DE1068863B - - Google Patents

Description

GERMAN

Compressed tablets are generally made by compressing one according to known methods Granules, d. H. a granular mass of a powdered mixture, in an ordinary tablet machine manufactured. The granules are manufactured and / or treated in such a way that they flow easily and in addition to suitable base materials, e.g. B. starch, sugar or the like, nor these masses adapted binders, such as gum arabic, gelatin and similar compositions, in some cases as well Lubricants such as B. Talc, and finally the active substances. The relative amounts of the various Fabrics can be sized differently. In general, the granules after two different procedures, namely either by so-called dry granulation or granulation with compression of the powdery components into relatively large units, which are then ground to granules by means of a suitable mill or a rolling mill or to be crumbled; or one applies the so-called wet granulation, in which the ingredients with a solution of e.g. B. gelatin are moistened, whereupon the mass thus obtained is pressed through a sieve to create a discontinuous mass which is then dried.

The granules produced by one of these two processes are then compressed into tablets. These tablets show a more or less homogeneous appearance and are not transparent. They show an amorphous or powdery break and easily disintegrate in water. They can be coated with sugar or the like to improve the taste of the tablets to cover and make swallowing easier. This type of tablet production is used in primarily used in the pharmaceutical industry, but sometimes also in the manufacture of Sweets.

Another type of tablet, better known as candy, is made from a dehydrated one or anhydrous mass made from mono- and di-saccharides, which at temperatures of 50 ° C and more are liquid or plastic. This mass can be suitably converted in two different ways Pieces to be divided. One method is to remove the still warm and plastic mass to convey between two engraved or recessed profiled, rotating rollers, so that a Band is formed in which the profiling has shaped tablets, which are held together by a thin film will; this band can be broken after cooling so that the individual tablets be exposed. These tablets are clear and generally homogeneous in appearance

Method of manufacture
compact air-sensitive active ingredients
containing tablets

Applicant:
E. & O. Collett & Co. AJS., Oslo

Representative:

Dr. W. Schalk and Dipl.-Ing. P. Wirth, patent attorneys, Frankfurt / M., Große Eschenheimer Str. 39

Claimed priority: Norway March 25, 1954

Appearance as well as a glass-like and homogeneous break.

The other method is to use special machines to turn the warm, plastic mass into a rod to form, which are divided into tablets or candies by means of pistons or similar suitable organs will. The appearance and properties of the tablets made by this process are similar the appearance and properties of the tablets produced by the aforementioned process.

This type of tablet or candy production is mainly used in the candy industry.

The method described at the beginning for the production of compressed tablets from granules are characterized in that the tablets produced are exactly the same shape and one and the same Have weight because the machines or devices used for this purpose are easily adjusted can and after setting to a certain type of granulate operated without changing the setting can be. Most substances are well suited for the production of tablets according to the one described at the beginning Procedure. However, this does not apply in the case of substances that are easily oxidized, e.g. B.

essential oils and the like, because the tablets produced in this way do not have a sufficiently dense structure.

The other process described above for making transparent tablets is characterized by

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by from that oxidizable substances by air, z. B. essential oils or the like., Are incorporated into the mass can and remain stable because the mass does not let air through after hardening and this Completely protects fabrics. On the other hand, this second method is not suitable for tablets that to serve pharmaceutical purposes, because they are profiled by the production means deepened Rollers easily get an unsatisfactory and asymmetrical shape. Furthermore, the method in which the tablets are cut from a rod, tablets with different weights, whereby moreover, tablets weighing less than 1000 mg are difficult to manufacture.

It is also known to air-sensitive tablets, namely tablets containing hygroscopic active substances by producing the starting material to which these substances have already been added until it is formed a coherent body is heated, a powder is made from it and this is then closed Compresses tablets that are not treated further. One can in this way while the harmful influence Avoid the hygroscopicity of the active substances on the tableting, but do not receive tablets, which would be sufficiently airtight to prevent the influence of atmospheric oxygen on easily oxidizable active substances to prevent.

It is also known, moldings made of hygroscopic substances for treatment in a Tableting machine are not suitable to produce by pouring these substances into molds and the molds are heated up to the sintering temperature or that these substances are pressed through a die presses, which is heated so far that a sintering of these substances takes place. That way you get Moldings that have sufficient strength to hold them together, but are looser in structure and are more porous than a tablet produced under the mechanical pressure of a tablet machine will. Such a process is therefore not suitable for protecting against external substances that are sensitive to oxygen Protect influences.

It is also known for the preservation of tablets, in particular those tablets which Contain oxidation-sensitive vitamins, these vitamins against external influences by embedding in suitable To protect substances such as fats or wax or gelatine and silicone resins. Also a protective cover, made with the help of carbohydrates can in some cases be enough Protect from oxidation-sensitive vitamins or other substances. In doing so, the vitamins were stirred into the melted base mass and cooled down. The tablets themselves will be then manufactured according to one of the known rolling or dividing processes.

In contrast, the invention is based on the object, even when using a tablet machine To protect oxygen-sensitive substances, namely tablets with a compact structure and uniform content of active substances, e.g. B. vitamin content to produce the advantages of the known Process produced tablets have, but avoid their disadvantages. This task is according to the invention, starting from the method in which a solid starting material at room temperature initially heated until a coherent body is formed, from which a powder is made produced and this is then pressed into tablets, solved in that from the Apsgangsmasse through

Incorporation of the air-sensitive active substances, e.g. B. of medicines, dyes, flavors, obtained and pulverized after cooling Base mass again after pressing into tablets, namely after leaving the tablet press is heated until sintering.

The method according to the invention gives the tablets a uniform and dense structure, which oxidize the active ingredients contained in them

ίο prevented. In carrying out this process, the tablets are preferably made by compressing a granulate or powder which is solid at room temperature but at a slightly higher temperature, e.g. B. at about 40 ° C, melts or sintered into a compact mass. Such a mass can, for. B. wholly or partly consist of mono-, di- and poly-saccharides, sugar-like polyalcohols such as sorbitol, mannitol and optionally additions of gelatin or gum arabic; it can be prepared by mixing the constituents mentioned and heating the mixture, with water optionally being able to be removed by evaporation. The mass is then cooled to room temperature, whereby it forms a hard, transparent and homogeneous, airtight mass. During a certain stage of the cooling process, in which the mass is still warm and plastic, therapeutic or other desired ingredients, e.g. B. essential oils, extracts or powdery ingredients, incorporated by stirring and finely dispersed in the mass. The mass hardened at room temperature is ground to a coarse powder, which can be regarded as a granulate, and which is then pressed into tablets, preferably in an ordinary tabletting machine. After the tablets have been pressed, they are opaque and resemble ordinary tablets made from ground mass. Since the individual particles have only been compressed mechanically, air has access to the interior of the tablets through cracks. Due to the special composition of the granules, however, these tablets can then be heated and then sinter together to form a compact mass and give almost the same consistency and appearance as the original mass it had before it was crumbled into a powder, without that this changes the shape of the tablets. The degree of heating must be limited upwards to the point at which the tablets would change their shape. The heating can, however, also be carried out at higher temperatures if the tablets are completely or partially coated before and / or after sintering, since the risk of change in shape is then lower. The coating can prevent the change in shape of the coated tablets even if the heating is driven so far that the tablet mass within the coating melts into a liquid state.

The following examples illustrate the process according to the invention:

example 1

300 g of glycose syrup, 700 g of granulated sugar, 100 g of water are heated to 145 ° C for removal of the water heated. After the mass has been cooled to 90 ° C., 25 g are added to it by stirring Lemon oil and 25 g powdered citric acid incorporated. The mass is then cooled to 20 ° C,

Claims (3)

ground in a mill or a roller mill to a coarse powder and then pressed into tablets weighing 500 mg, which are then placed in a bowl in a heating cabinet and heated to 55 ° C. for one hour. The tablets are then sintered or practically melted and form a compact, dense, coherent mass in which the lemon oil is completely distributed over the entire tablet and protected from the effects of air. ίο Example 2 A coarse powder is produced as in Example 1 and pressed into tablets. The tablets are coated with 60% sugar syrup and a mixture of 80% powdered sugar, 10% talc and 10% starch until the weight of the coated tablet has reached 800 mg. The heating is then brought about by keeping the coated tablets in a heating cabinet at 70 ° C. for 10 hours. Patent claims: 1. Process for the production of compact tablets containing air-sensitive active ingredients, in which a starting material that is solid at room temperature is initially up to the formation of a coherent one Body heated, made from this a powder and this is then pressed into tablets, characterized in that one from the starting material by incorporation of the air-sensitive active ingredients, e.g. B. Medicines, Colorants, flavorings, preserved at melting temperatures and after cooling pulverized base mass after pressing into tablets again, namely after leaving the The tablet press is heated until sintering without changing the tablet shape. 2. The method according to claim 1, characterized in that the tablets before and / or after Sintering are coated in a known manner, for. B. with sugar. 3. The method according to claim 2, characterized in that the heating at such a high temperature occurs that the mass located within the coating is more or less in liquid State is transferred. Considered publications:
German patent specifications No. 858 758, 859 357. © 909 648/377 11.59