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, non-central analgesics, drug delivery, 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: 2013-02-13
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 percent):

[0033] etodolac 62.4%

[0034] NaCl 15.6%

[0035] Polyoxyethylene N80 15.6%

[0036] Na 2 CO 3 5.5%

[0037] 95% ethanol solution appropriate amount

[0038] Sodium stearate fumarate balance

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

[0040] Cellulose acetate 71.4%

[0041] PEG4000 28.6%

[0042] The solvent prescription (percentage by weight) of dissolving coating film material:

[0043] Acetone 96.2%

[0044] Water 3.8%

[0045] Preparation Process:

[0046] Mix the prescribed amount of medicine with NaCl, N80, Na 2 CO 3Mix evenly, make soft material with 95% ethanol solution as binder, granulate with 20-mesh sieve, dry the wet granules, granulate with 18-mesh sieve, add lubricant sodium stearate fumarate to the dry granules, mix well and press One piece is the core. Dissolve cellulose acetate and porogen polyethylene glycol 4000 in a mixed solvent of acetone-water...

Embodiment 2

[0048] Tablet core prescription (weight percent):

[0049] etodolac 60.9%

[0050] NaCl 15.2%

[0051] Polyoxyethylene N80 15.2%

[0052] Na 2 CO 3 7.6%

[0053] 95% ethanol solution appropriate amount

[0054] Sodium stearate fumarate balance

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

[0056] Cellulose acetate 71.4%

[0057] PEG4000 28.6%

[0058] The solvent prescription (percentage by weight) of dissolving coating film material:

[0059] Acetone 96.2%

[0060] Water 3.8%

[0061] Preparation Process:

[0062] Mix the prescribed amount of medicine with 80 sieved NaCl, N80, Na 2 CO 3 Mix evenly, make soft material with 95% ethanol solution as binder, granulate with 20-mesh sieve, dry the wet granules, granulate with 18-mesh sieve, add lubricant sodium stearate fumarate to the dry granules, mix well and press One piece is the core. Dissolve cellulose acetate and porogen polyethylene glycol 4000 in a mixed solvent of acet...

Embodiment 3

[0064] Tablet core prescription (weight percent):

[0065] etodolac 65.5%

[0066] NaCl 19.6%

[0067] Polyoxyethylene N80 8.2%

[0068] Na 2 CO 3 5.7%

[0069] 95% ethanol solution appropriate amount

[0070] Sodium stearate fumarate balance

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

[0072] Cellulose acetate 76.9%

[0073] PEG4000 23.1%

[0074] The solvent prescription (percentage by weight) of dissolving coating film material:

[0075] Acetone 97.1%

[0076] Water 2.9%

[0077] Preparation Process:

[0078] Mix the prescribed amount of medicine with 80 sieved NaCl, N80, Na 2 CO 3 Mix evenly, make soft material with 95% ethanol solution as binder, granulate with 20-mesh sieve, dry the wet granules, granulate with 18-mesh sieve, add lubricant sodium stearate fumarate to the dry granules, mix well and press One piece is the core. Dissolve cellulose acetate and porogen polyethylene glycol 4000 in a mixed solvent of acet...

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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 released easily 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 an etodolac osmotic pump type controlled release preparation and a preparation method thereof. Background technique [0002] Etodolac is a potent non-steroidal anti-inflammatory drug (NSAIDs) synthesized in the 1960s, which differs from other NSAIDs in that it has a tetrahydropyranyl ring , are pyrancarboxylic acid NSAIDs. Etodolac is a new generation of cyclooxygenase-2 (COX-2) highly selective inhibitor, its advantage is that it has high and suitable COX-2 selectivity, and has little effect on COX-1 within the therapeutic dose , which protects the gastrointestinal mucosa while exerting a potent anti-inflammatory effect; its other advantage lies in the protective effect on human chondrocytes, and the in vitro study of Henrotin Y provides evidence that etodolac maintains cartilage integrity under inflammatory conditions . Etodolac is approved to control the s...

Claims

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Application Information

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Patent Type & Authority Patents(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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