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A kind of preparation method of the solid preparation of rivastigmine bitartrate

A technology of rivastigmine bitartrate and solid preparations, which is applied in the field of preparation of solid preparations, can solve problems such as uneven drug content, unstable drug release, and bitter taste, and achieve the goal of avoiding external effects, stable release, and uniform content Effect

Active Publication Date: 2018-11-13
赤峰赛林泰药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, when preparing small-scale drugs containing rivastigmine bitartrate, there are generally three difficulties in the preparation process. First, the dextrorotary product of rivastigmine bitartrate in the drug has a bitter taste; second, the content of the drug is uneven; Drug release is unstable and uniform, and it is difficult to solve it at the same time

Method used

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  • A kind of preparation method of the solid preparation of rivastigmine bitartrate
  • A kind of preparation method of the solid preparation of rivastigmine bitartrate
  • A kind of preparation method of the solid preparation of rivastigmine bitartrate

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Table 1 Processing capacity

[0039] Ball core specification

1.5mg

Rivastigmine bitartrate (mg)

2.4

Microcrystalline Cellulose (mg)

151.7

Hypromellose (mg)

4.3

Magnesium stearate (mg)

1.6

Purified water (mg)

85.7

[0040] (1) Preparation of ball core Ⅰ:

[0041] Microcrystalline cellulose (through 80 mesh sieve), rivastigmine bitartrate (through 100 mesh sieve). Mix the microcrystalline cellulose and the main ingredient according to the prescription amount in Table 1, and carry out dry blending by the method of equal volume increase, and mix evenly to obtain the mixed powder I.

[0042] Take 3.0kg hydroxypropyl methylcellulose to prepare 5% hydroxypropyl methylcellulose aqueous solution as the first binder, take 70% of the mixed powder I, add the first binder therein, and mix evenly to obtain a soft material. The soft material is turned into a strip with an extruder, and the strip-shaped soft material...

Embodiment 2

[0051] Table 2 Processing capacity

[0052] Ball core specification

3.0mg

Rivastigmine bitartrate (mg)

4.8

Microcrystalline Cellulose (mg)

149.3

Hypromellose (mg)

4.3

Magnesium stearate (mg)

1.6

Purified water (mg)

85.7

[0053] (1) Preparation of ball core Ⅰ:

[0054] With microcrystalline cellulose (passing through 80 mesh sieves), get the microcrystalline cellulose of formula quantity 149.3kg*80% and 4.8kg rivastigmine bitartrate (passing through 100 mesh sieves), adopt the method of equal increments to carry out dry mixing, mix uniform.

[0055] Take 3.0 kg of hydroxypropyl methylcellulose to prepare a 5% aqueous solution of hydroxypropyl methylcellulose, then add it to the dry-blended material, and mix evenly to obtain a soft material. Use an extruder to turn the soft material into a long strip, and use a rounder to cut and roll the long strip of soft material to form a pellet core I, and the diameter o...

Embodiment 3

[0064] Table 3 prescription quantity

[0065]

[0066]

[0067] (1) Preparation of ball core Ⅰ:

[0068] Corn starch (through 80 mesh sieve), rivastigmine bitartrate (through 100 mesh sieve). Mix the cornstarch and rivastigmine hydrotartrate according to the prescription amount in Table 3, and dry-blend them using the method of equal volume increase, and mix them evenly to obtain the mixed powder I.

[0069] Take 4.0kg of povidone K30 to prepare a 5% aqueous solution as the first binder, take 70% of the mixed powder I, add the first binder to it, and mix evenly to obtain a soft material. Use an extruder to turn the soft material into a long strip, and use a rounder to cut and round the long strip of soft material to form a pellet core. The diameter of the pellet core is about 0.3mm

[0070] (2) Primary fluidization and primary screening

[0071] Take 3.0kg of low-substituted hydroxypropyl cellulose to prepare a 5% aqueous solution, then add 10% mixed powder I, mix eve...

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Abstract

The invention discloses a method for preparing a solid preparation of rivastigmine mesotartarate, wherein the method comprises the following steps: (1) dry-mixing, extruding and rolling rivastigmine mesotartarate, a disintegrating agent and a first adhesive to form pellet cores I; (2) allowing the pellet cores I to pass through a fluidized bed, atomizing a second adhesive and a filling agent to prepare pellet cores II, and sieving to obtain a first oversize product and a first undersize product; (3) allowing the first oversize product to pass through the fluidized bed, spraying the second adhesive and the filling agent to obtain pellet cores III, sieving to obtain a second first oversize product and a second undersize product, wherein the second oversize product is the final solid preparation of rivastigmine mesotartarate; and (4) crushing the first oversize product and the second undersize product to obtain a fine powder, and adding the dry-mixed powder obtained in the step (1); and taking the re-prepared pellet cores I as a raw material, carrying out the step (2), the step (3) and the step (4), and circulating successively. The solid preparation prepared by the method not only can have the bitter taste covered, but also ensures uniform release and dispersion.

Description

technical field [0001] The invention relates to a preparation method of a solid preparation of rivastigmine bitartrate. Background technique [0002] Cholinesterase inhibitors are currently internationally recognized and most highly rated drugs for improving symptoms of Alzheimer's dementia. Rivastigmine is an amino acid formic acid brain selective cholinesterase inhibitor, which belongs to the second category Substitute products. Developed by Swiss Novartis Pharmaceuticals UK Co., Ltd., with the trade name "Essner", it was first launched in Switzerland in December 1997, and was approved by the FDA on April 21, 2000. [0003] Studies have shown that although the half-life of this product is relatively short, its inhibitory effect on cholinesterase can reach 10 hours, and it has better tolerance to mild and moderate Alzheimer's disease. Enzyme action, obtained a high evaluation in a prospective, randomized multi-center double-blind study conducted in 45 countries including ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/27A61K9/16A61P25/28
CPCA61K9/1652A61K31/27
Inventor 张丽华赵宏伟王艳峰崔玉杰季丽萍盛丽王洁婷马征
Owner 赤峰赛林泰药业有限公司