JPH0696536B2 - Internal suspension containing antacid - Google Patents

Description

TECHNICAL FIELD The present invention relates to an antacid-containing internal suspension, and more specifically, for various symptoms such as gastric pain, gastric weight, gastric hyperacidity, and heartburn. The present invention relates to an antacid-containing internal suspension that can rapidly produce effects after administration.

(Prior Art) Conventionally, stomach ache, stomach ache, hyperacidity, heartburn, stomach discomfort, stomach bloating, leaning (stomach leaning), chest tightness, belching, sneezing (nausea, upset stomach). , Upset hangover / nausea, nausea, nausea), vomiting, excessive drinking (overdose)
For various symptoms such as the above, solid preparations such as tablets, capsules, granules, fine granules or powders mainly containing an antacid are often used. However, it takes time for the solid preparation to disintegrate, and it takes time for the medicinal effect to appear after taking. On the other hand, if the dosage form is a liquid, it can be easily taken,
It diffuses rapidly in the stomach, attaches to the gastric mucosa, and can rapidly exert its effect. For this reason, recently, internal suspensions mainly composed of antacids have been found.

(Problems to be Solved by the Invention) However, none of the conventional internal suspensions mainly composed of an antacid is satisfactory in dispersibility and redispersibility. Generally, what is required as a suspension is
It is necessary that the sedimentation of dispersed particles is slow and that redispersion is easy. That is, it is necessary to suppress the sedimentation of the particles by making the dispersoid into fine particles or increasing the viscosity of the dispersion medium. However, even if the particles are finely pulverized into primary particles to produce a suspension agent, secondary particles in which a large number of particles are aggregated to form secondary particles are settled from the large particles, are deposited on the bottom of the container, and are aged over time. Will not be redistributed into. Further, if the viscosity of the dispersion medium is increased, it will be difficult to take the drug, the drug will not diffuse sufficiently in the stomach, and the onset of drug effect will be delayed.

Many methods of producing an aqueous suspension are known, and a method of using gum arabic, sodium carboxymethylcellulose, hydroxypropylmethylcellulose, hydroxyethylcellulose, gelatin, bentonite or the like as a dispersant is known. When a suspension is produced using the above-mentioned dispersant by a usual method for producing a suspension, the particles may coalesce with each other or the viscosity may increase. as a result,
Particles with a large particle size and particle density settle down, settle on the bottom of the container, and do not redisperse over time, resulting in a non-uniform formulation when taken.

(Means for Solving the Problem) As a result of intensive studies, the present inventors have used either starch or a starch derivative as a dispersant to form a network structure in which particles interact with each other. Thus, the present invention has been completed by obtaining an internal suspension containing an antacid which has a low viscosity and is excellent in dispersibility and redispersibility and which is cohesive and sedimentable.

That is, the antacid-containing internal suspension of the present invention is characterized by comprising an antacid and any of starch and starch derivatives.

As the antacid used in the present invention, dry aluminum hydroxide gel, magnesium aluminate silicate, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, magnesium oxide, magnesium hydroxide alumina, aluminum hydroxide gel , Aluminum hydroxide / sodium hydrogen carbonate coprecipitation product, aluminum hydroxide / magnesium carbonate mixed dry gel, aluminum hydroxide / magnesium carbonate / calcium carbonate coprecipitation product, magnesium hydroxide, magnesium carbonate, precipitated calcium carbonate,
Examples thereof include magnesium aluminometasilicate, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate, oyster bone, stone determination and boley, which are used alone or in a mixture of two or more kinds. Among these, strong antacid,
Since they are fine particles, it is preferable to use at least one selected from the group consisting of magnesium aluminometasilicate, synthetic hydrotalcite, magnesium hydroxide, aluminum hydroxide gel and magnesium oxide. The particle size of the antacid is usually 0.01 to 20 μm, preferably 0.01 to 5 μm.

The dispersant used in the present invention is either starch or starch derivatives. Examples of the starch include wheat starch, rice starch, corn starch, potato starch, waxy corn starch, waxy starch and the like. Examples of the starch derivative include starch ester such as acetic acid ester, succinic acid ester, nitric acid ester, phosphoric acid ester, and xanthogenic acid ester, and starch ether such as allyl ether and
Examples of the crosslinked starch such as methyl ether, carboxymethyl ether, hydroxyethyl ether, hydroxypropyl ether, and positive starch include formaldehyde crosslinked starch, epichlorohydrin crosslinked starch, and phosphoric acid crosslinked starch, and any of them may be used.

The mixing ratio of each of these components is usually 0.1 to 70 w / v% of the antacid, 0.05 to 20 w / v of either the starch or the starch derivative, with respect to the total amount of the antacid-containing internal suspension. %. If the blending ratio is out of this range, the dispersibility and redispersibility become poor, which is not desirable. Furthermore, preferably, the antacid is 0.1 to 30 w / v%, and either starch or starch derivative is 0.1 to 5.0 w / v%.

In the present invention, if necessary, aminoacetic acid, an anomic acid agent such as dihydroxyaluminum aminoacetate,
Aloe, cinnamon, gastric crude drug such as ginger, gastrointestinal function regulator such as carnitine chloride, bethanechol chloride, ursodesoxycholic acid, choleretic agent such as bile powder, kaolin, adsorbent such as natural aluminum silicate, lactic acid Coating agents such as calcium, fungal extracts, corydalis, licorice and other analgesic and antispasmodic agents, sodium azulene sulfonate, copper chlorophyllin sodium, mucosal repair agents such as histidine hydrochloride, sodium benzoate, methyl paraoxybenzoate, ethyl paraoxybenzoate, paraoxy Preservatives such as propyl benzoate, butyl paraoxybenzoate, dehydroacetic acid and its salts, citric acid, refined sucrose, glucose, flavoring agents such as D-sorbitol, antifoaming agents such as silicone resins, fragrances, coloring agents, etc. What you do is not regulated.

The method of producing the antacid-containing internal suspension of the present invention will be described by taking the formulation of Sample 1 in Table 1 as an example.

That is, (1) magnesium aluminometasilicate and magnesium hydroxide are weighed, 30 ml of purified water is added, and the mixture is stirred until uniform. (2) Weigh hydroxypropyl starch, add 45 ml of purified water, and stir while heating. Then, add (2) to (1) and stir vigorously to homogenize, add sodium benzoate, purified sucrose and flavor to dissolve and add purified water to make 100 ml, and fill a 30 ml brown glass bottle. It was sealed, sterilized and manufactured.

Sample 2 was manufactured according to sample 1.

Comparative samples a and b were manufactured according to sample 1 with the compositions shown in Table 2.

Sample 1 and sample 2 and sample a and sample b at 40 ° C. and 0
It was stored at 3 ° C for 3 months, and its change with time was examined. The results are shown in Table 3.

Sample 1 and Sample 2 show cohesive sedimentation, 40 ℃ and 0 ℃
The dispersibility and redispersibility were good even after 3 months under the conditions. On the other hand, the sample a exhibited free sedimentation property, and at both 40 ° C. and 0 ° C., it settled from particles having a large particle size and a large particle density, deposited on the bottom of the container to cause caking, and did not redisperse. The high viscosity sample b is 40 ℃
The dispersibility and redispersibility were both good at 0 ° C. and 0 ° C., but the viscosity was high and it was difficult to take.

(Example) Hereinafter, the present invention will be described in more detail with reference to examples.

Example 1 Formulation Magnesium metasilicate 3.0 g Aminoacetic acid 0.9 g Hydroxypropyl starch 2.0 g Sodium benzoate 0.07 g Purified sucrose 6.7 g Fragrance A small amount of purified water 100 ml Total amount according to sample 1 An internal suspension containing an acid agent was produced.

As a result of storing this sample at 40 ° C. and 0 ° C. for 3 months, good dispersibility and redispersibility were shown.

Example 2 Formulation Magnesium hydroxide 2.0 g Licorice extract 0.6 g Hydroxyethyl starch 2.0 g Sodium benzoate 0.07 g Purified sucrose 6.7 g Fragrance A small amount of purified water 100 ml Total antacid of the present invention according to sample 1 An internal suspension containing was prepared.

As a result of storing this sample at 40 ° C. and 0 ° C. for 3 months, good dispersibility and redispersibility were shown.

Example 3 Formulation Synthetic hydrotalcite 4.0 g Keihi flow extract 0.3 ml Ginger flow extract 0.3 ml Starch sodium phosphate 2.0 g Sodium benzoate 0.07 g Purified sucrose 6.7 g Flavor Fine amount Total 100 ml Sample An antacid-containing internal suspension of the present invention was produced according to 1.

As a result of storing this sample at 40 ° C. and 0 ° C. for 3 months, good dispersibility and redispersibility were shown.

Example 4 Formulation Aluminum hydroxide gel 1.0 g Magnesium hydroxide 1.0 g Hydroxypropyl starch 1.5 g Corn starch 0.5 g Sodium benzoate 0.07 g Purified sucrose 6.7 g Flavor A minute amount Purified water is added 100 ml Total amount According to sample 1 An internal suspension containing the antacid of the present invention was produced.

As a result of storing this sample at 40 ° C. and 0 ° C. for 3 months, good dispersibility and redispersibility were shown.

Example 5 Formulation Magnesium aluminometasilicate 3.0 g Magnesium hydroxide 0.5 ml Sodium starch glycolate 2.0 g Sodium benzoate 0.07 g Purified sucrose 6.7 g Fine amount of fragrance Purified water 100 ml Total according to sample 1 An internal suspension containing antacid was prepared.

As a result of storing this sample at 40 ° C. and 0 ° C. for 3 months, good dispersibility and redispersibility were shown.

Example 6 Formulation Magnesium aluminometasilicate 3.0 g Synthetic hydrotalcite 1.5 g Potato starch 2.0 g Sodium benzoate 0.07 g Purified sucrose 6.7 g Fragrance A minute amount of purified water 100.0 ml According to the sample 1 of the present invention An internal suspension containing an antacid was prepared.

As a result of storing this sample at 40 ° C. and 0 ° C. for 3 months, good dispersibility and redispersibility were shown.

(Effects of the Invention) As described above in detail, the antacid-containing internal suspension of the present invention is a formulation having excellent dispersibility and redispersibility, and should be uniformly dispersed and easily ingested during administration. Since it is a medicinal product capable of rapidly producing effects on various symptoms such as gastric pain, gastric weight, gastric hyperacidity, and heartburn, its industrial value is extremely large.

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Claims (2)

[Claims] 1. An antacid-containing internal suspension comprising an antacid and any one of starch and starch derivatives. 2. The antacid is at least one selected from the group consisting of magnesium aluminometasilicate, synthetic hydrotalcite, magnesium hydroxide, aluminum hydroxide gel and magnesium oxide. The suspension according to item 1.