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Binary co-amorphous substance and application thereof

An amorphous and binary system technology, applied in the field of medicine, can solve problems such as high energy consumption, high cost, and cumbersome preparation steps, and achieve high economic effect and low energy consumption

Pending Publication Date: 2022-07-12
TIANJIN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Patent CN109010348A proposes a lacidipine-spironolactone co-amorphous solid dispersion, but its preparation process is cumbersome and requires the addition

Method used

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  • Binary co-amorphous substance and application thereof
  • Binary co-amorphous substance and application thereof
  • Binary co-amorphous substance and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of Spironolactone / L-Tryptophan Co-Amorphous

[0031] The spironolactone and L-tryptophan were placed in a 5mL ball milling jar according to the molar ratio of 1:1, and steel balls with a diameter of 5mm were added, the ball milling frequency was adjusted to 20Hz, and the ball milling time was 120min, and the solid spironolactone / L was directly obtained. - Tryptophan co-amorph. figure 1 Spironolactone / L-tryptophan co-amorphous PXRD powder diffraction pattern prepared in Example 1, by figure 1 It can be seen that the spironolactone / L-tryptophan co-amorphous X-ray powder diffraction pattern does not have the characteristic Bragg peaks of the crystal, and presents the characteristic steamed bread peaks of the amorphous. figure 2 For the spironolactone / L-tryptophan co-amorphous differential scanning calorimetry spectrum prepared in Example 1, by figure 2 It can be seen that the DSC curve of the spironolactone / L-tryptophan coamorph exhibits a single glass tran...

Embodiment 2

[0033] Preparation of Spironolactone / L-Tryptophan Co-Amorphous

[0034] The spironolactone and L-tryptophan were placed in a 5mL ball milling jar according to the molar ratio of 1:1, and a steel ball with a diameter of 8mm was added, the ball milling frequency was adjusted to 25Hz, and the ball milling time was 90min, and the solid spironolactone / L was directly obtained. - Tryptophan co-amorph. Figure 8 Spironolactone / L-tryptophan co-amorphous PXRD powder diffraction pattern prepared in Example 2, by Figure 8 It can be seen that the spironolactone / L-tryptophan co-amorphous X-ray powder diffraction pattern does not have the characteristic Bragg peaks of the crystal, and presents the characteristic steamed bread peaks of the amorphous. Figure 8 and figure 1 The comparison shows that the preparation of spironolactone / L-tryptophan co-amorph in Example 2 and the preparation of spironolactone / L-tryptophan co-amorph in Example 1 are the same substance. After testing, its differ...

Embodiment 3

[0036] Preparation of Spironolactone / L-Tryptophan Co-Amorphous

[0037] Put spironolactone and L-tryptophan in a 5mL ball milling jar according to the molar ratio of 1:1, add steel balls with a diameter of 10mm, adjust the ball milling frequency to 30Hz, and the ball milling time to 60min to directly obtain solid spironolactone / L. - Tryptophan co-amorph. Figure 9 The spironolactone / L-tryptophan co-amorphous PXRD powder diffraction pattern prepared in Example 3, by Figure 9 It can be seen that the spironolactone / L-tryptophan co-amorphous X-ray powder diffraction pattern does not have the characteristic Bragg peaks of the crystal, and presents the characteristic steamed bread peaks of the amorphous. Figure 9 and figure 1 The comparison shows that the preparation of spironolactone / L-tryptophan co-amorph in Example 3 and the preparation of spironolactone / L-tryptophan co-amorph in Example 1 are the same substance. After testing, its differential scanning calorimetry, infrared...

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Abstract

The invention provides a binary co-amorphous substance and a preparation method and application thereof, the co-amorphous substance comprises a spirolactone/L-tryptophan or a spirolactone/L-phenylalanine co-amorphous substance, and the co-amorphous substance is formed by spirolactone and L-tryptophan as well as L-phenylalanine according to a molar ratio of 1: 1. Compared with a spirolactone bulk drug crystal, the spirolactone/L-tryptophan co-amorphous substance has the advantages that the solubility is improved by 3.22 times, and the dissolution rate is improved by 2.45 times; compared with a spirolactone bulk drug crystal, the spirolactone/L-phenylalanine co-amorphous substance has the advantages that the solubility is improved by 1.76 times, and the dissolution rate is improved by 1.59 times. The compound has a wide treatment prospect in the aspects of treating edema diseases, hypertension, primary aldosteronism and the like. The preparation method of the spirolactone/L-tryptophan and the spirolactone/L-phenylalanine binary co-amorphous substance is simple, no toxic organic solvent is added, the energy consumption is low, the efficiency is high, the preparation method is green and environment-friendly, and the application prospect is wide.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a binary co-amorph and a preparation method and application thereof, in particular to a spironolactone / L-tryptophan or spironolactone / L-phenylalanine binary co-amorph and Its preparation method and application. Background technique [0002] Spironolactone (CAS: 52-01-7), chemical name 17β-hydroxy-3-oxo-7α-(acetylthio)-17α-pregna-4-ene-21-carboxylic acid γ-lactone, is an artificial The synthesized compound, whose structure is similar to aldosterone, is a competitive inhibitor of aldosterone and belongs to weak diuretics, mainly acting on the distal convoluted tubule and collecting duct, and has no effect on other segments of the renal tubule, so the diuretic effect is weak. Clinically, it is usually used for adjuvant treatment of hypertension, treatment of primary aldosteronism and hypokalemia, and is often used in combination with other potent diuretics furosemide to reduce side ...

Claims

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Application Information

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IPC IPC(8): C07J31/00C07D209/20C07C229/36C07C227/42A61K31/585A61K9/00A61P9/12A61P13/00A61P3/12
CPCC07J31/003C07D209/20C07C229/36C07C227/42A61K9/0053A61P9/12A61P13/00A61P3/12C07B2200/07Y02A50/30
Inventor 龚俊波李茂林韩丹丹吴送姑侯宝红
Owner TIANJIN UNIV
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