Patent EA-000853-B1 (EA)
Title: Hydrolyzed cellulose granulations for pharmaceuticals
Inventor: KARETNY MRC S
IPC: A61K9/16
Filed: 1997-04-15
Abstract: 1. A process for the preparation of a granular formulation for compression into pharmaceutical tablets, comprising the steps of (a) intimately mixing particles of a pharmaceutical active with an uniform aqueous slurry of hydrolyzed cellulose to form a smooth uniform aqueous slurry consisting essentially of hydrolyzed cellulose and pharmaceutical active and (b) spray-drying the resulting slurry at a temperature below the charring temperature of the hydrolyzed cellulose and the melting point of the pharmaceutical active ingredient.  2. The process of claim 1 comprising the additional step of recovering a porous substantially spherical granular composition in which 90 percent of the granules are larger than 50 microns and smaller than 500 microns and the median granule size is in the range of 150 to 300 microns. 3. The process of claim 1 or 2 in which there is employed in the spray drying step an aqueous slurry consisting essentially of, on a dry basis, 1 percent to 97 percent by weight of pharmaceutical active and 3 percent to 99 percent by weight of hydrolyzed cellulose. 4. The process of claim 3 in which the pharmaceutical active ingredient is selected from the group consisting analgesics, antibiotics, cough and cold drugs, antiepileptics, antihistamines, cardiovascular drugs, gastrointestinal drugs, respiratory drugs, vitamins, and combinations of two or more of these classes of drugs. 5. The process of claim 4 in which the pharmaceutical active ingredient is selected from the group consisting of Ibuprofen, acetaminophen and pseudoephedrine hydrochloride. 6. The process of claim 5 in which the resulting slurry contains one or more compatible pharmaceutically acceptable additives selected from the group consisting of from 0.01 to 1 percent by weight of a surfactant, from 0.1 to 5 percent by weight of a disintegrant, and from 0.1 to 3 percent by weight a antiadherent/flow aid. 7. A substantially porous spherical granular composition for compression into pharmaceutical tablets consisting of 1 percent to 97 percent by weight of pharmaceutical active ingredient and 3 percent to 99 percent by weight of hydrolyzed cellulose. 8. The composition of claim 7 comprising spray dried particles consisting essentially of pharmaceutical active and hydrolyzed cellulose in which the hydrolyzed cellulose is firmly bonded to and substantially envelops particles of the pharmaceutical active material. 9. The composition of claim 7 in which 90 percent of the granules are larger than 50 microns and smaller than 500 microns and median granule size is in the range of 150 to 300 microns. 10. The composition of claim 7, 8 or 9 in which the pharmaceutical active ingredient is selected from the group consisting of analgesics, antibiotics, cough and cold drugs, antiepileptics, antihistamines, cardiovascular drugs, gastrointestinal drugs, respiratory drugs, vitamins, and combinations of two or more of these classes of drugs. 11. The composition of claim 10 in which the pharmaceutical is selected from the group consisting of ibuprofen and acetaminophen and pseudoephedrine hydrochloride. 12. The composition of claim 7, 8 or 9 additionally containing one or more compatible pharmaceutically acceptable additives selected from the group consisting of from 0.01 to 1 percent by weight of a surfactant, from 0.1 to 5 percent by weight of a disintegrant, and from 0.01 to 3 percent by weight of a flow aid. 13. Compressed pharmaceutical tablets comprising a compatible pharmaceutically acceptable lubricant and the composition of claim 7, 8, 9 or 11. 14. Compressed pharmaceutical tablets comprising a compatible pharmaceutically acceptable lubricant and the composition of claim 10.