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Nanoparticulate candesartan formulations

A nanoparticle, candesartan technology, applied in the direction of nanotechnology, nanotechnology, nanomedicine, etc., can solve the problem that the circulation level of angiotensin II does not exceed the effect of blood pressure

Inactive Publication Date: 2008-02-27
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increases in plasma renin activity and circulating levels of angiotensin II do not outweigh the effects of candesartan on blood pressure. effect

Method used

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  • Nanoparticulate candesartan formulations

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Embodiment Construction

[0026] The present invention relates to nanoparticulate compositions comprising candesartan (eg, candesartan cilexetil). The composition comprises: nanoparticulate candesartan particles having an effective average particle size of less than about 2000 nm, and at least one surface stabilizer.

[0027] As taught in the '684 patent, and as illustrated in the examples below, not all combinations of surface stabilizers and actives will result in stable nanoparticle compositions. However, it was surprisingly found that stable nanoparticulate candesartan formulations could be prepared.

[0028] Advantages of the nanoparticulate candesartan formulations of the present invention include, but are not limited to: (1) smaller size in tablets or other solid dosage forms; (3) the bioavailability is improved compared with the conventional form of candesartan; (4) the pharmacokinetic profile is improved; (5) the bioequivalence of the nanoparticulate candesartan composition is improved (6) t...

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Abstract

The present invention is directed to compositions comprising a candesartan, such as candesartan cilexitil. The candesartan particles of the composition have an effective average particle size of less than about 2000 nm. The candesartan compositions of the invention are useful in the treatment of hypertension or related cardiovascular conditions.

Description

field of invention [0001] The present invention relates to nanoparticulate compositions comprising candesartan (eg, candesartan cilexetil). The candesartan particles have an effective average particle size of less than about 2000 nm. The compositions of the present invention are useful in the treatment of hypertension or related cardiovascular disorders. Background of the invention [0002] A. Background on Nanoparticle Compositions [0003] Nanoparticle compositions, first described in US Patent No. 5,145,684 ("the '684 patent"), are particles composed of poorly soluble therapeutic or diagnostic agents having non-crosslinked surface stabilizers adsorbed to their surfaces. The '684 patent does not describe nanoparticulate compositions of benzimidazole derivatives. [0004] For example, methods of preparing nanoparticulate compositions are described in U.S. Patent Nos. 5,518,187 and 5,862,999, both entitled "Method of Grinding Pharmaceutical Substances"; U.S. Patent No. 5,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/20A61K47/38A61K31/4184
CPCA61K9/2013A61K9/145A61K9/2054A61K47/38A61K9/146A61K47/20A61K9/2018A61K9/2009A61K9/143A61K31/4184A61P9/00A61P9/12A61K9/14B82Y5/00
Inventor G·利弗西奇S·詹金斯
Owner ELAN PHRMA INT LTD
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