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Allisartan isoproxil solid dispersion as well as preparation method thereof and preparation containing solid dispersion

A technology of alisartan medoxomil and solid dispersion, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, pill delivery, etc. It can solve the problems of long process time, complicated process of fluidized bed top spraying method, etc. Process complexity and other issues

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

This method is complex in process, and usually requires a relatively long drying time in order to avoid excess organic solvent residues, which is not the best process for preparing solid dispersions
[0007] Chinese patent CN201510254020.6 and Chinese patent CN201510334498.X further optimized the formulation formulation on the basis of patent CN200880001668.0, and provided two improved solid dispersions of alisartan medoxomil, but the technical improvement did not involve changes in the preparation process, so The process of this method still has the defects that the fluidized bed top spraying process is complicated and the process time is relatively long

Method used

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  • Allisartan isoproxil solid dispersion as well as preparation method thereof and preparation containing solid dispersion
  • Allisartan isoproxil solid dispersion as well as preparation method thereof and preparation containing solid dispersion
  • Allisartan isoproxil solid dispersion as well as preparation method thereof and preparation containing solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Embodiment 1 solid dispersion preparation

[0082] type

Dosage

alisartan medoxomil

1

PVP-K30

2

Poloxamer

0.06

Magnesium stearate

0.03

[0083] (1) Mix allisartan medoxomil and auxiliary materials uniformly to make a physical mixture;

[0084] (2) Set the extrusion temperature to 130°C. After the temperature stabilizes, add the physical mixture in step (1) to the hot-melt extruder at a constant speed, and extrude strip-shaped extrudates;

[0085] (3) Cool the strip-shaped extrudate obtained in step (2) and pulverize it through a 60-mesh sieve to obtain a solid dispersion of alisartan medoxomil.

[0086] The XRD spectrogram of gained solid dispersion is compared with the XRD spectrogram of crude drug, pure adjuvant and physical mixture (contrast figure is as follows figure 1 Shown), by the comparison of the XRD powder diffraction pattern, it can be seen that Alisartan medoxomil exists in a nearly amorphous form in ...

Embodiment 2

[0087] Embodiment 2 solid dispersion preparation

[0088] type

Dosage

alisartan medoxomil

1

PVP-K30

1

Poloxamer

0.06

Magnesium stearate

0.03

[0089] (1) Mix allisartan medoxomil and auxiliary materials uniformly to make a physical mixture;

[0090] (2) Set the extrusion temperature to 115°C, and after the temperature stabilizes, add the physical mixture in step (1) into the hot-melt extruder at a constant speed, and extrude strip-shaped extrudates;

[0091] (3) Cool the strip-shaped extrudate obtained in step (2) and pulverize it through a 60-mesh sieve to obtain a solid dispersion of alisartan medoxomil.

[0092] Through detection, it is found that alisartan medoxomil exists in an approximately amorphous form in the solid dispersion, which shows that the melt extrusion process is successful in preparing the alisartan medoxomil solid dispersion.

Embodiment 3

[0093] Embodiment 3 solid dispersion preparation

[0094] type

Dosage

alisartan medoxomil

1

PVP-K30

0.8

polyethylene oxide

0.7

Poloxamer

0.06

talcum powder

0.03

[0095] (1) Alisartan medoxomil and auxiliary materials are mixed evenly to make a physical mixture;

[0096] (2) Set the extrusion temperature to 100°C, and after the temperature stabilizes, add the physical mixture in step (1) into the hot-melt extruder at a constant speed, and extrude strip-shaped extrudates;

[0097] (3) Cool the strip-shaped extrudate obtained in step (2) and pulverize it through a 60-mesh sieve to obtain a solid dispersion of alisartan medoxomil.

[0098] Through detection, it is found that alisartan medoxomil exists in an approximately amorphous form in the solid dispersion, which shows that the melt extrusion process is successful in preparing the alisartan medoxomil solid dispersion.

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Abstract

The invention provides an improved allisartan isoproxil solid dispersion. A hot-melting extrusion preparation process is achieved on the basis of formulation design, and technical advantages of the hot-melting extrusion process which is simple and convenient for preparation, relatively short in consumed time and the like are realized, so that dissolution performance of the solid dispersion is guarantee; and furthermore, an allisartan isoproxil preparation is developed based on the solid dispersion.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid dispersion of alisartan medoxomil, a preparation method thereof and a preparation containing the solid dispersion. Background technique [0002] Hypertension is a clinical syndrome mainly manifested by increased systemic arterial hypertension, and is the most common cardiovascular disease. According to reports, nearly 1 billion people in the world suffer from high blood pressure, and persistent high blood pressure is the main cause of damage to organs such as the heart, brain, kidney, and cardiovascular. [0003] 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 novel angiotensin II receptor antagonist. The compression effect is better than that of similar products (such as losartan). Alisartan medoxomil is m...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61K47/34A61K47/44A61K47/10A61K47/38A61K31/4178A61K9/20A61P9/12
CPCA61K9/2031A61K9/2054A61K9/2059A61K9/2063A61K9/2095A61K31/4178A61K47/32A61K47/34A61K47/38A61K47/44
Inventor 叶冠豪邵靖博侯彦先
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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