Patent EA-001506-B1 (EA)
Title: Coated trimebutine maleate tablet
Inventor: BENKERROUR LOUTFY
IPC: A61K9/30
Filed: 1997-07-11
Abstract: 1. A tablet for oral delivery, including a core containing trimebutine maleate as an active principle, at least one excipient, at least one binder, at least one acidifiant and additives for technological purposes, characterized in that the core has a water-soluble coating amount to 1 to 5% of the core weight, at least one water-soluble film-forming substance selected from the group containing acrylic polymers and cellulose polymers, such as hydroxypropylmethyl cellulose with viscosity comprising 2,5 to 15000 mPa.s, methylcellulose, ethylcellulose, hydroxypropylcellulose, and at least one substance, giving opacity selected from the group comprising ferric oxide and titanium oxide, said core components are used in the following ratio: trimebutine maleate 30 - 60 at least one excipient 15 - 45 at least one binder 2,5 - 25 at least one acidifiant 0,5 - 25 technological agents 0,75 - 7,5, of which 0,5 - 5% is a substance giving viscosity and 0,25 - 2,5% is a lubricant. 2. A tablet for oral delivery of claim 1, characterized in that the core further comprises 1 to 5% of at least one disintegration agent. 3. A tablet for oral delivery of claims 1 and 2, characterized in that the coating further comprises at least one softener, selected from the group comprising a macrogel with an average molecular weight 3000 to 6000, propylene glycol and polyoxyl 40 stearate. 4. A tablet for oral delivery of claims 1 to 3, characterized in that the coating further comprises an agent increasing its adhesion to the core selected from the group comprising lactose and microcrystalline cellulose. 5. A tablet for oral delivery of claims 1 to 4, characterized in that comprises a tartaric acid as an acidifiant in the amount of 0,5 to 2% enhancing quick release of trimebutine maleate or in the amount of 10 to 20% for prolonged release of trimebutine maleate. 6. A tablet for oral delivery of claims 1 to 4, characterized in that the coating comprises a mixture of hydroxypropylmethylcelluose with viscosity 2,5 to 17,5 mPa.s and titanium dioxide, or a mixture of hydroxypropylmethylcelluose with said viscosity, lactose or microcrystalline cellulose, polylethelene glycol with molecular weight 4000 or polyoxyl 40 stearate and titanium dioxide. 7. A tablet of quick disintegration, comprising a coated core of 200 or 400 mg and containing components of the following ratio: trimebutine maleate 50,00 lactose monohydrate 36,00 corn starch 7,00 hydroxypropylmethylcelluose (6 mPa.s) 1,00 sodium carboxymethylstarch 2,00 tartaric acid 1,00 silica gel 2,00 magnesium stearate 1,00 wherein the coating amounts 2% of the core weight and comprises hydroxypropylmethylcelluose (6 mPa.s), lactose, polylethelene glycol 4000 and titanium dioxide or hydroxypropylmethylcelluose (6 mPa.s), microcrystalline cellulose, polyoxyl 40 stearate and titanium dioxide. 8. A tablet of quick disintegration, comprising a coated core of 747 or 508 mg and containing components of the following ratio: trimebutine maleate 39,37 lactose monohydrate 23,60 corn starch 7,00 hydroxypropylmethylcelluose (4000 mPa.s) 1,00 sodium carboxymethylstarch 2,00 tartaric acid 1,00 silica gel 2,00 magnesium stearate 1,00 wherein the coating amounts 2% of the core weight and comprises hydroxypropylmethylcelluose (6 mPa.s) and titanium dioxide or hydroxypropylmethylcelluose (6 mPa.s), lactose, polyoxyl 40 stearate and titanium dioxide. 9. A process for preparing a tablet for oral delivery comprising mixing trimebutine maleate and inert components in a powder mixture or in an apparatus with a boiling bed and subsequent granulation of thus obtained homogeneous mixture with an aqueous solution of acidifiant to obtain wet granules, drying them in a boiling bed or in a ventilating drier at 60 degree C, their calibration, mixing in a powder mixture with silica gel and magnesium stearate and preparing a core by pressing the obtained granules on a rotation tablet-making machine with punches of the needed size, characterized in that a suspension is applied on the core in a centrifugal machine as of claims 1 to 6 at 35 to 45 degree C under conditions providing forming a uniform coating on the core, amounting 2% of the core weight.