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Preparation method of Azilsartan tablets

A technology of azilsartan tablet and disintegrant, which is applied in the field of medicine and achieves the effects of accelerated dissolution rate, consistent dissolution curve and good stability

Inactive Publication Date: 2015-11-11
JIANGSU ZHONGBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention provides an azilsartan tablet and a preparation method thereof. The preparation method controls the particle size of azilsartan, the weight ratio of azilsartan to lactose monohydrate and adjusts disintegrants, lubricants, diluents, etc. The types and proportions of solvents, solubilizers, and binders can not only solve the problem of dissolution rate, but also solve the problem of consistent dissolution in vitro

Method used

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  • Preparation method of Azilsartan tablets
  • Preparation method of Azilsartan tablets
  • Preparation method of Azilsartan tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Azilsartan 20g

[0030] Lactose monohydrate 120g

[0031] Starch 30g

[0032] Hypromellose E57g

[0033] Low-substituted hypromellose 15g

[0034] Polyethylene glycol 60006g

[0035] Magnesium stearate 1.0g

[0036] Preparation Process:

[0037] (1) Azilsartan is micronized, control D90<15 microns, and the prescription amount is weighed;

[0038] (2) Lactose monohydrate is passed through a 60-mesh sieve, and the prescription amount is weighed;

[0039] (3) Pass low-substituted hypromellose and starch through a 60-mesh sieve respectively, and weigh the prescription amount;

[0040] (4) Mix (1), (2), and (3), then add polyethylene glycol 6000 in equal amounts and mix, pass through a 60-mesh sieve and mix well; after mixing the above raw and auxiliary materials, add hydroxypropyl Soft material made of methyl cellulose E5; granulated by sieving, dried and granulated, then added with magnesium stearate, mixed evenly, and compressed into tablets.

Embodiment 2

[0042] Azilsartan 20g

[0043] Lactose monohydrate 140g

[0044] Starch 30g

[0045] Sodium carboxymethyl starch 8g

[0046] Povidone K304g

[0047] Talc powder 2g

[0048] Magnesium stearate 2g

[0049] Sodium Lauryl Sulfate 6g

[0050] Preparation Process:

[0051] (1) Azilsartan is micronized, control D90<15 microns, and the prescription amount is weighed;

[0052] (2) Lactose monohydrate is passed through a 60-mesh sieve, and the prescription amount is weighed;

[0053] (3) Pass hydroxymethyl starch sodium and starch through a 60-mesh sieve respectively, and weigh the prescription amount;

[0054] (4) Mix (1), (2) and (3), then add sodium lauryl sulfate in equal increments and mix, pass through a 60-mesh sieve and mix evenly; after mixing the above raw and auxiliary materials, add povidone K30 soft material; sieve and granulate, dry and granulate, then add magnesium stearate and talcum powder, mix evenly, and compress into tablets.

Embodiment 3

[0056] Azilsartan 20g

[0057] Lactose monohydrate 120g

[0058] Croscarmellose Sodium 6g

[0059] Tween-80 3.5g

[0060] Magnesium stearate 2g

[0061] Microcrystalline cellulose 6g

[0062] Hydroxypropyl Cellulose 5g

[0063] Preparation Process:

[0064] (1) Azilsartan is micronized, control D90<15 microns, and the prescription amount is weighed;

[0065] (2) Lactose monohydrate is passed through a 60-mesh sieve, and the prescription amount is weighed;

[0066] (3) Cross-linked sodium carboxymethyl cellulose and microcrystalline cellulose are respectively passed through a 60-mesh sieve, and the prescription amount is weighed;

[0067] (4) Mix (1), (2), and (3), then add Tween-80 in equal amounts and mix, pass through a 60-mesh sieve and mix well; after mixing the above raw and auxiliary materials, add hydroxypropyl Soft material made of cellulose; granulated by sieving, dried and granulated, then added with magnesium stearate, mixed evenly, and compressed into table...

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Abstract

The invention discloses a preparation method of Azilsartan tablets and belongs to the technical field of medicine. The preparation method comprises the following steps: 1, micronizing the Azilsartan, controlling D90 less than 15 micrometers, and conducting weighing according to formula dosage; 2, screening lactose monohydrate with a 60-mesh screen, and conducting weighing according to formula dosage; 3, screening a disintegrating agent and diluent with a 60-mesh screen respectively, and conducting weighing according to formula dosage; 4, mixing the auxiliary ingredients in the step 1, 2 and 3, adding solubilizer, conducting mixing, and screen the mixture with a 60-mesh screen; mixing the auxiliary ingredients uniformly, and adding adhesion agents for soft materials; conducting sieving, granulating, drying and arranging, adding lubricating agents, mixing the mixture uniformly, and tabletting. According to the preparation method, by controlling the particle diameter of the Azilsartan and the weight ratio between the Azilsartan and the lactose monohydrate and the varieties and adjusting the proportion of the disintegrating agents, the lubricating agents, the diluent, the solubilizer and the binding agents, the problem of dissolution rate can be solved, and the problem of external consistent dissolution is solved as well.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a preparation method of azilsartan tablets. Background technique [0002] Azilsartan is an angiotensin Ⅱ receptor antagonist drug for the treatment of hypertension. It is mostly used for the treatment of hypertension. It is also the only angiotensin Ⅱ receptor antagonist (sartan) drug in the late clinical stage. . The drug was launched by Japan's Takeda Pharmaceutical Company in 2012, and its efficacy in the clinical stage is remarkable. [0003] Azilsartan is an intolerant drug with a solubility in water of less than 9 μg / ml. The structural formula is as follows: [0004] [0005] Azilsartan is almost insoluble in water. When it is made into pharmaceutical preparations, it often needs to be treated in a special way to improve its dissolution rate in vitro, so as to ensure the absorption of the drug in the body and the clinical efficacy of the drug. CN1028952...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4245A61P9/12
Inventor 韩小军夏彬王飞唐景玉赵华阳
Owner JIANGSU ZHONGBANG PHARMA
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