Patent EA-003335-B1 (EA)
Title: Method for preparing an effervescent granulate comprising iron gluconate, granulate thus obtained and tablets containing the same
Inventor: CATALANO RICCARDO
IPC: A61K9/16
Filed: 1999-12-17
Abstract: 1. A method for preparing an effervescent granulate comprising a pharmacologically active ingredient, and citric acid and sodium bicarbonate as effervescent system, by means of wet granulation in a fluid-bed granulator, comprising the steps of: I. feeding a mixture comprising said active ingredient, citric acid and sodium bicarbonate into the said granulator which is simultaneously fed with a flow of air heated to about 70 degree C(+3 degree C) and having a moisture content of < 1.0 g/kg; II. wetting the said mixture with nebulized water; III. evaporating off the nebulizing water; characterized in that said mixture includes ferrous gluconate (2) as said pharmacologically active ingredient, and said step II is carried out when said mixture has reached a temperature of about 35 degree C(+3 degree C), and in said step III the temperature of said mixture is kept substantially constant at 35 degree C(+3 degree C), the method further comprising the following steps: IV. repeating steps II and III until a granulate with the desired features is obtained; and drying the said granulate with air heated to about 80 degree C(+3 degree C) until its moisture content is <=0.5% by weight, 2. A method according to claim 7, characterized in that, in step I, the magnitude of the air flow rate is between 3200 and 3800 m<3>/hour for each batch of about 265 kg of mixture to be granulated. 3. A method according to claim 1 or 2, characterized in that, in step II, the flow rate of nebulized water is preferably between 500 and 2000 ml/min. 4. A method according to any one of the preceding claims 1 to 3, characterized in that, in step II, the pressure of the flow of nebulized water is about 3 atmospheres. (3 x 1.013 bar). 5. A method according to any of claims 1 to 4, characterized in that tile total amount of water used in step II does not exceed 2% by weight of the mixture to be granulated. 6. A method according to any of claims 1 to 5, characterized in that the amount of nebulized water in each step does not exceed 0.5% by weight of the mass being processed. 7. An effervescent granulate obtained according to any of the preceding claims, comprising from 7 to 35% by weight of ferrous gluconate(2), from 25 to 45% by weight of citric acid and from 15 to 25% by weight of sodium bicarbonate. 8. An effervescent granulate according to claim 7, characterized in that it also comprises from 5 to 18% by weight of sorbitol, about 2% by weight of L-leucine and from 5 to 18% by weight of flavourings. 9. A granulate according to claim 7, characterized in that the ferrous gluconate is in the form of the dihydrate. 10. A tablet obtained by tabletting an effervescent granulate which is obtained according to any one of the preceding claims 1 to 6, the said tablet comprising from 7 to 35% by weight of ferrous gluconate, from 25 to 45% by weight of citric acid, from 15 to 25% by weight of sodium bicarbonate, from 5 to 18% by weight of sorbitol, about 2% by weight of L-leucine and from 5 to 11% by weight of flavourings.