Memantine hydrochloride sustained-release pellet and preparation method thereof

A technology of memantine hydrochloride and sustained-release pellets, applied in microcapsules, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as different dosage forms, increased solvent costs, and poor water solubility of ethyl cellulose, and achieve The production operation process is safe, the production energy consumption is avoided, and the stability is good.

Active Publication Date: 2022-07-15
北京丰科睿泰医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of ethyl cellulose, a large amount of high-concentration ethanol needs to be used for dissolution during the preparation process. In addition to increasing the cost of solvents, it also increases the explosion-proof performance requirements of equipment and safety production risks.
[0010] Patents CN 103816135 B and CN 105769794 B adjust the sustained-release pellets into microtablets or press the pellets into pellet tablets. Although the preparation process is relatively simple, they are different from the original formulations in dosage form, and cannot be compared in consistency, and are not Clinical advantages of multiple unit dosage forms

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] prescription:

[0037]

[0038] Preparation Process:

[0039] (1) drug-loading layer coating: Memantine hydrochloride raw material is pulverized by a jet mill to obtain memantine hydrochloride micropowder, particle diameter D 90 Controlled within the range of 15 μm; Memantine hydrochloride micropowder, povidone K30 and talc were dispersed in an appropriate amount of purified water to prepare a drug-loading layer coating liquid; The coating liquid of the drug-loading layer is wrapped on the surface of the sucrose pellet core by spraying method. During the coating process, the temperature of the material is controlled within the range of 25°C to 35°C. When the temperature of the material is below 35°C, the drug-loaded layer pellets are obtained.

[0040] (2) Coating of isolation layer: add hypromellose E5 to purified water at 60°C to 80°C, stir and disperse evenly, cool to room temperature, add polyethylene glycol 400 and talc, stir evenly, and prepare an isolation l...

Embodiment 2

[0044] prescription:

[0045]

[0046] Preparation Process:

[0047] (1) drug-loading layer coating: Memantine hydrochloride raw material is pulverized by a jet mill to obtain memantine hydrochloride micropowder, particle diameter D 90 Controlled within the range of 15 μm; Memantine hydrochloride micropowder, povidone K30 and talc were dispersed in an appropriate amount of purified water to prepare a drug-loading layer coating liquid; The coating liquid of the drug-loading layer is wrapped on the surface of the sucrose pellet core by spraying method. During the coating process, the temperature of the material is controlled within the range of 25°C to 35°C. When the temperature of the material is below 35°C, the drug-loaded layer pellets are obtained.

[0048] (2) Coating of isolation layer: add hypromellose E5 to purified water at 60°C to 80°C, stir and disperse evenly, cool to room temperature, add polyethylene glycol 400 and talc, stir evenly, and prepare an isolation l...

Embodiment 3

[0052] prescription:

[0053]

[0054] Preparation Process:

[0055] (1) drug-loading layer coating: Memantine hydrochloride raw material is pulverized by a jet mill to obtain memantine hydrochloride micropowder, particle diameter D 90 Controlled within the range of 15 μm; Memantine hydrochloride micropowder, povidone K30 and talc were dispersed in an appropriate amount of purified water to prepare a drug-loading layer coating liquid; The coating liquid of the drug-loading layer is wrapped on the surface of the sucrose pellet core by spraying method. During the coating process, the temperature of the material is controlled within the range of 25°C to 35°C. When the temperature of the material is below 35°C, the drug-loaded layer pellets are obtained.

[0056] (2) Coating of isolation layer: add hypromellose E5 to purified water at 60°C to 80°C, stir and disperse evenly, cool to room temperature, add polyethylene glycol 400 and talc, stir evenly, and prepare an isolation l...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a memantine hydrochloride-containing sustained-release pellet and a preparation method thereof. The memantine hydrochloride sustained-release pellet comprises a blank pellet core, a drug-loading coating layer, an isolation coating layer and a sustained-release coating layer, and a sustained-release material of the sustained-release coating layer is mainly composed of an ethyl cellulose aqueous dispersion and contains a proper proportion of hydroxyethyl cellulose. The memantine hydrochloride sustained-release pellet can be further prepared into sustained-release preparations such as granules, capsules or tablets. According to the memantine hydrochloride sustained-release pellet and the preparation method thereof, further aggregation and fusion of ethyl cellulose are retarded by utilizing an incompatible membrane formed by dispersedly wrapping hydrophobic ethyl cellulose with water-soluble hydroxyethyl cellulose and water absorption of the incompatible membrane, so that the memantine hydrochloride sustained-release pellet with better stability is obtained, no organic solvent such as ethanol is used, and the memantine hydrochloride sustained-release pellet is more economical, environment-friendly and safe and has good application prospects. The method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a pharmaceutical preparation containing memantine hydrochloride sustained-release pellets and a preparation method thereof. [0002] technical background [0003] The information disclosed in this Background section is only for enhancement of understanding of the general background of the invention and should not necessarily be taken as an acknowledgement or any form of suggestion that this information forms the prior art already known to a person of ordinary skill in the art. [0004] Memantine Hydrochloride, an N-methyl-D-aspartate (NMDA) receptor antagonist, is the first drug for the treatment of moderate-to-severe Alzheimer's disease dementia. Binds to NMDA receptor-operated cation channels, which may be related to its therapeutic effects. Forest Laboratories LLC. first developed memantine hydrochloride tablets in 2003 under the trade name of N...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/13A61K47/26A61K47/38A61K47/10A61P25/28A61K9/62A61K9/26
CPCA61K31/13A61K9/5078A61K9/5047A61K9/5031A61P25/28A61K9/5084A61K9/2081Y02A50/30
Inventor 兰颐邓莉莉杨义凡安明榜李铁军
Owner 北京丰科睿泰医药科技有限公司
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