JPS6346046B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a stable antacid-containing internal solution. Currently, the products on the market as internal liquid gastrointestinal medicines are gastrointestinal medicines whose main ingredients are herbal medicines. Although these products can be expected to have a stomach-healthy effect, they do not have a sufficient therapeutic effect on nausea, heartburn, etc. caused by hyperacidity. Therefore, if an antacid can be incorporated into an internal liquid preparation, it will become an internal liquid gastrointestinal drug that is also effective against hyperacidity. Most antacids are sparingly soluble in water, so they form an aqueous suspension. An internal liquid preparation containing an antacid is characterized by the fact that the antacid is suspended in the form of fine particles, so there is no need for the time needed for it to disintegrate as with solid preparations. Immediately, the antacid particles react with stomach acid,
Antacid effects appear faster than with solid formulations. Moreover, the coating effect on the gastric mucosa is also high because the antacid is in the form of fine particles. Therefore, oral liquid preparations containing antacids are more useful pharmaceuticals than solid preparations with the same antacid effect. As antacids, there are suspensions of magnesium hydroxide and magnesium aluminate metasilicate, but these have not reached the level of general use due to the stability and taste of the formulation. Many methods are known for producing aqueous suspensions, including methods using gum arabic, sodium carboxymethylcellulose, hydroxypropylmethylcellulose, gelatin, tragacanth, clay minerals, and the like. When an antacid is used as a suspending agent using such a method, particles settle and redispersion becomes impossible, and particles tend to aggregate if stored in a cold place. Generally, suspending agents stabilize the dispersion system by increasing the viscosity of the dispersion medium. However, simply by increasing the viscosity and slowing down the sedimentation rate of the particles, it is difficult to maintain a good suspended state for a long period of time, and it is unavoidable that the particles will sediment. In other words, it is thought that even if the suspended particles are sedimented, they can be easily redispersed by shaking a little to obtain a good suspended state. The present inventors have investigated various types of oral liquid preparations containing antacids, and have found a method that maintains a stable suspension state that is easy to take and that can reproduce that state even when stored for a long period of time, and has developed the present invention. completed. That is, the present invention resides in an antacid-containing liquid preparation for internal use, which is characterized by adding a suspending agent and an amino acid to an antacid. The antacid used in the present invention has a particle size of 0.01 to
at least one of magnesium aluminate metasilicate, synthetic hydrotalcite, magnesium hydroxide, aluminum hydroxide gel, and magnesium oxide, with a particle size of 20μ, preferably 0.01 to 10μ. As the suspending agent, at least one of calcium carboxymethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, sodium alginate, crystalline cellulose, vegum, and bentonite is used. The suitable range of use of the suspending agent is usually 0.005 to 5 w/v%, preferably 0.01 to 3 w/v%, based on the suspension.
It is. As the amino acid, at least one of alanine, arginine, glycine, glutamine, threonine, valine, histidine, lysine, leucine, isoleucine, aspartic acid, glutamic acid, and salts thereof is used. The amount of amino acids used is usually 0.001 to 5 w/v%, preferably 0.01 to 3 w/v%, based on the entire suspension. Table 1 shows the changes over time at 25±1°C and 3±1°C of the antacid-containing oral solution according to the present invention.

[Table] As shown in Table 1, No. 1 according to the present invention is 25±
As a result of storage at 1° C. for 3 months, the antacid particles were in a precipitated state, but when shaken a little, they were redispersed and became a good suspension. It also showed good redispersibility when stored at 3±1°C for 3 months. In contrast, no redispersion was observed in Comparative Examples No. 2 and No. 3. In the production of the antacid-containing internal solution according to the present invention, active ingredients, sweeteners, fragrances, preservatives, solubilizing agents, etc. can be added as appropriate. The type, amount, and method of addition of these active ingredients or additives can be selected in accordance with the methods commonly used in pharmaceutical manufacturing. Next, in order to explain in more detail the method for producing a liquid agent according to the present invention, specific examples thereof will be illustrated below. Example 1 Magnesium aluminate metasilicate 3.0g Glycine 0.9g Hydroxypropyl methylcellulose 0.1g Refined white sugar 9.0g Sodium benzoate 0.05g Flavor Total volume 100ml with slightly purified water Manufacturing method Add hydroxypropyl methylcellulose to an appropriate amount of purified water and dissolve by heating. Dissolve glycine, refined white sugar, and sodium benzoate in this, add magnesium aluminate metasilicate, homogenize, add flavoring, and then add purified water to bring the total volume to a boil.
Dilute to 100 ml, sterilize it by the usual method, and use it as a liquid preparation for internal use. Example 2 Magnesium aluminate metasilicate 3.0g Magnesium hydroxide 0.5g Histidine hydrochloride 0.18g Veegum 1.0g Refined sucrose 9.0g Sodium benzoate 0.05g Flavor Total volume 100ml with slightly purified water Manufacturing method Internal liquid preparation by the same method as Example 1 shall be. Example 3 Magnesium hydroxide 2.0g DL-alanine 1.0g Sodium carboxymethyl cellulose 0.1g Licorice extract 0.6g Refined sucrose 5.0g Sodium benzoate 0.06g Flavor Total volume 100ml with slightly purified water Production method Liquid for internal use using the same method as Example 1 shall be. Example 4 Synthetic hydrotalcite 4.0g Histidine hydrochloride 0.1g Keihi extract 0.3ml Keihi extract 0.3ml Sodium alginate 0.05g DL-menthol 0.02g Ethanol 0.1g Refined white sugar 6.0g Sodium benzoate 0.06g Add purified water to make a total volume of 100ml Manufacturing method Prepare a liquid preparation for internal use using the same method as in Example 1. Example 5 Aluminum hydroxide gel 1.0g Magnesium hydroxide 1.0g Lysine hydrochloride 0.1g Thiamine nitrate 0.005g Sodium riboflavin phosphate 0.002g Bentonite 0.03g Hydroxypropyl methylcellulose 0.08g Refined white sugar 5.5g Sodium benzoate 0.06g Flavor A small amount of purified water In addition, a total volume of 100 ml was prepared as a liquid for internal use using the same method as in Example 1. Example 6 Synthetic hydrotalcite 1.0g Glycine 0.6g L-glutamine 2.0g DL-alanine 2.0g Sodium L-aspartate 0.05g L-valine 0.2g DL-menthol 0.01g Carboxymethylcellulose calcium 0.01g Veegum 0.01g Ethanol 0.1g Benzoin Sodium chloride 0.06g Glucose 10.0g Add purified water to make a total volume of 100ml.Production method Use the same method as Example 1 to prepare a liquid for internal use. Examples 1 to 6 were stored at 25±1°C or 3±1°C for 3 months, and all exhibited good redispersibility.

Claims (1)

[Scope of Claims] 1. An antacid-containing internal solution prepared by adding a suspending agent and an amino acid to an antacid. 2. The liquid preparation according to claim 1, wherein the antacid is at least one of magnesium aluminate metasilicate, synthetic hydrotalcite, magnesium hydroxide, aluminum hydroxide gel, and magnesium oxide having a particle size of 0.01 to 20μ. . 3. The suspending agent is at least one of carboxymethylcellulose calcium, carboxymethylcellulose sodium, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, sodium alginate, crystalline cellulose, vegum, and bentonite.
The liquid preparation according to claim 1, which is a seed. 4. The liquid preparation according to claim 1, wherein the amino acid is at least one of alanine, arginine, glycine, glutamine, threonine, valine, histidine, lysine, leucine, isoleucine, aspartic acid, glutamic acid, and salts thereof.