JP2015024986A - Solid preparations - Google Patents

Abstract

[PROBLEMS] To produce needle-like (butterfly-like) crystals and fogging of the inner surface of a transparent glass container (bottle) for storage containing the solid preparation despite the incorporation of menthol, a sublimable component. A solid preparation containing no menthol and a method for producing the same are provided. SOLUTION: A solid preparation comprising menthol and blended with menthol in a solid preparation containing the menthol. [Selection figure] None

Description

  The present invention relates to a solid preparation containing menthol, which is a sublimable component.

  Menthol has sublimation properties, and when menthol is blended into a solid preparation, whisker, the occurrence of needle-like (wax-like) crystals on the tablet surface and the inside of a transparent glass bottle that is a storage container become cloudy, It has been known to cause a decline in commercial value (see Non-Patent Document 1).

  In order to prevent this, for example, a tablet is provided with a sugar coating method (see Patent Document 1). However, although it is a thin-layer sugar coating, disadvantages in terms of manufacturing time and cost cannot be denied.

  Therefore, there has been a demand for the development of a simpler and more effective menthol sublimation suppression technique.

JP 2002-179559 A

Michi Oi, “Study on Whisker Precipitation from Solid Formulations (11th Report) Whisker Precipitation in Coexistence of Various Excipients with l-Menthol” Pharmaceutical Science Vol.59 No.Supplement Page.233 (1999)

  Therefore, the present invention is a menthol-containing solid that does not cause fogging of the inner surface of a transparent glass bottle called a whisker, which is called a whisker, although it contains menthol, which is a sublimable component. It is an object to provide a preparation and a method for producing the same.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors have formulated needle-shaped (bowl-like) crystals on the surface of a solid preparation resulting from menthol by blending aspen into a solid preparation containing menthol. It was also found that no fogging occurred on the inner surface of a transparent glass container (bottle) for storage containing the solid preparation.

The embodiments of the present invention obtained from such findings are as follows.
(1) A solid preparation characterized by blending menthol and asakojin.
(2) The solid preparation of (1), wherein the content of menthol is 0.09 to 5.6% by mass of the whole preparation.
(3) The solid preparation according to (1) or (2) above, wherein 11 parts by mass or more of asakojin is blended with respect to 1 part by mass of menthol.
(4) The solid preparation of (1) to (3) above, which is a tablet.
(5) The tablet according to any one of (1) to (3) above, wherein the tablet is obtained by adding and mixing menthol to granule obtained by granulating asakojin and compressing the granule. Solid formulation.

  According to the present invention, a menthol blended preparation that easily suppresses the sublimability of menthol and does not cause clouding of the inner surface of a transparent glass container (bottle) for storage containing needle-like (fungus-like) crystals or the solid preparation. It became possible to provide.

  “Menthol” is 2-isopropyl-5-methylcyclohexanol. In the present invention, it may be either l-form or dl-form, and may contain menthol (such as peppermint oil). .

  The amount (containing) of menthol is preferably 0.09 to 5.6% by mass in the preparation.

  “Mashinin” is a fruit of Asa Cannabis sativa Linne (Moraceae), and is known as a herbal medicine having an intestinal stool effect.

  The blending (content) amount of Asakojin is preferably 11 parts by mass or more, more preferably 30 parts by mass or more with respect to 1 part by mass of menthol.

  Examples of the solid preparation of the present invention include tablets, powders, granules, capsules, pills, and the like, but since the problem of whisker generation appears particularly in the case of tablets, the significance of the present invention is great.

  When the solid preparation is a tablet, for example, menthol, assortment of makojin in an amount sufficient to suppress sublimation of the menthol, and other active ingredients, additives / excipients, etc. are mixed as necessary. It is obtained by granulating according to the conditions and compression-molding using a tableting machine, etc., but first, a powder blended with mashinjin is granulated, and then the powder containing menthol in the resulting blended granule It is preferable to obtain by adding and mixing the body, and compression-molding the menthol and hemp seed blended granules.

  In addition to blending menthol and aspen, other known active ingredients, additives / excipients, and the like can be blended in the solid preparation as long as the effects of the present invention are not impaired.

  The solid preparation can be obtained by mixing menthol, an amount of makijin that is sufficient to suppress sublimation of the menthol, and other active ingredients, additives / excipients and the like as required. If necessary, it may be granulated and compression-molded using a tableting machine or the like.

  Hereinafter, the present invention will be described in more detail with reference to Examples, Comparative Examples and Test Examples.

Example 1
First, the ingredients from assortment to lactose hydrate listed as granulating powders in Table 1 were weighed and mixed to obtain assortment powder. The powdered blend of aspen seeds was granulated with an agitation granulator (vertical granulator 5L; manufactured by POWREC) or a mortar using purified water as a granulating solvent, and dried to obtain granulated blended seeds. Ingredients from croscarmellose sodium to calcium hydrogen phosphate, which were listed as late additions, were weighed and mixed into the blended assorted granules to obtain menthol and blended granules. The granules containing menthol and asakojin were compression-molded using a simple tablet molding machine (HANDTAB-200; manufactured by Ichihashi Seiki Co., Ltd.) to obtain a tablet containing menthol and asakojin having a tablet weight of 392.5 mg.
The menthol content (formulation) in the tablet of Example 1 corresponds to 0.1% by mass in the tablet.

Example 2
In the formulation (composition) of Example 1, the amount of l-menthol was increased, the amount of calcium hydrogen phosphate was decreased, and the content (formulation) of l-menthol was adjusted to 1.0% by mass in the tablet. In accordance with Example 1, a tablet containing menthol and hemp seed with a tablet mass of 392.5 mg was obtained.

Example 3
In the formulation (composition) of Example 1, the amount of l-menthol was increased, the amount of calcium hydrogen phosphate was decreased, and the content (formulation) of l-menthol was adjusted to 2.9% by mass in the tablet. In accordance with Example 1, a tablet containing menthol and hemp seed with a tablet mass of 392.5 mg was obtained.

Comparative Example 1
The same amount of menthol as in Example 1 was blended, and a menthol-blended tablet having a tablet weight of 392.5 mg was obtained with a formulation (composition) excluding Asako.

Comparative Example 2
The same amount of menthol as in Example 2 was blended, and a menthol-blended tablet with a tablet mass of 418.8 mg was obtained with a formulation (composition) excluding Asakojin.

Comparative Example 3
The same amount of menthol as in Example 3 was blended, and a menthol blended tablet with a tablet mass of 418.8 mg was obtained with a formulation (composition) excluding Asakojin.

Test example 1
[Method]
Ten tablets each obtained in Examples 1 and 2 and Comparative Examples 1 to 4 were placed in a glass white bottle, sealed, and stored overnight at 65 ° C. Then, after storage at 5 ° C. for 1 day, the occurrence of whiskers was visually confirmed.
The results are shown in Table 1.
The evaluation criteria are as follows.
No whisker occurrence:-, whisker occurrence: +
[result]
From Table 1, the occurrence of whiskers was confirmed in Comparative Examples 1, 2 and 3 containing menthol and not blended with asako. On the other hand, it was confirmed that Examples 1, 2, and 3 containing Asako Jin can suppress the generation of whiskers.
From the above, it was found that blending makijin is effective in suppressing the occurrence of whiskers due to menthol blended in the solid preparation.

  According to the present invention, it is possible to provide a menthol-containing solid preparation that easily suppresses the sublimability of menthol and does not cause fogging on the inner surface even when stored in a container of needle-like (basket-like) crystals or transparent glass bottles. It was. Therefore, development of the pharmaceutical industry and the like is expected through the marketing of menthol-containing solid preparations with higher commercial value.

Claims (5)

  A solid preparation characterized by blending menthol and asako.   The solid preparation according to claim 1, wherein the content of menthol is 0.09 to 5.6 mass% of the whole preparation.   The solid formulation of Claim 1 or 2 which mix | blended 11 mass parts or more of Asakojin with respect to 1 mass part of menthol. It is a tablet, The solid formulation of Claims 1-3 characterized by the above-mentioned. The solid preparation according to any one of claims 1 to 3, which is a tablet obtained by adding and mixing menthol to granules obtained by granulating asakojin and compressing the granules.