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Drug combination containing etoricoxib and preparation method thereof

A technology of etoricoxib and composition, which is applied in the field of pharmaceutical compositions containing etoricoxib and its preparation, can solve the problems such as inability to effectively guarantee tablet hardness, low drug dissolution rate, and reduced drug dissolution rate.

Active Publication Date: 2016-01-20
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent (CN200580037915) discloses a Wurster granulation method for the preparation of oral granules of etoricoxib, which fails to effectively improve the bioavailability
Chinese patent (CN201410212618) discloses etoricoxib tablets and its preparation method. The invention adopts powder direct compression method to prepare etoricoxib tablets, which simplifies the operation, but direct compression will lead to different hardness of the obtained tablets. Limit the disintegration time of the preparation and reduce the dissolution rate of the drug
International patent (WO2014033526) discloses a pharmaceutical composition containing etoricoxib, which has a low drug dissolution rate compared to the standard product
[0006] Those skilled in the art know that the water solubility of etoricoxib raw material is poor, and the dissolution rate of the drug with little solubility is greatly affected by its specific surface area and the surface properties of the finished drug product. Although the tablet prepared by powder direct compression is easy to operate, the tablet The hardness of the tablet cannot be effectively guaranteed. The tablet hardness is low and easy to break, which is not conducive to storage and transportation. If the hardness is too high, it is not conducive to the disintegration of the preparation and seriously affects the dissolution effect of the drug.
Tablets prepared by wet granulation were slower to disintegrate and release drug into the dissolution medium at a slower rate

Method used

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  • Drug combination containing etoricoxib and preparation method thereof
  • Drug combination containing etoricoxib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Prescription composition:

[0031] Name of raw material Percentage (%w / w) Amount of raw and auxiliary materials (g) etoricoxib 25.0% 50.0 Calcium hydrogen phosphate anhydrous 35.0% 70.0 microcrystalline cellulose 35.0% 70.0 Croscarmellose sodium (internal) 1.5% 3.0 Sodium carboxymethyl starch (inside) 0.5% 1.0 Magnesium stearate (inside) 0.5% 1.0　 Croscarmellose sodium (external) 1.5% 3.0 Sodium carboxymethyl starch (external) 0.5% 1.0 Magnesium stearate (external) 0.5% 1.0 made into tablets 200mg / tablet Makes 1000 pieces

[0032] Preparation:

[0033] a) Weighing: Mix 50g etoricoxib, 70g anhydrous calcium hydrogen phosphate, 3g croscarmellose sodium, 1g carboxymethyl starch sodium and 70g microcrystalline cellulose, then add 1g stearin Magnesium acid mixed to obtain mixture I;

[0034] b) Granulation: Mixture I is granulated with a pressure roller dry granulator to obtain Mixtur...

Embodiment 2

[0039] Prescription composition:

[0040] Name of raw material Percentage (%w / w) Amount of raw and auxiliary materials (g) etoricoxib 30.0% 60.0 Calcium hydrogen phosphate anhydrous 16.5% 33.0 microcrystalline cellulose 49.5% 99.0 Croscarmellose sodium (internal) 1.125% 2.25 Carboxymethyl starch press (internal) 0.375% 0.75 Magnesium stearate (inside) 0.5% 1.0 Croscarmellose sodium (external) 1.125% 2.25　 Carboxymethyl starch press (external) 0.375% 0.75 Magnesium stearate (external) 0.5% 1.0 made into tablets 200mg / tablet Makes 1000 pieces

[0041] Preparation:

[0042] a) Weighing: mix 60g etoricoxib, 33g anhydrous calcium hydrogen phosphate, 2.25g croscarmellose sodium, 0.75g carboxymethyl starch sodium and 99g microcrystalline cellulose, then add 1g Magnesium stearate is mixed to obtain mixture I;

[0043] b) Granulation: Mixture I is granulated with a pressure roller dry granulator...

Embodiment 3

[0048] Prescription composition:

[0049] Name of raw material Percentage (%w / w) Amount of raw and auxiliary materials (g) etoricoxib 40.0% 80.0 Calcium hydrogen phosphate anhydrous 42.0% 84.0 microcrystalline cellulose 14.0% 28.0 Croscarmellose sodium (internal) 0.975% 1.95 Sodium carboxymethyl starch (inside) 0.325% 0.65 Magnesium stearate (inside) 0.5% 1.0 Croscarmellose sodium (external) 0.975% 1.95　 What about carboxymethyl starch (external) 0.325% 0.65 Magnesium stearate (external) 0.5% 1.0 made into tablets 200mg / tablet Makes 1000 pieces

[0050] Preparation:

[0051] a) Weighing: Mix 80g etoricoxib, 84g anhydrous calcium hydrogen phosphate, 2.25g croscarmellose sodium, 0.75g carboxymethyl starch sodium and 28g microcrystalline cellulose, then add 1g hardened Magnesium fatty acid is mixed to obtain mixture I;

[0052] b) Granulation: Mixture I is granulated with a pressure roller...

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Abstract

The invention provides a drug combination containing etoricoxib and a preparation method thereof, wherein the drug combination disclosed by the invention contains 10 to 60 percent by weight of etoricoxib, 24 to 80 percent by weight of filler, 2 to 12 percent by weight of disintegrating agents, 1 to 8 percent by weight of lubricating agent and other pharmaceutically acceptable excipients, wherein the disintegrating agents are sodium carboxymethyl starch and croscarmellose sodium. The invention solves the problem that the dissolution rate of etoricoxib preparations is low, and by a specific technical solution, the etoricoxib drug combination with a high dissolution rate is obtained.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a pharmaceutical composition and a preparation method thereof, in particular to a pharmaceutical composition containing etoricoxib and a preparation method thereof. Background technique [0002] Etoricoxib (Etoricoxib) is a highly selective cyclooxygenase-2 (COX-2) inhibitor, chemical name: [5-chloro-2-(6-methylpyridin-3-yl)-3- (4-Methylsulfonylphenyl)pyridine], its structural formula is as follows: [0003] [0004] Etoricoxib has anti-inflammatory, antipyretic, and analgesic effects, and is suitable for treating the symptoms and signs of osteoarthritis in the acute and chronic phases, and can also treat acute gouty arthritis. Etoricoxib has been approved by the supervision and management department for clinical use as a non-steroidal anti-inflammatory drug, and its performance has been improved compared with traditional anti-inflammatory drugs. It is the only coxib that...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/444A61P29/00A61P19/02A61P19/06
Inventor 赵焰平吴昀王辉邓丽君卢迪刘亚男
Owner BEIJING TIDE PHARMA
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