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A kind of valsartan amlodipine tablet and preparation method thereof

A technology of valsartan amlodipine tablet and amlodipine besylate, applied in the field of medicine, can solve the problems of low bioavailability, low in vitro dissolution rate, influence on drug absorption, etc. The effect of improving bioavailability

Active Publication Date: 2020-05-19
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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  • A kind of valsartan amlodipine tablet and preparation method thereof
  • A kind of valsartan amlodipine tablet and preparation method thereof
  • A kind of valsartan amlodipine tablet and preparation method thereof

Examples

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Effect test

Embodiment 1

[0044] Example 1. Preparation of Valsartan and Amlodipine Tablets

[0045] This example 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 The formula and preparation method of amlodipine sulfonate conversion factor of 0.721)) are as follows:

[0046] Composition of prescription:

[0047]

[0048]

[0049] Control environment humidity <RH25%.

[0050] The preparation method includes the following steps:

[0051] 1) Pretreatment of raw and auxiliary materials: Sieve crospovidone through 40 mesh, and magnesium stearate (additional) through 80 mesh, ready for use; Weigh the prescription amount of valsartan, crospovidone, magnesium stearate ( (Internal addition), amlodipine besylate, colloidal silicon dioxide, and microcrystalline cellulose are mixed in G10 wet mixing granulator for 2 minutes (mixing 3r / s, shearing 3r / s), and then sieving ...

Embodiment 2

[0060] Example 2. Preparation of Valsartan and Amlodipine Tablets

[0061] This example 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 The formula and preparation method of amlodipine sulfonate conversion factor of 0.721)) are as follows:

[0062] Composition of prescription:

[0063]

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

Embodiment 3

[0065] Example 3. Preparation of Valsartan and Amlodipine Tablets

[0066] This example 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 The formula and preparation method of amlodipine sulfonate conversion factor of 0.721)) are as follows:

[0067] Composition of prescription:

[0068]

[0069] The preparation method is basically the same as in 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 and amlodipine tablet and a preparation method thereof, and belongs to the field of medicine. Background technique [0002] Valsartan, chemical name: N-valeryl-N-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-L-valine, CAS number 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 -3,5-pyridinedicarboxylic acid-5-methyl, 3-ethylbenzenesulfonate, CAS number: 111470-99-6, the structural formula is shown in the following formula II: [0005] [0006] Valsartan and amlodipine are the world's number one angiotensin receptor antagonist (ARB) and the world's number one calcium channel blocker (CCB), respectively. 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(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