Hydrochloric acid acotiamide tablets and preparation method thereof

A technology of acotiamide hydrochloride tablets and acotiamide hydrochloride trihydrate, which is applied in the field of acotiamide hydrochloride tablets and its preparation, can solve the problem of drugs affecting drug absorption, low bioavailability, and low dissolution rate, etc. problems, to achieve good in vitro dissolution stability, small preparation process restrictions, and high bioavailability

Active Publication Date: 2016-03-23
WATERSTONE PHARMA WUHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because acotiamide is a poorly soluble drug, the dissolution rate is low, and the dissolution rate of the drug directly affects the absorption of the drug, resulting in low bioavailability and affecting the efficacy of the drug. This not only causes waste of the drug and is easy to take in large doses. many side effects
[0005] Usually, in the stage of preparing raw materials, it is necessary to refine, select crystals with small particle sizes or pulverize raw materials, control particle size, or improve the dissolution rate of preparation products by means of micro-powder, but these physical operations increase the operating procedures, usually Causes the increase of related substances in raw materials, changes in crystal form, moisture, etc., which affects product quality
[0006] Therefore, the current acotiamide pharmaceutical preparations still need to be improved

Method used

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  • Hydrochloric acid acotiamide tablets and preparation method thereof
  • Hydrochloric acid acotiamide tablets and preparation method thereof
  • Hydrochloric acid acotiamide tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0046] (1) Preparation of Acotiamide Hydrochloride Tablets

[0047] Wet granulation tableting:

[0048] 1) Sieve

[0049] Select a 20-mesh sieve, sieve to remove agglomerates, and obtain a uniform particle group, which is beneficial to the subsequent granulation, mixing, tableting and other processes.

[0050] 2) mixed

[0051] Mix the prescribed amount of acotiamide hydrochloride, filler and disintegrant evenly.

[0052] 3) Granulation

[0053] The mixture obtained in step 2) is added with a binder to make a soft material, and a 20-mesh screen is selected for granulation.

[0054] 4) drying

[0055] Dry the granules obtained in step 3) at 50-70° C., and control the moisture between 3.0% and 6.0%.

[0056] 5) Tablet

[0057] Add lubricant to the granules obtained in step 4), mix evenly, and press into tablets to obtain.

[0058] Powder direct compression:

[0059] In another aspect of the present invention, the present invention also proposes the method for preparing ...

specific Embodiment

[0076] The specific embodiment of the patent of the present invention is as follows:

[0077] Batch No. 1: Acotiamide hydrochloride trihydrate raw material obtained by refining at a lower rotational speed;

[0078] Batch No. 2: raw material of acotiamide hydrochloride trihydrate obtained by refining at a moderate rotational speed;

[0079] Batch No. 3: raw material of acotiamide hydrochloride trihydrate obtained by refining at a higher rotational speed.

Embodiment 1～ Embodiment 6

[0080] Embodiment 1~Example 6 investigates the impact of silicon dioxide on the dissolution of the acotiamide hydrochloride trihydrate raw material that different preparation processes make:

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PUM

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Abstract

The invention relates to hydrochloric acid acotiamide tablets and a preparation method thereof. The tablets are prepared from, by weight, 20-60 parts of hydrochloric acid trihydrate, 40-80 parts of a filling agent, 2-20 parts of a disintegrating agent, 1-8 parts of a binding agent and 0.5-6 parts of a lubricating agent. According to the hydrochloric acid acotiamide tablets and the preparation method thereof, by increasing the silicon dioxide using amount within a reasonable range, the indissolvable hydrochloric acid trihydrate in a 0.01-N hydrochloric acid medium can be better dissolved, the bioavailability and the stability of the hydrochloric acid trihydrate are improved, and overdependence on a raw material preparation technology is reduced. In addition, a formula and a preparation technology of the hydrochloric acid acotiamide tablets are simple and easy to operate, the production cost is saved, and the preparation product quality and the treatment effect are improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to acotiamide hydrochloride tablets and a preparation method thereof. Background technique [0002] Acotiamide hydrochloride is a trihydrate (compound shown in formula I), which is the world's first drug for the treatment of functional dyspepsia. It was developed by Japan Sari Shinyaku Co., Ltd. and was approved for marketing in Japan in February 2013. It is suitable for the treatment of postprandial fullness, functional dyspepsia, upper abdominal fullness, and early satiety. [0003] [0004] The currently marketed acotiamide hydrochloride trihydrate oral tablet mainly works by inhibiting acetylcholinesterase in the digestive tract, which can promote gastric motility, improve gastric accommodation disorders, and enhance gastric fundus expansion. However, because acotiamide is a poorly soluble drug, the dissolution rate is low, and the dissolutio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/426A61K47/02A61P1/14
Inventor 王珍钱丽娜刘大鹏祝小芬贾田周晓星高宏平秦志平
Owner WATERSTONE PHARMA WUHAN
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