JPS6323820B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a tablet composition, and more particularly to a tablet composition with excellent lubricating effect during tablet production. At present, tablets occupy a major position as a form of various products such as pharmaceuticals, foods, and food additives. These tablets are required to satisfy one or all of the following properties, such as disintegration, dispersibility, solubility, and effervescence, depending on the purpose of use. , dispersants, foaming agents, etc., have been studied in various ways. Furthermore, various substances have been developed for additives such as excipients, binders, and lubricants from the standpoint of tablet manufacturing. Incidentally, the selection of a lubricant is extremely important when manufacturing tablets. So far, magnesium stearate, potassium stearate, talc, starch, L-leucine, isoleucine, etc. have been known as lubricants, but some of these have limited amounts and are not sufficiently effective. Some have inconveniences, such as not being effective, some giving off a strange odor, and some being unsuitable for water-soluble tablets and not being acceptable as food additives.
None of them were fully satisfactory. In view of these circumstances, the present inventors have set conditions such as having excellent lubricity, being water-soluble, being acceptable as a food additive, being white, and having no adverse effect on the senses. As a result of intensive research in order to develop a satisfactory lubricant, it was discovered that L-valine, one of the essential amino acids, is suitable for this purpose, leading to the completion of the present invention. The present invention relates to a tablet composition characterized in that L-valine is added as a lubricant to a blend consisting of a base ingredient and an additive. In the present invention, there are various types of main ingredients, such as drugs, foods, luxury goods, sweeteners, etc. Similarly, there are various types of additives, and they are selected depending on the relationship with the base ingredient and the tablet manufacturing method, but examples include starches such as wheat starch, potato starch, and corn starch, glucose, sucrose, and lactose. Excipients (or diluents) such as sugars such as , sorbitol, and inorganic substances such as calcium phosphate and calcium sulfate; Binders such as starch, sucrose, gelatin, gum arabic, and methylcellulose; Starch, starch derivatives, cellulose, and cellulose derivatives disintegrants such as; blowing agents such as sodium hydrogen carbonate, etc. Furthermore, the above-mentioned known lubricants can also be used if necessary. The amount of L-valine used as a lubricant should be determined in consideration of the desired hardness of the tablet, and is usually about 2 to 10%. If it is desired to obtain tablets with relatively low hardness, L-valine may be added in an amount of 5% or more, preferably 5 to 8%. In particular, when using a sweetener as the main ingredient, such as a dipeptide sweetener represented by α-L-aspartyl-L-phenylalanine methyl ester (hereinafter abbreviated as AP), the tablet should be rapidly dissolvable. In order to meet such demands, tablets with low hardness can be obtained by setting the amount of L-valine added to about 6%. When manufacturing tablets from the tablet composition of the present invention,
Any of the direct powder compression method, wet granulation method and dry granulation method can be applied. The manufacturing process of tablets using the wet granulation method is as follows: A tablet composition containing appropriate amounts of each raw material is mixed with a wet material obtained by adding water, an organic solvent, syrup, or a mixture thereof as necessary. 〓After the mixture is mixed, it is granulated. In the dry granulation method, each raw material mixture is compressed into slug tablets,
Grind, sieve and granulate. The granules obtained by these operations are compressed into a final tablet to obtain a product. In the direct powder compression method, the blended raw materials are directly compressed into tablets using a forced feeder. Since the tablet composition of the present invention uses L-valine as a lubricant, it is suitable especially when a sweetener is used as the main ingredient and it is desired to produce a rapidly dissolving tablet, and it has good tableting properties. The desired tablet can be obtained. Next, examples of the present invention will be shown. Example 1 Tablets were manufactured by dry granulation using the tablet compositions shown in the table below.

[Table] The machine could be operated smoothly for both slug tableting and main tableting for each sample. Table 2 shows the weight, appearance, and dissolution time of the tablets for each sample.

[Table] As is clear from Table 2, all of the obtained tablets had low hardness and excellent solubility. On the other hand, when L-valine is not added, the frictional resistance of the tablet composition is large, so the tablet machine makes a squeaking sound, and the tablet sticks to the kinematics in the tablet machine as well. It was impossible to press the tablets. Example 2 A tablet composition consisting of 85% sugar (granulated sugar), 10% dextrin (trade name: AMYCOL 7H, manufactured by Nichiden Chemical Co., Ltd.) and 5% L-valine was compressed to form tablets with a diameter of 20 mm ( Tablet confectionery) was obtained. In this case, the tableting properties were good and there was no adhesion. On the other hand, for those without L-valine addition, the frictional resistance of the raw material is great, so it tends to stick to the kinematics.
As a result, the tablet press produced a creaking sound, making it impossible to press the tablets.

Claims (1)

[Scope of Claims] 1. A tablet composition characterized in that L-valine is added as a lubricant to a blend consisting of a base ingredient and an additive. 2. Claim 1, wherein the additive is at least one substance selected from the group consisting of excipients, binders, disintegrants, blowing agents, and lubricants (excluding L-valine). Tablet compositions as described. 3. The tablet composition according to claim 1, wherein the base ingredient is a dipeptide sweetener. 4 The dipeptide sweetener is α-L-aspartyl-
The tablet composition according to claim 3, which is L-phenylalanine methyl ester.