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Allisartan isoproxil solid dispersion and medicine composition containing allisartan isoproxil solid dispersion

A technology of allisartan medoxomil and solid dispersion, which is applied in the field of pharmaceutical preparations and can solve the problems of decreased dissolution performance, aging and the like

Active Publication Date: 2016-01-13
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, affected by factors such as prescriptions or storage conditions, the active ingredients in the solid dispersion will inevitably undergo rapid or slow aggregation and crystallization during storage, that is, the "aging phenomenon" of the solid dispersion, manifested as Preparation of preparations with qualified initial dissolution performance, the dissolution performance will decrease significantly after storage for a period of time, and the aging phenomenon will be particularly obvious when the amount of solid dispersion carrier is reduced

Method used

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  • Allisartan isoproxil solid dispersion and medicine composition containing allisartan isoproxil solid dispersion
  • Allisartan isoproxil solid dispersion and medicine composition containing allisartan isoproxil solid dispersion
  • Allisartan isoproxil solid dispersion and medicine composition containing allisartan isoproxil solid dispersion

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] prescription:

[0056]

[0057] preparation:

[0058] 1. Preparation of solid dispersion

[0059] Dissolve the drug and povidone K29 / 32 in an appropriate amount of dichloromethane-ethanol mixed solution, then add the aqueous solution of sodium lauryl sulfate and egg yolk lecithin, mix well, and set aside. Add crospovidone (I) into the fluidized bed, spray the prepared solution into the fluidized bed with a spray gun to granulate in the top spray mode, and dry to obtain the solid dispersion of alisartan medoxomil; further XRD experiment detection found that Alisartan The active ingredient of tannyl ester is highly dispersed in the solid dispersion, which proves that the preparation effect of the solid dispersion is as expected.

[0060] 2. Preparation of pharmaceutical composition

[0061] The solid dispersion is uniformly mixed with additional auxiliary materials, compressed into tablets to obtain plain tablets, and film-coated to obtain the alisartan medoxomil ph...

Embodiment 2

[0063] prescription:

[0064]

[0065] preparation:

[0066] 1. Preparation of solid dispersion

[0067] Dissolve the drug and povidone K29 / 32 in an appropriate amount of dichloromethane-ethanol mixed solution, then add an aqueous solution of sodium lauryl sulfate, mix well, and set aside. Add crospovidone (I) into the fluidized bed, spray the prepared solution into the fluidized bed with a spray gun to granulate in the top spray mode, and dry to obtain the solid dispersion of alisartan medoxomil; further XRD experiment detection found that Alisartan The active ingredient of tannyl ester is highly dispersed in the solid dispersion, which proves that the preparation effect of the solid dispersion is as expected.

[0068] 2. Preparation of pharmaceutical composition

[0069] The solid dispersion is uniformly mixed with additional auxiliary materials, compressed into tablets to obtain plain tablets, and film-coated to obtain the alisartan medoxomil pharmaceutical compositio...

Embodiment 3

[0071] prescription:

[0072]

[0073] preparation:

[0074] 1. Preparation of solid dispersion

[0075] Dissolve the drug and povidone K29 / 32 in an appropriate amount of dichloromethane-ethanol mixed solution, then add egg yolk lecithin, dissolve and mix evenly, and set aside. Microcrystalline cellulose and crospovidone (I) are added in the fluidized bed, and the prepared solution is sprayed into the fluidized bed with a spray gun to granulate in the top spray mode, and dried to obtain alisartan medoxomil solid dispersion; further XRD Experimental testing 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 expectations.

[0076] 2. Preparation of pharmaceutical composition

[0077] The solid dispersion is uniformly mixed with additional auxiliary materials, compressed into tablets to obtain plain tablets, and film-coated to obtain the alisartan medo...

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PUM

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Abstract

The invention provides a high-load allisartan isoproxil solid dispersion. On the premise of ensuring the preparation stability and the dissolution rate, surfactants are added; the content of active ingredients in the solid dispersion is effectively improved; and the medicine load capability of the solid dispersion is higher than that in the prior art. A medicine composition containing the allisartan isoproxil solid dispersion has the characteristics of good dissolution performance, high stability and the like, and conforms to the clinical medication requirements, and the medication compliance of a patient is improved.

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), chemical name: 2-butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl -Methyl]-imidazole-5-carboxylic acid, 1-[(isopropoxy)-carbonyloxy]-methyl ester, trade name: Xinlitan, 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 clinica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/4178A61K47/20A61K47/24A61K47/26A61K47/22A61K47/44A61K47/34A61K47/32A61K47/38A61P9/12
CPCA61K47/32A61K47/34A61K47/38A61K9/14A61K31/4178A61P43/00A61P9/12A61K9/146A61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2031A61K9/2054A61K9/2059A61K9/28
Inventor 叶冠豪卜水
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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