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Azilsartan solid dispersion as well as preparation method and medicament composition thereof

A technology of solid dispersion and azilsartan, which is applied in the directions of pharmaceutical combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of low solubility, low bioavailability, and preparation technology Complexity and other problems, to achieve the effect of simple steps, increased solubility and dissolution rate, and avoidance of residual solvents

Inactive Publication Date: 2015-06-24
HAINAN HAILI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The preparation method of azilsartan preparation in the prior art still has defects such as complex preparation process, low solubility, low dissolution rate and low bioavailability of the preparation, and further research and development is necessary to solve the above problems

Method used

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  • Azilsartan solid dispersion as well as preparation method and medicament composition thereof
  • Azilsartan solid dispersion as well as preparation method and medicament composition thereof
  • Azilsartan solid dispersion as well as preparation method and medicament composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of embodiment 1 solid dispersion

[0042] Azilsartan raw material 100g

[0043] Hydroxypropyl Methyl Cellulose E3LV 20g

[0044] Polysorbate 80 15g

[0045] Preparation method: (1) Weigh 20g of hydroxypropyl methylcellulose E3LV, dissolve in 1000ml of purified water; then add 15g of polysorbate 80, stir to dissolve; add 100g of azilsartan raw material, put in a basket grinder Medium grinding for 1 hour to azilsartan particle size D 90 (2) The air inlet temperature is set at 80-110°C, the resulting suspension is spray-dried in a fluidized bed, and then crushed through a 120-mesh sieve to obtain surface-modified Azithar Tan solid dispersion.

Embodiment 2

[0046] The preparation of embodiment 2 solid dispersion

[0047] Azilsartan raw material 100g

[0048] Hydroxypropyl Methyl Cellulose E50LV 20g

[0049] Sucrose Stearate 10g

[0050] Preparation method: (1) Weigh 20g of hydroxypropyl methylcellulose E50LV, dissolve it in 2000ml of purified water; then add 10g of sucrose stearate with an HLB of 8.0, stir and dissolve; add 100g of azilsartan raw material, Grind in a basket mill for 1 hour to azilsartan particle size D 90 (2) The air inlet temperature is set at 80-110°C, the resulting suspension is spray-dried in a fluidized bed, and then crushed to 120 mesh to obtain surface-modified azilsartan Solid dispersion.

Embodiment 3

[0051] The preparation of embodiment 3 solid dispersion

[0052]

[0053] Preparation method: (1) Weigh 30g of hydroxypropyl methylcellulose E50LV and dissolve it in 4000ml of purified water; then add 20g of sucrose stearate with an HLB of 8.0 and 200g of lactose, and stir to dissolve; add 100g of Azithar Azilsartan raw material, placed in a basket mill and ground for 2 hours to azilsartan particle size D 90 50 μm to obtain a homogeneous suspension. (2) The air inlet temperature is set at 80-110° C., the resulting suspension is spray-dried in a fluidized bed, and then pulverized through 120 mesh to obtain a surface-modified azilsartan solid dispersion.

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Abstract

The invention relates to an azilsartan solid dispersion as well as a preparation method and a medicament composition thereof. The preparation method of the azilsartan solid dispersion comprises the following steps: adding water into an azilsartan raw material and a surfactant, and grinding to obtain a suspension; and drying the suspension, and then crushing to obtain the azilsartan solid dispersion. The preparation method can increase the permeability and dissolution property of the azilsartan raw material to ensure that the solubility and dissolution rate of the azilsartan raw material are obviously increased, thereby improving the bioavailability of the azilsartan raw material; and moreover, the water replaces an organic solvent to ensure that the safety of the preparation process and the product is high. The solid dispersion obtained by the preparation method provided by the invention is high in solubility, and the medicament composition containing the solid dispersion is high in dissolution rate and good in stability.

Description

technical field [0001] The invention relates to a preparation containing insoluble drugs, a preparation method thereof, and a pharmaceutical composition, in particular to an azilsartan solid dispersion, a preparation method thereof, and a pharmaceutical composition. Background technique [0002] Azilsartan (English name Azilsartan), chemical name: 2-ethoxy-1-[[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazole-3 -yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid, the molecular formula is C 25 h 20 N 4 o 5 , Molecular weight: 456.45, this product is white or off-white crystalline powder, odorless. It is easily soluble in N,N-dimethylacetamide, slightly soluble in methanol, hardly soluble in ethanol (99.5%), almost insoluble in water. Azilsartan (Azilsartan, specification 20 mg, 40 mg), an angiotensin II receptor antagonist drug developed by Takeda Corporation of Japan, was approved for marketing in Japan in January 2012 for the treatment of hypertension. [0003] Azilsart...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K9/48A61K31/4245A61K47/32A61K47/38A61K47/26A61K47/34A61K47/44A61K47/20A61K47/24A61P9/12
Inventor 宋力余国新张晏蔡家昌
Owner HAINAN HAILI PHARMACEUTICAL CO LTD
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