JP2003073291A - Oral liquid formulation - Google Patents

Abstract

(57) Abstract: An oral liquid preparation containing a assembly extract and having a pH adjusted to 4 to 7. [Effect] In the liquid preparation for internal use of the present invention, the medicinal component in the assembly extract is stably maintained for a long period of time, so that the medicinal effect is maintained for a long period of time.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a liquid preparation for oral administration in which a medicinal component of an Assemblage extract is stably retained for a long period of time.

[0002]

2. Description of the Related Art Senburi (Swertia herba), a herbal medicine
Is a whole flowering plant of Swertia japonia Makino, which is classified as a bitter stomachic drug, and has medicinal effects such as gastric catarrh, gastric hyperacidity, and anorexia. The assembly contains swertiamarin, which is a bitter glycoside, as well as sweltianoline, erythrocentaurine, swelltriano, oleanolic acid, and gentianine.

Conventionally known as powdered preparations, powders, tablets and the like as preparations containing such gastric medicines as the above-mentioned assembly are powders, powders, tablets and the like, but in recent years absorption is rapid after administration and immediate effect is expected. As a result, oral liquid preparations are marketed.

[0004]

However, it has been found that the content of swertiamarin, which is one of its medicinal components, decreases with time when the assembly extract is incorporated into a liquid preparation for oral administration. Therefore, it is an object of the present invention to provide a liquid preparation for oral administration which stably holds the Aspergillus oryzae extract for a long period of time.

[0005]

Therefore, the present inventor has found that the cause of the decrease in the content of the assembly extract is temperature, concentration and pH.
As a result of examination from various points such as pH, pH is extremely important for the stability of the swertiamarin content in the assembly extract in the liquid formulation over time,
It was discovered that an oral liquid preparation having excellent swell thiamarin content stability over time can be obtained by adjusting the amount to 7, and the present invention has been completed.

[0006] That is, the present invention provides a liquid preparation for oral administration, which contains an Aspergillus orientalis extract and whose pH is adjusted to 4 to 7.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION The liquid preparation for oral administration of the present invention contains an assembly extract that is a bitter stomachic ingredient. Here, as the assembly extract, water, hot water, from the assembly of herbal medicine,
An extract extracted with a solvent such as ethanol or a water-ethanol mixed solution is used, but an extract with a water-ethanol mixed solution is particularly preferable.

[0008] The content of the assembly extract in the liquid preparation for oral administration according to the present invention is 5 to 3000 in terms of a daily dose converted to the original drug.
mg, especially 10 to 1500 mg is preferred.

The pH of the liquid preparation for oral administration of the present invention is 4 from the viewpoint of the temporal stability of the swertiamarin content in the assembly extract.
It is necessary that it is -7, 4.4-6.3 is preferable, 4.5-6.0 is more preferable, and 4.8-5.8 is particularly preferable.

To adjust the pH to 4-7, the pH in this range
It is preferable to use a buffering agent for Such buffers include citric acid, succinic acid, acetic acid, tartaric acid, hydrochloric acid, sulfuric acid, gluconic acid, lactic acid, fumaric acid, boric acid, maleic acid, phosphoric acid, methanesulfonic acid, malic acid, salts thereof, and the like. Examples of the buffering agent include: citric acid, sodium citrate, tartaric acid, sodium tartrate, malic acid, sodium malate, and the like. These buffers are added in an amount to adjust the pH within the above range.

In the liquid preparation for internal use of the present invention, medicinal components other than the Assemblage extract can be blended. The medicinal ingredient is not particularly limited as long as it is a medicinal ingredient that acts on the digestive system, for example, aniseed fruit, aloe, fennel, turmeric, oyster, life-prolonging grass, eugon, oubakku, oren, processed ginger, gauze, cuckoo, Calamus root,
Campi, chaff, pheasant, cinnamon, gentian, kojin, koboku, goshuyu, pepper, colombo, konzulango, salamander, yamana, perilla, shukusha, ginger, oyster, blue skin, stone root, centaurium,
Amaranthus, Soyo, Large scent, Rhubarb, Chixen carrot, Clove, Chimpanzee, Capsicum, Spruce, Animal gall, Nigaki, Nikuzuku, Carrot, Mint, Hihatu, Juniper, Hop, Homika, Suisho, Mokkou, Yakuchi, Ryutan, Ryokan Extracts of natural stomachic herbs such as; betaine hydrochloride, glutamate hydrochloride, carnitine chloride, bethanechol, dry yeast and other stomachic agents; dried aluminum hydroxide gel, magnesium aluminate silicate, magnesium silicate, synthetic aluminum silicate,
Synthetic hydrotalcite, magnesium oxide, alumina magnesium hydroxide, aluminum hydroxide gel, aluminum hydroxide / sodium hydrogen carbonate coprecipitation product, aluminum hydroxide / magnesium carbonate mixed dry gel, aluminum hydroxide / magnesium carbonate / calcium carbonate Precipitated products, magnesium hydroxide, sodium hydrogen carbonate, magnesium carbonate, precipitated calcium carbonate, magnesium aluminometasilicate, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate, crow bone, stone determination, boley, aminoacetic acid, dihydroxyaluminum Antacids such as aminoacetate and funnel extract; starch digestive enzyme, protein digestive enzyme, fat digestive enzyme, fibrin digestive enzyme, ursodesoxycholic acid, oxycholanates, cholic acid, bile powder,
Bile extract (powder), dehydrocholic acid, digestive agents such as animal gall; intestinal regulators such as red bud, acacia yak, ubay, ketsumeishi, gem ginger, acrinol, berberine chloride, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, berberine tannate. , Bismuth subsalicylate, bismuth subnitrate, bismuth subcarbonate, bismuth subgallate, tannic acid, albumin tannate, methylenethymol tannin, kaolin, natural aluminum silicate, aluminum hydroxynaphthoate, pectin, medicinal carbon, precipitated calcium carbonate, Antidiarrheal agents such as calcium lactate, calcium hydrogen phosphate, Acacia catechu, eucalyptia, psyllium, lauren, kujin, ginseng, quintet, hawthorn, eucalypt; oxyphencyclimine hydrochloride, disa hydrochloride Kuromin, hydrochloric Mechikisen, scopolamine hydrobromide, methyl bromide atropine,
Methyl anisotropin bromide, methyl scopolamine bromide,
Methyl bromide-1-hyoscyamine, methylbenactidium bromide, belladonna extract, isopropamide iodide, diphenylpiperidinomethyldioxolane iodide, funnel extract, fungal root alkaloid citrate, papaverine hydrochloride, ethyl aminobenzoate , Analgesic, licorice, cinnamon, peony, and other analgesic / spasmodic agents; sodium azulene sulfonate, aldioxa, glycyrrhizic acid and its salts, and licorice extract, L-glutamine, potassium copper chlorophyllin, sodium copper chlorophyllin,
Histidine hydrochloride, porcine gastric wall pepsin hydrolyzate, porcine gastric acid hydrolyzate, methylmethionine sulfonium chloride, mucous membrane repair components such as red bud, Engosaku, licorice and the like can be blended.

Further, the liquid preparation for oral administration of the present invention includes stabilizers such as sodium aspartate, sodium alginate, sodium edetate, sodium sulfite and sodium bisulfite; sweeteners such as sorbitol and sucrose; sodium chloride and L-glutamic acid. Flavoring agents such as sodium, honey and apple juice; coloring agents such as caramel; flavoring agents such as l-menthol, mint flavor, cherry flavor, etc.
Flavoring agents such as essential oils such as lemon oil, orange oil and spearmint oil; preservatives such as sodium benzoate and butyl paraoxybenzoate; dissolution aids such as polyoxyethylene hydrogenated castor oil and ethanol .

The liquid preparation for oral administration of the present invention is useful as an oral liquid gastrointestinal drug, and it is usually a preparation having a dose of 20 to 100 mL, and it is preferable to prepare a preparation for taking 1 to 3 times a day.

[0014]

The present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.

Examples 1 to 12 and Comparative Examples 1 and 2 Liquid oral preparations containing the Aspergillus oryzalis extract were prepared according to the formulations shown in Tables 1 and 2. The crude drugs in the table are as follows.

(1) Assemblage extract (1 mL of this product corresponds to 1 g of the crude drug. Extraction solvent: aqueous ethanol) (2) Ginger flow extract (1 mL of this product corresponds to 1 g of the crude drug. Extraction solvent: Aqueous ethanol solution) (3) Ginseng extract (1 g of this product corresponds to 4 g of crude drug. Extraction solvent: ethanol aqueous solution) (4) Turmeric flow extract (1 mL of this product corresponds to 1 g of crude drug. Extraction solvent: ethanol Aqueous solution) (5) Cayce oil (essential oil obtained by steam distillation of cinnamon) (6) Clove oil (essential oil obtained by steam distillation of clove) (7) Fennel oil (essential oil obtained by steam distillation of fennel)

[0017]

[Table 1]

[0018]

[Table 2]

Test Examples Liquid formulations of Examples 1 to 12 and Comparative Examples 1 and 2 were treated at a temperature of 70.
After storing under conditions of ° C for 3 days, the residual amount of swertiamarin in the preparation was quantified by high performance liquid chromatography. As a result, as shown in Table 3, even under the severe condition of 70 ° C., swertiamarin was stable in the liquid preparation containing the Aspergillus oryzalis extract within the pH range of 4 to 7. Also, 70
Even under the severe conditions of ℃, Sweltia marine has a pH of 4.4-
Within the range of 6.3, 50% or more remains, and the pH is 4.5 to 6.
In the range of 0, 60% or more remained, and in the range of pH 4.8 to 5.8, 70% or more remained, which was stable.

[0020]

[Table 3]

[0021]

INDUSTRIAL APPLICABILITY The liquid preparation for oral administration of the present invention has a long-lasting medicinal effect because the medicinal component in the assembly extract is kept stable for a long time.

   ─────────────────────────────────────────────────── ─── Continued front page    (72) Inventor Misao Murata             221-271 Namikicho, Narita City, Chiba Prefecture (72) Inventor Tetsuo Kaneko             2-23-7 Tamatsukuri, Narita City, Chiba Prefecture (72) Inventor Katsumi Imamori             2521-86 Shimodashi Nitta, Yotsukaido City, Chiba Prefecture F term (reference) 4C076 AA12 BB01 CC16 DD19 DD38                       DD41 DD67 EE53 FF63                 4C088 AB67 AC01 BA08 BA13 BA31                       CA04 MA17 MA52 NA03 ZA69

Claims (2)

[Claims] 1. A liquid preparation for oral administration, which contains the assembly extract and whose pH is adjusted to 4 to 7. 2. The liquid preparation for internal use according to claim 1, which has a pH adjusted to 4.4 to 6.3.