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A kind of etoricoxib oral microemulsion preparation and preparation method thereof

A technology of etoricoxib and milk preparations, applied in anti-inflammatory agents, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of poor solubility and low bioavailability, and achieve the goal of masking bitterness, increasing solubility, and improving bioavailability Effect

Inactive Publication Date: 2019-07-26
JINAN KANGHE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve the problems of poor solubility of etoricoxib, low dissolution rate and low bioavailability, and adopt the form of preparing it into an oil-in-water oral microemulsion preparation to improve solubility and further improve bioavailability

Method used

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  • A kind of etoricoxib oral microemulsion preparation and preparation method thereof
  • A kind of etoricoxib oral microemulsion preparation and preparation method thereof
  • A kind of etoricoxib oral microemulsion preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Prescription composition:

[0035] Name of raw material percentage 10 prescription bottles etoricoxib 1％ 1g Soybean oil 3％ 3g polyoxyethylene castor oil 5％ 5g Propylene Glycol 4％ 4g polyethylene glycol 400 3％ 3g sodium benzoate 0.1％ 0.1g Deionized water 83.9％ 83.9g

[0036] Preparation Process:

[0037] (1) Take 1g of etoricoxib, add 3g of soybean oil to dissolve at room temperature;

[0038] (2) Add 5 g of polyoxyethylene castor oil, 4 g of propylene glycol and 3 g of polyethylene glycol 400 into (1), stir magnetically for 5 min, add about 28 g of deionized water, and continue stirring for 10 min to form a coarse milk;

[0039] (3) Transfer the mixture in (2) to a high-pressure homogenizer, add 0.1g of sodium benzoate, add the remaining 55.9g of deionized water, turn on the high-pressure homogenizer, perform high-pressure homogenization for 5 minutes, and repeat 3 times to prepare micro dairy products...

Embodiment 2

[0041] Prescription composition:

[0042] Name of raw material percentage 10 prescription bottles etoricoxib 1％ 1g Medium-chain triglycerides 5％ 5g ethyl oleate 2％ 2g

[0043] polyoxyethylene castor oil 7％ 7g glycerin 10％ 10g aspartame 0.1％ 0.1g lemon zest 0.25％ 0.25g sodium benzoate 0.2 0.2g distilled water 74.45％ 74.45g

[0044] Preparation Process:

[0045] (1) Take 1g etoricoxib, add 5g medium carbon chain triglycerides and 2g ethyl oleate to dissolve at room temperature;

[0046] (2) Add 7g of polyoxyethylene castor oil and 10g of glycerin to (1), sonicate for 10min, add 25g of distilled water and continue sonicating for 10min to form a coarse milk;

[0047] (3) Transfer the mixture in (2) to a high-pressure homogenizer, add 0.1g of aspartame, 0.25g of lemon essence, add the remaining 49.45g of distilled water, turn on the high-pressure homogenizer, homogenize under high pressure f...

Embodiment 3

[0049] Prescription composition:

[0050] Name of raw material percentage 100 prescription bottles etoricoxib 2％ 2g castor oil 10％ 10g Polyoxyethylene Hydrogenated Castor Oil 7％ 7g Propylene Glycol 10％ 10g aspartame 0.2％ 0.2g pineapple flavor 0.25％ 0.25g sodium benzoate 0.3％ 0.3g Deionized water 70.25％ 70.25g

[0051] Preparation Process:

[0052] (1) Take 2g of etoricoxib, add it to 10g of castor oil and heat to 40°C to dissolve;

[0053] (2) Add 7 g of polyoxyethylene castor oil and 10 g of propylene glycol into (1), stir mechanically for 10 min, add 23 g of deionized water, and continue stirring for 10 min to form a coarse milk.

[0054](3) Transfer the mixture in (2) to a high-pressure homogenizer, add 0.2g aspartame, 0.25g pineapple essence and 0.3g sodium benzoate, add the remaining 47.25g deionized water, turn on the high-pressure homogenizer, and Homogenize for 5 minutes and repeat 3 times to p...

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Abstract

The invention relates to an etoricoxib oral microemulsion preparation and a preparation method thereof. The weight percentage of each component in the invention is: etoricoxib 1-3%, oil phase 3-10%, emulsifier 3-10%, Co-emulsifier 3-10%, sweetener 0-0.2%, flavor 0-0.5%, preservative 0.1-0.5% and water 70-90%; the preparation method is: firstly add etoricoxib to the oil phase Dissolving; then adding emulsifiers and co-emulsifiers into the oil phase to form a coarse emulsion; finally transferring the coarse emulsion to a high-pressure homogenizer, adding water, and homogenizing under high pressure to prepare a microemulsion preparation. In the present invention, etoricoxib is wrapped in oil-in-water microemulsion droplets, which not only improves the bad taste of the drug, but also solves the problem of etoricoxib being difficult to dissolve in water, improves dissolution, and increases bioavailability; in addition, sweeteners are added and flavor, which increases the compliance of patients with medication; and the raw material medicine used in the preparation method does not need special treatment, no special equipment, simple operation, stable product quality, and is suitable for large-scale production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an etoricoxib oral microemulsion preparation and a preparation method thereof. Background technique [0002] Etoricoxib English name: Etoricoxib, Chinese chemical name: 5-chloro-2-(6-methylpyridin-3-yl)-3-(4-methylsulfonylphenyl)pyridine; physical state is white or White crystalline powder, soluble in ethanol, isopropyl acetate, ethanol and toluene, slightly soluble in isopropanol, almost insoluble in water (solubility in water 3.28×10 -3 g / L), half-life t 1 / 2 is 22h; its structure is as follows: [0003] [0004] This product is developed and produced by Merck. It was first launched in the UK in 2002. The approved indications are for the treatment of osteoarthritis, rheumatoid arthritis, musculoskeletal pain, postoperative pain, dysmenorrhea, arthritis, ankylosing Spondylitis, a selective COX-2 inhibitor, has anti-inflammatory, analgesic and antipyretic effects, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/444A61K47/44A61K47/14A61K47/26A61K47/10A61P19/02A61P29/00
Inventor 张颖杨江勇杨延昆彭艳丽应杰杰
Owner JINAN KANGHE MEDICAL TECH
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