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Method for preparing micro-particle-size water(W)/oil(O)/water(W) multiple emulsion carrying medicine

A technology of multiple emulsions and multiple emulsions, which is applied in the fields of emulsion delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problem of reducing lymph affinity, the advantages of targeted release, poor emulsion stability, and not being too intense To achieve the effect of improving stability and bioavailability, mild operating conditions, and narrow particle size distribution

Inactive Publication Date: 2012-02-29
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The traditional preparation methods of multiple emulsions mainly include mechanical stirring, homogenization, ultrasonic emulsification, membrane emulsification, etc. These methods are relatively intense, but not too intense, because excessive shearing will cause the emulsion droplets to be excessively broken up and cannot form. Double emulsion structure, or cause the demulsification of the inner milk (also known as colostrum) phase, so the emulsion droplets of multiple emulsions prepared by these methods are relatively large (generally between 10-100 microns), and the particle size is very uneven
According to the theory of colloids and emulsions, the larger the particle size of the emulsion, the lower the uniformity, and the worse the stability of the emulsion, and the larger the particle size of multiple emulsion droplets, it will significantly reduce its drug absorption and lymph affinity. , targeted release and other advantages

Method used

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  • Method for preparing micro-particle-size water(W)/oil(O)/water(W) multiple emulsion carrying medicine
  • Method for preparing micro-particle-size water(W)/oil(O)/water(W) multiple emulsion carrying medicine
  • Method for preparing micro-particle-size water(W)/oil(O)/water(W) multiple emulsion carrying medicine

Examples

Experimental program
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Embodiment 1

[0026] Preparation of Microemulsion Droplets W / O / W Multiple Emulsions Encapsulating Vitamin C

[0027] 1) Weigh the amount of vitamin C and sodium chloride (mass percentage between 0.05% and 1%), and dissolve them in an appropriate amount of deionized water at a temperature in the range of 10-80°C and stirring at 1000rpm, Insulated storage; weigh 0.1%-30% mass concentration of polyoxyethylene (30) dipolyhydroxystearate (trade name Arlacel P135) and dissolve it in refined peanut oil at a temperature of 10-80°C and stirring at 1000rpm , mix the water phase and the oil phase, emulsify with a high-speed shear method of 5000-10000rpm, and obtain a W / O primary emulsion (hereinafter referred to as colostrum) with vitamin C in the inner water phase;

[0028] 2) Weigh a 1:1 compound of Tween 80 and Span 80 with a mass concentration of 0.1%-20% and dissolve it in deionized water at a temperature of 10-80°C and stirring at 1000rpm as the external water phase, Then add the colostrum prep...

Embodiment 2

[0031] Preparation of W / O / W Multiple Emulsions of Small-sized Emulsion Droplets Encapsulating Anticancer Drug Retinoic Acid

[0032]1) Weigh the formula amount of retinoic acid and sodium chloride (mass percentage between 0.1%-1%), and dissolve it in an appropriate amount of deionized water under the temperature condition in the range of 10-80°C and stirring at 1000rpm, Weigh the 1:9 compound of 0.1%-30% Tween 80 and Span 80 and dissolve it in liquid paraffin at a temperature of 10-80°C and stirring at 1000rpm, mix the water phase and the oil phase, and use 5000-10000rpm high-speed shear method for emulsification to obtain a W / O primary emulsion (hereinafter referred to as colostrum) with retinoic acid in the inner water phase;

[0033] 2) Weigh a 1:1 compound of Tween 80 and Span 80 with a mass concentration of 0.1%-20% and dissolve it in deionized water at a temperature of 10-80°C and stirring at 1000rpm as the external water phase, Then add the colostrum prepared in step 1...

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Abstract

The invention discloses a method for preparing micro-particle-size W / O / W multiple emulsion carrying a medicine, which belongs to the technical field of medicinal preparations. The method comprises three steps: 1, dissolving the medicine to be carried and electrolyte for providing a osmotic pressure condition in a water phase together, emulsifying the water phase and an oil phase containing lipophilic emulsion stabilizer, and obtaining W / O initial emulsion; 2, mixing the initial emulsion and an external water phase containing a hydrophilic emulsion stabilizer, roughly dispersing and obtaining coarse multiple emulsion with a big particle size; and 3, diluting the coarse emulsion with deionized water, stirring gently, and obtaining the multiple emulsion product with a micro particle size. The principle of the preparation method is to promote emulsion drops of the coarse multiple emulsion to expand and break under a diluted condition by regulating the osmotic pressure of the internal water phase of the multiple emulsion so as to produce the multiple emulsion drops with a particle size of 1 to 10 micro meters. In the invention, the operation conditions are mild, the particle sizes of the multiple emulsion drops are small, the particle size range is narrow, the medicine entrapment rate is high, the stability of the preparation is high, the controlled-release and sustained-release effects on the carried medicine are good, and the lymph affine effect and targeted release effect of the emulsion are played more fully.

Description

technical field [0001] The invention relates to a method for preparing a W / O / W multiple emulsion with a small particle size loaded with drugs, relates to a method for preparing multiple emulsions of various water-soluble drugs, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] Multiple emulsions refer to multiple emulsions formed by dispersing one emulsion product in another continuous phase. Compared with simple emulsions that have only one dispersed phase and one continuous phase, multiple emulsions have a dispersed phase 1 / The multi-compartment structure of dispersed phase 2 / continuous phase 3 can realize more functions. For example, easily degradable bioactive substances or functional components that are not suitable for direct contact with air, light, digestive tract or digestive media can be embedded in dispersed phase 1 or dispersed phase 2 according to their solubility, and then loaded into continuous phase 3 , so that...

Claims

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Application Information

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IPC IPC(8): A61K9/113A61K47/14A61K47/22A61K47/24A61K47/26A61K47/34
Inventor 魏慧贤崔正刚高海燕
Owner JIANGNAN UNIV
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