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Application of macrocyclic host molecule as medicinal solubilizing agent

A technology of main molecules and solubilizers, applied in the field of pharmacy, can solve problems such as local phlebitis and achieve the effect of improving solubility

Active Publication Date: 2019-10-29
SOUTH UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the solubility of these two commercially available dantrolene sodium injections has been adjusted, they both have a high pH, ​​which can cause severe local phlebitis in clinical application

Method used

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  • Application of macrocyclic host molecule as medicinal solubilizing agent
  • Application of macrocyclic host molecule as medicinal solubilizing agent
  • Application of macrocyclic host molecule as medicinal solubilizing agent

Examples

Experimental program
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Embodiment 1

[0081] The present embodiment provides a kind of preparation method and concentration detection method of dantrolene sodium aqueous solution:

[0082] (1) Determination of standard curve:

[0083] After dissolving dantrolene sodium in methanol, prepare a solution of dantrolene sodium with a concentration of 0.5mg / mL, 0.25mg / mL, 0.125mg / mL, 0.0625mg / mL, 0.03125mg / mL, and analyze and detect it by HPLC. The detection wavelength is 1mL / min, the detection wavelength is 330nm and 263nm respectively, the mobile phase is methanol-water (70 / 30, v / v), and the standard curve is obtained by fitting the peak area of ​​dantrolene sodium with its concentration: y=89.91+13898.15x , R 2 = 0.9999. (below related to the embodiment of dantrolene sodium or comparative example all follow this standard curve).

[0084] (2) Preparation and detection of dantrolene sodium aqueous solution:

[0085] At room temperature, 1 mg, 2 mg, 3 mg, 4 mg, 5 mg and 6 mg of dantrolene sodium were added to 1 mL of...

Embodiment 2

[0089] The present embodiment provides a kind of preparation method and concentration detection method of tepotinib aqueous solution:

[0090] (1) Determination of standard curve:

[0091] After dissolving tepotinib with methanol, configure the tepotinib solution with a concentration of 0.51mg / mL, 0.255mg / mL, 0.1275mg / mL, 0.06375mg / mL, 0.031875mg / mL, 0.0159375mg / mL, 0.00796875mg / mL, and use HPLC analysis and detection, the flow rate is 1mL / min, the detection wavelength is 330nm and 263nm respectively, the mobile phase is methanol (0.1% diethylamine)-water (0.1% diethylamine) (85 / 15, v / v), and tepotinib The peak area and its concentration were fitted to obtain a standard curve: y=194.74+39067.21x, R 2 = 0.9994. (The following examples or comparative examples related to tepotinib all follow this standard curve).

[0092] (2) Preparation and detection of tepotinib aqueous solution:

[0093] At room temperature, 1 mg, 3 mg, 4 mg, 5 mg and 6 mg of tepotinib were added to 1 mL o...

Embodiment 3

[0097] The present embodiment provides a kind of preparation method and concentration detection method of dantrolene sodium aqueous solution:

[0098]At room temperature, add 6 mg of dantrolene sodium into 1 mL of an aqueous solution containing 10 mg of solubilizer A (adjust the pH to 7.5 with acetic acid), dissolve it ultrasonically for 1 hour, and let it stand for 10 hours. Filter to remove insoluble drug, detect with HPLC, flow velocity is 1mL / min, detection wavelength is 330nm, mobile phase is methanol-water (70 / 30, v / v), this experiment is repeated three times and gets average value, the peak area obtained Substituted into the standard curve, the concentration of dantrolene sodium obtained was 3.22 mg / mL (solubility).

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Abstract

The invention relates to application of a macrocyclic host molecule as a medicinal solubilizing agent. The macrocyclic host molecule is provided with the structure shown in the formula 1 (please see the specification for the formula 1). The invention specifically further relates to a medicine solution. The medicine solution includes an active component and the solubilizing solvent, the active component includes dantrolene sodium or tepotinib, and the solubilizing solvent has the structure shown in the formula 1 (please see the specification for the formula 1). According to the application andthe medicine solution, the macrocyclic host molecule shown in the formula 1 with high solubility in water and low toxicity to cells is used, solubility of a medicine in a water phase can be significantly improved, thus blood concentration of the medicine is increased to reduce medication frequency, and the side effect does not exist.

Description

technical field [0001] The present invention relates to the technical field of pharmacy, in particular to the application of a macrocyclic main molecule as a drug solubilizer, and in particular to the application of a macrocyclic main molecule as a drug solubilizer, a drug solution and its preparation method, detection method and application. Background technique [0002] Drug solubility has a significant impact on drug absorption and efficacy. Dantrolene sodium is a muscle relaxant, the only clinical drug for the treatment of malignant hyperthermia. Malignant hyperthermia is a rare genetic disorder induced by volatile inhaled anesthetics or depolarizing muscle relaxants (succinylcholine), resulting in dysregulation of intracellular calcium ions, resulting in severe skeletal muscle hypermetabolism. Dantrolene sodium is a post-synaptic muscle relaxant that reduces muscle cell excitation-contraction coupling. The specific mechanism of action is that dantrolene sodium inhibit...

Claims

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Application Information

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IPC IPC(8): A61K47/22A61K9/08A61K9/19A61K31/4178A61K31/506A61P21/02A61P29/00G01N30/02
CPCA61K47/22A61K9/08A61K9/19A61K31/4178A61K31/506A61P21/02A61P29/00G01N30/02
Inventor 蒋伟马延龙
Owner SOUTH UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA
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