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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 low bioavailability and poor solubility, and achieve the effects of increasing solubility, masking bitter taste, and improving dissolution rate

Inactive Publication Date: 2016-02-24
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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  • Etoricoxib oral microemulsion preparation and preparation method thereof
  • Etoricoxib oral microemulsion preparation and preparation method thereof
  • 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 f...

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...

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-pre...

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Abstract

The invention relates to an etoricoxib oral microemulsion preparation and a preparation method thereof. The etoricoxib oral microemulsion preparation comprises the following components in percentage by weight: 1-3% of etoricoxib, 3-10% of oil phase, 3-10% of emulsifier, 3-10% of co-emulsifier, 0-0.2% of sweetening agent, 0-0.5% of essence, 0.1-0.5% of preservative and 70-90% of water. The preparation method comprises the following steps: firstly, adding the etoricoxib in the oil phase and dissolving; secondly, adding the emulsifier and the co-emulsifier in the oil phase to form crude emulsion; and finally, transferring the crude emulsion into a high-pressure homogenizer, adding water, and homogenizing under high pressure to obtain the microemulsion preparation. Oil-in-water type microemulsion liquid drops wrap the etoricoxib, bad taste of medicines is improved, the problem that the etoricoxib is difficultly dissolved into water is solved, dissolution is improved, and bioavailability is also improved. In addition, through addition of the sweetening agent and the essence, medication compliance of a patient is improved. Raw materials used in the preparation do not need to be subjected to special treatment, special equipment is not required, the preparation method is easy to operate, quality of products is stable, and the etoricoxib oral microemulsion preparation 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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IPC IPC(8): A61K9/107A61K31/444A61K47/44A61K47/14A61K47/26A61K47/10A61K47/34A61P19/02A61P29/00
Inventor 张颖杨江勇杨延昆彭艳丽应杰杰
Owner JINAN KANGHE MEDICAL TECH
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