A kind of dispersible 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 reduced valsartan permeability, so as to improve bioavailability , The effect of improving bioavailability

Active Publication Date: 2011-11-30
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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  • A kind of dispersible tablet of valsartan and preparation method thereof
  • A kind of dispersible tablet of valsartan and preparation method thereof
  • A kind of dispersible 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 it in an appropriate amount of ethanol. Under magnetic stirring, slowly dissolve the ethanol solution of valsartan Add the saturated aqueous solution of hydroxypropyl-β-cyclodextrin, continue to stir at room temperature for 3 hours after all the addition is complete, and remove most of the ethanol by rotary evaporation at 45°C. Put it into a shallow tray and put it in the freezer of the refrigerator. The pre-freezing time is 12 hours and the temperature is -50°C. ...

Embodiment 2-8

[0049] Embodiment 2-8 valsartan dispersible tablet

[0050] For the convenience of narration, the prescription of embodiment 2-8 valsartan dispersible tablet is shown in Table 1. In the table, "Example 2" indicates 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 process of the valsartan dispersible tablet of embodiment 2: take prescription quantity hydroxypropyl-beta-cyclodextrin appropriate amount and dissolve in appropriate amount of water to make saturated aqueous solution, valsartan crosses 120 mesh sieves, dissolves in appropriate amount of ethanol, in 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 was continued at room temperature f...

Embodiment 9

[0061] Embodiment 9 Relative bioavailability research of valsartan dispersible tablet

[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 pharmaceutical preparations, and in particular relates to a dispersible tablet of valsartan and a preparation method thereof. Due to the low bioavailability of oral absorption of valsartan, the individual differences in medication are relatively large, for this reason the invention provides a dispersible tablet of valsartan, which contains valsartan, hydroxypropyl-β-cyclodextrin and Fillers, disintegrants, binders, lubricants. Valsartan is easily soluble in water after inclusion with hydroxypropyl-β-cyclodextrin (HP-β-CD), and improves the stability of the drug, promotes the release of the drug in the body, increases absorption, and improves bioavailability , to reduce inter-individual variability.

Description

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

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/40A61K47/36A61K47/38A61K31/41A61K9/20A61P9/12
Inventor 赵志全张帅王洪臣
Owner LUNAN PHARMA GROUP CORPORATION
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