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Composition consisting of hydroxyl-containing auxiliary materials and pyrimidine type compounds, and pharmaceutical preparation containing composition

A technology for pharmaceutical preparations and compositions, applied in the field of medicine, can solve problems such as improving the skin safety of the former

Inactive Publication Date: 2019-10-15
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Pyrimidine is a common functional group in the drug structure and has a wide range of pharmacological activities. However, there is currently no technical teaching on adding pyrimidine compounds to alcohol and / or phenol excipients to improve the skin safety of the former

Method used

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  • Composition consisting of hydroxyl-containing auxiliary materials and pyrimidine type compounds, and pharmaceutical preparation containing composition
  • Composition consisting of hydroxyl-containing auxiliary materials and pyrimidine type compounds, and pharmaceutical preparation containing composition
  • Composition consisting of hydroxyl-containing auxiliary materials and pyrimidine type compounds, and pharmaceutical preparation containing composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0131] Embodiment 1 Preparation of a composition composed of hydroxyl-containing adjuvant and pyrimidine compound

[0132] The hydroxyl-containing excipients and pyrimidine compounds described in the present invention are fully mixed in a specific mass ratio to obtain the product.

Embodiment 2

[0141] Example 2 Preparation of a composition for external use containing a hydroxyl-containing adjuvant and a pyrimidine compound and minoxidil

[0142] Prescription (1000 unit dose)

[0143] prescription number active ingredient Composition (1kg) Other accessories Prescription 1 3kg Minoxidil Excipient 1—Compound 1 5L propylene glycol, 5L ethanol, the balance is water Prescription 2 3kg Minoxidil Excipient 4—Compound 4 5L propylene glycol, 5L ethanol, the balance is water Prescription 3 3kg Minoxidil Excipient 7—Compound 7 5L propylene glycol, 5L ethanol, the balance is water Prescription 4 3kg Minoxidil Excipient 13—Compound 13 5L propylene glycol, 5L ethanol, the balance is water Prescription 5 3kg Minoxidil Excipient 26—compound 13 5L propylene glycol, 5L ethanol, the balance is water Prescription 6 3kg Minoxidil Excipient 28—compound 14 5L propylene glycol, 5L ethanol, the balance is water ...

Embodiment 3

[0147] Example 3 Preparation of a composition containing a hydroxyl-containing adjuvant and a pyrimidine compound and a minoxidil cream

[0148] Prescription (1000 unit dose)

[0149]

[0150]

[0151]

[0152] Preparation

[0153] Oil phase: Weigh the prescribed amount of glyceryl monostearate, stearic acid, simethicone, and azone (mass ratio: 1000:1) and put them on a water bath at 80°C to heat, melt and add to the recipe amount of minoxidil;

[0154] Water phase: weigh the prescribed amount of propylene glycol and triethanolamine respectively, measure 430L of purified water and heat it on a water bath at 80°C to make it uniform; add the prescribed amount of sodium methyl p-hydroxybenzoate to 20L of water to dissolve; add the oil phase to water phase, stir and emulsify, and keep warm for 30 minutes; then lower the temperature to 45°C, add an aqueous solution of sodium methyl p-hydroxybenzoate, and stir evenly to obtain the product.

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PUM

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Abstract

On one hand, the invention provides a composition consisting of hydroxyl-containing auxiliary materials and pyrimidine type compounds. The hydroxyl-containing auxiliary materials comprise micromolecule auxiliary materials and polymer auxiliary materials. The composition can significantly reduce the effect of the hydroxyl-containing auxiliary materials for restraining dendritic epidermis T cells (DETC), so that the skin safety characteristics can be improved. On the other hand, the invention provides a pharmaceutical preparation containing the composition, and particularly provides an externaluse dosage form. In a plurality of embodiments, the external use dosage form uses minoxidil as an active component.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition composed of a hydroxyl-containing auxiliary material and a pyrimidine compound and a pharmaceutical preparation containing the composition. Background technique [0002] Ethanol is a common excipient in external preparations, especially external solutions, and is usually used as a solvent, so it is used in a large amount. Chronic alcohol abuse is associated with increased incidence and severity of skin infections. T cells located in the skin mediate a variety of immune functions that play important roles in tissue homeostasis and skin immunity. A study by Parlet CP et al. (AlcoholClin Exp Res. 2014 May; 38(5):1356-64) found that long-term intake of ethanol in mice can lead to a decrease in the number and function of various skin T cell subsets. On this basis, the present inventors used the method disclosed by Youhei Uchida et al. (J.Immunol.2011, 186:...

Claims

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Application Information

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IPC IPC(8): A61K47/22A61K47/10A61K47/18A61K47/32A61K31/506
CPCA61K9/0014A61K31/506A61K47/10A61K47/18A61K47/22A61K47/32
Inventor 向飞
Owner 黄泳华
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