Oral tablet of acotiamide hydrochloride trihydrate and preparation method thereof

A technology of acotiamide hydrochloride trihydrate and oral tablet, which is applied in the field of oral tablet of acotiamide hydrochloride trihydrate and its preparation, can solve the problem of too large and too heavy tablet, enlargement of preparation shape, Swallowing problems and other problems, to achieve the effect of shrinking tablet size, reducing the amount of excipients, and reducing product costs

Active Publication Date: 2016-07-20
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a large increase in excipients will significantly increase the shape of the preparation, especially for drugs with high single doses
The currently marketed acotiamide tablet (Japan Zeli Shinyaku Co., Ltd.) has a single dose of 100mg, but its tablet weight is 250mg, that is, the active ingredient only accounts for about 40% of the tablet weight.
In order to prevent unreasonable drug specifications from causing confusion to clinical medication, the State Food and Drug Administration requires that the dosage should be reasonably determined according to the usage and dosage of the drug, generally not less than the minimum single dosage. The single dosage of acotiamide hydrochloride is 100mg, containing hydrochloric acid The total weight of acotiamide 100mg oral tablet is about 250mg. If the tablet is too large or too heavy, it will cause certain swallowing problems, especially for some patients with dysphagia such as the elderly and children, who have poor compliance

Method used

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  • Oral tablet of acotiamide hydrochloride trihydrate and preparation method thereof
  • Oral tablet of acotiamide hydrochloride trihydrate and preparation method thereof
  • Oral tablet of acotiamide hydrochloride trihydrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] prescription:

[0028] Material composition Prescription ratio (g) Acotiamide Hydrochloride Trihydrate 50 starch 35 starch 9 Croscarmellose Sodium 3 Magnesium stearate 3 Production volume 500 pieces

[0029] Preparation method: 1) Weigh each material separately; 2) Fully mix acotiamide hydrochloride trihydrate and 35 g of starch, and add appropriate amount of water to granulate after mixing; 3) Dry in a wet granule drying box until the moisture content of the granules is not more than 3.0 %, drying temperature is 45°C; 4) The dry granules are passed through a 20-mesh sieve for granulation; 5) The obtained granules are mixed with 9 g of starch, croscarmellose sodium and magnesium stearate; 6) According to the theoretical tablet weight (200mg ) tablet.

Embodiment 2

[0031] prescription:

[0032] Material composition Prescription ratio (g) Acotiamide Hydrochloride Trihydrate 75 pregelatinized starch 10 microcrystalline cellulose 8.5 sodium starch glycolate 5 Micropowder silica gel 1.5 25% ethanol aqueous solution Appropriate amount Production volume 750 tablets

[0033] Preparation method: 1) Weigh each material separately; 2) Fully mix acotiamide hydrochloride trihydrate and pregelatinized starch, add an appropriate amount of 25% ethanol aqueous solution to granulate after mixing; 3) Dry the wet granules in a drying oven until The moisture content of the granules is not more than 4.0%, and the drying temperature is 50°C; 4) The dry granules are sieved through a 40-mesh sieve; 5) The obtained granules are mixed with microcrystalline cellulose, sodium starch glycolate and micropowder silica gel; 6) According to the theoretical tablet weight ( 133.3mg) into tablets.

Embodiment 3

[0035] prescription:

[0036] Material composition Prescription ratio (g) Acotiamide Hydrochloride Trihydrate 60 microcrystalline cellulose 30.3 pregelatinized starch 5 Crospovidone 1.7 talcum powder 3 10% ethanol aqueous solution Appropriate amount Production volume 600 pieces

[0037] Preparation method: 1) Weigh each material separately; 2) Fully mix acotiamide hydrochloride trihydrate and microcrystalline cellulose, add an appropriate amount of 10% ethanol aqueous solution to granulate after mixing; 3) Dry the wet granules in a drying oven until The moisture content of the granules is not more than 4.0%, and the drying temperature is 40°C; 4) The dry granules are sized; 5) The obtained granules are mixed with pregelatinized starch, crospovidone and talc; 6) According to the theoretical tablet weight (166.7mg) Tablet.

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PUM

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Abstract

The invention discloses o an oral tablet of acotiamide hydrochloride trihydrate and a preparation method thereof. The acotiamide hydrochloride trihydrate disclosed by the invention adopts a water insoluble filler as the first filler, and aims to still maintain the original particle shape when drug particles contact a dissolution medium and other solutions so as to prevent acotiamide hydrochloride from gathering, thus achieving a good dissolution effect. At the same time, through additional adding of a second filler and a disintegrating agent, the material is ensured with good compressibility and dissolution performance. According to the acotiamide hydrochloride tablet and the preparation method provided by the invention, the operation is simple, the dosage of auxiliary materials is significantly reduced, the tablet weight is small, and while the dissolution rate is guaranteed, the patient compliance is also improved.

Description

technical field [0001] The invention relates to an oral tablet of acotiamide hydrochloride trihydrate and a preparation method thereof. Background technique [0002] Acotiamide hydrochloride (acotiamide) is a choline M1 receptor antagonist and the first FD treatment drug in the world. By acting on choline receptors and cholinesterase, it can improve gastric motility disturbance and delayed gastric emptying , so as to improve the postprandial fullness, upper abdominal distension and early satiety of FD. It is used to treat functional dyspepsia (FD). The dosage is 100mg of acotiamide hydrochloride trihydrate each time, three times a day. [0003] When acotiamide hydrochloride trihydrate meets water, it is easy to reunite and form a gel-like hydration layer on the surface, which prevents water from further entering the granules, resulting in incomplete dissolution. This property leads to "collapse and insolubility" in the formulation, which reduces dissolution and bioavailab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/426A61P1/14
Inventor 欧阳汝霖黄和意高翼陶艳汤丹彭贵子左联卢智俊袁永玲
Owner REGENEX PHARMA LTD
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