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Brand new drug composition containing levamlodipine besylate and candesartan cilexetil and preparation method thereof

A kind of technology of levamlodipine besylate and candesartan cilexetil, which is applied in the new pharmaceutical composition containing levamlodipine and candesartan cilexetil and the field of preparation thereof

Active Publication Date: 2012-02-15
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] For overcoming above-mentioned defect, the inventor starts with levamlodipine besylate which is insoluble in water, and has made a kind of levamlodipine besylate crystal through a large amount of refining tests, and this crystal can improve benzene to a certain extent. The solubility of levamlodipine sulfonate, and it is more surprising to find that the pharmaceutical composition adopting the crystal and candesartan cilexetil can well overcome the above-mentioned defects

Method used

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  • Brand new drug composition containing levamlodipine besylate and candesartan cilexetil and preparation method thereof
  • Brand new drug composition containing levamlodipine besylate and candesartan cilexetil and preparation method thereof
  • Brand new drug composition containing levamlodipine besylate and candesartan cilexetil and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] [embodiment 1] preparation of levamlodipine besylate crystal

[0075] 1) dissolving levamlodipine besylate in a mixed solvent of dichloromethane and ethanol to obtain a dichloromethane / ethanol solution of levamlodipine besylate;

[0076] 2) Add n-heptane dropwise to the dichloromethane / ethanol solution of levamlodipine besylate obtained in step 1) under an ultrasonic field until crystallization occurs;

[0077] 3) Turn off the ultrasonic field, let stand, filter, wash the filter cake with dichloromethane and ethanol respectively, and dry to obtain the levamlodipine besylate crystal.

[0078] Gained levamlodipine besylate crystals use Cu-Kα rays to measure characteristic peaks in the X-ray powder diffraction pattern obtained at 2θ of 8.0°, 12.1°, 15.4°, 17.0°, 19.8°, 21.6°, 23.0° , 24.3°, 25.7°, 27.4°, 30.7° and 33.5° display, such as figure 1 shown.

[0079] Below is embodiment 2-9, and preparation method is with embodiment 1, and its concrete process parameter is sh...

Embodiment 1

[0085] [Formulation Example 1] Film-coated tablets of levamlodipine besylate and candesartan cilexetil

[0086] 1. Prescription

[0087] Tablet prescription:

[0088]

[0089]

[0090] Coating Solution Prescription:

[0091]

[0092] 2. Preparation process

[0093] (1) Candesartan cilexetil is passed through an 80-mesh sieve, for subsequent use;

[0094] (2) Microcrystalline cellulose, compressible starch, croscarmellose sodium, silicon dioxide and magnesium stearate were respectively baked at 60°C for 4 hours, passed through a 60-mesh sieve, and set aside;

[0095] (3) Take the above-mentioned standby candesartan cilexetil, microcrystalline cellulose, croscarmellose sodium, silicon dioxide and magnesium stearate according to the recipe quantity, and mix them uniformly by equal addition method to obtain mixed powder;

[0096] (4) Take by weighing the levamlodipine besylate crystal prepared in Example 1 of the prescription amount, mix with the mixed powder obtaine...

Embodiment 2

[0101] [Formulation Example 2] Film-coated tablets of levamlodipine besylate and candesartan cilexetil

[0102] 1. Prescription

[0103] Tablet prescription:

[0104]

[0105]

[0106] Coating Solution Prescription:

[0107]

[0108] 2. Preparation process: same as preparation example 1, the difference is that the levamlodipine besylate used is the levamlodipine besylate crystal prepared in Example 2, and step 2) is to bake at 80°C 2 hours, through 80 mesh sieves.

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Abstract

The invention relates to a brand new drug composition containing levamlodipine besylate and candesartan cilexetil and a preparation method thereof. The composition comprises the active ingredients such as levamlodipine besylate and candesartan cilexetil and pharmaceutically acceptable auxiliaries, wherein levamlodipine besylate is levamlodipine besylate crystals; and the characteristic peak in the X-ray powder diffraction pattern obtained after measuring the crystals with a Cu-Kalpha ray is displayed at 2theta, namely 8.0 degrees, 12.1 degrees, 15.4 degrees, 17.0 degrees, 19.8 degrees, 21.6 degrees, 23.0 degrees, 24.3 degrees, 25.7 degrees, 27.4 degrees, 30.7 degrees and 33.5 degrees. The drug composition and the preparation method have the following advantages: the crystals can improve the solubility of levamlodipine besylate to some extent, thus amlodipine besylate in the drug composition is dissolved out more quickly and the drug composition has a better curative effect and good stability; and the method adopts a direct powder compression technology, has the advantages of simple technology, short production period and low production cost and is easy to realize industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a novel pharmaceutical composition containing levamlodipine 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 cile xetil, molecular formula: C 33 h 34 N 6 o 6 , 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K31/4184A61K9/20A61P9/12
Inventor 马鹰军钟正明罗韬王小树
Owner HAINAN JINRUI PHARMA
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