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Naproxen orally-taken micro-emulsion preparation and preparation method thereof

A technology of emulsion preparation and naproxen, which is applied in anti-inflammatory agents, emulsion delivery, non-central analgesics, etc., can solve the problems of unstable drug content, cumbersome preparation process, and short biological half-life, so as to improve bioavailability High degree, broad application prospects, and simple production process

Inactive Publication Date: 2011-04-06
XUZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because naproxen is almost insoluble in water, its biological half-life is short, and its oral administration dose is large, it will cause different degrees of gastrointestinal adverse reactions after oral administration, and it also has certain toxicity to the kidney and heart, and its bioavailability is low.
Making naproxen into sustained-release preparations or enteric-coated preparations can reduce gastrointestinal adverse reactions, but the preparation process is relatively cumbersome due to the coating method used in the production process; it is made into ordinary tablets and capsules, and after oral administration The bioavailability is not high; it is inconvenient to make a suppository for administration; it is easy to prepare a drop pill, but the drug content is unstable; the gel transdermal drug delivery preparation and transdermal patch are inconvenient to use, easily pollute clothes, and have no effect slow

Method used

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  • Naproxen orally-taken micro-emulsion preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Take 1.8g of naproxen, 8.0g of medium-chain triglycerides, 30.0g of emulsifier Tween 8030.0g and 10.0g of co-emulsifier polyethylene glycol-400 (PEG-400) and heat to 25°C, stir and mix to obtain the oil phase ; Measure 55.0ml of water for injection, 66.7mg of sodium sulfite, and 69.0mg of xylitol, stir to dissolve, and heat to 25°C to obtain an aqueous phase. Stir and mix the oil phase and the water phase at a temperature of 25° C., filter to obtain a microemulsion, fill, stopper, cap, and sterilize at 121° C. for 15 minutes to obtain naproxen oral microemulsion. The average particle diameter of the microemulsion is (38.6±2.0) nm, the content of naproxen is 1.77% (W / V), and other indexes meet the requirements of pharmaceutical oral microemulsion.

Embodiment 2

[0032] Take 1.0g of naproxen, 5.0g of medium-chain triglycerides, 2.5g of emulsifier Tween 802.5g and 7.5g of 1,2-propanediol and heat to 25°C and stir to obtain an oil phase; measure 70.0ml of water for injection, sodium sulfite 69.6 mg and 87.00 mg of aspartose were stirred to dissolve, and heated to 25°C to obtain an aqueous phase. Stir and mix the oil phase and the water phase at a temperature of 25° C., filter to obtain a microemulsion, fill, stopper, cap, and sterilize at 121° C. for 15 minutes to obtain naproxen oral microemulsion. The average particle size of the microemulsion is (19.0±2.1) nm, the content of naproxen is 0.99% (W / V), and other indexes meet the requirements of pharmaceutical oral microemulsion.

Embodiment 3

[0034] Take 1.0 g of naproxen, 6.0 g of macrogol glycerol oleate (Labrafil M1944CS), 16.0 g of emulsifier polyoxyethylene castor oil (CremophorEL) and 8.0 g of co-emulsifier 1,2-propylene glycol and heat to 25° C. Mix well to obtain an oil phase; measure 75.0 ml of water for injection, 75.0 mg of sodium metabisulfite, and 80.0 mg of xylitol, stir to dissolve, and heat to 25°C to obtain an aqueous phase. Stir and mix the oil phase and the water phase at a temperature of 25° C., filter to obtain a microemulsion, fill, stopper, cap, and sterilize at 121° C. for 15 minutes to obtain naproxen oral microemulsion. The average particle diameter of the microemulsion is (29.8±1.5) nm, the content of naproxen is 0.96% (W / V), and other indexes meet the requirements of pharmaceutical oral microemulsion.

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Abstract

The invention relates to an orally-taken micro-emulsion preparation and a preparation method thereof, in particular a naproxen orally-taken micro-emulsion preparation and a preparation method thereof, belonging to the technical field of medicines. The orally-taken micro-emulsion preparation uses naproxen as the main pharmacological ingredient and contains medicinal oil, emulsifier, assistant emulsifier and water for injection. The naproxen orally-taken micro-emulsion preparation is orally administrated and has clear appearance; the grain diameter evenly ranges within 10nm-100nm; all phase are of the same property and have thermodynamic stability; the medicine loading rate ranges from 0.0%-3.5%; the preparation process is simple; and the quality is stable and can be easily controlled. The naproxen prepared into the orally-taken micro-emulsion preparation can be absorbed through lymphatic vessels as a result of lower surface tension of the micro-emulsion, therefore, the first-pass effect of the liver and obstacles for macromolecule to pass through the gastrointestinal tract epithele cell membranes can be overcome.

Description

technical field [0001] The invention relates to an oral microemulsion in the field of pharmaceutical technology and a preparation method thereof, in particular to a naproxen oral microemulsion preparation and a preparation method thereof. Background technique [0002] Naproxen, whose chemical name is (+) α-methyl-6-methoxy-2-naphthalene acetic acid, is a non-steroidal aromatic propionic acid successfully developed by Syntex Co. Antipyretic analgesic anti-inflammatory drug. Naproxen is a reversible inhibitor of cyclooxygenase, which acts by inhibiting the conversion of arachidonic acid to thromboxane and various prostaglandins mediated by cyclooxygenase. Its chemical structural formula is as follows: [0003] [0004] Naproxen has been widely used all over the world because of its good analgesic and anti-inflammatory effects and few adverse reactions. Because oral administration is convenient and the dose is easy to control, it is the most commonly used route of adminis...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/192A61P29/00
Inventor 刘毅印晓星庄雪梅刘莉张玲刘玲尹翠缑灵山陈效毅
Owner XUZHOU MEDICAL COLLEGE
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