Candesartan cilexetil
Inventors
Wu, Qiaomei • Gao, Huiyan • Chen, Hao • Yan, Qiping • Peng, Junqing • Hu, Gongyun
Assignees
Zhejiang Huahai Pharmaceutical Co Ltd • Alfred E Tiefenbacher GmbH and Co KG
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Publication Number
US-8193226-B2
Publication Date
2012-06-05
Expiration Date
Abstract
Candesartan cilexetil-containing granules which include a sugar alcohol and a binder and which are produced by granulation with an alcoholic granulating liquid. The granules are suitable for producing tablets in which the candesartan cilexetil is present in a form stabilized with regard to decomposition.
Core Innovation
The invention relates to stable solid oral pharmaceutical compositions comprising candesartan cilexetil in the form of granules and tablets, in which decomposition is reduced. The approach prepares candesartan cilexetil as granules by granulation of a premix that contains candesartan cilexetil, a sugar alcohol, and a binder with an alcoholic granulating liquid.
A key element is using a sugar alcohol as a component together with a binder, and granulating with an alcoholic granulating liquid that is preferably anhydrous. The sugar alcohol is selected from mannitol, sorbitol, and optionally mixtures, with further sugar alcohol options listed such as erythritol, xylitol, maltitol, and lactitol.
The binder envelopes the sugar alcohol and enables a homogeneous dispersion that limits decomposition chain reactions. The granulate is dried to a moisture content of equal to or less than 2 wt% and then compressed into tablets, optionally with other additives.
Claims Coverage
The document includes two independent claims covering a granulate composition and a tablet production method. Across the claim set, the inventive subject matter is defined by candesartan cilexetil, a sugar alcohol, a binder, and granulation with an alcoholic granulating liquid followed by drying and compression.
Granulate with candesartan cilexetil, sugar alcohol, and binder made by alcoholic granulation
A granulate comprising candesartan cilexetil, a sugar alcohol and a binder, produced by granulation with an alcoholic granulating liquid.
Dry granulate tablet production via alcoholic granulation, drying, and compression
A method for producing a tablet comprising candesartan cilexetil by producing a granulate by granulation of a premix comprising candesartan cilexetil, a sugar alcohol and a binder with an alcoholic granulating liquid, drying the granulate to obtain a dry granulate, and compressing the dry granulate into a tablet, if necessary with other additives.
Overall, the claims center on a candesartan cilexetil granulate containing a sugar alcohol and a binder, produced by granulation with an alcoholic granulating liquid, followed by drying to a defined moisture endpoint and compressing into tablets.
Stated Advantages
Provides increased stability against decomposition in comparison with reference tablets prepared by lactose and water granulation.
Documented Applications
Stable solid oral pharmaceutical compositions of candesartan cilexetil provided as granules and compressed into tablets.
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