JPS62142132A - Novel clathrate - Google Patents

Abstract

PURPOSE:A novel clathrate that is prepared by clathrating guaiacol with cyclodextrin, thus converting guaiacol which is used as an antidiarrheric and an intestinal function-controlling drug into clathrate which an be fluidized without taste and smell, giving no paralytic feeling. CONSTITUTION:Guaiacol which has storing antiseptic and microcidal actions is used as a guest and cyclodextrin, preferably the beta-isomer is used as a host to form a clathrate of about 1:1 molar ratio (namely the content of guaiacol is about 10wt%) of no taste and no smell. Even when the clathrate is heated at 60 deg.C in a flowing air, the guaiacol is kept in the clathrate. EFFECT:Guaiacol could not have been prepared other than pills, but the present invention can give other preparation such as tablets, granules or capsules. Moreover, as it has no smell and taste, it can be used to contribute to the national health without giving patients hatred feeling.

Description

DETAILED DESCRIPTION OF THE INVENTION (Field of Application of the Invention) The present invention provides a laxative, a laxative, and a laxative. It is tasteless and has a numbing effect, making it useful as a medicine! The present invention relates to a novel inclusion compound ah of guaiacol that is indistinguishable.

(Prior Art) Guaiacol and medicinal creosote containing guaiacol as a main component have strong antiseptic and bactericidal effects, and have long been used as antidiarrheal agents and intestinal regulators. but,
Since all of these are oily, the production of solid preparations containing them requires the use of well-established excipients, etc.
There are many restrictions, and for this reason, all guaiacol or medicinal creosote preparations containing guaiacol as a main ingredient are in the form of gunpowder, whether in the East or the West.

However, in order to mold it into gunpowder, it is necessary to knead, spread, ginomaru,
It is not suitable for producing polyacids such as tablets because it requires troublesome steps and skill such as rolling (rolling).Furthermore, the gunpowder used in the drug mentioned above is extremely difficult to take due to its unique odor and taste. On the other hand, it has the disadvantage of imparting a numbing sensation, which is characteristic of phenolic compounds, to the oral mucosa that comes into contact with it.

(Objective of the Invention) The main object of the present invention is to convert guaiacol or medicinal creosote containing guaiacol as a main component into a fluid powder that is almost tasteless and odorless.

The present invention further includes, as a subsidiary object, the provision of a diarrhoea/intestinal regulating drug that can be easily formulated as a tablet, powder, granule, hard capsule, or the like.

(Means for Achieving Object 1) In the course of carrying out various studies in order to achieve Object 1 above, the present inventors discovered that guaiacol and medicinal (wood tar-based) creosote can be easily treated with cyclodextrin. This clathrate compound is a fluid powder that is almost tasteless and odorless, and is easy to take internally as it is, but it is unlikely to cause any contraindications when mixed with other medicinal ingredients.
Furthermore, we confirmed that when these clathrate compounds are taken orally, guaiacol or creosote acts effectively in the gastrointestinal tract, thus discovering that the new clathrate compounds are extremely useful as medicines. .

According to the knowledge of the present inventor, when Creont is used as a guest and cyclodextrin is used as a host to clathrate the former into the latter, the molecular ratio of host to guest is always about 1 = 1 in terms of guaiacol. , that is, the ratio of 1-fold stirring is about 10
% of Guayacornu yields a tasteless and odorless white clathrate containing creosote. and heat this compound at 60°C.
Guests do not escape even when heated in flowing air.However, when this compound is dissolved in water, it emits an odor similar to guaiacol, and when mixed with ferric chloride solution, it turns from purple to M4 cloudy blue, dirty green, and creosote. Or, it shows a color reaction peculiar to guaiacol.

Furthermore, although the cyclodextrin clathrate of creosote completely dissolves in 50 times the amount of water, Fresote itself does not completely dissolve even in 50,000 times the amount of water.

Furthermore, since this cyclodextrin clathrate of creosote exhibits antibacterial activity against Escherichia coli and Staphylococcus aureus similar to that of corresponding concentrations of creosote in vitro, inhibition of antibacterial activity by cyclodextrin is expected. Rather, in addition to the fact that the solubility in wood increases as mentioned above and the fact that an aqueous solution has a color reaction similar to creosote, this clathrate compound can be used in the gastrointestinal tract using conventional herbal medicines and other excipients. It is expected that the dispersibility and solubility in the gastrointestinal tract will be improved compared to other products.

The encapsulated compound of the present invention can be prepared by thoroughly mixing a host and a guest in an appropriate solvent in the same manner as in the production method of known encapsulated compounds.
It can be obtained by removing the solvent, but the method that seems to be the most economical from experience is guaiacol or creosote 1
A mixture of 0fi parts and 20 to 30 parts of ethanol is mixed with 90 to 100 parts of cyclodextrin and 150 to 20 parts of water.
After mixing with the 0-ply seam and stirring and mixing for about 1 hour, the mixture is dried at about 60° C., the solvent is removed, and dried until the hydrated coral becomes about 4%.

According to Ihi's method, when creosote is used as a guest, guaiacol, as well as the other four main components such as cresol and xylenol, are almost completely included in W, and the composition remains constant even after many repeated experiments. Ta.

The cyclodextrin in the present invention includes α-1β
Although it is possible to use either - or γ-cyclodextrin, β-type cyclodextrin is optimal in terms of both digestibility and economy. Incidentally, although the above data are based on β-type cyclodextrin, substantially the same results can be obtained using other types of cyclodextrin or a mixture of each type of cyclodextrin.

(Effect of the invention) According to the unreleased IJI, guaiacol or medicated creosote, which could not be formulated with anything other than gunpowder, can be used in tablets, granules,
It can be formulated into dosage forms that can be mass-produced, such as capsules, and since it is tasteless and odorless, it does not give patients a bad feeling, making it a great contribution to maintaining the health of the nation.

Claims (3)

[Claims] (1) A novel clathrate compound characterized by being guaiacol clathrated with cyclodextrin. (2) The clathrate compound according to claim 1, wherein the guaiacol is pharmaceutical creosote. (3) The clathrate compound according to claim 1 or 2, wherein the cyclodextrin is β type.