Oral tablet containing candesartan cilexetil and benzene sulfonate amlodipine and preparation method for oral tablet

A technology of amlodipine besylate and candesartan cilexetil, which is applied in the field of medicine, can solve problems such as one-sided unqualified, reduced dissolution characteristics of candesartan, and reduced disintegration of solid preparations, so as to achieve rapid dissolution and avoid Sticking phenomenon, avoiding disintegration and reducing the effect

Active Publication Date: 2012-09-19
ZHEJIANG HUAHAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main disadvantage of this technical solution is that since the formulation uses an oily substance with a low melting point such as polyethylene glycol as a stabilizer, the polyethylene glycol is likely to melt due to the pressure and heat of the material during the tableting process, resulting in stickiness. phenomenon, one-sided unqualified and other quality problems are prone to occur, and when adding low-melting point oily substances to improve the stability of the solid dosage form, the disintegration degree of the solid dosage form will be reduced, and the dissolution characteristics of candesartan from the solid dosage form will be significantly reduced
[0009] In addition, amlodipine besylate is a poorly soluble drug, and the amlodipine unilateral preparations currently on the market are all rapid release, that is, the release rate is greater than 85% in 15 minutes.

Method used

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  • Oral tablet containing candesartan cilexetil and benzene sulfonate amlodipine and preparation method for oral tablet
  • Oral tablet containing candesartan cilexetil and benzene sulfonate amlodipine and preparation method for oral tablet
  • Oral tablet containing candesartan cilexetil and benzene sulfonate amlodipine and preparation method for oral tablet

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Experimental program
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Effect test

Embodiment 1

[0045]

[0046]Three prescriptions used copovidone at different ratios, among which: the ratio of copovidone used in prescription 1 was 2.0%; the ratio of copovidone used in prescription 2 was 3.0%; the ratio of copovidone used in prescription 3 was 4.0% %, the proportion of copovidone used in prescription 4 was 6.0%.

[0047] The particle size of candesartan cilexetil is D (V，0.9) =41μm, the particle size of amlodipine besylate is D (V，0.9) = 53 μm, absolute ethanol is removed during production.

[0048] The preparation method is as follows: dissolve the prescription amount of glycerin in an appropriate amount of absolute ethanol to make an adhesive for use; mix candesartan cilexetil, amlodipine besylate and other granulation auxiliary materials in a granulation pot to obtain the mixture A: Add the ethanol solution binder of glycerin into the granulation pot and granulate together with mixture A to obtain wet granules, dry the wet granules to obtain dry granules; mix dry...

Embodiment 2

[0061] The particle size of candesartan cilexetil is D (V，0.9) =22μm, the particle size of amlodipine besylate is D (V，0.9) =93 μm, absolute ethanol is removed during production.

[0062] The preparation method is as follows: dissolve the prescription amount of glycerin in an appropriate amount of absolute ethanol to make an adhesive for use; mix candesartan cilexetil, amlodipine besylate and other granulation auxiliary materials in a granulation pot to obtain the mixture A: Add the ethanol solution binder of glycerin into the granulation pot and granulate together with mixture A to obtain wet granules, dry the wet granules to obtain dry granules; mix dry granules with lubricant to obtain mixed granules; use rotary tablet press for mixed granules Carry out tabletting, tablet weight 130mg, make 5000 tablets.

[0063] According to dissolution assay method (Chinese Pharmacopoeia 2010 edition appendix XC second method), use the 900ml pH6.5 phosphate buffer that adds 0.35%...

Embodiment 3

[0068] The particle size of candesartan cilexetil is D (V，0.9) =57μm, the particle size of amlodipine besylate is D (V，0.9) = 33 μm, absolute ethanol is removed during production.

[0069] The preparation method is as follows: dissolve the prescription amount of glycerin in an appropriate amount of absolute ethanol to make an adhesive for use; mix candesartan cilexetil, amlodipine besylate and other granulation auxiliary materials in a granulation pot to obtain the mixture A: Add the ethanol solution binder of glycerin into the granulation pot and granulate together with mixture A to obtain wet granules, dry the wet granules to obtain dry granules; mix dry granules with lubricant to obtain mixed granules; use rotary tablet press for mixed granules Carry out tabletting, tablet weight 130mg, make 5000 tablets.

[0070] According to dissolution assay method (Chinese Pharmacopoeia 2010 edition appendix XC second method), use the 900ml pH6.5 phosphate buffer that adds 0.35...

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Abstract

The invention discloses an oral tablet containing candesartan cilexetil and benzene sulfonate amlodipine. The oral tablet consists of benzene sulfonate amlodipine, candesartan cilexetil and medicinal auxiliary materials, wherein the medicinal auxiliary materials contain a stabilizing agent and other auxiliary materials such as one or more of a filling agent, a binding agent and a lubricating agent. The tablet containing candesartan cilexetil and benzene sulfonate amlodipine is attractive in surface and stable in quality. The invention also provides a preparation method for the oral tablet; and the process is simple, low in cost and suitable for commercial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a candesartan cilexetil / amlodipine besylate oral tablet. Background technique [0002] Candesartan cilexetil is a novel angiotensin II receptor antagonist that has attracted widespread attention in the antihypertensive market. This type of drug selectively blocks the function of AngII in the circulation and tissue, and has a significant antihypertensive effect and a long-lasting effect. Its compound structure and synthesis method have been disclosed in EP 0459136, and its structural formula is as follows: [0003] [0004] Amlodipine besylate is a new type of calcium antagonist, which is mainly used clinically for the treatment of hypertension and angina pectoris. Has the following structural formula: [0005] [0006] Amlodipine besylate has shown a better synergistic effect in the combined treatment of hypertension with candesartan cilexetil. [0007] Can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K9/20A61K47/36A61P9/10A61P9/12A61K31/4184
Inventor 施祥杰陈浩胡李斌徐谷花彭俊清李巧霞
Owner ZHEJIANG HUAHAI PHARMA CO LTD
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