JP2000281562A - Gel composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a gel-like composition which can exhibit excellent storage stability without deactivating a water-soluble medicine, by formulating the water-soluble medicine, a vegetable polymer gelling agent and a specific sweetener. SOLUTION: This gel-like composition comprises (A) a water-soluble medicine, (B) a vegetable polymer gelling agent, (C) a sugar alcohol, and (D) water. The component A is preferably a medicine having a solubility of >=1 g/L in 25 deg.C water, such as lysozyme chloride, bromhexine hydrochloride or cyanocobalamin. The component B is preferably selected from carrageenan, xanthan gum, and locust bean gum. The component C is preferably selected from sorbitol, maltitol, erythritol, mannitol, and the like. The composition preferably contains the component C in an amount of 0.5-65 wt.%. Thereby, the gel-like composition which has excellent storage stability and can easily be administered even into aged person or children who have low swallowing abilities is provided.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a gel composition. More specifically, the present invention relates to a gel composition containing a water-soluble drug, having excellent storage stability, and having good ingestibility.

[0002]

2. Description of the Related Art Heretofore, drugs such as lysozyme chloride and bromhexine hydrochloride have been administered in dosage forms such as granules, capsules and tablets.

[0003] However, these dosage forms are difficult to take for elderly people and children with low swallowing ability, and even healthy adults require water at the time of dosing, so that they cannot be taken anytime and anywhere. Did not.

[0004]

Therefore, the present inventor has proposed:
It can be easily taken by elderly people and children with low swallowing ability, and
Consider administration as a gel that does not require water when taking
Formulation studies have been conducted. However, when a water-soluble drug such as bromhexine hydrochloride is gelated and sucrose is added as a sweetener, the drug is inactivated, and there is a problem that stability cannot be maintained.

An object of the present invention is to provide a gel composition containing a water-soluble drug such as lysozyme chloride or bromhexine hydrochloride and having excellent storage stability.

[0006]

The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, when a sugar alcohol is added as a sweetener instead of sucrose, a water-soluble drug such as lysozyme chloride is contained in the gel. Was found to be stably retained. That is, the present invention is a gel composition comprising a water-soluble drug, a vegetable polymer gelling agent, a sugar alcohol and water.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION The water-soluble drug in the present invention is
A drug having a solubility in water at 25 ° C. of 1 g / L or more, specifically, lysozyme chloride, bromhexine hydrochloride, vitamin B12 (for example, cyanocobalamin,
Hydroxocobalamin, mecobalamin, etc.). These drugs may be used alone or in combination of two or more.

As the gelling agent in the present invention, a vegetable polymer gelling agent is preferable. This is because the storage stability of animal gelling agents is not good, so that the use of sugar alcohols instead of sucrose cannot maintain the stability of drugs and gels.

[0009] Vegetable polymeric gelling agents include carrageenan, xanthan gum and locust bean gum.

The amount of these gelling agents is from 0.01 to 20% by weight of carrageenan in the composition, and preferably from 0.1 to 10% by weight from the viewpoints of ingestibility and stability with time. Xanthan gum accounts for 0.01 to 5% by weight of the composition, and preferably 0.1 to 0.6% by weight from the viewpoint of moldability and the like. For locust bean gum, 0.01 to
10% by weight, and 0.1% in terms of stability over time.
~ 5% by weight is preferred.

These gelling agents are used alone or in combination of two or more. From the viewpoint of moldability, stability over time, etc., three types of carrageenan, xanthan gum and locust bean gum are used in combination. Is preferred. Most preferably, the weight ratio of carrageenan, xanthan gum and locust bean gum is 0.5-2: 1: 1.

[0012] The sugar alcohol in the present invention is blended for imparting sweetness to the gel composition to make it easy to take. Such sugar alcohols include sorbitol, maltitol, erythritol, mannitol, xylitol and trehalose.

The content of these sugar alcohols is 0.5 to 65% by weight in the composition, and 3 to 40% by weight in order to maintain the stability of the above-mentioned drug and obtain a gel composition having good ingestibility.
% By weight is preferred. The sugar alcohols may be used alone or in combination of two or more.

The water of the present invention is indispensable for forming a gel. The amount of the water varies depending on the type and amount of other components, the desired strength of the gel, and the like. 10 to 99% by weight. If the content is less than 10% by weight, a gel suitable for taking is not formed.

Further, the gel composition of the present invention may contain other additives (sweeteners, flavoring agents, fragrances, emulsifiers, stabilizers, fillers, preservatives, etc.) which can be used for pharmaceuticals. It can be blended within a range that does not impair the stability. For example, stevioside, sweeteners such as thaumatin, citric acid, flavoring agents such as cocoa powder, polyoxyethylene hydrogenated castor oil, surfactants such as polyoxyethylene sorbitan fatty acid ester, methylparaben, ethylparaben,
Preservatives such as propylparaben and butylparaben, ED
Examples include stabilizers such as TA (ethylenediaminetetraacetate), erythorbic acid, and BHT (dibutylhydroxytoluene), and fillers such as light anhydrous silicic acid.

The gel composition according to the present invention can be produced by a conventional method for obtaining this kind of gel. For example, a water-soluble drug, a vegetable polymer gelling agent, a sugar alcohol such as maltitol are mixed with other additives, dispersed in required water, and then dissolved by heating. It can be manufactured by filling in a suitable container so as to have a shape and a shape, and cooling and solidifying.

[0017]

According to the present invention, it has become possible to provide a stable gel composition containing a water-soluble drug such as lysozyme chloride, bromhexine hydrochloride, cyanocobalamin, hydroxocobalamin and mecobalamin.

[0018]

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

(Example 1) Sodium citrate 0.4
g, citric acid 0.1 g, carrageenan 1 g, locust bean gum 0.5 g, xanthan gum 0.5 g, propylparaben 0.02 g, and calcium lactate 0.5 g were mixed together with sorbitol 25 g, and the resulting powder was mixed with water 4
After stirring at room temperature for 30 minutes or more,
The solution A was prepared by heating and dissolving it at 0 ° C. or higher.

Next, 6 g of lysozyme chloride was dissolved in 30 g of water and heated to 50 to 60 ° C. to prepare a solution B.

The solution A and the solution B were mixed under reduced pressure in order to remove bubbles while maintaining the temperature at 50 to 60 ° C. This is diameter 1
A cylindrical container having a depth of 3 mm and a depth of 12 mm was filled to a height of 10 mm, and was cooled and solidified at 30 ° C. or lower to obtain a desired gel composition.

Example 2 A gel was prepared in the same manner as in Example 1 for the components shown in Table 1.

(Example 3) A gel was prepared in the same manner as in Example 1 for the components shown in Table 1.

Example 4 Gels were prepared in the same manner as in Example 1 for the components shown in Table 1.

Example 5 A gel was prepared in the same manner as in Example 1 for the components shown in Table 1.

Comparative Example 1 A gel was prepared in the same manner as in Example 1 for the components shown in Table 1.

[0027]

[Table 1]

(Test Example) All of the gels obtained in Examples 1 to 5 could be easily taken without water.

The stability of the gels obtained in Examples and Comparative Examples was examined. Table 2 shows the results.

The content of the active ingredient was measured by high performance liquid chromatography or the like.

[0031]

[Table 2]

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI theme coat ゛ (reference) A61K 47/36 A61K 37/54 F term (reference) 4C076 AA36 BB01 CC15 CC24 DD38 DD43 EE58 FF35 FF36 FF52 4C084 AA03 DC22 MA35 MA52 NA03 NA09 ZA631 ZA632 4C086 AA01 AA02 DA39 MA03 MA05 MA35 MA52 NA03 NA09 ZC24 4C206 AA01 AA02 FA31 MA03 MA05 MA55 MA72 NA03 NA09 ZA63

Claims (5)

[Claims] 1. A water-soluble drug, a vegetable polymer gelling agent,
A gel composition comprising a sugar alcohol and water. 2. The gel composition according to claim 1, wherein the water-soluble drug is a drug having a solubility in water at 25 ° C. of 1 g / L or more. 3. The gel composition according to claim 1, wherein the drug having a solubility in water at 25 ° C. of 1 g / L or more is lysozyme chloride, bromhexine hydrochloride, cyanocobalamin, hydroxocobalamin or mecobalamin. 4. The gel composition according to claim 1, wherein the vegetable polymer gelling agent is one or more selected from the group consisting of carrageenan, xanthan gum and locust bean gum. 5. The gel composition according to claim 1, wherein the sugar alcohol is one or more selected from the group consisting of sorbitol, maltitol, erythritol, mannitol, xylitol and trehalose.