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Valsartan/hydrochlorothiazide tablet and preparation method thereof

A technology for chlorothiazide tablets and hydrochlorothiazide is applied in the field of medicine and can solve the problems of increased degradation products, low in vitro dissolution rate, influence on drug absorption and the like

Active Publication Date: 2018-09-25
BEIJING BAIAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, since both valsartan and hydrochlorothiazide are insoluble in water, they have the disadvantages of slow dissolution rate, low dissolution rate in vitro, and low bioavailability, which have a great impact on the absorption of drugs
In addition, valsartan is sensitive to water, absorbs moisture, increases moisture, increases degradation products, and has poor chemical stability. Valsartan / hydrochlorothiazide tablets have very important practical significance

Method used

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  • Valsartan/hydrochlorothiazide tablet and preparation method thereof
  • Valsartan/hydrochlorothiazide tablet and preparation method thereof
  • Valsartan/hydrochlorothiazide tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1, preparation valsartan / hydrochlorothiazide sheet

[0047] The present embodiment provides the prescription and preparation method for preparing 1000 valsartan / hydrochlorothiazide tablets, as follows:

[0048] Prescription composition:

[0049]

[0050]

[0051] Control the ambient humidity RH≤40%.

[0052] The preparation method comprises the following steps:

[0053] 1) Grinding hydrochlorothiazide to obtain hydrochlorothiazide powder (particle size range D90≤130 μm), passing crospovidone XL through a 40-mesh sieve, and magnesium stearate (additional) passing through a 80-mesh sieve;

[0054] 2) Weigh valsartan, crospovidone XL, copovidone S630 (internal addition), magnesium stearate (internal addition), hydrochlorothiazide, colloidal silicon dioxide, microcrystalline cellulose PH102 and mix in wet method Mix in the granulator for 2 minutes (stirring 3r / s, shearing 3r / s) and pass through a 40-mesh sieve to disperse;

[0055] 3) Pre-mixing: put the ...

Embodiment 2

[0062] Embodiment 2, preparation valsartan / hydrochlorothiazide sheet

[0063] The present embodiment provides the prescription and preparation method for preparing 1000 valsartan / hydrochlorothiazide tablets, as follows:

[0064] Prescription composition:

[0065]

[0066] The preparation method is basically the same as in Example 1.

Embodiment 3

[0067] Embodiment 3, preparation valsartan / hydrochlorothiazide sheet

[0068] The present embodiment provides the prescription and preparation method for preparing 1000 valsartan / hydrochlorothiazide tablets, as follows:

[0069] Prescription composition:

[0070]

[0071]

[0072] The preparation method is basically the same as in Example 1.

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Abstract

The invention provides a valsartan / hydrochlorothiazide tablet and a preparation method thereof. The valsartan / hydrochlorothiazide tablet is prepared from the following raw material substances in partsby mass: 80 parts of valsartan, 12.5 parts of hydrochlorothiazide, 20 to 28 parts of microcrystalline cellulose PH102, 3 to 10 parts of copovidone S630, 1.0 to 2.0 parts of colloidal silicon dioxide,18 to 22 parts of polyvinylpolypyrrolidone XL, 3.50 to 5.00 parts of magnesium stearate and 3 to 7.5 parts of film coating premixing agents (gastric dissolution type), wherein the mass part ratio ofmicrocrystalline cellulose to copovidone S630 is (3 to 4):1. The copovidone S630 is used for replacing partial microcrystalline cellulose PH102; the dissolution rate of valsartan and the hydrochlorothiazide is increased; in addition, copovidone S630 is added into the coating solution, so that the water sensitivity of the valsartan / hydrochlorothiazide tablet is improved, so that the chemical stability of valsartan is enhanced.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a valsartan hydrochlorothiazide tablet and a preparation method thereof. Background technique [0002] Valsartan (Valsartan), chemical name: N-pentanoyl-N-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-L-valine, American Chemical Abstracts registration number CAS: 137862-53-4, its structural formula is as follows: [0003] [0004] Hydrochlorothiazide, chemical name: 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide-1,1-dioxide, American Chemical Abstracts Registration No. CAS: 58-93-5, its structural formula is as follows: [0005] [0006] Valsartan / hydrochlorothiazide compound preparation is a safe and orally effective antihypertensive drug widely used in clinic. Valsartan inhibits the activity of angiotensin II (AII) by specifically antagonizing angiotensin II receptor type I (AT1), thereby reducing blood pressure. Hydrochlorothiazide is a thiazide diure...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K47/32A61K47/38A61K31/549A61K31/41A61P9/12
CPCA61K9/2027A61K9/2054A61K9/284A61K9/2866A61K31/41A61K31/549A61P9/12A61K2300/00
Inventor 李志东利虔林均富马景梅苑晨勇
Owner BEIJING BAIAO PHARMA
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