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Rivastigmine capsules and preparation method thereof

A technology of rivastigmine bitartrate and capsules, which is applied in the field of rivastigmine bitartrate preparation and its preparation, rivastigmine bitartrate capsule and its preparation field, which can solve the problems of easy deliquescence and difficult storage, etc., and achieve moisture absorption Low, conducive to storage, uniform particle size distribution effect

Inactive Publication Date: 2012-12-05
ZHEJIANG JINGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] According to literature reports, rivastigmine bitartrate has hygroscopicity and is easy to deliquescence under the condition of relative humidity of 55%, so it is not easy to store

Method used

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  • Rivastigmine capsules and preparation method thereof
  • Rivastigmine capsules and preparation method thereof
  • Rivastigmine capsules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] prescription:

[0033]

[0034] Preparation: Weigh 0.08kg of hypromellose and add it to a 5L stainless steel bucket, add about 2kg of purified water, stir and dissolve to obtain a 4% hypromellose aqueous solution; weigh 0.048kg of rivastigmine bitartrate and add it to about 0.5kg In the hypromellose aqueous solution, stir to obtain a clear solution; pour 1.442kg of microcrystalline cellulose into the fluidized bed granulator; then spray the hypromellose aqueous solution containing rivastigmine bitartrate on micro Prepare granules on crystalline cellulose, set the inlet air temperature to 50°C; adjust the inlet air temperature to 60°C, and continue to coat the granules with the remaining hypromellose aqueous solution until the weight gain reaches 3.5%. Dry the granules to control the weight loss on drying to less than 2.0% (background temperature 105°C); add additional silicon dioxide and magnesium stearate, and mix well; use hypromellose capsule shells to fill the ca...

Embodiment 2

[0048] prescription:

[0049]

[0050]

[0051]Note: prescription D does not belong to the present invention, here as a comparative example.

[0052] Preparation: Weigh 36g of hypromellose and add it to a 2000ml beaker, add 1800g of purified water to prepare a 2% hypromellose aqueous solution; weigh the batch amount (9.6g) of rivastigmine bitartrate and add it to 360g of hydroxypropyl methylcellulose In the aqueous solution of propyl methylcellulose, stir to obtain a clear solution; the starch1500 and (454.4g) microcrystalline cellulose of the batch amount (90g) are poured into the fluidized bed granulator and mixed; Spray the propyl methylcellulose aqueous solution on the mixture to obtain granules, set the inlet air temperature to 50°C; adjust the inlet air temperature to 60°C, and continue to coat the granules with the remaining hypromellose aqueous solution until the weight gain is 4.5 %. The granules are dried, and the weight loss on drying is controlled to 1.5% (...

Embodiment 3

[0058] prescription:

[0059]

[0060] Preparation: Weigh hypromellose according to the prescription in the above table and add them into stainless steel barrels, add purified water to prepare a 2% hypromellose aqueous solution; In the hypromellose aqueous solution of / 9 weight, stir to obtain clear solution; Pour the mannitol and the microcrystalline cellulose of batch amount into the fluidized bed granulator and mix; Then the hypromellose containing rivastigmine bitartrate The cellulose aqueous solution was sprayed on the mixture to obtain granules, and the air inlet temperature was set to 50°C; the air inlet temperature was adjusted to 60°C, and the remaining part of the hypromellose aqueous solution was used to coat the granules until the granule weight increased by about 7%. Dry the granules, and control the loss on drying to 2.5% (background temperature 105°C); add additional silicon dioxide and magnesium stearate, and mix well; use hypromellose capsule shells to fil...

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Abstract

The present invention relates to rivastigmine capsules and a preparation method thereof. The capsule contains rivastigmine adopted as an active ingredient, hydroxy propyl methyl cellulose adopted as a binder and a film forming material, and other medicinal auxiliary materials. The preparation method comprises: adopting a fluidized bed process to prepare particles, and further adopting hydroxy propyl methyl cellulose to carry out coating on the particles, wherein the prepared product has characteristics of low hygroscopicity and good storage stability so as to easily store the product, and the particles prepared according to the method of the present invention have characteristics of good fluidity and uniform particle size distribution. In addition, the preparation process is stable, quality is controllable, and various detection indexes of the finished product meet requirements, such that low production cost is ensured, and the method is suitable for industrial production.

Description

technical field [0001] The invention relates to a rivastigmine bitartrate preparation and a preparation method thereof, in particular to rivastigmine bitartrate capsules and a preparation method thereof, and belongs to the technical field of chemicals. Background technique [0002] Rivastigmine bitartrate belongs to the third generation of drugs for improving choline system function, and it is a carbamate acetylcholinesterase (AchE) inhibitor and butyrylcholinesterase (BuchE) inhibitor that selectively acts on the brain. Fully functioning cholinergic neurons degrade the release of acetylcholine to promote cholinergic nerve conduction, and are clinically used to treat mild and moderate Alzheimer's dementia. The original research company is Novartis Pharmaceuticals, and the marketed dosage forms include capsules, oral solutions and transdermal sustained-release films. Rivastigmine Bitartrate Capsules were first launched in Switzerland in 1997 under the trade name Specificat...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/27A61K47/38A61P25/28
Inventor 高慧燕张利峰陈见阳王光强
Owner ZHEJIANG JINGXIN PHARMA
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