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AbstractA diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration. The pellet has a dissolution rate in vitro which when measured in a dissolution apparatus (Paddle) according to U.S. Pharmacopoeia XXI in 0.05 M KCl at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement. Not more than 80% of the total diltiazem is released after six hours of measurement and not less than 85% of the total diltiazem is released after 13 hours of measurement.Other References
| InventorsAssigneeApplicationNo. 120952 filed on 11/16/1987US Classes:424/461, Containing polysaccharide (e.g., cellulose sugars, etc.)424/459, Organic coatings424/462, Containing solid synthetic polymers424/470, Where particles are granulated424/493, Containing polysaccharides (e.g., sugars)424/494, Cellulose derivatives424/495, Ethyl cellulose424/497Containing solid synthetic polymersField of Search424/461, Containing polysaccharide (e.g., cellulose sugars, etc.)424/462, Containing solid synthetic polymers424/489, Particulate form (e.g., powders, granules, beads, microcapsules, and pellets)424/474, Coated pills or tablets424/470, Where particles are granulated424/477, Containing proteins or derivatives thereof424/479, Containing polysaccharide (e.g., sugar, etc.)424/481, Containing natural gums or resins424/482, Containing solid synthetic polymers424/490, Coated (e.g., microcapsules)424/494, Cellulose derivatives424/493, Containing polysaccharides (e.g., sugars)424/495, Ethyl cellulose424/497Containing solid synthetic polymersExaminersPrimary: Page, Thurman K.Attorney, Agent or FirmUS Patent References3965255, Controlled drug releasing preparationsIssued on: 06/22/1976 Inventor: Bloch , et al.4230687, Encapsulation of active agents as microdispersions in homogeneous natural polymeric matrices Issued on: 10/28/1980 Inventor: Sair , et al.4263273, Pharmaceutical preparation comprising a cardiac glycoside with a polymer coating Issued on: 04/21/1981 Inventor: Appelgren , et al.4361546, Retard form of pharmaceuticals with insoluble porous diffusion coatings Issued on: 11/30/1982 Inventor: Stricker , et al.4432966, Compressed tablets for disintegration in the colon comprising an active ingredient containing nucleus coated with a first layer containing microcrystalline cellulose which is coated with an enteric organic polymer coating Issued on: 02/21/1984 Inventor: Zeitoun , et al.4496558, Pharmaceutical compositions and methods for producing alpha antagonism Issued on: 01/29/1985 Inventor: DeMarinis , et al.4499066, Pharmaceutical sustained-release compositions Issued on: 02/12/1985 Inventor: Moro , et al.4555399, Aspirin tablet Issued on: 11/26/1985 Inventor: Hsiao4592753, Drug delivery device Issued on: 06/03/1986 Inventor: Panoz4600645, Process for treating dosage forms Issued on: 07/15/1986 Inventor: Ghebre-Sellassie , et al.4606909, Pharmaceutical multiple-units formulation Issued on: 08/19/1986 Inventor: Bechgaard , et al.4609542, New pharmaceutical forms for administration of medicaments by oral route, with programmed release Issued on: 09/02/1986 Inventor: Panoz , et al.4610870, Controlled release formulation Issued on: 09/09/1986 Inventor: Jain , et al.4666702, Dosage units for controlled release of active material Issued on: 05/19/1987 Inventor: Junginger4684516, Sustained release tablets and method of making same Issued on: 08/04/1987 Inventor: Bhutani4756911Controlled release formulation Issued on: 07/12/1988 Inventor: Drost , et al. Foreign Patent References
International ClassesA61K 009/62A61K 009/16 A61K 009/26 Foreign Application Priority Data1983-12-22 IE |