JP3008297B2 - Caffeine whisker inhibitor tablets - Google Patents

Description

Description: TECHNICAL FIELD The present invention relates to a tablet, and more particularly to a caffeine-containing tablet in which whisker generation of caffeine is suppressed.

(Conventional technology) Caffeine-oriented tablets grow as whiskers (needle-shaped crystals) from the inside, intertwine,
There is a problem that the surface of the tablet has a moldy appearance and significantly impairs its commercial value.

To prevent the occurrence of whisker of caffeine compound,
A method of mixing caffeine-containing powder or granules with charcoal, silicic anhydride and / or montmorillonite (JP-B-56
(Japanese Unexamined Patent Publication (Kokai) No. 2-23714) and uncoated tablets in which an antacid is blended with caffeine (JP-A-2-85214).

(Problems to be Solved by the Invention) However, it cannot be said that the former method is sufficient to suppress the generation of whiskers of caffeine.

In addition, since the latter uncoated tablet contains a large amount of an antacid, which is a basic substance, not only is it difficult to reduce the size of the tablet, but also it may be contraindicated with other components.

An object of the present invention is to provide a caffeine-containing tablet that reliably and easily prevents whisker generation of caffeine.

(Means for Solving the Problems) The present inventors have conducted research to solve the above problems,
Drugs other than caffeine were granulated, and it was found that tablets prepared with only caffeine in powder form could suppress the generation of whiskers of caffeine, thereby completing the present invention.

The preparation of the present invention is a caffeine whisker-suppressing tablet obtained by mixing powdered caffeine with a granular drug.

In the present invention, the granular drug refers to a drug obtained by adding an excipient, a binder, a disintegrant, and the like to a drug, uniformly mixing the resultant, and then granulating the drug according to a conventional method.

 The tablet of the present invention can be produced by the following method.

That is, a drug excluding caffeine and an excipient are uniformly mixed and pulverized, a binder is added thereto, granulated, and then dried to produce a granular drug according to a conventional method.

A lubricant, a disintegrant, powdered caffeine, and the like are added to the granulated drug, mixed uniformly, and then tableted according to a conventional method to produce a target tablet.

As a drug, aspirin, acetaminophen, ethenzamide, salicylamide, isotipendyl hydrochloride, diphenhydramine hydrochloride, carbinoxamine maleate,
dl-chlorpheniramine maleate, dextromethorphan hydrobromide, codeine phosphate, dihydrocodeine phosphate, noscapine, dl-methylephedrine hydrochloride, potassium guaiacol sulfonate, thiamine hydrochloride, riboflavin, bisibutiamine, ascorbic acid, etc. Can be used.

Other components other than drugs include lubricants (for example,
Magnesium stearate, potassium stearate,
Hydrogenated castor oil, talc, macrogol 4000, 6000, stearic acid, etc.), binders (eg starch paste,
Gelatin solution, gum arabic solution, hydroxypropyl cellulose, glucose solution, sucrose solution, water, ethanol,
Excipanol), excipients (eg, light anhydrous silicic acid, calcium carbonate, kaolin, crystalline cellulose,
Starch, lactose, sucrose, glucose, etc.), disintegrants (starch, agar, gelatin, CMC-Na, CMC-Ca, crystalline cellulose, calcium carbonate, etc.), coloring agents and the like can be blended.

(Effects of the Invention) According to the present invention, it is not necessary to increase the number of steps, and therefore, it is possible to provide a caffeine-containing tablet in which the generation of whiskers of caffeine is suppressed very inexpensively and reliably.

(Examples) Hereinafter, the present invention will be described in detail with reference to examples and test examples.

Example 1 9 g of acetaminophen, carbinoxamine maleate
0.075 g, dihydrocodeine phosphate 0.24 g, noscapine 0.4
8 g, dl-methylephedrine hydrochloride 0.6 g, potassium guaiacol sulfonate 2.5 g, bisibutiamine 0.264 g, riboflavin 0.12 g, lysozyme chloride 0.66 g, light silicic anhydride
0.6 g, crystalline cellulose 9.72 g, and hydroxypropyl cellulose 4.5 g were mixed well with a V-type mixer (manufactured by Tokuju Corp.), and mixed and pulverized through a 0.5 mm screen. A binder solution was added to the mixture to obtain granules, which were dried at 60 ° C. using a fluidized bed drier (manufactured by Powrex), and crushed to obtain granules.

2.5 g of anhydrous caffeine, 0.15 g of magnesium stearate and 0.3 g of hydrogenated castor oil were added to the granules in powder form and mixed with a V-type mixer (same as above).

The mixture was tableted at a tableting pressure of 1.0 to 1.5 t to obtain 90 tablets.

Example 2 According to Example 1, 9 g of acetaminophen, 0.05 g of isothipendyl hydrochloride, 0.4 g of diphenhydramine hydrochloride, 0.24 g of dextromethorphan hydrobromide, codeine phosphate
0.24 g, noscapine hydrochloride 0.24 g, ascorbic acid 2.5 g, light anhydrous silicic acid 3.5 g, crystalline cellulose 4.5 g, hydroxypropyl cellulose 8 g, lactose 0.13 g, after producing granules, to which anhydrous caffeine 0.75 g, Tableting was performed using 0.15 g of magnesium stearate and 0.3 g of hydrogenated castor oil in powder form to obtain 90 tablets.

Example 3 According to Example 1, 7.5 g of ethenzamide, 7 g of acetaminophen, 2 g of bromovalerylurea, and 4.5 g of crystalline cellulose were used.
g, hydroxypropylcellulose 7.5 g, after producing granules using lactose 0.3 g, to which anhydrous caffeine 0.75 g,
0.15 g magnesium stearate and 0.3 castor oil
Using g as a powder, tableting was performed to obtain 90 tablets.

Test Example In Example 1, anhydrous caffeine was transferred to the granule component to form granules, and only magnesium stearate and hydrogenated castor oil were added to the granules in powder form, mixed, and tableted to produce comparative tablets.

The tablets obtained in Example 1, the comparative tablets, the comparative tablets wrapped in paper with silica gel, and the comparative tablets wrapped in paper with activated carbon were placed in glass bottles, respectively, stored at 40 ° C. and 50 ° C., and observed over time with a microscope. Then, the following scores were evaluated.

(Score) 0: No whisker is observed.

1: Slight (1-2) whiskers are observed.

2: It is recognized that whiskers are generated.

3: Whisker is observed to be dense.

 Table 1 shows the results.

The tablets of Example 1 showed only slight whisker formation after 6 months.

On the other hand, in the comparative tablet, whiskers were remarkably generated after one month in the tablet alone and in the case of the addition of silica gel, and in the case of the addition of activated carbon, the degree was only slightly lower.

──────────────────────────────────────────────────続 き Continuation of front page (72) Inventor Yuji Koyama 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (56) References JP-A-63-267733 (JP, A) JP-A-2 -85214 (JP, A) Pharmaceutical Magazine, Vol. 96, No. 10, (1976), p. 1223-1228 (58) Field surveyed (Int. Cl. ⁷ , DB name) A61K 31/52 A61K 9/20 CA (STN)

Claims (1)

(57) [Claims] 1. A caffeine whisker-suppressing tablet comprising a powdered caffeine mixed with a granular drug.