Dispersing tablet of valsartan and preparation method thereof

A technology of dispersible tablet and valsartan, which is applied in the field of valsartan dispersible tablet and its preparation, can solve the problems of low valsartan permeability, complexity, and decreased valsartan permeability, etc., and achieve improved bioavailability , The effect of improving bioavailability

Active Publication Date: 2010-06-16
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The permeability of valsartan is very low and also depends on the pH environment. In the gastrointestinal tract, when the pH of the environment increases from acidic to neutral, the permeability of valsartan decreases
Due to the complex biopharmaceutical properties of valsartan, it is challenging to develop dosage forms of valsartan with less individual variation and improved bioavailability

Method used

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  • Dispersing tablet of valsartan and preparation method thereof
  • Dispersing tablet of valsartan and preparation method thereof
  • Dispersing tablet of valsartan and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Valsartan 20g

[0038] Hydroxypropyl-β-cyclodextrin 60g

[0039]Mannitol 20g

[0040] Compressible starch 10g

[0041] Microcrystalline Cellulose 10g

[0042] Croscarmellose Sodium 5g

[0043] 2% polyvinylpyrrolidone aqueous solution 100g

[0044] Magnesium Stearate 1g

[0045] Preparation Process:

[0046] Take the prescribed amount of hydroxypropyl-β-cyclodextrin and dissolve it in an appropriate amount of water to make a saturated aqueous solution. Pass valsartan through a 120-mesh sieve and dissolve in an appropriate amount of ethanol. Under magnetic stirring, slowly dissolve the ethanol solution of valsartan. Add to the saturated aqueous solution of hydroxypropyl-β-cyclodextrin, continue stirring at room temperature for 3 hours after all addition, and remove most of the ethanol by rotary evaporation at 45°C. Put it into a shallow dish, put it in the freezer of the refrigerator, the pre-freezing time is 12h, the temperature is -50℃, when the temperature of th...

Embodiment 2-8

[0049] Embodiment 2-8 Valsartan dispersible tablet

[0050] For the convenience of description, the prescription of embodiment 2-8 valsartan dispersible tablets is shown in Table 1. In the table, "Example 2" means the prescription of Example 2, and "Example 3" - "Example 8" respectively indicate "Prescription of Example 3" - "Prescription of Example 8".

[0051] Table 1 embodiment 2-8 valsartan dispersible tablet prescription

[0052]

[0053] The preparation technology of the valsartan dispersible tablet of embodiment 2: take the recipe quantity hydroxypropyl-β-cyclodextrin and dissolve it in an appropriate amount of water to prepare a saturated aqueous solution, pass through a 120-mesh sieve, dissolve in an appropriate amount of ethanol, and put it in an appropriate amount of ethanol. Under magnetic stirring, the ethanol solution of valsartan was slowly added to the saturated aqueous solution of hydroxypropyl-β-cyclodextrin. After all the addition was completed, stirring...

Embodiment 9

[0061] Example 9 Study on relative bioavailability of valsartan dispersible tablets

[0062] 1 Materials and methods

[0063] 1.1 Drugs and Reagents

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PUM

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Abstract

The invention belongs to the field of medicine preparations, which in particular relates to a dispersing tablet of valsartan and a preparation method thereof. Because the valsartan has lower bioavailability when being orally taken and absorbed and larger difference between application individuals, the invention provides the dispersing tablet of the valsartan, which contains the valsartan, hydroxy propyl-beta-schardinger dextrin, a filling agent, a disintegrating agent, an adhesive and a lubricant. After the valsartan is included by the hydroxy propyl-beta-schardinger dextrin (HP-beta-CD), the valsartan is very easy to dissolve in water, enhances the stability of the medicine, promotes the in-vivo release of the medicine, increases the absorption, enhances the bioavailability and lowers the difference between the application individuals.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a valsartan dispersible tablet and a preparation method thereof. Background technique [0002] ACE inhibitors developed in the 1980s are a class of very effective blood pressure lowering drugs. ACE inhibitors have the following advantages in pharmacology: (1) They are better than general vasodilators. (2) better than calcium antagonists, does not cause water and sodium retention, and does not increase heart rate; (3) better than α-blockers, does not cause orthostatic hypotension; (4) better than the old generation of blood pressure lowering (5) better than nitrates, no drug resistance, no liver first-pass effect; (6) no rebound phenomenon after drug withdrawal. However, ACE inhibitors have insurmountable adverse reactions, such as non-dose-related irritating dry cough (5%-20%), and fatal angioedema of the pharynx, larynx, respiratory tract and lung. Valsartan has ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/41A61K47/36A61K47/38A61P9/12
Inventor 赵志全张帅王洪臣
Owner LUNAN PHARMA GROUP CORPORATION
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