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Irbesartan sodium micro composite powder and tablets and preparation method thereof

A composite powder and irbesartan technology, which is applied in pharmaceutical formulation, powder delivery, pill delivery, etc., can solve the problems of insufficient improvement of irbesartan bioavailability, uneven distribution, large drug particles, etc. , to achieve the effect of good application prospect, simple process and high dissolution rate

Active Publication Date: 2012-01-11
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Through the above method, the bioavailability of irbesartan has been improved, but these methods all have the problems of complex process and high production cost. More importantly, the prepared drug particles of the above method are large and unevenly distributed, and the irbesartan The bioavailability of besartan is not fully enhanced
However, there are no related reports about the preparation of micro-composite powders of irbesartan and tablets thereof

Method used

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  • Irbesartan sodium micro composite powder and tablets and preparation method thereof
  • Irbesartan sodium micro composite powder and tablets and preparation method thereof
  • Irbesartan sodium micro composite powder and tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] A: Weigh 5g of irbesartan raw material drug and dissolve it in 100mL of tetrahydrofuran; weigh 0.5g of mannitol and dissolve it in 1.5L of water. Under the condition of controlling the system temperature at 10°C, mix and stir the drug solution and aqueous solution to obtain drug slurry material, wherein the average particle size of the drug particles is 600nm;

[0058] B: Weigh 0.5g of microcrystalline cellulose, 0.5g of starch, and 0.3g of cross-linked polyvinylpyrrolidone and disperse them in the slurry obtained in step A;

[0059] C: Spray-dry the slurry obtained in step B to obtain amorphous irbesartan micro-composite powder, in which the mass of irbesartan is 73%; the spray-drying conditions are: feed flow rate is 30mL / min, inlet temperature 130°C, compressed air pressure is 0.5MPa.

[0060] D: Weigh 1.5 g of the composite powder obtained in step C, add an appropriate amount of 4% PVP ethanol-water solution, granulate, and dry at 70°C to obtain dry granules. The v...

Embodiment 2

[0063] A: Weigh 6g of irbesartan raw material drug and dissolve it in 600mL of methanol; weigh 0.8g of lactose and dissolve it in 6L of water, and mix and stir the drug solution and aqueous solution under the condition of controlling the system temperature at 15°C to obtain drug slurry , wherein the average particle size of the drug particles is 400nm;

[0064] B: Weigh 0.8g of microcrystalline cellulose and 0.7g of carboxymethyl starch and nano-disperse them in the slurry obtained in step A;

[0065] C: Spray-dry the slurry obtained in step B to obtain amorphous irbesartan micro-composite powder, in which the mass of irbesartan is 72%; the spray-drying conditions are: feed flow rate is 20mL / min, inlet temperature 120°C, compressed air pressure is 0.6MPa.

[0066] D: Weigh 0.15g lactose, 0.15g microcrystalline cellulose, 0.08g sodium carboxymethyl starch, mix evenly with 2g of the composite powder obtained in step C, add an appropriate amount of 2% PVP ethanol-water solution,...

Embodiment 3

[0069] A: Weigh 4g of irbesartan raw material and dissolve it in 300mL N,N-dimethylformamide; weigh 1g of polyethylene glycol and 0.2g of sodium lauryl sulfate and dissolve it in 1.5L of water. Under the condition of temperature of 25°C, the drug solution and the aqueous solution are mixed and stirred to obtain a drug slurry, wherein the average particle size of the drug particles is 900nm;

[0070] B: Weigh 0.8g lactose, 0.7g starch and disperse in the slurry obtained in step A;

[0071] C: Spray-dry the slurry obtained in step B to obtain amorphous irbesartan micro-composite powder, in which the mass of irbesartan is 59%; the spray-drying conditions are: feed flow rate is 15mL / min, inlet temperature 165°C, compressed air pressure is 0.7MPa.

[0072] D: Weigh 0.1g lactose, 0.1g starch, 0.2g croscarmellose sodium, mix evenly with 2g of the composite powder obtained in step C, add an appropriate amount of 3% PVP ethanol-water solution, granulate, and heat at 55°C Dried to obt...

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Abstract

The invention discloses irbesartan sodium micro composite powder and tablets and a preparation method thereof, in particular to amorphous and crystallization irbesartan sodium micro composite powder and tablets and a preparation method thereof, and belongs to the field of nanometer medicinal preparations. In the method, the amorphous and crystalline irbesartan sodium micro composite powder and corresponding tablets are prepared by combining a liquid-phase precipitation method with a spray drying technology. In the amorphous irbesartan sodium micro composite powder and the tablets thereof, theaverage grain diameter of medicinal granules is between 200 and 900 nanometers, more than 90 percent of amorphous sodium micro composite powder can be dissolved out within 10 minutes, and more than 90 percent of amorphous sodium micro tablets can be dissolved out within 5 minutes. In the crystalline irbesartan sodium micro composite powder and the tablets thereof, the average grain diameter of the medicinal granules is between 500 and 2,000 nanometers, more than 90 percent of crystalline sodium micro composite powder can be dissolved out within 15 minutes, and more than 95 percent of crystalline sodium micro tablets can be dissolved out within 15 minutes.

Description

technical field [0001] The invention relates to an irbesartan micro-composite powder and a tablet and a preparation method thereof, in particular to an amorphous and crystalline irbesartan micro-composite powder and a tablet and a preparation method thereof, belonging to nano-pharmaceutical preparations field. technical background [0002] Irbesartan (irbesartan), chemical name: 2-butyl-3-[4-[2-(1H-tetrazol-5-yl)phenyl]benzyl]-1,3-diazaspiro- [4.4] Non-1-en-4-one, its structural formula is: [0003] [0004] Irbesartan is an angiotensin II receptor antagonist, mainly used in the treatment of essential hypertension, mild to moderate hypertension, and can effectively inhibit the development of hereditary hypertension, prevent postoperative restenosis and Chronic kidney injury. Clinical trials have shown that irbesartan is more effective in treating hypertension than other drugs in the same category, and has less side effects. It is a good first-line antihypertensive drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/4184A61K9/20A61P9/12
Inventor 陈建峰张智亮乐园王洁欣
Owner BEIJING UNIV OF CHEM TECH
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