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Valsartan spray-dried nanosuspension and preparation method of valsartan spray-dried nanosuspension

A nano-suspension and valsartan technology, which is applied in the fields of emulsion delivery, drug combination, and cardiovascular system diseases, and achieves the effects of simple preparation method, good fluidity, and reduced dosage of excipients

Inactive Publication Date: 2013-02-13
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The spray-dried nanosuspension with valsartan as the main agent has not been reported so far

Method used

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  • Valsartan spray-dried nanosuspension and preparation method of valsartan spray-dried nanosuspension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh 1 g of the valsartan raw material drug and dissolve in 10 ml of methanol to form solution A. Separately take 500 mg of Poloxamer 407 and dissolve in 500 ml of double-distilled water to form solution B. The solution B was placed under a magnetic stirring condition of 500 rpm, and then the solution A was quickly injected, and the stirring was continued for 10 minutes to obtain a blue-opalescent valsartan nanosuspension. The average particle diameter of this suspension measured by the Malvern laser particle size analyzer is 155nm, see attached figure 1 .

Embodiment 2

[0036] Weigh 1g of valsartan raw material and 1g of poloxamer 407 and add it into 100ml of double-distilled water for high-shear sufficient pre-dispersion, then transfer it to a high-pressure homogenizer for high-pressure homogenization under the condition of 500bar pressure cycle for 15 times to obtain a bluish Chromo-opalescent valsartan nanosuspension. The average particle diameter of this suspension measured by the Malvern laser particle size analyzer is 68nm, see attached figure 2 .

Embodiment 3

[0038] Weigh 1.2g of valsartan crude drug, add 10ml of sodium hydroxide solution (0.6mol / L) to dissolve it, and form solution A. Another 600mg of poloxamer 407 was dissolved in 300ml of hydrochloric acid solution (0.2mol / L) to form solution B. Place B under magnetic stirring, then quickly inject solution A, and continue stirring for ten minutes to obtain a nanosuspension.

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Abstract

The invention discloses a valsartan nanosuspension, a spray-dried power, and a preparation method of the valsartan nanosuspension and the spray-dried power. A valsartan spray-dried nanosuspension and a preparation method of the valsartan spray-dried nanosuspension belong to the field of nano-drug preparations. The valsartan spray-dried nanosuspension consists of 1 part of valsartan, 0.1-1 part of a stabilizing agent and 10-100 parts of a spray-drying protecting agent by mass; the valsartan spray-dried nanosuspension is prepared by an anti-solvent precipitation method and / or a high-pressure homogenizing method and / or an acid-alkali neutralization method in combination with a spray-drying technology. The drug particles in the spray-dried powder are reduced to a nano-grade, and the hydrophilicity, the in vitro dissolution rate and the bioavailability of the valsartan are greatly improved. The powder can be directly processed or be processed together an excipient into tablets, capsules and the like. The valsartan spray-dried nanosuspension has the advantages of simple preparation process, stable product quality and easy implementation of productization.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to valsartan nano-suspension and its spray-dried and solidified powder, and the invention also discloses a preparation method thereof. Background technique [0002] Valsartan (molecular formula: C 24 h 29 N 5 o 3 , Molecular weight: 435.53 Chemical name: (S)-N-(1-oxopentyl-N-[[2,-(1H-5-tetrazolyl)][1,1-biphenyl]-4 -] Methyl) valine) is the first non-peptide orally active angiotensin receptor antagonist, highly selective and highly potent at the receptor level to block angiotensin Binding to receptor AT1, blocking angiotensin mediated physiological effects. It can inhibit vasoconstriction and the release of aldosterone, and produce a good antihypertensive effect. It is suitable for various types of mild and moderate hypertension, especially for secondary hypertension caused by kidney damage. Valsartan does not act on angiotensin-converting enzyme, renin and other r...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/14A61K31/41A61P9/12
Inventor 王思玲姜同英孙长山马秋平
Owner SHENYANG PHARMA UNIVERSITY
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