JP2000302670A - Medicinal gel composition containing sucralose - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a medicinal gel composition hardly causing stickiness even if the occurrence of oozing out is caused. SOLUTION: This medicinal composition comprises a high-molecular gelatinizing agent [a polysaccharide or a derivative thereof, such as sodium alginate, curdlan, carrageenan, xanthan gum, locust bean rubber, gellan gum, pectin, agar, gum guaiac, glucomannan, tamarind seed gum, chitin, chitosan and dextrin, gelatin, PVA(polyvinyl alcohol), polyacrylic acid, water, and a sucralose (4,1', 6'-trichloro-4,1',6'-trideoxy-galactose or 1',6'-dichloro-1', 6'-deoxy-β-D- fructoguranosyl-4-chloro-4-deoxy-α-D-galactopyranoside).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to a pharmaceutical composition in the form of a gel. More specifically, the present invention relates to a gel pharmaceutical composition containing sucralose and having no stickiness even when water is separated.

[0002]

2. Description of the Related Art In recent years, gels such as jellies have attracted attention in the field of oral pharmaceuticals as a dosage form that can be easily taken by elderly people and children with low swallowing ability and can be taken by healthy adults anytime and anywhere without water. Have been.

[0003] However, if sucrose is added as a sweetener to make it easier to take the gel, the discoloration of the gel and the reduction of the medicinal component may be caused, and the caloric intake is restricted as in a diabetic patient. There was a problem that it was not good for some people.

[0004] On the other hand, when a sugar alcohol such as maltitol is blended, discoloration of the gel and reduction of the medicinal component can be prevented, and the caloric value can be suppressed to a low level. In some cases, the surface became sticky, resulting in a decrease in commercial properties.

[0005]

SUMMARY OF THE INVENTION An object of the present invention is to provide a gel-type pharmaceutical composition which is not sticky even if water separation occurs with time.

[0006]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to solve the above-mentioned problems. As a result, when sucralose was added as a sweetening agent to produce a gel, the gel was produced even if water separation occurred over time. Was found to be non-sticky. The present invention completed on the basis of such findings is a gel pharmaceutical composition comprising a polymer gelling agent, water and sucralose.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION The polymer gelling agent used in the present invention is not particularly limited as long as it is a polymer generally used as a gelling agent. Regardless.

Examples of such a polymer gelling agent include sodium alginate, curdlan, carrageenan, xanthan gum, locust bean gum, gellan gum, pectin, agar, guar gum, glucomannan,
Examples include polysaccharides such as tamarind seed gum, chitin, chitosan, and dextrin and derivatives thereof, gelatin, PVA (polyvinyl alcohol), and polyacrylic acid.
These gelling agents may be used alone or in combination of two or more.

Among these polymer gelling agents, vegetable polymer gelling agents are preferred in terms of storage stability of the drug. Examples of the vegetable polymer gelling agents include carrageenan,
Gellan gum, xanthan gum and locust bean gum are preferred. Furthermore, it is preferable to mix and combine one of carrageenan or gellan gum and xanthan gum and locust bean gum,
More preferably, in the composition, 0.01 to 5 parts by weight of carrageenan or gellan gum and 0.01 to 2 parts of xanthan gum.
Parts by weight, locust bean gum in a ratio of 0.01 to 5 parts by weight.

In the present invention, water is an essential component for forming a gel, and the amount of water varies depending on the type and amount of other components and the strength of the gel agent. Normal,
It is 10 to 99% by weight in the composition. If it is less than 10% by weight, the gel is too hard to be taken without water.

The sucralose used in the present invention is
4,1 ′, 6′-trichloro-4,1 ′, 6′-trideoxy-galactose or 1 ′, 6′-dichloro-
1 ′, 6′-dideoxy-β-D-fructofuranosyl-4-chloro-4-deoxy-α-D-galactopyranoside, 0.001 to 0.5% by weight based on the whole composition And more preferably 0.01
~ 0.1% by weight.

[0012] Pharmaceutical ingredients that can be incorporated in the present invention include:
There is no particular limitation as long as it is a pharmaceutical component suitable for oral administration, but, for example, crude drugs, analgesics, antiasthmatics, decongestants, antitussives, antihistamines, antiemetic, alkaloids, laxatives, appetite suppressants, central nervous system stimulants , Expectorants, lipid lowering agents, anti-inflammatory enzyme agents, anti-cancer agents, anti-cholesterol agents, anti-inflammatory agents, antibiotics, vitamins and the like.

More specifically, sodium picosulfate, acetaminophen, ibuprofen, diclofenac sodium, oxaprozin, sofacalcon,
Bromhexine hydrochloride, ketotifen, ranitidine, cimetidine, famotidine, riboflavin butyrate, carbinoxamine maleate, lysozyme chloride, amylase, trypsin, pepsin, cyanocobalamin, hydroxocobalamin, mecobalamin, cobalamide, α-chymotrypsin, bromelain, serathiopeptinase, protease , Vancomycin, cyclosporine, loperamide hydrochloride, spokolamin, meclizine hydrochloride, chlorpheniramine maleate, dihydrocodeine phosphate, ground yellow, licorice and the like.

[0014] These pharmaceutical components may be used alone or in combination of two or more.

Further, the gel pharmaceutical composition of the present invention may contain other additives (sweetener, flavoring agent, flavor,
Emulsifiers, stabilizers, fillers, preservatives, etc.) can be blended within a range that does not impair the stability of the gel or drug. 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 thereof include stabilizers such as TA (ethylenediaminetetraacetate), erythorbic acid, and BHT (dibutylhydroxytoluene), and fillers such as light anhydrous silicic acid.

The gel pharmaceutical composition according to the present invention can be produced by a conventional method for obtaining this kind of gel. For example, a polymeric gelling agent, sucralose, is mixed with a pharmaceutical component and other additives, dispersed in required water, and then heated and dissolved, and the liquid is adjusted to a size and shape suitable for oral administration. It can be manufactured by filling in a container and solidifying by cooling.

[0017]

Industrial Applicability According to the present invention, it has become possible to provide a gel-type pharmaceutical composition which does not become sticky even if water is separated over time while the pharmaceutical component is stably retained in the gel. In addition, such a gelled pharmaceutical composition was also favorable in terms of flavor.

[0018]

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

(Example 1) 3.0 g of ibuprofen, 0.4 g of sodium citrate, 0.1 g of citric acid, 1 carrageenan
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 sucralose 0.1 g.
2 g, stirred at room temperature for 30 minutes or more, and then heated and dispersed at 60 ° C. or more to prepare solution A.

Next, 0.4 g of lysozyme chloride, 0.08 g of bromhexine hydrochloride, and 0.05 g of carbinoxamine maleate
g and dihydrocodeine phosphate 0.16 g were dissolved in 30 g of water, and the mixture was heated to 50 to 60 ° C. to prepare solution B.

While keeping the temperature of the liquid A and the liquid B at 50 to 60 ° C., they were mixed under reduced pressure to remove bubbles. 13m in diameter
m, a cylindrical container having a depth of 12 mm was filled so as to have a height of 10 mm, and was cooled and solidified at 30 ° C. or lower to obtain an intended gel-like pharmaceutical composition.

Examples 2 to 10 Gels were prepared in the same manner as in Example 1 for the components shown in Table 1.

Comparative Examples 1 to 3 Gels were prepared in the same manner as in Example 1 for the components shown in Table 1.

[0024]

[Table 1]

(Test Example) Examples 1 to 10 and Comparative Example 1
With respect to the gels obtained in Nos. 1 to 3, stability over time and the like were examined.
Table 2 shows the results.

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

[0027]

[Table 2]

When sucralose was added as a sweetener (Examples 1 to 10), the flavor was good and the active ingredient was stably retained. Further, when water separation occurs (Example 3,
Even in 4, 7), no stickiness occurred.

On the other hand, in Comparative Examples 1 to 3, sucrose, aspartame, and maltitol were added as sweeteners instead of sucralose.

When sucrose was added (Comparative Example 1), stickiness due to water separation occurred, and the active ingredient could not be stably retained.

When aspartame was added (Comparative Example 2), stickiness did not occur even when water was removed, but the flavor was reduced.

When maltitol is blended (Comparative Example 3)
Had a good flavor, and the active ingredient was stably retained, but caused stickiness due to water separation.

Claims (3)

[Claims] 1. A gel pharmaceutical composition comprising a polymer gelling agent, water and sucralose. 2. The gelled pharmaceutical composition according to claim 1, wherein the polymer gelling agent is carrageenan, gellan gum, xanthan gum or locust bean gum. 3. The amount of sucralose in the composition is 0.00
The gel pharmaceutical composition according to claim 1, which is present in an amount of 1 to 0.5% by weight.