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Benzenesulfonic acid levamlodipine crystal and pharmaceutical composition containing same

A technology of levamlodipine besylate and composition, which is applied in the field of levamlodipine besylate crystals, can solve the problems of slow drug onset, no solubility, slow absorption, etc., and achieve the effect of enhancing curative effect

Active Publication Date: 2014-06-18
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] 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 Insufficient solubility, its solubility in water is only 0.053mg / mL, which makes it slowly absorbed in the human body, takes a long time to reach the peak concentration (Cmax) after administration, 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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  • Benzenesulfonic acid levamlodipine crystal and pharmaceutical composition containing same
  • Benzenesulfonic acid levamlodipine crystal and pharmaceutical composition containing same
  • Benzenesulfonic acid levamlodipine crystal and pharmaceutical composition containing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] [Example 1] Preparation of crystals of levoamlodipine besylate

[0088] 1) Dissolve levoamlodipine besylate in a mixed solvent of dichloromethane and ethanol to obtain a dichloromethane / ethanol solution of levoamlodipine besylate;

[0089] 2) Add n-heptane dropwise to the dichloromethane / ethanol solution of levoamlodipine besylate obtained in step 1) under an ultrasonic field until crystals precipitate;

[0090] 3) Turn off the ultrasonic field, stand still, filter, and the filter cake is washed with dichloromethane and ethanol, and dried to obtain the crystals of levoamlodipine besylate.

[0091] The characteristic peaks in the X-ray powder diffraction pattern of the obtained L-Amlodipine besylate crystals measured by Cu-Kα rays are 8.0°, 12.1°, 15.4°, 17.0°, 19.8°, 21.6°, 23.0° in 2θ. , 24.3°, 25.7°, 27.4°, 30.7° and 33.5° display.

[0092] The following are Examples 2-9, the preparation method is the same as that of Example 1, and the specific process parameters are shown in ...

preparation Embodiment 1

[0097] [Formulation Example 1] Levoamlodipine besylate tablets

[0098] 1. Prescription

[0099]

[0100] 2. Preparation process:

[0101] (1) Bake the microcrystalline cellulose, sodium starch glycolate and magnesium stearate at 60°C for 2 hours, pass through a 60-mesh sieve, and set aside;

[0102] (2) Weigh the above-mentioned spare microcrystalline cellulose, sodium starch glycolate and magnesium stearate according to the prescription amount, and mix them evenly by adding the same amount to obtain a mixed powder;

[0103] (3) Weigh the prescription amount of the levoamlodipine besylate crystals prepared in Example 1, and mix them with the mixed powder obtained in step 3) to obtain the pharmaceutical composition powder, and sample for testing;

[0104] (4) Direct powder compression of the obtained pharmaceutical composition powder to obtain the pharmaceutical composition.

[0105] (5) Determine the content of the main drug, calculate the tablet weight, press the tablet with a die with ...

preparation Embodiment 2

[0106] [Formulation Example 2] Levoamlodipine besylate tablets

[0107] 1. Prescription

[0108]

[0109] 2. Preparation process: same as preparation example 1, the difference is that the crystals of levoamlodipine besylate are the crystals of levoamlodipine besylate prepared in example 2, and step 2) is baking at 65°C. Pass through an 80-mesh sieve.

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Abstract

The invention relates to a benzenesulfonic acid levamlodipine crystal, a preparation method thereof and a brand new pharmaceutical composition containing the crystal. According to an X-ray powder diffraction pattern obtained by measuring the benzenesulfonic acid levamlodipine crystal by utilizing a Cu-K alpha ray, characteristic peaks are displayed when 2theta is equal to 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 pharmaceutical composition contains the benzenesulfonic acid levamlodipine crystal and pharmaceutically acceptable auxiliary materials, wherein the pharmaceutically acceptable auxiliary materials are microcrystalline cellulose, carboxymethyl starch sodium and magnesium stearate. According to the benzenesulfonic acid levamlodipine crystal, the dissolubility of benzenesulfonic acid levamlodipine is improved, and a tablet prepared from the crystal has an improved biological availability.

Description

[0001] This application is a divisional application of Chinese patent application 201110238802.2. [0002] Original application date: 2011-8-19 [0003] Original application number: 201110238802.2 [0004] Original application invention creation name: a crystal of levoamlodipine besylate, its preparation method and a new pharmaceutical composition containing the crystal Technical field [0005] The invention belongs to the field of pharmaceutical preparations, and relates to a crystal of levamlodipine besylate, a preparation method thereof and a brand-new pharmaceutical composition containing the crystal. Background technique [0006] L-Amlodipine 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: [0007] [0008] L-Amlodipine besylate is a 1,4-dih...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/90C07C309/29C07C303/44A61K31/4422A61P9/12A61P9/10
Inventor 马鹰军王小树
Owner HAINAN JINRUI PHARMA CO LTD