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A kind of levamlodipine besylate crystal, its preparation method and a new pharmaceutical composition containing the crystal

A technology of levamlodipine besylate and a composition, which is applied in the field of levamlodipine besylate crystals, can solve the problems of slow onset of drug effect, no solubility, low overall level of blood drug concentration, etc., and achieves enhanced curative effect. Effect

Active Publication Date: 2011-12-14
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, because levamlodipine besylate is insoluble in water, sufficient solubility is a necessary condition for the drug to obtain good bioavailability. However, levamlodipine besylate is in water, especially in a state close to the physiological pH7.4 The solubility in water is only 0.053mg / mL, which makes it slowly absorbed in the human body, and the time to reach the peak concentration (Cmax) after administration is longer, and the overall level of blood drug concentration is low, especially after administration. Blood levels are very low in the early postoperative period, and the drug works very slowly, slow-acting

Method used

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  • A kind of levamlodipine besylate crystal, its preparation method and a new pharmaceutical composition containing the crystal
  • A kind of levamlodipine besylate crystal, its preparation method and a new pharmaceutical composition containing the crystal
  • A kind of levamlodipine besylate crystal, its preparation method and a new pharmaceutical composition containing the crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] [embodiment 1] preparation of levamlodipine besylate crystal

[0084] 1) dissolving levamlodipine besylate in a mixed solvent of dichloromethane and ethanol to obtain a dichloromethane / ethanol solution of levamlodipine besylate;

[0085] 2) Add n-heptane dropwise to the dichloromethane / ethanol solution of levamlodipine besylate obtained in step 1) under an ultrasonic field until crystallization occurs;

[0086] 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.

[0087] 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.

[0088] Below is embodiment 2-9, and preparation method is with embodiment 1, and its concrete process parameter is sh...

preparation Embodiment 1

[0094] [Preparation Example 1] Levoamlodipine Besylate Tablets

[0095] 1. Prescription

[0096]

[0097] 2. Preparation process:

[0098] (1) Microcrystalline cellulose, sodium starch glycolate and magnesium stearate were baked at 60°C for 2 hours respectively, passed through a 60-mesh sieve, and set aside;

[0099] (2) Take above-mentioned standby microcrystalline cellulose, carboxymethyl starch sodium and magnesium stearate by recipe quantity, adopt equal amount incremental method to mix, obtain mixed powder;

[0100] (3) take by weighing the levamlodipine besylate crystal prepared in Example 1 of the prescription amount, mix with the mixed powder obtained in step 3), obtain the pharmaceutical composition powder, and take a sample for detection;

[0101] (4) The obtained pharmaceutical composition powder is subjected to direct powder compression to obtain the pharmaceutical composition.

[0102] (5) Determine the content of the main drug, calculate the weight of the t...

preparation Embodiment 2

[0103] [Preparation Example 2] Levoamlodipine Besylate Tablets

[0104] 1. Prescription

[0105]

[0106] 2. Preparation process: the same as in the preparation example 1, the difference is that the levamlodipine besylate crystals are the levamlodipine besylate crystals prepared in Example 2, and step 2) is baked at 65°C for 3 hour, through a 80-mesh sieve.

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Abstract

The invention relates to levamlodipine besylate crystals, a preparation method thereof and a brand-new medicinal composition containing the crystals. Characteristic peaks in an X-ray powder diffraction pattern obtained by measuring the levamlodipine besylate crystals by using Cu-K alpha rays are displayed as 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 degrees at 2 theta. The medicinal composition comprises the levamlodipine besylate crystals and pharmaceutically acceptable excipients, wherein the pharmaceutically acceptable excipients are microcrystalline cellulose, sodium starch glycolate and magnesium stearate. The crystals improve the dissolubility of levamlodipine besylate; and tablets prepared from the crystals have improved bioavailability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a levamlodipine besylate crystal, a preparation method thereof and a new pharmaceutical composition containing the crystal. Background technique [0002] Levoamlodipine besylate is white or off-white powder, its chemical name is (s)-(-)-3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4- (2-Chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, molecular formula C 20 h 25 N 2 o 5 Cl·C 6 h 6 o 3 S, molecular weight 567.1, structural formula: [0003] [0004] Levoamlodipine besylate is a 1,4-dihydropyridine calcium antagonist or slow channel blocker. Amlodipine besylate has two isomers, left-handed and right-handed, and the calcium ion antagonistic activity of the left-handed isomer is 1000 times that of the right-handed isomer and twice that of the racemic isomer. Levoamlodipine besylate is currently a commonly used drug for the treatment of hy...

Claims

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Application Information

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IPC IPC(8): C07D211/90C07C309/29C07C303/44A61K31/4422A61K9/20A61P9/12A61P9/10
Inventor 马鹰军王小树
Owner HAINAN JINRUI PHARMA
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