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Tablet Formulation comprising Voriconazole and no polymer binders (e.g. Povidone)

IP.com Disclosure Number: IPCOM000199114D
Publication Date: 2010-Aug-26
Document File: 2 page(s) / 39K

Publishing Venue

The IP.com Prior Art Database

Abstract

Stable tablet formulations comprising Voriconazole, but not a polymer binder, by replacing Povidone with certain non-polymer binders, such as alginic acid, pregelatinised starch, guar gum, carregeenan or gelatine are disclosed herein.

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Tablet Formulation comprising Voriconazole and no polymer binders (e.g. Povidone)

Voriconazole, sold under the trade name Vfend® (Pfizer), is a broad spectral triazol antifungal agent to treat serious fungal infections caused by Aspergillus, Scedosporium and Fusarium, flucanozole-resistant Candida and candidaemia in patients with normal white blood cell counts. The drug is used as oral suspension, lyophilised powder and as tablet.

Vfend® tablets contain Voriconazole (50mg or 200mg) and as a binder Povidone, also known as Polyvinylpyrrolidone (PVP), as well as lactose monohydrate, pregelatinized starch, croscarmellose sodium, povidone, magnesium stearate and a coating containing hypromellose, titanium dioxide, lactose monohydrate and triacetin. The tablets were thereby obtained by a wet granulation process and subsequent compression into tablets.

The use of the Povidone as a binder is well known, documented and implemented in many other pharmaceutical products. However, Povidone is a water-soluble polymer made from the monomer N-vinylpyrrolidone and therefore a rather costly excipient. Due to economic or other reasons, there is a need for tablet formulations of Voriconazole that do not contain a polymer binder, such as Povidone.

We developed stable tablet formulations comprising Voriconazole (50mg or 200mg), but not a polymer binder, by replacing Povidone with certain non-polymer binders, such as alginic acid, pregelatinised starch, guar gum, carregeenan or gelatine. The tablets were obtained either by wet granulation or dry granulation (roller compaction), and then by coating using standard (e.g. hypermellose based), non-functional film coat. The tables below show spec...