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Preparation process of trelagliptin succinate tablet

A troxagliptin succinate, preparation process technology, applied in the field of preparation of troxagliptin succinate tablets, can solve the problems of easy adhesion and compressibility, prone to splitting, poor compressibility, etc., and achieve good flow and compressibility, ensuring product quality attributes, and simplifying the production process

Active Publication Date: 2022-01-28
宁波高新区美诺华医药创新研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The fluidized bed preparation process used in the original preparation is relatively complicated, and the feasibility of the process is greatly affected by the pharmacological properties of the raw materials. The high proportion of 74% API has brought many problems, including easy aggregation, easy adhesion, and poor compressibility and fluidity. Easy to split, etc. Although fluidized bed granulation can meet the requirements of smooth process, there are still risks such as low content, low yield, and splits, which require special means to improve and optimize
Due to the risks brought by the process, the cost of research and development is increased, and the complexity of the process reduces production efficiency and increases production costs.
[0003] The bulk density of troxagliptin succinate is low, the air in the pores of the granulation intermediate particles is difficult to discharge, and the compressibility is poor, which makes the problem of fragmentation prone to occur during the tableting process; at the same time, troxagliptin succinate is easy to aggregate, which will affect Fluidized granulation process, resulting in batch-to-batch variance, needs to be improved

Method used

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  • Preparation process of trelagliptin succinate tablet
  • Preparation process of trelagliptin succinate tablet
  • Preparation process of trelagliptin succinate tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Tablets are prepared with the formula shown in Table 1, and the specific process is as follows:

[0026] In the first step, mix the prescription amount of trexagliptin succinate with HPC-L:HPMC powder at a ratio of 4:1, dissolve it in water, and make a 0.3% w / w solution of solute.

[0027] The second step is to add the above solution into the spray drying equipment, the air inlet temperature is 160°C, the feeding speed is 5mL / min, the atomization pressure is 0.5MPA, and the dry air source is used for drying and heating. 3 The / h flow rate is transported to the drying room, and the granules are sieved with a granulator in the spray dryer, with a 0.99mm sieve.

[0028] In the third step, the granules obtained by sieving, microcrystalline cellulose, mannitol, and croscarmellose sodium are uniformly mixed in a mixer, and then sodium stearyl fumarate is added for mixing to obtain a tablet-making product. Granules: Using a rotary tablet press, use a 11*5.6mm die to tablet th...

Embodiment 2

[0033] Prepare tablet with formula shown in table 2, concrete process is as follows:

[0034] In the first step, mix the prescription amount of trexagliptin succinate with HPC-L:HPMC powder at a ratio of 4:1, dissolve it in water, and prepare a solute 3% w / w solution.

[0035] The second step is to add the above solution into the spray drying equipment, the air inlet temperature is 120°C, the feeding speed is 5mL / min, the atomization pressure is 0.5MPa, and the dry air source is used for drying and heating. 3 The / h flow rate is transported to the drying room, and the granules are sieved with a granulator in the spray dryer, with a 0.99mm sieve.

[0036] In the third step, the granules obtained by sieving, microcrystalline cellulose, mannitol, and croscarmellose sodium are uniformly mixed in a mixer, and then sodium stearyl fumarate is added for mixing to obtain a tablet-making product. Granules: Using a rotary tablet press, use a 11*5.6mm die to tablet the granules to obtain...

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Abstract

The invention discloses a preparation process of a trelagliptin succinate tablet, which comprises the following steps of: mixing a carrier with an API raw material according to a preferable ratio, and granulating by using spray drying equipment under preferable parameters, so that the granule has better granule property and regular appearance property compared with an original grinding fluidized bed, and has smaller bulk volume and good flowability and compressibility compared with pure API; the risk of tablet cracking caused by difficulty in discharging air in gaps of materials in tablets and poor compressibility due to physical properties of fluidization granulation and API is avoided, so that the design range of technological parameters is wider, the technological process is more controllable and stable, various process feasibility problems caused by poor physical attributes of API, fluffy particles after fluidization granulation, poor compressibility and the like can be solved, process control is easy to realize, product quality attributes are guaranteed, meanwhile, the production process can be simplified, the production efficiency can be improved, and the production cost can be saved.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a preparation process of trexagliptin succinate tablets. Background technique [0002] The fluidized bed preparation process used in the original preparation is relatively complicated, and the feasibility of the process is greatly affected by the pharmacological and chemical properties of the raw materials. The high proportion of 74% API has brought many problems, including easy aggregation, easy adhesion, and poor compressibility and fluidity. Easy to split, etc. Although fluidized bed granulation can meet the requirements of smooth process, there are still risks such as low content, low yield, and split, which require special means to improve and optimize. Because the risks brought by the process increase the cost of research and development, the complexity of the process reduces the production efficiency and increases the production cost. [0003] The bulk density of troxag...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/20A61K31/513A61K47/38
CPCA61K9/2866A61K9/2054A61K31/513
Inventor 邰航胡继凯姚振江叶连挺程凌飞
Owner 宁波高新区美诺华医药创新研究院有限公司
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