Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Reexamination Certificate
1999-05-14
2001-08-14
Nutter, Nathan M. (Department: 1711)
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
C127S015000, C127S016000, C127S030000, C127S058000, C127S060000, C426S658000, C426S660000, C568S863000, C568S872000
Reexamination Certificate
active
06274727
ABSTRACT:
The invention relates to a composition, comprising one or more polyols, which has a prolonged deformability and can be processed to give tablets, compacts or boiled sweets having improved properties.
Numerous publications and patent applications disclose compositions for the production of tablets, compacts or even boiled sweets (EP-A-0 240 773, EP-A-0 462 066 or DE-A1-43 16 537), in which all sorts of physiologically tolerable substances are used as excipients for pharmaceutical active compounds or flavourings. These include, in particular, cellulose derivatives and their salts, carbohydrates, sugars, water-soluble polymers such as N-vinylpyrrolidone/vinyl acetate copolymers, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid and its salts, polymethacrylic acid and its salts, polyalkylene oxides such as polyethylene oxide, polypropylene oxide and also copolymers of ethylene and propylene oxides, polysaccharides such as alginic acid, their alkali metal and ammonium salts, carrageenans, galactomannans, tragacanth, agar-agar, gum arabic, xanthan gum, chitin derivatives, such as chitosan, pectins, such as sodium carboxymethylamylopectin and starches and also mixtures of these water-soluble polymers. Water-soluble is in this case understood as meaning that, at 20° C., at least 0.5 g, preferably 2 g, of the polymer can optionally dissolve in colloidal form or dissolve with gel formation in 100 g of water.
In the production of tablets, coated tablets, lozenges or boiled sweets, good water solubility of the excipient matrix is of particular importance for bioavailability and rapid absorption.
Water solubility is admittedly also of importance for a pleasant taste and sensation in the mouth, but the surface composition and the taste sensation during sucking also play a relatively large part in this connection. In the case of the known excipient materials, this is nor afforded without problems. While one has a negative taste pattern, the others lead on account of their physical condition to irregular, granular surfaces or, on account of their short processability, to uneven, possibly sharp-edged surfaces.
Usually, premixtures are prepared in order to obtain a homogeneous distribution of an added active compound in the excipient matrix, the various components are fused with one another or the active compounds are mixed by kneading in an existing polymer melt. Problems in these processes are the uniform dose, the homogenous mixing and the continuous procedure.
For the administration of pharmaceutical active compounds in tablet, coated tablet or lozenge form, in order to guarantee a constant dose the active compound must be homogeneously dispersed in the excipient matrix. This is a particular problem when using poorly soluble active compounds.
The object of the invention is therefore on the one hand to make available a composition which can be carefully processed in a temperature range to give the desired products, i.e. to give tablets, compacts or boiled sweets, in which added active compounds are not damaged. The object of the invention is also to make available a process which can be carried out continuously, whereby tablets, compacts, lozenges or boiled sweets can be prepared which have a smooth surface which is also retained during sucking, and have a pleasant taste and sensation in the mouth and also a homogeneous dispersion of active compounds and flavourings contained therein. It is furthermore an object of the invention to make available compositions which can be employed in this process and, due to long deformability, can be processed in a simple manner to give the desired products.
The object is achieved by compositions comprising previously co-sprayed polyol, in particular by compositions comprising one or more polyols from the group consisting of xylitol, sorbitol or lactitol, maltitol, erythritol or mannitol, and optionally carbohydrates from the group consisting of starch, cellulose, and also, depending on the product, optionally one or more active compounds, one or more colourants, one or more natural sweeteners, one or more synthetic sweeteners, acidifying agents, flavourings, aromatizers and customary auxiliaries.
The object is also achieved by a process for the production of a plastic, shaped or unshaped material in which a composition consisting mainly of one or more polyols is extruded in a temperature range from 30 to 170° C. and optionally shaped. In particular, the object is achieved by previously co-sprayed compositions, which are extruded and the extrudate obtained in this manner is then processed further in subsequent shaping units.
It is known, for the production of lozenges, compacts or sweets, to extrude mixtures of the individual components and to fuse them with one another at temperatures below 200° C. The extrudate can be divided by calendering or by comminution using rotating knives into equal-volume, still-shapable pieces having a solid surface, which can be processed directly subsequently by compressing to give tablets. It is also known to add active compounds and other additives by means of suitable equipment during extrusion. It still causes problems here, however, even today to achieve a really homogeneous active compound mixture and to obtain a product having a really smooth surface.
Experiments have shown that compositions based on sorbitol, xylitol, lactitol or other substances analogous to sugar, such as maltitol, erythritol, mannitol or others which can optionally additionally contain carbohydrates from the group consisting of starch and cellulose, can be shaped in a simple manner to give extrudates which can be processed further readily and for a long time. Compositions which contain these polyols in the mixture can also be processed in the same manner and readily.
It was also found that polyol-containing materials which have a high xylitol content can be processed particularly readily. Those materials in particular have exceedingly good processing properties whose components have been pretreated before extrusion in the co-spraying process described in Patent Application DE 19617487.2 and processed together to give a finely divided powder. This powder employed for the extrusion is not only a mixture of two or more different powders but a powder in which even the individual particles consist of a mixture of the individual components as a result of the co-spraying, i.e. mixed crystals are obtained. In comparison with powder mixtures customarily used, these powders have a lower melting point, and plastic materials obtained therefrom are also deformable for a long time and readily after extrusion. This deformability can be further prolonged by the addition of suitable crystallization retardants known to the person skilled in the art, which can be added during the co-spraying. Advantageously, in compositions based on co-sprayed polyols or polyol mixtures according to the invention, the addition of plasticizers or flow-regulating agents which are otherwise necessary can be dispensed with.
Owing to the prior co-spray drying of the individual components, powders are obtained which, as they are formed and collected in the co-spraying process, can be continuously extruded. Between or during the processing stages of the co-spraying and the extrusion, active compounds, additives and customary pharmaceutical auxiliaries, such as fillers, lubricants, mould release agents, flow-regulating agents, plasticizers, colourants, stabilizers, acidifying agents, flavourings and aromatizers can be added to the powder mixtures.
Fillers which can be added are those generally known to the person skilled in the art, such as oxides of magnesium, aluminium, silicon and titanium, but also others.
If required, in certain cases suitable flow-regulating agents such as, for example, mono-, di- and triglycerides of the long-chain fatty acids, waxes, carnauba wax or lecithins can be added. In general, however, these additives are not needed in the compositions according to the invention.
Besides low molecular weight polyalkylene oxides such as polyethylene glycol, polypropyle
Maul Karin
Schwarz Eugen
Merck Patent Gesellschaft mit beschrankter Haftung
Millen White Zelano & Branigan P.C.
Nutter Nathan M.
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