology of memantine hydrochloride and donepezil, which is applied in the fields of pharmaceutical formulations, neurological diseases, capsule delivery, etc., can solve the problems of industrial scale-up difficulties, production workshops that cannot meet the requirements, and high requirements for capsule filling equipment, so as to avoid uneven filling , to avoid the effect of special requirements

Inactive Publication Date: 2016-08-03
BEIJING KANG LISHENG PHARMA TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The industrial scale-up of this kind of process is difficult, and the requirements for capsule filling equipment are relatively high, and many production workshops cannot meet the requirements
Moreover, it is mentioned in the patent that lactose is used as an auxiliary material for the preparation of donepezil granules. Lactose is prone to Maillard reaction for memantine hydrochloride and produces lactose adducts, which is not conducive to the stability of the preparation.

Method used

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  • Memantine hydrochloride and donepezil hydrochloride composite preparation
  • Memantine hydrochloride and donepezil hydrochloride composite preparation
  • Memantine hydrochloride and donepezil hydrochloride composite preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] A compound preparation of memantine hydrochloride donepezil, prepared from the following components,

[0049] Memantine Hydrochloride 14.0g

[0050] Donepezil Hydrochloride 10.0g

[0051] Microcrystalline Cellulose Pellet Core 70.0g

[0052] Ethyl cellulose aqueous dispersion 24.0g

[0053] Povidone 6.0g

[0054] Opadry 3.3g

[0055] Its preparation method comprises the following steps:

[0056] 1) memantine hydrochloride and povidone (3.0g) are dissolved in 50% ethanol solvent, wrapped on the surface of the microcrystalline cellulose pellet core,

[0057] 2) adopt ethylcellulose aqueous dispersion to carry out the coating of slow-release layer,

[0058] 3) Opadry (1.3g) was added with water to configure an 8% aqueous solution, and wrapped on the surface of the pellets as the isolation layer 1,

[0059] 4) donepezil hydrochloride and povidone (3.0g) are dissolved in a solvent of 50% ethanol, wrapped on the next layer of microcrystalline cellulose pellet core, as ...

Embodiment 2

[0069] A compound preparation of memantine hydrochloride donepezil, prepared from the following components,

[0070] Memantine Hydrochloride 14.0g

[0071] Donepezil Hydrochloride 10.0g

[0072] Microcrystalline cellulose pellet core 62.0g

[0073] Ethylcellulose aqueous dispersion 32.0g

[0074] Povidone 6.0g

[0075] Opadry 3.3g

[0076] Its preparation method comprises the following steps:

[0077] 1) memantine hydrochloride and povidone (3.0g) are dissolved in 50% ethanol solvent, wrapped on the surface of the microcrystalline cellulose pellet core,

[0078] 2) adopt ethylcellulose aqueous dispersion to carry out the coating of sustained-release layer,

[0079] 3) Opadry (1.3g) was added with water to be configured into an 8% aqueous solution, and wrapped on the surface of the pellets as the isolation layer 1,

[0080] 4) donepezil hydrochloride and povidone (3.0g) are dissolved in a solvent of 50% ethanol, wrapped on the next layer of microcrystalline cellulose pel...

Embodiment 3

[0089] A compound preparation of memantine hydrochloride donepezil, prepared from the following components,

[0090] Memantine Hydrochloride 14.0g

[0091] Donepezil Hydrochloride 10.0g

[0092] Microcrystalline Cellulose Pellet Core 66.0g

[0093] Ethyl cellulose aqueous dispersion 28.0g

[0094] Povidone 6.0g

[0095] Opadry 3.3g

[0096] Its preparation method comprises the following steps:

[0097] 1) memantine hydrochloride and povidone (3.0g) are dissolved in 50% ethanol solvent, wrapped on the surface of the microcrystalline cellulose pellet core,

[0098] 2) adopt ethylcellulose aqueous dispersion to carry out the coating of sustained-release layer,

[0099] 3) Opadry (1.3g) was added with water to be configured into an 8% aqueous solution, and wrapped on the surface of the pellets as the isolation layer 1,

[0100] 4) donepezil hydrochloride and povidone (3.0g) are dissolved in a solvent of 50% ethanol, wrapped on the next layer of microcrystalline cellulose pe...

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PUM

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Abstract

The present invention adopts memantine hydrochloride and donepezil hydrochloride as the active ingredients of the medicine, and co-wraps the memantine hydrochloride and donepezil hydrochloride on the pellets, and controls the slow release of memantine hydrochloride and the rapid release of donepezil hydrochloride through multi-layer coating, It is finally filled in capsules, which also avoids the problem of uneven filling that may exist in capsules mixed with pellets and granules, and is easier to realize industrial production. There is no lactose and other excipients that can undergo Maillard reactions with memantine hydrochloride, ensuring formulation stability.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a compound preparation of memantine hydrochloride donepezil, in particular to a capsule containing memantine hydrochloride sustained-release pellets and donepezil hydrochloride quick-release pellets. Background technique [0002] Memantine hydrochloride donepezil compound preparation is a drug used to treat patients with moderate to severe Alzheimer's type dementia. The recommended dose is 28mg memantine hydrochloride / 10mg donepezil hydrochloride / day, or 10mg memantine hydrochloride / 10mg donepezil hydrochloride / day, for patients with severe renal impairment, the recommended dose is 14mg memantine hydrochloride extended-release / 10mg donepezil hydrochloride, or 5mg hydrochloride Memantine / 10mg donepezil hydrochloride once a day. [0003] Memantine hydrochloride-donepezil hydrochloride capsules were jointly developed by Actavis and Adamas Pharmaceuticals, and were approved for market...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/62A61K31/13A61K31/445A61P25/28
CPCA61K31/13A61K9/5047A61K9/5078A61K31/445
Inventor 程刚
Owner BEIJING KANG LISHENG PHARMA TECH DEV
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