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Valsartan amlodipine tablet and preparation method thereof

A technology of valsartan amlodipine tablets and amlodipine besylate, which is applied in the field of medicine, can solve the problems of low in vitro dissolution rate, influence of drug absorption, and low bioavailability, so as to increase residence time and improve bioavailability Degree, increase the effect of solubility

Active Publication Date: 2018-11-13
BEIJING BAIAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Valsartan is almost insoluble in water, and amlodipine besylate is slightly soluble in water, which has the disadvantages of slow dissolution rate, low in vitro dissolution rate, and low bioavailability, especially when the plasma concentration of valsartan reaches its peak within 3 hours. The average absolute bioavailability of valsartan is 23±7%, which has a great influence on the absorption of the drug

Method used

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  • Valsartan amlodipine tablet and preparation method thereof
  • Valsartan amlodipine tablet and preparation method thereof
  • Valsartan amlodipine tablet and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1, preparation valsartan amlodipine sheet

[0045] The present embodiment provides the preparation of 100,000 valsartan and amlodipine tablets (each containing valsartan 80mg, amlodipine 5mg, 6.935mg amlodipine besylate is equivalent to 5mg amlodipine (amlodipine and benzene Amlodipine sulfonate conversion factor is 0.721)) prescription and preparation method, specifically as follows:

[0046] Prescription composition:

[0047]

[0048]

[0049] Control the ambient humidity <RH25%.

[0050] The preparation method comprises the following steps:

[0051] 1) Pretreatment of raw and auxiliary materials: sieve crospovidone 40 mesh, magnesium stearate (additional) sieve 80 mesh, and set aside; take the prescription amount of valsartan, crospovidone, magnesium stearate ( internally added), amlodipine besylate, colloidal silicon dioxide, and microcrystalline cellulose were mixed in a G10 wet mixing granulator for 2 minutes (stirring 3r / s, shearing 3r / s), and t...

Embodiment 2

[0060] Embodiment 2, preparation valsartan amlodipine sheet

[0061] The present embodiment provides the preparation of 100,000 valsartan and amlodipine tablets (each containing valsartan 80mg, amlodipine 5mg, 6.935mg amlodipine besylate is equivalent to 5mg amlodipine (amlodipine and benzene Amlodipine sulfonate conversion factor is 0.721)) prescription and preparation method, specifically as follows:

[0062] Prescription composition:

[0063]

[0064] The preparation method is basically the same as Example 1 of the present invention.

Embodiment 3

[0065] Embodiment 3, preparation valsartan amlodipine sheet

[0066] The present embodiment provides the preparation of 100,000 valsartan and amlodipine tablets (each containing valsartan 80mg, amlodipine 5mg, 6.935mg amlodipine besylate is equivalent to 5mg amlodipine (amlodipine and benzene Amlodipine sulfonate conversion factor is 0.721)) prescription and preparation method, specifically as follows:

[0067] Prescription composition:

[0068]

[0069] The preparation method is basically the same as Example 1 of the present invention.

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Abstract

The invention discloses a valsartan amlodipine tablet and a preparation method thereof. The valsartan amlodipine tablet comprises the following substances as raw materials in parts by weight: 80 partsof valsartan, 5 parts of amlodipine besylate (counted by amlodipine), 50-100 parts of microcrystalline cellulose PH102, 8-30 parts of crospovidone XL, 0.1-10 parts of poloxamer 188, 1-5 parts of magnesium stearate, 1- 3 parts of copovidone S630, 1-5 parts of colloidal silicon dioxide and 4-10 parts of a film coating premix (gastric). Through addition of the poloxamer 188 into a medicinal auxiliary material of the valsartan amlodipine tablet, the solubility of the valsartan is improved and the retention time thereof in the gastrointestinal tract is prolonged, so that absorption is improved, and thus the bioavailability of the valsartan amlodipine tablet is improved; through addition of the copovidone S630 into a coating solution, the solubility and the bioavailability of the valsartan canbe also improved, and thus the bioavailability of the valsartan amlodipine tablet is further improved. The preparation method of the valsartan amlodipine tablet is stable, and is suitable for large-scale preparation.

Description

technical field [0001] The invention relates to a valsartan amlodipine tablet and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Valsartan, chemical name: N-pentanoyl-N-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-L-valine, CAS No. 137862 -53-4, the structural formula is shown in the following formula Ⅰ: [0003] [0004] Amlodipine besylate, chemical name: (±)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl -5-methyl-3,5-pyridinedicarboxylate, 3-ethyl benzenesulfonate, CAS number: 111470-99-6, the structural formula is shown in Formula II below: [0005] [0006] Valsartan and amlodipine are respectively the world's number one angiotensin receptor blocker (ARB) and the world's number one calcium channel blocker (CCB). Valsartan and Amlodipine Tablets are the world's first ARB / CCB compound preparation developed by Novartis Pharmaceuticals Co., Ltd. This product is a film-coated tablet, which is whit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K47/32A61K47/10A61K31/41A61K31/4422A61P9/12
CPCA61K9/2031A61K9/284A61K31/41A61K31/4422A61P9/12A61K2300/00
Inventor 利虔马景梅林均富李惠苑晨勇
Owner BEIJING BAIAO PHARMA
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