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Composition containing acotiamide hydrochloride and preparation method of composition

A technology of acotiamide hydrochloride trihydrate and acotiamide hydrochloride, which is applied in the field of compositions containing acotiamide hydrochloride and its preparation, can solve the problems of easy water loss, high ratio, and slow dissolution rate, etc. Achieve the effects of avoiding crystal transformation, excellent comprehensive performance, and accelerating disintegration speed

Pending Publication Date: 2019-10-29
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Acotiamide hydrochloride is slightly soluble in water, and is almost insoluble in pH 1.0 hydrochloric acid medium, which causes the problem that the solubility of acotiamide hydrochloride is small and the dissolution rate is slow
At the same time, acotiamide hydrochloride is prone to dehydration under low humidity (<20% RH) conditions, and is converted from trihydrate to monohydrate, thereby affecting the stability of the tablet
At the same time, acotiamide hydrochloride itself has poor fluidity and a high proportion in the preparation, which cannot meet the requirements of the direct compression process
[0007] Since the wet granulation process needs to be dried at high temperature, and the raw material drug is easy to lose bound water during the drying process, resulting in a high risk of stability of the final product
At the same time, acotiamide hydrochloride itself has poor fluidity and a high proportion in the preparation, which cannot meet the requirements of the direct compression process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] To study the influence of temperature and humidity on the stability of the crystal form of acotiamide hydrochloride, the raw material drug, that is, the active ingredient, was respectively placed under the humidity conditions of 18% RH and 35% RH, and the change of its moisture content was investigated.

[0071] (1) 20℃ / 18%RH Moisture Inspection

[0072] Under the condition of 20°C / 18%RH, test its moisture content at different storage times, the results are shown in Table 1, and the corresponding scatter plots are shown in figure 1 shown.

[0073] Table 1 20℃ / 18%RH moisture survey data

[0074] Placement time (h) Moisture (%) 0 9.98 2 9.65 4 9.18 6 8.98 8 8.51 10 7.24 12 6.35 24 5.47 32 4.72 40 4.39 48 4.35 60 4.38

[0075] The data show that acotiamide hydrochloride trihydrate is an unstable crystal form under lower humidity conditions; as the standing time prolongs, two molecules of water ar...

Embodiment 2

[0090] Particle size of raw materials: Acotiamide hydrochloride is slightly soluble in water, and almost insoluble in pH 1.0 hydrochloric acid medium, which causes the problem of low solubility and slow dissolution rate of acotiamide hydrochloride tablets.

[0091] Table 4 raw materials

[0092] Drugs / Excipients Dosage (g) Acotiamide hydrochloride trihydrate* 100* lactose 78 Microcrystalline Cellulose PH101 32 Hydroxypropyl Cellulose 10 Low-substituted hydroxypropyl cellulose 10 inner plus +10 extra silica 7.5 Magnesium stearate 2.5 Film Coating Premix 7.5 production 257g / 1000 pieces

[0093] Note: * is the amount of feed calculated by anhydrous

[0094] Weigh the prescribed amount of acotiamide hydrochloride trihydrate, filler, glidant, disintegrant (internal added part), and adhesive and place it in a three-dimensional mixer and mix for 20 minutes. The above mixture is granulated in a dry granulator wit...

Embodiment 3

[0102] Addition method of disintegrant: Investigate the methods of all internal addition, all external addition and internal and external addition of disintegrant (internal and external addition ratio 1:1).

[0103] The raw materials used are shown in Table 6.

[0104] Table 6 raw materials

[0105] Drugs / Excipients Dosage (g) Acotiamide hydrochloride trihydrate* 100* lactose 78 Microcrystalline Cellulose PH101 32 starch 10 Low-substituted hydroxypropyl cellulose 20 talcum powder 7.5 Magnesium stearate 2.5 Film Coating Premix 7.5 production 257g / 1000 pieces

[0106] Note: * is the amount of feed calculated by anhydrous

[0107] Group 1:

[0108] Addition of disintegrant: mechanically pulverize acotiamide hydrochloride trihydrate, and weigh the prescribed amount of active ingredients, fillers, glidants, disintegrants, and binders and place them in three-dimensional mixing Mix in the machine for 20 minutes...

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Abstract

The invention relates to the field of medicine preparation, in particular to a composition containing acotiamide hydrochloride and a preparation method of the composition. The composition containing acotiamide hydrochloride is mainly prepared from an active ingredient and an auxiliary material by dry granulation; and the active ingredient is acotiamide hydrochloride and / or a hydrate thereof. An acotiamide hydrochloride tablet is prepared by a dry granulation process, and the risk that the active ingredient is prone to being subjected to crystal form transformation in the drying process in wetgranulation is avoided; and the obtained acotiamide hydrochloride tablet is good in stability and dissolution rate.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a composition containing acotiamide hydrochloride and a preparation method thereof. Background technique [0002] Acotiamide Hydrochloride Tablets Jointly developed by Japan's Sawari Shinyaku Co., Ltd. and Astellas Pharmaceutical Group, it is used for the treatment of functional dyspepsia (FD) symptoms such as epigastric flatulence and premature satiety. The drug inhibits acetylcholine by inhibiting the activity of peripheral acetylcholinease Degradation, thereby improving many FD symptoms. [0003] The English name or Latin name of Acotiamide Hydrochloride Hydrochloride Tablets, Chinese chemical name N-[2-(isopropylamino)ethyl]-2-(2-hydroxy-4,5-dimethoxybenzene Formylamino)thiazole-4-carboxamide hydrochloride trihydrate, chemical structural formula: [0004] [0005] Molecular formula is C 21 h 30 N 4 o 5 S·HCl·3H 2 O, the molecular weight is 541.06. [0006] Aco...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/426A61P1/14
CPCA61K9/2054A61K9/2095A61K9/28A61K31/426
Inventor 朱朝露吴昀卢迪
Owner BEIJING TIDE PHARMA
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