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A drug-loaded emulsion of a liquid crystal-coated crystalline drug and a preparation method thereof

A liquid crystal emulsification and drug technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of poor biofilm permeability, poor smearing skin feel, low transdermal absorption rate, etc., to achieve high skin safety, Overcome permeability and overcome the effect of low transdermal absorption rate

Active Publication Date: 2022-02-01
EAST CHINA UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a transdermal pharmaceutical preparation that utilizes a liquid crystal emulsification system to enhance the skin barrier function and improve the poor water solubility of the pharmaceutical active component API and the poor biofilm permeability, thereby improving the existing crystal drug. The shortcomings of poor smearability, poor water solubility, and low transdermal absorption rate

Method used

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  • A drug-loaded emulsion of a liquid crystal-coated crystalline drug and a preparation method thereof
  • A drug-loaded emulsion of a liquid crystal-coated crystalline drug and a preparation method thereof
  • A drug-loaded emulsion of a liquid crystal-coated crystalline drug and a preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] A drug-loaded layered liquid crystal emulsion, comprising the following raw materials in parts by weight:

[0082] Lecithin liquid crystal emulsifier 1.0 parts

[0083] 10.0 parts of saturated isopropyl myristate

[0084] Ketoprofen drug 0.4 parts

[0085] Capo U21 0.2 parts

[0086] 0.4 parts of 10% sodium hydroxide

[0087] 0.5 parts of 1,2-hexanediol

[0088] Purified water 87.5 parts

[0089] The implementation steps of above-mentioned formula are:

[0090] (1) Weighing the following raw materials in parts by weight, i.e. the oil phase, and preheating it in a constant temperature water bath at 75-80°C;

[0091] Lecithin liquid crystal emulsifier 1.0 parts

[0092] 10.0 parts of saturated isopropyl myristate

[0093] Ketoprofen drug 0.4 parts

[0094] (2) Weigh the following raw materials in parts by weight, i.e. the water phase, and preheat it in a constant temperature water bath at 75-80°C;

[0095] Capo U21 0.2 parts

[0096] Add water to 100.0 parts

...

Embodiment 2

[0101] Operate the same as in Example 1, only changing the grease to isopropyl palmitate to prepare the drug-loaded layered liquid crystal emulsion, and the polarized light test results are as follows: figure 2 shown.

Embodiment 3

[0103] Operate the same as in Example 1, only change the oil into caprylic acid / capric triglyceride, and prepare the drug-loaded layered liquid crystal emulsion. The polarized light test results are as follows: image 3 shown.

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a drug-loaded emulsion of liquid crystal-coated crystalline drugs and a preparation method thereof. The emulsion contains crystal drug and liquid crystal emulsifier. In the liquid crystal-coated drug-carrying emulsion with crystalline drug of the present invention, there is a layered liquid crystal structure similar to the structure of the stratum corneum of human skin, and at the same time, there is also a crystalline drug crystal structure inside it. The drug-loaded emulsion of the present invention overcomes the shortcomings of traditional drug active components such as poor water solubility and low biofilm permeability, and has the advantages of high skin safety, multiple sustained-release characteristics, and a drug loading rate of nearly 100%. The development of high-efficiency drug-loaded emulsion formulations with better retention rate of active pharmaceutical ingredients, better formulation stability and more effective drug active ingredients provides a new design idea.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. Specifically, the present invention relates to a drug-loaded emulsion of liquid crystal-coated crystalline drug and its preparation method and application. Background technique [0002] The poor water solubility of drugs and the low permeability of epithelial cells are two key factors affecting the absorption of drugs by the human body. Existing studies have shown that as many as 60-70% of the active ingredients in the discovery stage have the disadvantage of poor water solubility, and 10-20% of the active ingredients have the problem of poor biofilm permeability, which in turn leads to a higher rate of transdermal absorption. Inferior question. Therefore, how to use preparation methods to make such drug molecules have sufficient bioavailability is of great significance for improving the corresponding drug efficacy in the actual clinical application process. At the same tim...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/24A61K47/26A61K47/28A61K47/10A61K47/06A61K47/14A61K47/32A61K45/06A61K31/192A61K31/122A61P29/00
CPCA61K9/107A61K9/0014A61K47/24A61K47/26A61K47/28A61K47/10A61K47/06A61K47/14A61K47/32A61K45/06A61K31/192A61K31/122A61P29/00
Inventor 尚亚卓胡佳杰杨淑琴倪琢瑶刘洪来
Owner EAST CHINA UNIV OF SCI & TECH
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