Allisartan isoproxil solid dispersion and pharmaceutical composition

A technology of solid dispersion and allisartan medoxomil, which is applied in the directions of drug combinations, sugar-coated pills, pharmaceutical formulations, etc., can solve the problem of low drug loading in solid dispersions, failure to achieve clinical administration weight and antihypertensive effect, and poor patient compliance. And other issues

Inactive Publication Date: 2015-11-25
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are flaws in the preparation scheme in the prior art, which is manifested in that the drug loading of the solid dispersion is not high, so that the content of the active ingredient in the pharmaceutical composition is low, and the corresponding unit preparation weight is relatively large, so that during the administration process The patient's compliance is poor, and the clinical dosage weight and antihypertensive effect have not been optimized

Method used

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  • Allisartan isoproxil solid dispersion and pharmaceutical composition
  • Allisartan isoproxil solid dispersion and pharmaceutical composition
  • Allisartan isoproxil solid dispersion and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] prescription:

[0044]

[0045] preparation:

[0046] 1. Preparation of solid dispersion

[0047] Dissolve the medicine and Povidone K29 / 32 in an appropriate amount of dichloromethane-ethanol mixed solution, add cross-linked Povidone (I) in the fluidized bed, and spray the prepared solution into the fluidized bed with a spray gun. In-bed granulation and drying to obtain a solid dispersion of allisartan medoxomil; further XRD experiments found that the active ingredient of allisartan medoxomil was highly dispersed in the solid dispersion, proving that the preparation effect of the solid dispersion reached expectations.

[0048] 2. Preparation of pharmaceutical composition

[0049] The solid dispersion is uniformly mixed with other materials, pressed into tablets to obtain plain tablets, and film-coated to obtain the alisartan medoxomil pharmaceutical composition.

Embodiment 2

[0051] prescription:

[0052]

[0053] preparation:

[0054] 1. Preparation of solid dispersion

[0055] Dissolve the medicine and Povidone K29 / 32 in an appropriate amount of dichloromethane-ethanol mixed solution, add cross-linked Povidone (I) in the fluidized bed, and spray the prepared solution into the fluidized bed with a spray gun. In-bed granulation and drying to obtain a solid dispersion of allisartan medoxomil; further XRD experiments found that the active ingredient of allisartan medoxomil was highly dispersed in the solid dispersion, proving that the preparation effect of the solid dispersion reached expectations.

[0056] 2. Preparation of pharmaceutical composition

[0057] The solid dispersion is uniformly mixed with other materials, pressed into tablets to obtain plain tablets, and film-coated to obtain the alisartan medoxomil pharmaceutical composition.

Embodiment 3

[0059] prescription:

[0060]

[0061]

[0062] preparation:

[0063] 1. Preparation of solid dispersion

[0064] Medicine and povidone K29 / 32 are dissolved in an appropriate amount of dichloromethane-ethanol mixed solution, microcrystalline cellulose and crosslinked povidone (I) are added in the fluidized bed, and the prepared solution is top-sprayed with a spray gun The method was sprayed into a fluidized bed to granulate, and dried to obtain a solid dispersion of alisartan medoxomil; further XRD experiments found that the active ingredient of alisartan medoxomil was highly dispersed in the solid dispersion, which proved that the preparation effect of the solid dispersion reached the expectation.

[0065] 2. Preparation of pharmaceutical composition

[0066] The solid dispersion is uniformly mixed with other materials, pressed into tablets to obtain plain tablets, and film-coated to obtain the alisartan medoxomil pharmaceutical composition.

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PUM

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Abstract

An allisartan isoproxil solid dispersion with high drug load and good stability. A pharmaceutical composition comprising the solid dispersion is also disclosed. The pharmaceutical composition containing allisartan isoproxil has the advantages of good stability, good solubility, good patient compliance, etc.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to a solid dispersion of alisartan medoxomil and a pharmaceutical composition containing the solid dispersion. 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 antagonist. Chinese patent CN200680000397.8 discloses the structural formula of the allisartan medoxomil compound. The allisartan medoxomil is less toxic and has a better antihypertensive effect than similar products (such as losartan). Its antihypertensive effect. Alisartan medoxomil is an ester derivative of EXP3174, its solubility in water is small, and the preparations obtained by conventional preparation methods are difficult to meet the needs of clinical medication. [...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4178A61K47/32A61K47/38A61K47/34A61P9/12A61P9/00A61P9/10A61P13/12A61P27/02
CPCA61K9/14A61K9/146A61K9/19A61K9/2013A61K9/2018A61K9/2027A61K9/2054A61K9/2077A61K9/284A61K31/4178A61K47/32A61K47/34A61K47/38A61P9/00A61P9/10A61P9/12A61P13/12A61P27/02
Inventor 叶冠豪卜水
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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