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New crystal form of levamlodipine besylate

A kind of technology of levamlodipine besylate and levamlodipine besylate, applied in the field of levamlodipine besylate crystal form, can solve the problem that solubility, thermal stability, light stability, dissolution and bioavailability are not very good Meet the requirements of pharmaceutical preparations and other issues, and achieve the effects of increasing bioavailability, good stability, and simple preparation methods

Pending Publication Date: 2020-12-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The known crystal forms of levamlodipine besylate cannot meet the requirements of pharmaceutical preparations in terms of solubility, thermal stability, photostability, dissolution rate, bioavailability, etc., so more crystal forms need to be developed. On the one hand, more crystal forms of levamlodipine besylate are provided for pharmaceutical applications;

Method used

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  • New crystal form of levamlodipine besylate
  • New crystal form of levamlodipine besylate
  • New crystal form of levamlodipine besylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add levamlodipine besylate (5.05g) into ethanol / purified water (V 乙醇 :V 水 =1:8, 450ml) in the mixed solution, heated to 50°C and stirred to dissolve, continued to insulate and stir for 0.5h, then filtered, and the filtrate was lowered to room temperature at a rate of 0.5°C / min; the filtrate was placed in a beaker, sealed The membrane was sealed, punctured, volatilized, crystallized for 3 days, filtered, and dried under reduced pressure at 45°C to constant weight to obtain the crystalline form of L-amlodipine besylate with a yield of 98.2%, an optical purity of 99.97%, and a purity of 99.92%.

Embodiment 2

[0043] Add levamlodipine besylate (5.03g) into acetone / purified water (V 丙酮 :V 水 =1:6, 400ml) in the mixed solution, heated to 40°C and stirred to dissolve, continued to insulate and stir for 1 hour, then filtered, and the filtrate was cooled to room temperature at a rate of 0.5°C / min; the filtrate was placed in a beaker, sealed with Seal, pierce, volatilize, crystallize for 2 days, filter, and dry under reduced pressure at 45°C to constant weight to obtain the crystalline form of L-amlodipine besylate with a yield of 97.7%, an optical purity of 99.95%, and a purity of 99.82%.

Embodiment 3

[0045] Levoamlodipine besylate (5.02g) was added to methanol / purified water (V 甲醇 :V 水 =1:7, 450ml) in the mixed solution, heated to 50°C and stirred to dissolve, continued to insulate and stir for 0.5h, then filtered, and the filtrate was cooled to room temperature at a rate of 0.5°C / min; the filtrate was placed in a beaker, sealed The membrane was sealed, punctured, volatilized, crystallized for 3 days, filtered, and dried under reduced pressure at 45°C to constant weight to obtain the crystalline form of L-amlodipine besylate with a yield of 97.5%, an optical purity of 99.93%, and a purity of 99.84%.

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Abstract

The invention provides a crystal form of levamlodipine besylate , and relates to the technical field of crystal form drug molecules. The levamlodipine besylate crystal form is radiated by Cu-Kalpha, and X-ray diffraction patterns represented by 2 theta have characteristic peaks at 7.69 + / -0.2 degrees, 11.35 + / -0.2 degrees, 13.45 + / -0.2 degrees, 14.54 + / -0.2 degrees, 16.63 + / -0.2 degrees, 17.32 + / -0.2 degrees, 18.78 + / -0.2 degrees, 22.22 + / -0.2 degrees, 26.07 + / -0.2 degrees, 28.76 + / -0.2 degrees, 29.96 + / -0.2 degrees, 35.80 + / -0.2 degrees, and 39.41 + / -0.2 degrees; the crystallographic measurement parameters are as follows: a monoclinic system with a space group of P21, the crystal cell parameters being as follows: 26.1230 (7), alpha=90.00 degrees, beta=96.496 (2) degrees and gamma=90.00 degrees, and a cell volume. The invention also provides a related preparation method and application. The levamlodipine besylate crystal form is good in stability, a medicine prepared from the levamlodipine besylate crystal form is high in dissolution rate, the bioavailability is improved, and the medicine effect is improved.

Description

technical field [0001] The invention relates to the technical field of crystal drug molecules, in particular to a crystal form of levamlodipine besylate. Background technique [0002] In recent years, studies have found that different crystal forms of drugs can change their physical and chemical properties (density, hardness, solubility, stability, optical and electrical properties, etc.), dissolution rate, biological effects, etc. It has important practical value in science. Crystalline drug molecules include polymorphs, hydrates, solvates, and salts of drug molecules. Through drug crystallization, not only can the crystallographic parameters of crystalline drug molecules be clarified, but also the type of solvent molecules in the crystal form can be determined. And the number (such as: crystal water molecules), plays a very important role in understanding and mastering the spatial arrangement and physical and chemical properties of drug molecules. [0003] Levoamlodipine...

Claims

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Application Information

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IPC IPC(8): C07D211/90C07C309/29C07C303/32A61P9/12
CPCC07D211/90C07C303/32A61P9/12C07B2200/13C07C309/29
Inventor 翟立海王聚聚郭立红梁茂征
Owner LUNAN PHARMA GROUP CORPORATION
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