JP2003104912A - Administration-assisting food - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a powdery administration-assisting food capable of surely keeping effects of decreasing the bitter taste of a basic medicine and making swallowing thereof easy, and further capable of being smoothly changed into a viscous liquid, without forming undissolved lumps of powder, even when used ordinary temperature. SOLUTION: This powdery administration-assisting food decreases the bitter taste of the basic medicine and makes the swallowing thereof easy, wherein the food is used by adding water to the food immediately before it is used and solely mixing them without heating so as to form the viscous liquid.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a medication supplement that reduces bitterness of basic drugs and facilitates swallowing, and is in the form of a powder that becomes a viscous liquid simply by adding water just before use and mixing. Regarding medication supplements.

[0002]

2. Description of the Related Art Many studies have been made for the purpose of improving drug compliance.
Japanese Patent Publication No. 2 discloses a swallowing aid drink for medicines. In addition, jelly-like drinks (highly viscous liquid foods) have been sold on the market for the purpose of supplementing medication. By mixing the drug with a highly viscous liquid, the purpose is to smooth the passage through the throat and to mask the bitterness and the like of the drug with sweetness and flavor. However, since the highly viscous liquid contains 80% or more of water, there is a disadvantage in storage and portability after opening or for a long time. In addition, in order to solubilize the thickening polysaccharides and other gelling agents at the time of production, 70 ° C
It is necessary to heat it back and forth, or to fill it in a bag or the like formed of aluminum laminated film or the like.

Many methods for reducing the bitterness of drugs, health foods, etc. have already been disclosed. For example, Japanese Patent Laid-Open No. 4-3
Japanese Patent No. 46937 discloses a jelly containing agar, gelatin and κ-carrageenan as a gelling agent, and masks a bitter substance by enclosing it in the jelly.

Further, JP-A-11-92402 discloses a pharmaceutical composition containing a hydrophilic substance having a positive charge and an anionic polymer substance in a basic drug, and a basic composition having an unpleasant taste is particularly disclosed. In order to conceal a drug, blending of an anionic polymer substance such as carrageenan has been devised. Since it is difficult to dissolve an anionic polymer substance in water without heating, a method for dissolving an anionic polymer substance has been disclosed. However, a hydrophilic substance having a positive charge that aids solubility is disclosed. However, the molecular weight is as high as about 10,000 to 2,000,000, and it is not easy to dissolve itself.

Generally, a method of dissolving a polymer substance in water includes a method of heating and a large amount (20 to 3 of the polymer substance).
There is a method in which it is dissolved after mixing with an excipient such as sugar (0 times or more). In the method of mixing with an excipient, if the polymer substance is blended in an amount of 10% by weight or more, the solubility becomes poor. However, when the polymer substance contributes to masking the bitterness, a certain amount of blending is required. This method is disadvantageous because it must be secured. In any case, in order to dissolve the polymer substance in water, there were restrictions on the manufacturing process or the formulation design.

[0006]

Therefore, according to the present invention, while maintaining the effect of reducing the bitterness of the basic drug and facilitating swallowing, a smooth powder having a smooth consistency without forming a powder at room temperature is obtained. It is an object to provide a powdered ingestion supplement that is a liquid.

[0007]

Means for Solving the Problems The present invention (1) is a medication supplement for reducing bitterness of a basic drug and facilitating swallowing. Water is added immediately before use and mixed without heating. It is a powdered drug supplement that becomes a viscous liquid by itself.

The present invention (2) further comprises an anionic polymer substance in an amount of 10% by weight or more in the presence of an anti-dusting agent.
It is the medication supplement according to the invention (1).

Furthermore, the present invention (3) is the medication supplement according to the invention (2), wherein the anionic polymer substance is carrageenan, sodium alginate, xanthan gum and / or sodium carboxymethylcellulose.

The present invention (4) is also the medication supplement according to the invention (2) or (3), wherein the anti-dusting agent is sodium hydrogen carbonate and an organic acid.

Further, in the present invention (5), the anionic polymer substance is a kappa-type and / or iota-type carrageenan, and the anti-dust agent is an ionic substance containing calcium ion, potassium ion and / or sodium ion. Is,
It is the medication supplement according to the invention (2).

[0012]

BEST MODE FOR CARRYING OUT THE INVENTION A preferred component for reducing bitterness of a basic drug and facilitating swallowing in the present invention is an anionic polymer substance. Here, the anionic polymer substance is
Comprised of a 6-membered ring having a carboxyl group or a sulfate group,
It is a polymer in which certain units are regularly and repeatedly bonded, and preferably 1,000 water having a temperature of 20 ° C. or higher and lower than 100 ° C.
It is a polymer that dissolves 1 g or more in ml. Further, the anionic polymer substance has a viscosity of a 2 wt% aqueous solution at 25 ° C. of preferably 15 to 50,000 mPa · s, more preferably 100 to 20,000 mPa · s, and further preferably 200 to
It is 8,000 mPa · s. In addition, this viscosity is based on a B-type viscometer measuring method (BM type: manufactured by Tokyo Keiki Co., Ltd.).

Preferred examples of the anionic polymer substance include:
Examples include carrageenan, sodium alginate, xanthan gum, and sodium carboxymethyl cellulose. Further, a plurality of kinds of anionic polymer substances may be used in combination.

The anionic polymer substance according to the present invention can be produced by a conventional method. In addition, for example, from Taito Corporation, "Taito gel K-9" (kappa type carrageenan), "Taito gel SV" (iota type carrageenan), "Taito gel HMV" (lambda type carrageenan), "Taito gel V"
IS-Y "(xanthan gum), Kibun Food Chemifa Co., Ltd." duck algin "(sodium alginate),
It is sold by Daicel Chemical Industries, Ltd. under the product name "CMC Daicel" (carboxymethyl cellulose sodium).

The content of the anionic polymer substance according to the present invention is preferably 5 to 50% by weight, more preferably 10 to 30% by weight, based on the total amount of the powdered medication supplement. .

The powdered drug supplement may contain a polymer substance other than the anionic polymer substance.
Preferred examples of other polymer substances include guar gum, locust bean gum, pectin, pregelatinized starch (modified starch), methylcellulose, hydroxypropylmethylcellulose, hydroxyethylmethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone and polyvinyl alcohol. Can be mentioned.

The powdered drug supplement according to the present invention preferably contains an anti-dusting agent. As a result, even if water is added just before use and mixed without heating, a powdered medication supplement can be made into a viscous liquid without the generation of a refill. In particular, when the content of the anionic polymer substance is 10% by weight or more with respect to the total amount of the powdered drug supplement, the powder is easily formed when the water is added, which is particularly effective in this case. is there.

Examples of the anti-dusting agent include a foaming component. Specifically, sodium hydrogen carbonate and an organic acid can be mentioned. When water is added to the mixed powder of these two, it reacts violently and foams while generating carbon dioxide gas. In this case, sodium hydrogen carbonate has a particle size of preferably 0.01 to 500 μm, more preferably 0.1 to 200 μm.
μm. Furthermore, the sodium hydrogen carbonate is preferably 0.01 to 10 times, more preferably 0.05 to 5 times, and more preferably 0.1 to 2 times the weight of the anionic polymer substance. More preferably, the amount is double. On the other hand, the organic acid preferably has a particle size of 0.01 to 5
The thickness is 00 μm, more preferably 0.1 to 200 μm. Suitable examples of organic acids include citric acid, malic acid, lactic acid,
Succinic acid, ascorbic acid, adipic acid, maleic acid,
Examples thereof include water-soluble organic acids such as tartaric acid and erythorbic acid. Further, the organic acid is preferably 0.01 to 10 times the amount based on the weight of the anionic polymer substance,
The amount is more preferably 0.05 to 5 times,
It is more preferable that the amount is double. The ratio of sodium hydrogen carbonate to the organic acid is not particularly limited as long as it is within the above-mentioned blending amount range.

When kappa-type and / or iota-type carrageenan is used as the anionic polymer substance,
A salt containing calcium ion, potassium ion or sodium ion may be used as the anti-dust agent. This combination also allows for uniform distribution in water. Suitable examples of this ionic substance containing calcium ion, potassium ion or sodium ion include calcium lactate, calcium gluconate, calcium chloride, potassium chloride, potassium monohydrogen phosphate, potassium dihydrogen phosphate, potassium carbonate, potassium hydrogen carbonate, Contains calcium, potassium or sodium ions such as potassium citrate, potassium tartrate, sodium chloride, sodium monohydrogen phosphate, sodium dihydrogen phosphate, sodium carbonate, sodium hydrogen carbonate, sodium citrate, sodium tartrate, sodium sulfate, etc. An ionic substance is mentioned. The ionic substance containing calcium ion, potassium ion and sodium ion is preferably 0.01 to 10 times the amount based on the weight of carrageenan, and 0.0
The amount is preferably 5 to 5 times, more preferably 0.1 to 2 times.

The pharmaceutical supplement according to the present invention contains, if necessary, sugars such as dextrin, glucose, fructose, lactose, sucrose, maltose, mannitol and sorbitol, sweeteners such as aspartame and stevia, strawberry flavors and banana flavors. And the like, amino acids such as glycine and serine, pH adjusting agents, water-soluble vitamins, coloring agents, and flavoring agents such as cocoa powder.

The basic drug for which bitterness is reduced by the medication supplement according to the present invention is not particularly limited, but examples of the basic drug having an unpleasant taste include clarithromycin, azithromycin, erythromycin and chlorampheni. Cole, cefotiam hexetil hydrochloride, cefcanel daloxate, renampicillin hydrochloride, bacampicillin hydrochloride, tarampicillin hydrochloride, berberine chloride, digitoxin, sulpirine hydrochloride, azelastine hydrochloride, etilefrine hydrochloride, diltiazem hydrochloride, propranolol hydrochloride, promethazine hydrochloride, pipaverine hydrochloride, ,
Aminophylline, phenobarbital, calcium pantothenate, donevezil hydrochloride, aminoguanidine hydrochloride and the like can be mentioned.

The drug supplement according to the present invention has a solubility of preferably 200 seconds or less, more preferably 100 seconds or less, still more preferably 50 seconds or less. In addition, the value of "solubility" in this specification is 200 ml beaker (body diameter 67 m
80 ml of water (water temperature 20 ± 5 ° C) was put into m, height 89 mm) and stirred at a speed of 400 rpm with a disk-shaped rotor (made by Nalgene, Starhead) having a diameter of 35 mm and a thickness of 12 mm, It is the time until the solid matter cannot be visually confirmed after the polymer material-containing powder composition is added.

[0023]

EXAMPLES The present invention will now be described with reference to examples, but the present invention is not limited to these examples.

Here, the bitterness masking effect carried out in the examples was evaluated by a sensory test, and the evaluation criteria are as follows:
Staged. +3: very bitter, +2: bitter, +1: slightly bitter, ± 0: neither can be said, −1: bitter, the following preparations having bitterness were used. Zithromax Fine Granules for Children (Pfizer Pharmaceutical Co., Ltd .: Azithromycin Hydrate Preparation), Clarice Children's Dry Syrup (Taisho Pharmaceutical Co., Ltd .: Clarithromycin Preparation)

Further, the swallowing assisting effect was evaluated by a sensory test, and the evaluation criteria were the following three grades. ×: Difficult to swallow, Δ: Neither can be said, ○: Easy to swallow In addition, in the test of the swallowing auxiliary effect, tablet-like helsing
One tablet of multi-vitamin tablet (manufactured by Sankyo Co., Ltd.) was used.

Example 1 and Comparative Example 1 (with anionic polymer)
Effect of Solubility of Anti-Graining Agent) 3 g of κ-carrageenan, 1 g of sodium hydrogen carbonate, 1 g of citric acid, and 10 g of sorbitol were mixed to obtain a powder composition. Solubility was measured using 1 g of this. Further, the type of anionic polymer substance was changed to obtain powder compositions, and the solubility was measured. The results are shown in Table 1. A powder composition obtained by mixing 3 g of the anionic polymer and 10 g of sorbitol was used as Comparative Example 1.

[0027]

[Table 1]

Example 2 and Comparative Example 2 (Carrageenan and Io)
Effect of Solubility of Organic Substances) 3 g of κ-carrageenan, 1 g of calcium lactate, 4 g of pregelatinized starch and 10 g of sorbitol were mixed to obtain a powder composition. Solubility was measured using 1 g of this. Further, calcium lactate was changed to potassium chloride and sodium citrate to obtain a powder composition, and the solubility was measured. The results are shown in Table 2. A powder composition containing no ionic substances such as calcium lactate, potassium chloride and sodium citrate was used as Comparative Example 2.

[0029]

[Table 2]

Example 3 and Comparative Example 3 (with anionic polymer)
Bitterness masking effect of foaming component) Sodium alginate 3 g, sodium hydrogen carbonate 1 g,
1 g of citric acid and 10 g of sorbitol were mixed to obtain a powder composition. 10 ml of water was added to 1.5 g of the mixture, and when gelled, 1 g of Zithromax was added and further mixed, and a sensory test was conducted by 10 test subjects. Furthermore, 0.5 g of Clarice was mixed instead of Zithromax and a sensory test was conducted. The results are shown in Table 3.
A powder composition containing 6 g of pregelatinized starch instead of sodium alginate was used as Comparative Example 3.

[0031]

[Table 3]

Example 4 and Comparative Example 4 (Carrageenan and Io)
Bitterness-masking effect of anionic substances) 2 g of κ-carrageenan, 0.5 g of calcium lactate, 6 g of pregelatinized starch and 10 g of sorbitol are mixed to obtain a powder composition. To 1.5 g of this is added 10 ml of water and mixed to form a gel. When it became a state, 1 g of Zithromax was added and further mixed, and a sensory test was conducted by 10 test subjects. Furthermore, Clarice 0.5g instead of Zithromax
Were mixed and a sensory test was conducted. The results are shown in Table 4. A powder composition obtained by mixing 6 g of pregelatinized starch excluding κ-carrageenan and calcium lactate and 10 g of sorbitol was used as Comparative Example 4.

[0033]

[Table 4]

Example 5 and Comparative Example 5 (with anionic polymer)
Bitterness masking effect of foaming component) xanthan gum 2 g, guar gum 1 g, sodium hydrogen carbonate 1.2 g, citric acid 0.6 g, sorbitol 10 g
Were mixed to obtain a powder composition. 10g water to 1.5g
Was added and mixed, and when it became a gel, 1 g of Zithromax was added and further mixed, and a sensory test was conducted by 10 test subjects. Furthermore, 0.5 g of Clarice was mixed instead of Zithromax and a sensory test was conducted. The results are shown in Table 5. A powder composition containing 4 g of pregelatinized starch instead of xanthan gum was used as Comparative Example 5.

[0035]

[Table 5]

Example 6 and Comparative Example 6 (of an anionic polymer)
Swallowing assisting effect) κ-carrageenan 3 g, sodium hydrogen carbonate 1.2 g,
0.6 g of citric acid and 10 g of sorbitol were mixed to obtain a powder composition. To 1.5 g of this, 10 ml of water was added and mixed to form a gel, and a sensory test was conducted by 10 test subjects. Furthermore, the kind of anionic polymer was changed, the powder composition was obtained, and the sensory test was done. The results are shown in Table 6. A composition containing no anionic polymer, that is, a powder composition prepared by mixing 1.2 g of sodium hydrogen carbonate, 0.6 g of citric acid and 10 g of sorbitol was prepared.
Comparative Example 6 was prepared by dissolving 10 ml of water and dissolving.

[0037]

[Table 6]

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/12 A61K 47/12 47/36 47/36 47/38 47/38 F term (reference) 4B018 MD01 MD33 MD37 MD38 ME14 4B041 LC01 LC03 LD01 LE01 LH10 LH11 LH16 LK01 LK07 4C076 AA29 BB01 CC40 DD25 DD38 DD41 DD43 EE32T EE36T EE58T FF16 FF67

Claims (5)

[Claims] 1. A drug supplement for reducing bitterness of a basic drug and facilitating swallowing, a powder which becomes a viscous liquid only by adding water immediately before use and mixing without heating. -Like medication supplements. 2. The drug supplement according to claim 1, which contains 10% by weight or more of an anionic polymer substance in the presence of an agent for preventing powdering (mamako). 3. The medication supplement according to claim 2, wherein the anionic polymer substance is carrageenan, sodium alginate, xanthan gum and / or sodium carboxymethyl cellulose. 4. The drug supplement according to claim 2, wherein the anti-dusting agent is sodium hydrogen carbonate and an organic acid. 5. The anionic polymer substance is a kappa-type and / or iota-type carrageenan, and the anti-dusting agent is an ionic substance containing calcium ion, potassium ion and / or sodium ion. Medication supplements.