Etodolac osmotic pump type controlled-release preparation and preparation thereof

A technology of etodolac and controlled-release preparations, applied in the directions of anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of increased difficulty in the development of osmotic pump tablets, poor solubility, pH dependence, and large therapeutic doses, etc. The effect of achieving long-lasting blood drug concentration, reducing the number of medication times, and stabilizing blood drug concentration

Inactive Publication Date: 2008-09-10
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The large therapeutic dose of etodolac has poor solubility and pH dependence, which makes the development of osmotic pump tablets more difficult

Method used

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  • Etodolac osmotic pump type controlled-release preparation and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Tablet core prescription (weight percentage):

[0033] Etodolac 62.4%

[0034] NaCl 15.6%

[0035] Polyoxyethylene N80 15.6%

[0036] Na 2 CO 3 35.5%

[0037] 95% ethanol solution

[0038] Sodium fumarate stearate balance

[0039] Semi-permeable membrane prescription (weight percentage):

[0040] Cellulose acetate 71.4%

[0041] PEG4000 28.6%

[0042] Solvent prescription for dissolving coating film material (weight percentage):

[0043] Acetone 96.2%

[0044] Water 3.8%

[0045] Preparation Process:

[0046] Combine the prescribed amount of medicine with NaCl, N80, and Na 2 CO 3 Mix well, use 95% ethanol solution as binder to make soft material, granulate with 20-mesh sieve, after the wet granules are dried, use 18-mesh sieve to sizing, dry granules and lubricant sodium stearate fumarate, mix and press The tablet is the core. Dissolve cellulose acetate and pore-forming agent polyethylene glycol 4000 in a mixed solvent of acetone-water, and coat the tablet cores...

Embodiment 2

[0048] Tablet core prescription (weight percentage):

[0049] Etodolac 60.9%

[0050] NaCl 15.2%

[0051] Polyoxyethylene N80 15.2%

[0052] Na 2 CO 3 7.6%

[0053] 95% ethanol solution

[0054] Sodium fumarate stearate balance

[0055] Semi-permeable membrane prescription (weight percentage):

[0056] Cellulose acetate 71.4%

[0057] PEG4000 28.6%

[0058] Solvent prescription for dissolving coating film material (weight percentage):

[0059] Acetone 96.2%

[0060] Water 3.8%

[0061] Preparation Process:

[0062] Combine the prescribed amount of medicine with NaCl, N80, and Na 2 CO 3 Mix well, use 95% ethanol solution as binder to make soft material, granulate with 20-mesh sieve, after the wet granules are dried, use 18-mesh sieve to sizing, dry granules and lubricant sodium stearate fumarate, mix and press The tablet is the core. Dissolve cellulose acetate and pore-forming agent polyethylene glycol 4000 in a mixed solvent of acetone-water, and coat the tablet core with ...

Embodiment 3

[0064] Tablet core prescription (weight percentage):

[0065] Etodolac 65.5%

[0066] NaCl 19.6%

[0067] Polyoxyethylene N80 8.2%

[0068] Na 2 CO 3 5.7%

[0069] 95% ethanol solution

[0070] Sodium fumarate stearate balance

[0071] Semi-permeable membrane prescription (weight percentage):

[0072] Cellulose acetate 76.9%

[0073] PEG4000 23.1%

[0074] Solvent prescription for dissolving coating film material (weight percentage):

[0075] Acetone 97.1%

[0076] Water 2.9%

[0077] Preparation Process:

[0078] Combine the prescribed amount of medicine with NaCl, N80, and Na 2 CO 3 Mix well, use 95% ethanol solution as binder to make soft material, granulate with 20-mesh sieve, after the wet granules are dried, use 18-mesh sieve to sizing, dry granules and lubricant sodium stearate fumarate, mix and press The tablet is the core. Dissolve cellulose acetate and pore-forming agent polyethylene glycol 4000 in a mixed solvent of acetone-water, coat the tablet core with a co...

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Abstract

The invention belongs to the pharmaceutical preparation field and discloses an osmotic pump type controlled release preparation of etodolac and a preparation method thereof. An osmotic pump tablet comprises a tablet core and a controlled release semipermeable coating film that is coated outside the tablet core and with a hole for releasing drug. The tablet core comprises materials by following weight percentage: 60.9 to 65.5 percent of etodolac, 27.1 to 31.2 percent of osmotic pressure active material, 5.5 to 8.0 percent of an auxiliary material that can ensure the basic remedy to be releasedeasily and the rest is other auxiliary materials. The osmotic pump controlled release semipermeable coating film comprises by materials by following weight percentage: 71.4 to 76.9 percent of semipermeable high molecular coating material and 23.1 to 28.6 percent of pore-forming agent. The manners of pore-forming include a mechanical drilling and a laser boring. By adjusting the prescription of the tablet core and the coating film in the invention, the speed of constant release of drug can be effectively regulated so as to obtain a steadier, lasting and effective blood concentration, thus reducing the side effect of drug and times of dosage, and promoting the compliance of a sufferer. The osmotic pump type controlled release preparation of etodolac of the invention can be widely used for treating diseases like rheumatoid arthritis, arthritis deformans and osteoarthritisetc.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to etodolac osmotic pump type controlled release preparations and a preparation method thereof. Background technique [0002] Etodolac (etodolac) is a powerful non-steroidal anti-inflammatory drug (NSAIDs) synthesized in the 1960s. The difference from other non-steroidal anti-inflammatory drugs is that it has a tetrahydropyran parent ring , Is pyran carboxylic acid NSAIDs. Etodolac is a new generation of cyclooxygenase-2 (COX-2) highly selective inhibitor. Its advantage is that it has high and appropriate COX-2 selectivity and has minimal impact on COX-1 within the therapeutic dose. It protects the gastrointestinal mucosa while exerting a potent anti-inflammatory effect; its other advantage lies in its protective effect on human chondrocytes. The in vitro study of Henrotin Y provides evidence that etodolac maintains cartilage integrity under inflammatory conditions . Et...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/407A61P29/00
Inventor 潘卫三李兴凯杨星钢聂淑芳周丽莹关津
Owner SHENYANG PHARMA UNIVERSITY
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