KR20030019902A - Liquid preparations for internal use - Google Patents

Abstract

PURPOSE: To provide an oral solution preparation that can retain the efficacy of the preparation for a long period of time because the active components in the sialid extract are preserved stably for a long period of time. CONSTITUTION: The oral solution preparation includes the sialid extract as the active components and has a pH adjusted to 4-7.

Description

Underwear Liquid Formulation {LIQUID PREPARATIONS FOR INTERNAL USE}

The present invention relates to an oral liquid formulation in which the medicinal component of the extract is stably maintained for a long time.

Swertia herba is the outpost of the flowering period of Swertia japonia Makino. It is classified as Gourmet Stomach, and has effects on stomach catarrh, hyperacidity and loss of appetite. In the beginning of the month of the gentian, Swertiamarin, which is a bitter glycoside, includes swertianarin, erythrosentaurin, swertoriano, oleanoic acid, and gentianine.

Powder formulations, powdered medicines, tablets and the like are conventionally known as formulations containing such hygiene medicines such as the beginning of the month. However, in recent years, an oral liquid formulation has been released since the absorption after taking the drug is fast and immediate effect can be expected.

However, it has been found that, when the extract of early October, the extract is formulated into an internal liquid formulation, the content of swertiamarin, which is one of its active ingredients, decreases over time.

Accordingly, it is an object of the present invention to provide an oral liquid preparation having a long-term and stable extract of early spring.

The present inventors have investigated the causes of the content drop of the extract of early spring, from various points such as temperature, concentration, pH, and the like. Is extremely important, and furthermore, by adjusting the pH to 4-7, it was found that an oral liquid formulation having excellent time stability of the swertia marine content was obtained, and thus, the present invention was completed.

That is, the present invention is to provide an oral liquid formulation containing an extract of early spring and adjusting the pH to 4-7.

Best Mode for Carrying Out the Invention

The oral liquid preparation of the present invention contains an extract of the herbaceous vinegar which is a bitter dry stomach ingredient. Here, as the extract of the early spring, an extract extracted with a solvent such as water, hot water, ethanol, and a water-ethanol mixture from a crude herbaceous extract, is used, but an extract by a water-ethanol mixture is particularly preferable.

As for content of the extract of the extract of the beginning of the month of the present invention in the oral liquid formulation of this invention, 5-3000 mg, especially 10-1500 mg are preferable in conversion of original herbal as a daily dose.

PH of the internal liquid liquid preparation of this invention needs to be 4-7 from the point of the stability with time of the swertiamarine content in the extract of the beginning of the month, 4.4-6.3 are preferable, 4.5-6.0 are more preferable, 4.8-5.8 This is particularly preferred.

In order to adjust pH to 4-7, it is preferable to use the buffer for making pH of this range. 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. , Citric acid, sodium citrate, tartaric acid, sodium tartarate, malic acid, sodium malate and the like are preferable. These buffers are combined in amounts to adjust the pH to the above range. Moreover, you may use together these acids and alkali metal hydroxide, especially sodium hydroxide as a buffer system.

In the internal liquid liquid formulation of the present invention, it is possible to mix medicinal ingredients other than the extract of early spring. The active ingredient is not particularly limited as long as it is an active ingredient that acts on the digestive system. For example, an aniseum (Pimpinella anisum) fruit, aloe, fennel fruit, turmeric, oak (오), yeonmyeongcho (延命) Green, golden, yellow wall, yellow lotus, processed garlic, azul, brown, mosquito Rami Root, skin, crust, ground Cinnamon, cinnamon, gentiana, red ginseng, safflower, sesame oil, lodging, carumbah root, condurango, sancho, sanna, perillae perillas fructus, Amoni Semen, Ginger, Soybean Paste, Cheongpi, Seok Geun Suk, Centaurium, Creation, Perillae Herba, Conventional Fragrance, Rhubarb, Bamboo Rice Ginseng, sperm, dermis, pepper, red pepper, animal gallbladder, dead tree, nutmeg, ginseng, peppermint, long pepper, white peach, hops, nox bomica nux vomica), Extracts of hygiene medicines such as Buckbean, Mokyang, Alpiniae Fructus, Gentian, Alpiniae Officinari Rhizoma, etc .; Healthy agents such as betaine hydrochloride, glutamic acid hydrochloride, carnitine chloride, betanechol chloride and dry yeast; Dry aluminum hydroxide gel, magnesium silicate, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, magnesium oxide, alumina magnesium hydroxide, aluminum hydroxide gel, aluminum hydroxide and sodium hydrogen carbonate coprecipitation product, aluminum hydroxide and magnesium carbonate mixed dry gel , Aluminum hydroxide, magnesium carbonate, calcium carbonate coprecipitation product, magnesium hydroxide, sodium bicarbonate, magnesium carbonate, precipitated calcium carbonate, magnesium metasilicate aluminate, anhydrous calcium phosphate, calcium hydrogen phosphate, squid bone, crystallization (石決明) Antacids such as Ostreae Testa, aminoacetic acid, dihydroxyaluminum aminoacetate, and Scopolia extract; Digestive agents such as starch digestive enzyme, protein digestive enzyme, fat digestive enzyme, fibrin digestive enzyme, urodesoxycholic acid, oxycholates, cholic acid, bile powder, bile extract (powder), dehydrocholic acid and animal gallbladder; Formal preparations such as red bean bag, hyacinth medicine, omae, malaria, postal mail and the like; Acrinol, berberine chloride, guayacol, creosote, phenyl salicylate, guayacol carbonate, berberine carbonate, tannin berberine, chusalicylic acid bismuth, bismuth bismuth, bicarbonate bismuth, chagaric bismuth, tannic acid, Albumin tannin, methylene thimoltannic acid, kaolin, natural aluminum silicate, hydroxynaphthoate, aluminum pectin, medicinal charcoal, precipitated calcium carbonate, calcium lactate, calcium hydrogen phosphate, sun medicinal herbs, omega, yellow wall, yellow lotus, red ginseng Branch offices such as postal mail, offender, mountain lion and Myrica Bark; Oxyphene hydrochloride hydrochloride, Dicyclomine hydrochloride, Methiquicene hydrochloride, Scopolamine hydrobromide, methylatropine bromide, methylanisotropin bromide, methylscopolamine bromide, methyl bromide 1-hiyosciamine (1-hyscyamine methylbromide), methyl bromide bromide, belladonna extract, iodide propamide, iodide diphenylpiperidinomethyldioxolane, scofolia extract, scofolia root total alkaloid citrate, papaverine hydrochloride, amino Analgesic economics such as ethyl benzoate, encosac, licorice, humbac and peony; Sodium azulene sulfonate, Aldioxa, glycylic acid and its salts and licorice extracts, L-glutamine, copper chlorophyllin potassium, sodium chlorophyllin hydrochloride, histidine hydrochloride, pig gastric pepsin digest, pig gastric acid hydrolyzate, methyl Mucosal restorative components, such as methionine sulfone nuchloride, red eye bag, Enco sac, and licorice, etc. can be mix | blended.

Moreover, the internal liquid liquid formulation of this invention contains stabilizers, such as sodium aspartate, sodium alginate, sodium edetate, sodium sulfite, sodium hydrogen sulfite; Sweeteners such as sorbitol and sucrose; Mating agents such as sodium chloride, sodium L-glutamate, honey, and apple juice; Coloring agents such as caramel; flavoring agents such as fragrances such as l-menthol, mint flavor and cherry flavor, and essential oils such as lemon oil, orange oil and spearmint oil; Preservatives such as sodium benzoate and butyl paraoxybenzoate; Dissolution aids, such as polyoxyethylene hardened castor oil and ethanol, etc. can be mix | blended.

The internal liquid liquid preparation of the present invention is useful as an internal liquid gastrointestinal drug, and is usually a one-dose dosage of 20 to 100 ml, and is preferably used as a preparation for taking one to three times a day.

Example

Although an Example is given to the following and this invention is demonstrated to it in more detail, this invention is not limited to these at all.

Examples 1 to 12 and Comparative Examples 1 and 2

In the formulations shown in Table 1 and Table 2, an oral liquid formulation containing an early-month extract was prepared.

The herbal medicines in the table are as follows.

(1) Early spring extract (1 ml of this product is equivalent to 1 g of crude medicine. Extract solvent: ethanol aqueous solution)

(2) Ginger extract (1 ml of this product corresponds to 1 g of the original drug. Extraction solvent: ethanol aqueous solution)

(3) Ginseng extract (1g of this product is equivalent to 4g of crude medicine. Extraction solvent: ethanol aqueous solution)

(4) Turmeric extract (1 ml of this product is equivalent to 1 g of crude medicine. Extraction solvent: ethanol aqueous solution)

(5) Cinnamon oil (essential oil obtained by steam distillation of cinnamon)

(6) sperm oil (essential oil obtained by steam distillation of sperm)

(7) Fennel oil (essential oil obtained by steam distillation of fennel)

In addition, the component amount in the prescription shown in Table 1 and Table 2 showed the quantity in 30 ml of one side, and pH adjustment was performed with citric acid and sodium hydroxide.

Time stability test

After the liquid formulations of Examples 1 to 12 and Comparative Examples 1 and 2 were stored for 3 days under conditions of a temperature of 70 ° C., the residual amount of swetithiamarin in the formulation was quantified by high performance liquid chromatography.

As a result, as shown in Table 3, even in the harsh conditions of 70 ° C, swyrthiamarin in the liquid formulation containing extract at the beginning of the year was stable within the range of pH 4-7. Further, even under severe conditions of 70 ° C, swertia marine remains 50% or more within the range of pH 4.4 to 6.3, 60% or more remains within the range of pH 4.5 to 6.0, and within the range of pH 4.8 to 5.8. It remained more than 70% and was stable.

The oral liquid preparation of the present invention lasts for a long time because the active ingredient in the extract of early January is stable for a long time.

Claims (2)

An oral liquid formulation containing gentian and early spring extract, and having a pH adjusted to 4-7. The oral liquid formulation according to claim 1, wherein the pH is adjusted to 4.4 to 6.3.