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Orally taken emulsion and its prepn

An emulsion and oil-in-water technology, applied in the field of oil-in-water oral emulsions, can solve the problems affecting the interfacial stability of emulsion droplets, the overall physical stability of the emulsion system, the physical instability of the emulsion, and the instability of the emulsion formulation.

Inactive Publication Date: 2007-11-07
朱芳海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the liquid drug emulsion preparation method is used to prepare the solid drug emulsion, due to the physical rigidity, density, buoyancy and other particularities of the solid drug, too large or too small particle size will significantly affect the interface stability of the emulsion droplets. Or the overall physical stability of the emulsion system, which will lead to various physical instability phenomena of the emulsion: such as delamination, flocculation, demulsification, precipitation, etc., making the emulsion preparation extremely unstable

Method used

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  • Orally taken emulsion and its prepn
  • Orally taken emulsion and its prepn
  • Orally taken emulsion and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add 2.0g phospholipids, 1.0g sucrose ester, and about 80g deionized water to 15g edible soybean oil containing 1.0g ibuprofen. Add appropriate amount of hydrochloric acid or sodium hydroxide to adjust the pH value of the colostrum to be stable between 5-9, and then pass through the high-pressure homogenization equipment to further pulverize the average particle size of the emulsion to between 50-500nm, and the total amount of the constant-volume emulsion to 100 grams, a stable emulsion can be obtained.

[0042] The above-mentioned ibuprofen may also be steroidal anti-inflammatory drugs such as ketoprofen and fenbufen.

Embodiment 2

[0044] Same as Example 1, the difference is that in 1.0g edible corn oil containing 0.1 gram progesterone, add 2.0g phospholipids, 0.1g polyethylene glycol fatty acid ester or other HLB value between 8-25 non-ionic surface Active agent, according to the acidity and alkalinity of the primary emulsion, add an appropriate amount of sulfuric acid or sodium acetate to it, adjust the pH value of the primary emulsion to 5-9, and then pass through the high-pressure homogenization equipment to further pulverize the average particle size of the emulsion to 1nm- Between 1000nm.

Embodiment 3

[0046] Add 1.25g of phospholipids, 0.12g of PEG fatty acid ester, and about 90g of deionized water to 0.05g of edible olive oil containing 0.001g of diethylstilbestrol. After primary emulsification with high-shear emulsification equipment, add Appropriate amount of phosphoric acid or sodium carbonate, adjust the pH value of the colostrum to stabilize between 5-9, and then through the high-pressure homogenization equipment, the average particle size of the emulsion is further crushed to between 50-500nm, and the total volume of the emulsion reaches 100 grams. A stable emulsion can be obtained.

[0047] The above-mentioned diethylstilbestrol can also be other hormone steroid solid drugs such as testosterone, nandrolone phenylpropionate, daprazole, and mifepristone.

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Abstract

The present invention relates to orally taken oil-in-water emulsion with medicine in solid state at normal temperature and its preparation process. The emulsion contains solid state medicine, liquid state edible oil, lecithin, water soluble high molecular matter as assisting emulsifier, and is prepared through regulating emulsion particle size, regulating pH value, and other steps. It has stable physical performance, less stimulation to gastrointestinal tract, good taste and high bioavailability.

Description

technical field [0001] The present invention relates to an improved emulsion, in particular to an oil-in-water oral emulsion containing solid medicine at normal temperature. Background technique [0002] Because the emulsion can homogenize the original oil-water immiscible two-phase system into a relatively uniform homogeneous liquid system, its characteristics are for some oily or water-insoluble drugs to be prepared as a uniform preparation that exists in the form of an aqueous solution , is undoubtedly a good dosage form. The main surfactant used in lipid nanoparticles (LNP) is phospholipid or its derivatives or modifications, and the surface of the formed emulsion droplet has the effect of phospholipid bimolecular liquid crystal structure similar to biological cells. Outstanding biocompatibility and affinity, so emulsions with phospholipids as surfactants are more and more widely used in pharmaceutical emulsion preparations, and are generally administered as intravenous...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/44A61K45/00
Inventor 朱芳海
Owner 朱芳海
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