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Acarbose pharmaceutical composition and preparation method thereof

A technology of acarbose and its composition, which is applied in the field of acarbose pharmaceutical composition and its preparation, and can solve the problems of poor appearance, easy aggregation, flammability and explosion of tablets, etc.

Active Publication Date: 2020-07-07
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]Embodiment 1: One-step granulation process prepares acarbose tablet

[0045] Raw materials Prescription amount per tablet / 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) Acarbose, starch and microcrystalline cellulose weighed in step 1) Pour the element into the material pot of the fluidized bed, turn on the heating, enter the air for mixing and preheating, the air inlet temperature is 40-42°C, and when the exhaust air temperature rises to 35-37°C, disperse the silica to Prepare a spray liquid in water to spray the material in the fluidized bed material pot, the spray speed is 10-12rpm, and the concentration is 10%-12%. After the spraying is over, dry the material for 20 ...

Embodiment 2

[0047] Embodiment 2 One-step granulation process prepares acarbose tablet

[0048] Raw materials Prescription amount per tablet / 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) Acarbose, starch and microcrystalline cellulose weighed in step 1) Pour the element into the material pot of the fluidized bed, turn on the heating, enter the air for mixing and preheating, the air inlet temperature is 78-80°C, and when the exhaust air temperature rises to 53-55°C, disperse the silica to Prepare a spray liquid in water to spray the material in the fluidized bed feed pot, the spray speed is 18-20rpm, and the concentration is 68%-70%. After the spraying is over, dry the material for 60min, s...

Embodiment 3

[0050] Embodiment 3 One-step granulation process prepares acarbose tablet

[0051] Raw materials Prescription amount per tablet / 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 acarbose, starch and silicified microcrystalline cellulose weighed in step 1) Put it into the multifunctional fluidized bed material pot, turn on the heating, enter the air for mixing and preheating, the inlet air temperature is 60~62℃, when the exhaust air temperature rises to 43~45℃, use water as a spray liquid to the multifunctional fluidized bed The material in the feeding pot is sprayed at a spray speed of 10-12rpm. After the spraying is over, the material is dried for 40 minutes, and the drying is stopped t...

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Abstract

The invention relates to an acarbose pharmaceutical composition and a preparation method thereof. The pharmaceutical composition comprises acarbose, a filling agent and a lubricant, and optionally comprises a glidant. The pharmaceutical composition is prepared by using a one-step granulation process. Water or a low-concentration ethanol solution is used as a wetting agent, and thereby the danger of using a high-concentration ethanol solution as a wetting agent is avoided; the change of two steps of granulation and drying into one step is realized, and the trouble of transferring materials is eliminated; and silica is dispersed into the wetting agent and added into the materials by spraying, or silicified microcrystalline cellulose is used, so that the problem that direct addition of silicaeasily causes electrostatic aggregation and large dissolution RSD is solved, and the more uniform quality is ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an acarbose pharmaceutical composition and a preparation method thereof. Background technique [0002] Acarbose (acarbose, trade name Baitangping / Baitangping), the 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 α-glucosidase inhibitor developed by German Bayer company for clinical use. It was launched in Germany in 1990 and sold in my country in 1994. It can be used for the treatment of insulin-dependent or insulin-dependent Dependent diabetes can also be used in combination with other oral hypoglycemic drugs or insulin. Because it is almost not absorbed through the intestines, there are few systemic adverse reactions, and only mild to moderate local gastrointestinal discomfort ...

Claims

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Application Information

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Patent Type & Authority Applications(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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