Drug-loaded emulsion of liquid crystal coated crystal drug and preparation method thereof
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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, overcome the effect of low transdermal absorption rate
Active Publication Date: 2021-06-18
EAST CHINA UNIV OF SCI & TECH +1
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[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
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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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Abstract
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a drug-loaded emulsion of a liquid crystal coated crystal drug and a preparation method thereof. The emulsion comprises a crystal drug and a liquid crystal emulsifier. A lamellar liquid crystal structure similar to a human skin cuticle structure exists in the drug-loaded emulsion of the liquid crystal coated crystal drug, and meanwhile, a crystal drug crystal structure also exists in the emulsion. The drug-loaded emulsion provided by the invention overcomes the defects of poor water solubility, low biofilm permeability of active components of traditional drugs, and has the advantages of high skin safety, multiple slow release characteristics, drug entrapment rate of nearly 100% and the like; and provides a new design idea for the development of an efficient drug-loaded emulsion preparation with higher retention rate of the active pharmaceutical ingredients, better preparation stability and more effective entrapment of the active pharmaceutical ingredients.
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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