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Acarbose pharmaceutical composition and preparation method thereof

A technology for acarbose and composition is applied in the field of acarbose pharmaceutical composition and its preparation, which can solve the problems of difficult process control, unstable hardness, slow dissolution and release, etc., achieves low dissolution rate and avoids flammability Explosive risk, rapid dissolution and release effect

Active Publication Date: 2022-07-26
GAN&LEE PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the common preparation methods of acarbose pharmaceutical composition include wet granulation process, direct compression process and dry granulation process. Among them, the traditional wet granulation process usually uses high-concentration ethanol solution as a wetting agent for granulation, and there are flammable Explosive danger. When water is used as a wetting agent, acarbose becomes sticky when exposed to water and is easy to agglomerate, so that the process is difficult to control. The obtained tablets have poor appearance and slow dissolution and release; direct pressure process requires the flow of raw and auxiliary materials Otherwise, it is very easy to obtain products with uneven quality, resulting in unstable hardness and large RSD of dissolution; dry granulation process requires special equipment, and the preparation efficiency is low

Method used

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  • Acarbose pharmaceutical composition and preparation method thereof
  • Acarbose pharmaceutical composition and preparation method thereof
  • Acarbose pharmaceutical composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044]Example 1: One-step granulation process to prepare acarbose tablets

[0045] Raw materials Single tablet prescription amount / mg Experimental dosage / g Acarbose 50 100 starch 43.95 87.9 microcrystalline cellulose 43.95 87.9 silica 1.4 2.8 Magnesium stearate 0.7 1.4 total 140 280

[0046] Preparation method: 1) Weigh acarbose, starch, microcrystalline cellulose, silicon dioxide and magnesium stearate respectively; 2) Weigh the acarbose, starch and microcrystalline cellulose weighed in step 1). The raw material is poured into the fluidized bed material pot, the heating is turned on, and the air inlet is mixed and preheated. The air inlet temperature is 40 to 42 °C. When the exhaust air temperature rises to 35 to 37 °C, the silica is dispersed under stirring conditions. Prepare a spray liquid in water to spray the material in the fluidized bed material pot, the spray speed is 10-12rpm, the concentration is 10%-12%, a...

Embodiment 2

[0047] Example 2 One-step granulation process to prepare acarbose tablets

[0048] Raw materials Single tablet prescription amount / mg Experimental dosage / g Acarbose 100 100 starch 87.9 87.9 microcrystalline cellulose 87.9 87.9 silica 2.8 2.8 Magnesium stearate 1.4 1.4 total 280 280

[0049] Preparation method: 1) Weigh acarbose, starch, microcrystalline cellulose, silicon dioxide and magnesium stearate respectively; 2) Weigh the acarbose, starch and microcrystalline cellulose weighed in step 1). The raw material is poured into the fluidized bed material pot, the heating is turned on, and the air inlet is mixed and preheated. The air inlet temperature is 78 to 80 °C. When the exhaust air temperature rises to 53 to 55 °C, the silica is dispersed under stirring conditions. Prepare a spray liquid in water to spray the material in the fluidized bed pot, the spray speed is 18-20rpm, the concentration is 68%-70%, after the s...

Embodiment 3

[0050] Example 3 One-step granulation process to prepare acarbose tablets

[0051] Raw materials Single tablet prescription amount / mg Experimental dosage / g Acarbose 50 100 starch 43.25 86.5 Silicified microcrystalline cellulose 46.05 92.1 Magnesium stearate 0.7 1.4 total 140 280

[0052] Preparation method: 1) Weigh acarbose, starch, silicified microcrystalline cellulose and magnesium stearate respectively; 2) Pour the weighed acarbose, starch and silicified microcrystalline cellulose in step 1). Put it into the multi-functional fluidized bed material pot, turn on the heating, and mix and preheat the air inlet. The air inlet temperature is 60-62 °C. When the exhaust air temperature rises to 43-45 °C, water is used as a spray to the multi-functional fluidized bed. The material in the feeding pot is sprayed, and the spraying speed is 10-12 rpm. After the spraying is completed, the material is dried for 40 minutes, and the dryi...

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Abstract

The present invention relates to acarbose pharmaceutical composition and its preparation method. The pharmaceutical composition comprises acarbose, a filler, a lubricant, and optionally a glidant, and is prepared by a one-step granulation process. The present invention uses water or low-concentration ethanol solution as the wetting agent, avoiding the danger of using high-concentration ethanol solution as the wetting agent; realizing two steps of granulation and drying into one step, saving the trouble of transferring materials; Silica is dispersed in the wetting agent and added to the material by spraying or using silicified microcrystalline cellulose to solve the problem of electrostatic aggregation and dissolution of large RSD caused by direct addition of silica, and to ensure more uniform quality.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more particularly relates to acarbose pharmaceutical composition and a preparation method thereof. Background technique [0002] Acarbose (acarbose, trade name Baitangping / Baitangping), chemical name is O-4,6-dideoxy-4[[(1S,4R,5S,6S)4,5,6-trihydroxy -3-(Hydroxymethyl)-2-cyclohexene]amino]-(-D-glucopyranosyl(1→4)-O-)-D-glucopyranosyl(1→4)- D-glucopyranose, the structural formula is shown in formula I. Acarbose is the first clinical α-glucosidase inhibitor developed by Bayer Company in Germany. It was launched in Germany in 1990 and sold in my country in 1994. It can be used to treat insulin-dependent or Dependent diabetes mellitus can also be used in combination with other oral hypoglycemic drugs or insulin. Because it is hardly absorbed through the intestines, there are few systemic adverse reactions, only mild to moderate local gastrointestinal discomfort, which can improve the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/16A61K47/38A61K47/04A61K31/7036A61P3/10
CPCA61K9/2095A61K9/1652A61K9/1611A61K31/7036A61P3/10
Inventor 祁伟力张海朝黄林平张一宁
Owner GAN&LEE PHARMA
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