Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1998-10-21
2000-12-26
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424488, 424493, 424499, 424479, 424464, 424440, 424441, A61K 914
Patent
active
061655112
DESCRIPTION:
BRIEF SUMMARY
The invention relates to a composition obtainable by co-spray-drying or co-fluidized-bed granulation essentially consisting of at least two polyols and, if appropriate, a binder, having a content of at least one non-hygroscopic polyol of more than 80% by weight, and to its use as a tableting aid.
Polyols and polyol mixtures are used to a great extent as noncariogenic additives and carriers, inter alia for pharmaceutical active compounds, tablets to be chewed and sucked, and other products of the pharmaceutical and confectionery industries. Polyols are generally produced by hydrogenation of their underlying sugars. In solid form, they can be obtained both by crystallization and by spray-drying.
The particular advantage of some polyols is that they are also suitable for direct pressing without further aids and additives.
Non-hygroscopic polyols are those polyols which, at a relative humidity of 80%, absorb less than 5% water at room temperature in the course of 7 days.
The known polyols, mannitol, lactitol, isomaltitol, xylitol, have low hygroscopicity of this type, but exhibit poor tableting behaviour (low tablet hardness, crusting, high abrasion). Achieving high tablet hardnesses is fundamentally advantageous, since carriers are frequently used only in small amounts in pharmaceutical formulations and active compounds can drastically decrease the tablet hardnesses, so that a desired formulation cannot be tableted.
Whereas lactitol, isomaltitol and xylitol are rarely used in the production of compressed articles, mannitol is widely used in pharmaceutical formulations.
However, the use of mannitol represents an increase in the amount of work, since it must generally be granulated wet prior to compression with the remaining formula constituents. Directly tabletable mannitol is also commercially available, but, in comparison with sorbitol, it can achieve only unsatisfactory tablet hardnesses.
Using sorbitol, in particular in the case of spray-drying, very good tablet hardnesses are achieved with correspondingly smooth surface of the compressed articles. However, the hygroscopicity of sorbitol is considerably higher than that of the other polyols, which restricts its applicability.
DE 32 45 170 proposes preparing a polyol combination of sorbitol and 10-15% by weight of mannitol by spray-drying. This is intended to increase the flexural strength of the tablets. However, the hygroscopicity remains essentially unchanged. There is no indication there that polyol combinations which were prepared by spray-drying and have mannitol as principle component can achieve improved properties, in particular high binding capacity for active compounds at lower hygroscopicity.
EP 0 528 604 describes a sorbitol and xylitol composition obtainable by co-melting. However, this leads to tablets having a comparatively low hardness.
The object was therefore to provide a polyol composition which can be prepared without problems and whose tableting properties, in particular with regard to tablet hardness and binding capacity, are improved in comparison with known polyols.
It has now been found that a polyol composition obtainable by co-spray-drying comprising at least 80% by weight of one or more non-hygroscopic polyols, on tableting at the same compression pressure, on the one hand gives higher tablet hardnesses and a much smoother surface, and on the other hand has a markedly lower hygroscopicity in comparison with sorbitol.
The invention thus relates to a composition essentially consisting of at least two polyols obtainable by co-spray-drying, which composition comprises at least 80% by weight of at least one non-hygroscopic polyol, in particular mannitol.
The term polyol means sugar alcohols of the general formula
In particular, the term polyols means hexitols, such as sorbitol and mannitol, pentitols, such as xylitol, however, other possibilities are also C.sub.4 polyalcohols, such as erythritol, or C.sub.12 polyalcohols, such as lactitol. The term polyol composition means a composition of a plurality of polyols which differ markedly
REFERENCES:
patent: 5876754 (1999-03-01), Wunderlich et al.
Maul Karin
Moschl Gernot
Schwarz Eugen
Benston, Jr. William E.
Merck Patent Gesellschaft mit beschrankter Haftung
Page Thurman K.
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