Prucalopride succinate tablet composition and preparation method thereof

A technology of prucalopride and succinic acid, which is applied in the direction of drug combinations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of time-consuming, labor-intensive, and complex equipment that are not suitable for industrial production and other problems, achieve high uniformity and bioavailability, solve the problem of content uniformity, and improve the effect of content uniformity

Pending Publication Date: 2020-05-22
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, prucalopride succinate tablets are small-scale preparations, and the main ingredient accounts for 0.4-0.8% of the prescription volume. Such a small proportion has brought challenges to industrial production. Generally, powder mixing uniformity problems are prone to occur, which in turn leads to Dosage uniformity problems
[0005] In addition, in the prior art, the patent document CN103070865 discloses a tablet of prucalopride succinate, which contains 5% starch slurry, and uses a wet granulation process, because prucalopride succinate Li and lactose will generate toxic lactose adducts in the presence of water, and the adducts will increase with time. Therefore, the tablet composition disclosed in this patent document has toxic and side effects that threaten human health
[0006] Patent document CN104352465 micronizes prucalopride succinate, controls the particle size distribution of key excipients, controls the mixing method and time, and solves the tablet weight difference caused by material uniformity and particle fluidity through a special granulation process , but this method is complicated in equipment, cumbersome and lengthy, time-consuming and labor-intensive, and is not suitable for industrial production
[0007] Patent document CN10406

Method used

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  • Prucalopride succinate tablet composition and preparation method thereof
  • Prucalopride succinate tablet composition and preparation method thereof
  • Prucalopride succinate tablet composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A composition of prucalopride succinate, calculated as prucalopride, comprises the following ingredients:

[0040]

[0041]

[0042] The average particle size of prucalopride succinate was 5.551 microns with a particle size distribution of D90<10 microns.

[0043] In order to confirm the impact of the average particle size of the bulk drug on the composition, only the average particle size of the bulk drug prucalopride succinate was changed when other conditions were the same, and compared with comparative examples 1 and 2 with larger average particle sizes. The specific comparison results are shown in Table 1 below:

[0044] Table 1 Content uniformity and dissolution rate data of prucalopride succinate with different particle sizes

[0045]

[0046] Provided in Table 1 within the scope of the composition of the present invention, the dissolution and content uniformity of the formulation obtained by changing the average particle size of prucalopride succinate ...

Embodiment 2

[0048] A composition of prucalopride succinate, calculated as prucalopride, comprises the following components:

[0049]

[0050] The average particle size of prucalopride succinate was 6.395 microns with a particle size distribution of D90<10 microns.

Embodiment 3

[0052] A composition of prucalopride succinate, calculated as prucalopride, comprises the following components:

[0053]

[0054] The average particle size of prucalopride succinate was 6.395 microns with a particle size distribution of D90<10 microns.

[0055] In order to confirm the impact of the amount of silicon dioxide added on the composition, only the added amount of silicon dioxide was changed when other conditions were the same, and the examples 2 and 3 with more silicon dioxide added were compared with the silicon dioxide added. Comparative examples 3 and 4 are compared, and the specific comparison results are shown in Table 2 below:

[0056] Table 2 Content uniformity and dissolution data at different additions of silica

[0057]

[0058]

[0059] Table 2 shows the angle of repose and the dissolution rate comparison data of not adding silicon dioxide, adding a small amount of silicon dioxide and adding the required amount of silicon dioxide in the present ...

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Abstract

The invention relates to a prucalopride succinate tablet composition and a preparation method thereof, and provides a prucalopride succinate tablet composition which is non-toxic, good in stability, high in uniformity and biological availability, simple in technology and low in cost, and a preparation method of the prucalopride succinate tablet composition.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a tablet composition containing prucalopride succinate and a preparation method thereof. Background technique [0002] Chronic constipation has become a global problem that endangers public health. It is more common in women and the elderly. It not only seriously affects the quality of life of patients, but may also induce other serious diseases, such as anorectal disease, fecal ulcer and hepatic encephalopathy. and increase the risk of cardiovascular events. The treatment of chronic constipation usually uses laxatives, but laxatives are not effective in improving the symptoms of constipation. [0003] Prucalopride succinate is a dihydrobenzofuran drug with the chemical name 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl) -4-piperidinyl]-7-benzofurancarboxamide succinate, a selective, high-affinity serotonin (5-HT4) receptor agonist with prokinetic activity and ineffective in treati...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/38A61K47/26A61K9/28A61K31/4525A61P1/12
CPCA61K9/2054A61K9/2018A61K9/2095A61K9/28A61K31/4525A61P1/12
Inventor 拥青她姆陈中亚周炳城
Owner JIANGSU HANSOH PHARMA CO LTD
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