Amlodipine and candesartan pharmaceutical composition and preparation method thereof

A technology of candesartan cilexetil and amlodipine, applied in the field of medicine, can solve the problem of slow onset of action of amlodipine besylate, limited synergy, accumulation, limited complementary effect, slow onset of action of amlodipine besylate, etc. problems, to achieve the effect of improving bioavailability, good disintegration performance and dissolution, and increasing specific surface area

Active Publication Date: 2012-02-08
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In the prior art, amlodipine and amlodipine salts (such as amlodipine maleate, amlodipine besylate, amlodipine mesylate, etc.) are almost insoluble in water and are slowly absorbed in the human body. The peak blood drug concentration is reached within 6-12 hours, and the overall level of blood drug concentration is low, especially the initial blood drug concentration after administration is very low. Reach the peak concentration of the blood concentration, the drug has a rapid onset of action, and the time difference between the two drugs when they reach the peak blood concentration after simultaneous administration is far away, and the synergistic, cumulative and complementary effects are very limited
For example, Chinese patent CN101371834A discloses a pharmaceutical composition containing amlodipine besylate and candesartan cilexetil, the weight ratio of amlodipine besylate and candesartan cilexetil is 1: 1-6, the The pharmaceutical composition has a certain synergistic effect in lowering blood pressure and dilating blood vessels, but the onset of amlodipine besylate is slow, and the synergistic effect of the pharmaceutical composition of amlodipine besylate and candesartan cilexetil is

Method used

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  • Amlodipine and candesartan pharmaceutical composition and preparation method thereof
  • Amlodipine and candesartan pharmaceutical composition and preparation method thereof
  • Amlodipine and candesartan pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Add 9g of amlodipine maleate, 21ml of ethanol, 42ml of dimethyl sulfoxide, and 7ml of deionized water into a 100ml reaction kettle, adjust the pH to 6 with triethylamine or acetic acid, stir for 30min, seal it, and place it in an oven at 125°C After 3 days, take out the reaction kettle, place the reaction kettle in a 40KHz ultrasonic field to cool down naturally, wait for the reaction kettle to cool down slowly to 70°C, open the reaction kettle, add 70°C deionized water dropwise, white crystalline powder precipitates, and cool to room temperature And turn off the ultrasonic wave, filter, wash with dichloromethane and ethanol, and dry in vacuum for 2 hours to obtain amlodipine maleate hydrate crystals. The particle size range of the crystal is 75-150 μm, mp: 178-180°C.

[0054] Adopt U.S. Perkin-Elmer company PE 2400 II elemental analyzer, elemental analysis (%) calculated value is: C (52.22), H (5.84), Cl (6.42), N (5.08), O (30.44); Elemental analysis ( %) Found: C (5...

Embodiment 2

[0058] Add 9g of amlodipine maleate, 21ml of ethanol, 42ml of dimethyl sulfoxide, and 7ml of deionized water into a 100ml reaction kettle, adjust the pH to 6.5 with triethylamine or acetic acid, stir for 30min, seal it, and place it in an oven at 130°C After 3 days, the reactor was taken out, and the reactor was placed in a 40KHz ultrasonic field to cool down naturally. After the reactor was slowly cooled to 75°C, the reactor was opened, and deionized water at 75°C was added dropwise. White crystalline powder precipitated, and cooled to room temperature. And turn off the ultrasonic wave, filter, wash with dichloromethane and ethanol, and dry in vacuum for 3 hours to obtain amlodipine maleate hydrate crystals. The particle size range of the crystal is 75-150 μm, mp: 178-180°C.

[0059] Adopt U.S. Perkin-Elmer company PE 2400 II elemental analyzer, elemental analysis (%) calculated value is: C (52.22), H (5.84), Cl (6.42), N (5.08), O (30.44); Elemental analysis ( %) Found: C (...

Embodiment 3

[0063] Ingredients as follows:

[0064]

[0065] 1000 pieces are made

[0066] Preparation:

[0067] The raw and auxiliary materials were respectively crushed through 80-mesh sieve, the microcrystalline cellulose and amlodipine maleate hydrate crystals were mixed, and then mixed with candesartan cilexetil, compressible starch and low-substituted hydroxypropyl cellulose, cross-linked The polyvinylpyrrolidone is mixed evenly, and then mixed with magnesium stearate for 5 minutes, the intermediate is tested, and the composition chip is obtained by direct tableting.

[0068] Finally, the prescribed amount of magnesium stearate is added, mixed evenly, and after the intermediate is qualified, the medicinal composition chip is obtained by direct tableting; and the film coating is obtained.

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Abstract

The invention relates to an amlodipine and candesartan pharmaceutical composition. The pharmaceutical composition comprises the following components in parts by weight: 2.5-5 parts of amlodipine hydrate crystal, 4-16 parts of candesartan, 5-50 parts of compressible starch, 10-60 parts of microcrystalline cellulose, 15-40 parts of low-substituted hydroxypropyl cellulose, 10-45 parts of cross-linked polyvinyl pyrrolidone and 1-3 parts of magnesium stearate, wherein the amlodipine is amlodipine maleate hydrate crystal with a molecular formula of C24H29ClN2O9.1.5H2O. The pharmaceutical composition has the advantages that: amlodipine maleate has rapid and stable action, and can be stably released within 24 hours; and the pharmaceutical composition has strong synergism, accumulation and complementation effects, and has high bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition of amlodipine and candesartan cilexetil and a preparation method thereof. Background technique [0002] Candesartan cilexetil, Chinese alias: (±)-1-[[(cyclohexyloxy)carbonyl]oxo]ethyl-2-ethoxy-1-[[2′-(1H-tetrazolium Base-5)-[1,1′-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylate, English name: Candesartan cilexetil, molecular formula: C33H34N6O6, molecular weight: 610.67, The structural formula is as follows: [0003] [0004] Candesartan cilexetil is rapidly hydrolyzed into the active metabolite candesartan in the body. Candesartan is a selective angiotensin II receptor (AT1) antagonist that antagonizes vascular tension by binding to vascular smooth muscle AT1 receptors The vasoconstriction effect of factor II, thereby reducing the peripheral vascular resistance. It is also believed that candesartan can exert a certain antihype...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K31/4184A61K9/28A61K47/36A61K47/38A61K47/32A61K47/12A61P9/12A61P9/00
Inventor 马鹰军王小树钟正明罗韬
Owner HAINAN JINRUI PHARMA
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