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Method for tabletting metoprolol succinate pellets

A technology of torolol pellets and succinic acid, which is applied in the directions of pill delivery, pharmaceutical formulations, microcapsules, etc., can solve the problems of increasing processes and costs, and achieves the advantages of reducing production links, small bulk density, and reducing stratification. Effect

Active Publication Date: 2019-12-20
WUHAN OPTICS VALLEY YATAI PHARM RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is necessary to control the material, particle size and porosity of the pellet core. Currently, the blank pellet cores on the market include MCC (microcrystalline cellulose), sugar pellets, starch pellets, etc., and these pellet cores all have the main performance when they are under pressure. It is the permanent deformation of the pellets rather than fragmentation; at the same time, for the tableting of the pellets, the conventional method is to prepare the extra matrix by wet granulation and then mix and press the pellets, which increases the process and cost. Therefore, The present invention proposes a preparation method of metoprolol succinate sustained-release tablets

Method used

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  • Method for tabletting metoprolol succinate pellets
  • Method for tabletting metoprolol succinate pellets
  • Method for tabletting metoprolol succinate pellets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of blank pellet core

[0029] Table 1 Blank pellet core A prescription composition:

[0030] composition proportion% Microcrystalline cellulose30% Silica70% Hypromellose10%

[0031] Preparation steps of blank pellet core:

[0032] (1) Ingredients and mixing: Weigh microcrystalline cellulose and silicon dioxide according to the prescription ratio and mix them evenly;

[0033] (2) Binder configuration: Weigh hypromellose according to the prescription ratio, mix it to 5% concentration, and stir evenly;

[0034] (3) Preparation: Place the uniformly mixed blank pellets in the centrifugal granulator, turn on the equipment, adjust the rotation speed of the main machine to 100-300r / min for the adhesive obtained in step 2, and combine the configured adhesive with The solvent is mixed and added to the storage tank, the rotating spraying speed is: 5-20r / min, and the spray gun pressure should be 0.5-1.5MPa;

Embodiment 2

[0035] Example 2: Preparation of blank pellet core

[0036] Table 2 Blank pellet core B prescription composition:

[0037] composition% Microcrystalline cellulose70% Silica30% Hypromellose10%

[0038] (1) Ingredients and mixing: Weigh the microcrystalline cellulose and silicon dioxide according to the prescription ratio and mix them evenly;

[0039] (2) Binder configuration: Weigh hypromellose according to the prescription ratio, mix it to 5% concentration, and stir evenly;

[0040] (3) Preparation: Place the uniformly mixed blank pellets in the centrifugal granulator, turn on the equipment, adjust the rotation speed of the main machine to 100-300r / min for the adhesive obtained in step 2, and combine the configured adhesive with The solvent is mixed and added to the storage tank, the rotating spraying speed is: 5-20r / min, and the spray gun pressure should be 0.5-1.5MPa;

Embodiment 3

[0041] Example 3: Preparation of blank pellet core C

[0042] Table 3 Blank pellet core C prescription composition:

[0043] composition% Microcrystalline cellulose10% Silica90% Hypromellose10%

[0044] (1) Ingredients and mixing: Weigh the microcrystalline cellulose and silicon dioxide according to the prescription ratio and mix them evenly;

[0045] (2) Binder configuration: Weigh hypromellose according to the prescription ratio, mix it to 5% concentration, and stir evenly;

[0046] (3) Preparation: Place the uniformly mixed blank pellets in the centrifugal granulator, turn on the equipment, adjust the rotation speed of the main machine to 100-300r / min for the adhesive obtained in step 2, and combine the configured adhesive with The solvent is mixed and added to the storage tank, the rotating spraying speed is: 5-20r / min, and the spray gun pressure should be 0.5-1.5MPa;

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Abstract

The invention provides a method for tabletting metoprolol succinate pellets. The method comprises the following steps of: applying medicine on a blank pellet core, coating a slow release layer, addingadditional auxiliary materials, and performing mixing and tabletting. The blank pellet core consists of a main material, an adhesive and a solvent. The main material, the adhesive and the solvent account for 60 to 90 percent, 10 to 30 percent and 2 to 15 percent of the total mass respectively. The main material consists of microcrystalline cellulose and silicon dioxide. The preparation method ofthe blank pellet core is prepared by a centrifugal granulation method. The obtained blank pellet core has excellent roundness and brittleness, can be used for preparing and tabletting sustained-release pellets, the breakage rates of pellets and sustained-release films before and after tabletting are low, the release behavior before and after tabletting has no obvious change, and the technical requirements of pellet tabletting are met. Meanwhile, microcrystalline cellulose 101, microcrystalline cellulose 200 and hydroxypropyl cellulose are added in the tabletting link, so that the layering of the pellets and blank matrix in the tabletting link is avoided, and the problem of brittleness which is easy to occur in the pellet tabletting link is solved.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to a method for compressing metoprolol succinate pellets. Background technique [0002] In the development of pelletized tablets, pellet compression is a challenging process problem. The ideal sustained and controlled release coated pellets are required to be able to disintegrate into independent pellets quickly in the gastrointestinal fluid after oral administration, and the release characteristics of the pellets are not or rarely affected by the tableting process and can still remain Maintain its slow and controlled release characteristics. The pellets can be deformed, but they should not break. The factors that affect the release characteristics of pellets after tableting mainly include the following aspects: coating film materials, the amount of plasticizer in the coating film, the core material and its porosity and particle size, the excipients used for tablet...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K47/38A61K47/04A61K31/138
CPCA61K9/2054A61K9/2081A61K9/2095A61K9/5078A61K31/138A61K47/02A61K47/38
Inventor 程传松王珍甘冰叶瑾王远苹柯兴发项斌
Owner WUHAN OPTICS VALLEY YATAI PHARM RES INST CO LTD
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