Dexketoprofen tromethamine sustained release particles and preparation method and sustained release medicinal preparation thereof

A technology of dexketoprofen tromethamine and sustained-release microparticles, applied in the field of medicine, can solve the problems of large side effects of dexketoprofen tromethamine, ulcers or bleeding symptoms, etc. Small concentration, the effect of reducing side effects

Active Publication Date: 2014-02-26
西安远大德天药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, dexketoprofen tromethamine has relatively large side effects. Long-term application can cause gastrointestinal ulcers or bleeding symptoms, and gastrointestinal pain, indigestion, diarrhea, dry mouth, lethargy, headache, dizziness, and excessive sweating can also occur. Wait

Method used

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  • Dexketoprofen tromethamine sustained release particles and preparation method and sustained release medicinal preparation thereof
  • Dexketoprofen tromethamine sustained release particles and preparation method and sustained release medicinal preparation thereof
  • Dexketoprofen tromethamine sustained release particles and preparation method and sustained release medicinal preparation thereof

Examples

Experimental program
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Embodiment 1

[0034] The dexketoprofen trometamol slow-release microparticles of the present embodiment are made by coating the dexketoprofen trometamol microparticles with a coating solution; the dexketoprofen trometamol microparticles are combined with The mass ratio of coating liquid is 1: 1; Described dexketoprofen tromethamine microparticle is made of the raw material of following percentage by weight: dexketoprofen tromethamine 10%, diluent 60%, stable Agent 10%, binding agent 20%; Described coating solution is made of the raw material of following percentage by weight: coating material 2%, porogen 5%, solvent 93%; Described diluent is microcrystalline cellulose; The stabilizer is sodium bisulfite; the binder is water; the coating material is ethyl cellulose; the porogen is polyvinylpyrrolidone; the solvent is ethanol with a mass purity of 95% .

[0035] The preparation method of the dexketoprofen trometamol slow-release microparticles of the present embodiment is:

[0036] Step 1, pr...

Embodiment 2

[0045] This embodiment is the same as Example 1, except that the diluent is lactose, starch or mannitol, or at least two of microcrystalline cellulose, lactose, starch and mannitol; the stabilizer Cystine, cysteine ​​or hydrochloric acid with a concentration of 0.5mol / L to 2mol / L, or cystine, cysteine, sodium bisulfite and hydrochloric acid with a concentration of 0.5mol / L to 2mol / L At least two kinds of hydrochloric acid; the binder is a hydroxypropyl methylcellulose aqueous solution with a mass concentration of 0.5% to 8%, an aqueous starch solution with a mass concentration of 1% to 10%, or a starch aqueous solution with a mass concentration of 1% to 10% % dextrin aqueous solution; the coating material is cellulose acetate, cellulose acetate derivatives (such as: cellulose acetate phthalate (CAP), cellulose acetate tetrahydrophthalate (CATH ) and cellulose acetate methyltetrahydrophthalate (CAMT), etc.), polyacrylic resin, shellac or waxes (such as: glyceryl monostearate, e...

Embodiment 3

[0047] The dexketoprofen trometamol slow-release microparticles of the present embodiment are made by coating the dexketoprofen trometamol microparticles with a coating solution; the dexketoprofen trometamol microparticles are combined with The mass ratio of coating liquid is 4: 1; Described dexketoprofen tromethamine microparticle is made of the raw material of following percentage by weight: dexketoprofen tromethamine 30%, diluent 35%, stable Agent 5%, binding agent 30%; Described coating liquid is made of the raw material of following percentage by weight: coating material 10%, porogen 1%, plasticizer 2%, solvent 87%; Described diluent It is microcrystalline cellulose and starch; the stabilizer is cysteine; the binder is water; the coating material is polyacrylic acid resin; the porogen is polyethylene glycol; The plasticizer is glycerol triacetate; the solvent is water.

[0048] The preparation method of the dexketoprofen trometamol slow-release microparticles of the pres...

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Abstract

The invention discloses dexketoprofen tromethamine sustained release particles which are prepared by coating the dexketoprofen tromethamine sustained release particles with coating liquid, wherein the mass ratio of the dexketoprofen tromethamine sustained release particles to the coating liquid is 1-10:1, the dexketoprofen tromethamine sustained release particles are prepared from the following raw materials by weight: 10-50% of dexketoprofen tromethamine, 15-60% of diluent, 0-10% of stabilizer and 20-40% of adhesive, and the coating liquid is prepared from the following raw materials by weight: 2-20% of coating material, 0-5% of porogen, 0-5% of plasticizer and 70-97% of solvent. In addition, the invention also discloses a preparation method and sustained release medicinal preparation of the dexketoprofen tromethamine sustained release particles. After being taken, the dexketoprofen tromethamine sustained release particles can widely spread in gastrointestinal tract, and medicines are released slowly and continuously, so that irritation of the medicines to gastrointestinal tract can be reduced, even eliminated.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to dexketoprofen tromethamine sustained-release microparticles, a preparation method thereof and a sustained-release preparation. Background technique [0002] Ketoprofen is a derivative of ibuprofen, its chemical name is 2-(3-benzoylphenyl) propionic acid, also known as m-benzoyl hydrogenated atropic acid, a 2-aryl propionic acid non-steroidal anti-inflammatory drugs (NSAIDs). In 1972, it was successfully developed and listed by Rhone-poulenc company in France. In addition to inhibiting cyclooxygenase, it also has the effect of inhibiting lipoxygenase and reducing bradykinin, thereby reducing the pain sensation at the site of inflammatory injury. There are many domestic documents and patents about the dosage form of ketoprofen at present. The patent No. is 97112580.5, the patent called Ketoprofen Sustained-release Tablet and its process method discloses a kind of t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/52A61K31/192A61K47/44A61K47/38A61K47/36A61K47/34A61K47/32A61P29/00
Inventor 唐星王亚轩
Owner 西安远大德天药业股份有限公司
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