Allisartan isoproxil pharmaceutical composition, preparation containing pharmaceutical composition and preparation method of pharmaceutical composition

A technology of alisartan medoxomil and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of high tablet weight, low load of alisartan medoxomil preparations, and insufficient support for industrial production, and achieve low production costs and strong process controllability , the effect of simple operation

Inactive Publication Date: 2017-12-08
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent Example 8 discloses a preparation method of alisartan medoxomil nanosuspension, which contains povidone and sodium dodecyl sulfate (SDS), but based on the properties of alisartan medoxomil, the effervescent There are certain quality fluctuations in the preparation of nanoparticles by this method, which makes the process stable enough to support industrial production; in addition, this method uses more pharmaceutical excipients (povidone, SDS, etc.), and has not achieved the optimal combination of raw mater

Method used

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  • Allisartan isoproxil pharmaceutical composition, preparation containing pharmaceutical composition and preparation method of pharmaceutical composition
  • Allisartan isoproxil pharmaceutical composition, preparation containing pharmaceutical composition and preparation method of pharmaceutical composition
  • Allisartan isoproxil pharmaceutical composition, preparation containing pharmaceutical composition and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

0.05

[0068] (1) Dissolve the prescription amount HPMC E5 in water to prepare a 3mg / mL aqueous solution;

[0069] (2) add recipe quantity alisartan medoxomil to step (1) gained aqueous solution, airtight container, reduce container internal pressure to 20Kpa, stir and make it be suspended in aqueous phase and return to normal pressure;

[0070] (3) Add 0.1mm ball milling beads to the suspension obtained in step (2), and grind alisartan medoxomil to an average particle size value of 272.1nm (PDI=0.062), and the micrograph of the resulting nanosuspension is as follows figure 1 As shown, the particle size distribution diagram is shown in figure 2 shown;

[0071] (4) Add half of the volume of the suspension to the suspension obtained in step (3) and the protective agent of the prescribed amount to obtain the alisartan medoxomil pharmaceutical composition (suspension);

[0072] (5) Spray drying the alisartan medoxomil pharmaceutical composition (suspension) obtained in st...

Embodiment 2

0.02

[0076] (1) Dissolve the prescription amount HPMC E50 in water to prepare an aqueous solution of 1.5 mg / mL;

[0077] (2) Add prescription amount of alisartan medoxomil to step (1) gained aqueous solution, airtight container, reduce container internal pressure to 20Kpa, stir and recover normal pressure after making it be suspended in aqueous phase;

[0078] (3) Add 1.5 mm ball milling beads to the suspension obtained in step (2), and replace it with 1.0 mm ball milling beads after grinding for 45 minutes, and grind alisartan medoxomil to an average particle size of 515.1 nm (PDI=0.237);

[0079] (4) Add half of the volume of the suspension to the suspension obtained in step (3) and the protective agent of the prescribed amount to obtain the alisartan medoxomil pharmaceutical composition (suspension);

[0080] (5) Spray drying the alisartan medoxomil pharmaceutical composition (suspension) obtained in step (4) to obtain the alisartan medoxomil pharmaceutical composit...

Embodiment 3

0.05

[0084] (1) Dissolve the prescription amount of PVP K30 in water to prepare a 0.8 mg / mL aqueous solution;

[0085] (2) Add prescription amount of alisartan medoxomil to step (1) gained aqueous solution, airtight container, reduce container internal pressure to 20Kpa, stir and recover normal pressure after making it be suspended in aqueous phase;

[0086] (3) Add 1.0 mm ball milling beads to the suspension obtained in step (2), and replace it with 0.2 mm ball milling beads after grinding for 45 minutes, and grind alisartan medoxomil to an average particle size of 365.4 nm (PDI=0.222);

[0087] (4) Add half of the volume of the suspension to the suspension obtained in step (3) and the protective agent of the prescribed amount to obtain the alisartan medoxomil pharmaceutical composition (suspension);

[0088] (5) Spray drying the alisartan medoxomil pharmaceutical composition (suspension) obtained in step (4) to obtain the alisartan medoxomil pharmaceutical compositio...

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Abstract

The invention provides an allisartan isoproxil pharmaceutical composition. Through the stabilizing and protecting effects of a prescription, allisartan isoproxil can be conveniently prepared into nano-scale particles through a milling process, the nano-scale particles are stably dispersed in a pharmaceutical composition, and allisartan isoproxil exists in the form of the stable nanoparticles in the follow-up process. The invention further provides an allisartan isoproxil preparation which has the characteristics of high loading capacity, high stability and the like.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an alisartan medoxomil pharmaceutical composition, a preparation containing the pharmaceutical composition and a preparation method thereof. Background technique [0002] Alisartan medoxomil (CAS: 947331-05-7), the chemical name is 2-butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl- Methyl]-imidazole-5-carboxylic acid, 1-[(isopropoxy)-carbonyloxy]-methyl ester, is a new type of angiotensin II receptor blocker, which is hydrolyzed by esterase after oral administration Losartan 5-carboxylate (EXP3174), exerts antihypertensive effect. The results of preclinical studies and phase I, II, and III clinical studies all show that it has a good antihypertensive effect, and has high safety, good tolerance and compliance. However, due to the poor water solubility of alisartan medoxomil, the prior art mostly adopts the solution of solid dispersion to realize its clinical use....

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4178A61K47/38A61K47/10A61K47/32A61P9/12
CPCA61K9/146A61K31/4178
Inventor 叶冠豪侯彦先邵靖博
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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