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Lacidipine-spirolactone co-amorphous solid dispersion and preparation thereof

A technology of solid dispersion and lacidipine, which is applied in the field of medicine, can solve problems such as limiting oral bioavailability, and achieve the effect of improving in vitro dissolution rate, good economy, and low cost

Active Publication Date: 2018-12-18
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For BCS class II drugs, the solubility of the drug is the main factor limiting its dissolution rate, which in turn limits its oral bioavailability

Method used

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  • Lacidipine-spirolactone co-amorphous solid dispersion and preparation thereof
  • Lacidipine-spirolactone co-amorphous solid dispersion and preparation thereof
  • Lacidipine-spirolactone co-amorphous solid dispersion and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] The molar ratio of lacidipine to spironolactone is 3:1. Weigh 0.5g lacidipine bulk drug and 0.15g spironolactone bulk drug, add appropriate amount of ethanol to dissolve until clarified. Rotate the solvent under reduced pressure at 20-60° C., and dry the residue in vacuum for 24 hours to obtain the obtained product. Measure the dissolution rate of lacidipine according to the dissolution measurement method described below to be 5.1%, and the dissolution rate of spironolactone is: 46.2%.

Embodiment 2

[0070] The molar ratio of lacidipine to spironolactone is 1:1. Weigh 0.5g lacidipine bulk drug and 0.46g spironolactone bulk drug, add appropriate amount of ethanol to dissolve until clarified. The preparation process is the same as in Example 1. Measure the dissolution rate of lacidipine according to the dissolution rate determination method described below to be 21%, and the dissolution rate of spironolactone is: 57%.

Embodiment 3

[0072] The molar ratio of lacidipine to spironolactone is 1:3. Weigh 0.5g lacidipine bulk drug and 1.37g spironolactone bulk drug, add appropriate amount of ethanol to dissolve until clarified. The preparation process is the same as in Example 1. Measure the dissolution rate of medicine according to the dissolution rate determination method described below to be 56%, and the dissolution rate of spironolactone is: 60.4%.

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Abstract

The invention belongs to the technical field of medicines and in particular relates to lacidipine-spirolactone co-amorphous solid dispersion and a preparation method thereof. According to the preparation method, lacidipine and spirolactone, which have a cooperative blood pressure lowering effect, are carriers for each other, and the co-amorphous solid dispersion is prepared by adopting a solvent volatilization method. The co-amorphous solid dispersion is formed by combining the lacidipine and the spirolactone according to the mol ratio of 1 to (1 to 9); Cu-Kalpha radiation is utilized, and a powder X-ray diffraction spectrum shown as a 2theta angle does not have a sharp diffraction peak; peak positions and peak strength of the co-amorphous solid dispersion are obviously changed in a Fourier infrared spectrum. Compared with a lacidipine crystal and a spirolactone crystal, the co-amorphous solid dispersion has the advantages that the dissolution rates and dissolvability of the lacidipineand the spirolactone are remarkably improved. The preparation method of the solid dispersion is simple and feasible and has good repeatability; amplified production is easy to carry out and industrial transformation is carried out; the preparation method has a good clinical application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a lacidipine-spironolactone co-amorphous solid dispersion and a preparation method thereof. Background technique [0002] The chemical name of Lacidipine is: (E)-4-[2-[3-(1,1-dimethylethoxy)-3-oxo-1-propenyl]phenyl]- Diethyl 1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate is a specific, potent and long-lasting dihydropyridine calcium channel blocker, mainly selective Block calcium channels in vascular smooth muscle, expand peripheral arteries, reduce peripheral vascular resistance, reduce cardiac afterload, and lower blood pressure. It is clinically used as the first-line drug for the treatment of hypertension. In terms of physical properties, lacidipine is a white or off-white crystalline powder, unstable when exposed to light, easily soluble in ethyl acetate, soluble in acetone, slightly soluble in methanol and ethanol, and almost insoluble in water. The melt...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61K31/4422A61K9/14A61P9/12
CPCA61K9/14A61K31/4422A61K31/585A61P9/12A61K2300/00
Inventor 孙进何仲贵王昭蒙孙孟驰
Owner SHENYANG PHARMA UNIVERSITY
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