Oral components

Abstract

The present invention aims to provide an oral composition that can improve allergic conjunctivitis. [Solution] By taking the daily dose of Meirōin extract in two divided doses per day, an excellent improvement effect on allergic conjunctivitis can be obtained.

Description

Technical Field

[0004] , , ,

[0001] The present invention relates to an oral composition for improving allergic conjunctivitis.

Background Art

[0002] Conjunctivitis is broadly classified into infectious and non-infectious types according to its cause. Infectious conjunctivitis includes bacterial conjunctivitis and viral conjunctivitis, and non-infectious conjunctivitis includes allergic conjunctivitis.

[0003] Allergic conjunctivitis is a disease in which external allergens such as pollen and house dust cause itching and / or congestion in the eyes. As a countermeasure against allergic conjunctivitis, anti-allergic eye drops such as epinastine-containing eye drops (Patent Document 1), steroid eye drops, etc. are selected.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] On the other hand, for allergic conjunctivitis, anti-allergic eye drops may not be easily cured due to recurrence of eye itching or congestion. In such cases, there is also an option to apply steroid eye drops, but there are also patients who show resistance to the use of steroids. Furthermore, for those who usually wear contact lenses, options other than eye drops for allergic conjunctivitis are desired.

[0006] Therefore, an object of the present disclosure is to provide an oral composition capable of improving allergic conjunctivitis.

Means for Solving the Problems

[0007] The inventors of this invention conducted diligent research to solve the aforementioned problems and found that taking the daily dose of Meirōin extract in two divided doses per day produced excellent improvement effects against allergic conjunctivitis. This disclosure was completed based on this finding and further research.

[0008] In other words, this disclosure provides inventions in the following embodiments. Item 1. An oral composition for improving allergic conjunctivitis, containing Meirōin extract as the active ingredient, and intended to be taken in two divided doses per day. Item 2. An oral composition according to Item 1 for relieving itchy eyes. Item 3. An oral composition according to item 1 or 2 for improving conjunctivitis. Item 4. An oral composition according to any one of items 1 to 3 for improving seasonal allergic conjunctivitis. Item 5. An oral composition according to any one of items 1 to 4 for improving perennial allergic conjunctivitis. Item 6. The oral composition described in Item 1 for use by contact lens wearers. Item 7. A method for improving allergic conjunctivitis, in which an effective amount of Meirōin extract is administered orally twice a day to patients who require improvement of allergic conjunctivitis. Item 8. Use of Meirōin extract for the manufacture of oral compositions for the improvement of allergic conjunctivitis. Item 9. Meirōin extract for use in improving allergic conjunctivitis. [Effects of the Invention]

[0009] According to this disclosure, excellent improvement effects can be obtained against allergic conjunctivitis. [Modes for carrying out the invention]

[0010] The oral composition disclosed herein is used to improve allergic conjunctivitis, contains Meirōin extract as an active ingredient, and is characterized by being taken in two divided daily doses. The oral composition disclosed herein will be described in detail below. In this specification, numerical ranges indicated by two numbers and "~" include those two numbers as the lower and upper limits. For example, the notation 2~15% by weight means 2% by weight or more and 15% by weight or less.

[0011] Meirōin Extract As for the crude drugs that make up Meirōin, those listed in the "New Handbook of General-Use Kampo Prescriptions" (supervised by the Pharmaceutical Affairs Bureau of the Ministry of Health and Welfare, edited by the Kampo Expert Committee of the Japan Pharmaceutical Association, published by Yakugyo Jiho Co., Ltd.) can be used. The Meirōin extract used in this disclosure is usually an extract of a crude drug formulation consisting of Poria cocos, Cinnamon bark, Atractylodes macrocephala, Licorice, Plantago asiatica, Asarum sieboldii, and Coptis japonica. A specific composition of the crude drug formulation of Meirōin is, for example, Poria cocos 4-6 (parts by weight, the same applies hereinafter), Cinnamon bark 3-4, Atractylodes macrocephala 2-4, Licorice 2, Plantago asiatica 2-3, Asarum sieboldii 1.5-2, and Coptis japonica 1.5-2.

[0012] The Meirōin extract used in this disclosure can be obtained by extracting the aforementioned crude drug preparation by a known method. The method for extracting the crude drug preparation can be the same as the method for extracting ordinary herbal extracts. For example, an extraction method can be used in which approximately 10 to 20 times the weight of the crude drug preparation is added to water, and the mixture is stirred at approximately 80 to 100°C for approximately 1 to 3 hours. After extraction, the solids are removed by solid-liquid separation such as centrifugation and filtration, and if necessary, the mixture is subjected to concentration and / or drying to obtain the Meirōin extract.

[0013] When obtaining Meirōin extract as an extract powder, the extract, from which the solid components have been removed, can be concentrated as needed and then subjected to drying treatments such as spray drying, vacuum concentration drying, or freeze-drying. Furthermore, when subjecting the extract to drying (especially spray drying), excipients such as dextrin may be added as needed. Adding excipients in this way makes it possible to shorten the drying time. The type and amount of excipients added are the same as those used when manufacturing general herbal extract powders.

[0014] Furthermore, to obtain Meirōin extract as a soft extract, the extract from which the solid components have been removed can be concentrated by vacuum concentration or the like. Alternatively, an appropriate adsorbent (e.g., anhydrous silicic acid, starch, etc.) may be added to the soft extract to form an adsorbent powder.

[0015] The extract of Meirōin may be in the form of either an extract powder or a soft extract.

[0016] Other ingredients The oral composition of this disclosure may consist solely of Meirōin extract, or it may contain additives and / or bases depending on the formulation. Such additives and bases, whether present or absent, are not particularly limited to those that are pharmaceutically acceptable, but examples include excipients, binders, disintegrants, lubricants, isotonic agents, plasticizers, dispersants, emulsifiers, solubilizers, wetting agents, stabilizers, suspending agents, adhesives, coating agents, glossing agents, water, oils and fats, waxes, hydrocarbons, fatty acids, higher alcohols, esters, water-soluble polymers, surfactants, metal soaps, lower alcohols, polyhydric alcohols, pH adjusters, buffers, antioxidants, UV inhibitors, preservatives, flavoring agents, fragrances, powders, thickeners, dyes, chelating agents, etc. These additives may be used individually or in combination of two or more. Furthermore, the content of these additives and bases is appropriately determined depending on the type of additive and base used, as well as the formulation of the oral composition.

[0017] In addition, the oral composition of the present disclosure may or may not contain nutritional components and / or other pharmacological components in addition to the Minglangyin extract, as necessary. The nutritional components and pharmacological components, regardless of whether they are contained or not, are not particularly limited as long as they are pharmaceutically acceptable. For example, antacids, stomachic agents, digestive agents, other intestinal regulators, antispasmodics, mucosal repair agents, anti-inflammatory agents, astringents, antiemetics, antitussives, expectorants, anti-inflammatory enzyme agents, sedative hypnotics, antihistamines, caffeine compounds, cardiotonic diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, other crude drugs, other crude drug extracts, vitamins, menthols, etc. These nutritional components and pharmacological components may be used alone or in combination of two or more. Also, the content of these components is appropriately set according to the type of components used and the dosage form of the oral composition, etc.

[0018] Dosage form The dosage form of the oral composition of the present disclosure is not particularly limited as long as it can be administered orally. For example, solid preparations such as powders, fine granules, granules (including dry syrups), tablets, pills, capsules (soft capsules, hard capsules), etc.; semi-solid preparations such as jelly preparations; liquid preparations such as liquids, suspensions, syrups, etc. Among these dosage forms, solid preparations are preferably used from the viewpoints of stability and / or portability of the contained components.

[0019] To prepare the oral composition of the present disclosure into the above dosage form, it may be formulated according to the usual formulation methods employed in the pharmaceutical field using the Minglangyin extract and additives, bases, nutritional components and / or other pharmacological components added as necessary.

[0020] Purpose The oral composition of the present disclosure is used to improve allergic conjunctivitis.

[0021] Allergic conjunctivitis is a non-infectious allergic conjunctivitis. The types of allergic conjunctivitis are not particularly limited, and include acute allergic conjunctivitis, seasonal allergic conjunctivitis (caused by seasonal allergens such as pollen and spores, coinciding with the life cycle of the plant in question), and perennial allergic conjunctivitis (caused by non-seasonal allergens such as dust, mites, and animal scales). Among these allergic conjunctivitis, the oral composition of this disclosure is preferably applied to seasonal allergic conjunctivitis and perennial allergic conjunctivitis, where the symptoms of allergic conjunctivitis tend to recur, and is more preferably applied to perennial allergic conjunctivitis.

[0022] Specific symptoms of allergic conjunctivitis include, for example, itchy eyes and red eyes.

[0023] The oral composition disclosed herein is highly effective in improving allergic conjunctivitis and can therefore be applied to people who wear contact lenses, which are a contributing factor to the aggravation of allergic conjunctivitis.

[0024] Specific methods for improving allergic conjunctivitis include taking the medication after the onset of acute allergic conjunctivitis, seasonal allergic conjunctivitis, or perennial allergic conjunctivitis to treat these conditions, and taking the medication before the onset of seasonal allergic conjunctivitis to prevent or alleviate the condition.

[0025] The dosage of the oral composition disclosed herein is set appropriately according to the age, sex, constitution, etc. of the person taking the medication, but for example, a daily dose of 8.5 to 22 g, preferably 11 to 15 g, of Meirōin extract in terms of crude drug equivalent is given. In this disclosure, "Meirōin extract in terms of crude drug equivalent" refers to the dry weight of the total amount of crude drug preparations necessary to obtain the amount of Meirōin extract to be included.

[0026] The oral composition disclosed herein is taken in two divided doses per day. This results in a higher improvement in allergic conjunctivitis and a significant reduction in side effects (increased frequency of urination due to diuretic effect) compared to taking the daily dose in three divided doses per day.

[0027] The duration of administration of the oral composition of this disclosure is not particularly limited and may be, for example, 3 to 14 days, 4 to 10 days, or 5 to 7 days. [Examples]

[0028] The present invention will be described in detail below with reference to examples, but the present invention is not limited to these examples.

[0029] 1. Preparation of Meirōin extract A herbal medicine preparation for Meirōin (consisting of 4.0g of Poria cocos, 2.7g of Cinnamon bark, 2.0g of Atractylodes macrocephala, 1.3g of Licorice, 1.3g of Plantago asiatica, 1.3g of Asarum sieboldii, and 1.3g of Coptis japonica per day (totaling 13.9g)) was prepared, and the herbal medicine preparation was added to 10 times its weight in water, heated, and extracted at 90°C for 1 hour. The extract was subjected to solid-liquid separation, concentrated, and then spray-dried to obtain 1.6g (daily dose) of dried extract powder.

[0030] 2. Test Method 2-1. Twenty-four individuals complaining of perennial allergic conjunctivitis were divided into two groups of 12 each (a two-dose group and a three-dose group) to ensure that the severity of their symptoms (specifically, persistent itching and redness of the eyes due to chronic inflammation) was roughly equivalent. Each group included 10 regular contact lens wearers. The two-dose group took 1.6g of Meirōin extract daily, divided into two doses, every day. The three-dose group took 1.6g of Meirōin extract daily, divided into three doses, every day. In both groups, Meirōin extract was taken before or between meals, and no participants missed doses during the study period. Satisfaction with the effectiveness of the medication against itching or redness of the eyes was evaluated using a five-point scale shown in Table 1 five days after the start of administration, and the presence or absence of increased urination frequency as a side effect was evaluated using a two-point scale shown in Table 2. The percentage of participants who responded at each stage was calculated.

[0031] 2-2. Ten patients complaining of bacterial conjunctivitis were divided into two groups of five (a two-dose group and a three-dose group) to ensure similar levels of symptom severity. The two-dose group took 1.6g of Meirōin extract daily, divided into two doses, every day. The three-dose group took 1.6g of Meirōin extract daily, divided into three doses, every day. In both groups, Meirōin extract was taken before or between meals, and no patients missed doses during the study period. Patients who regularly wore contact lenses continued to wear them during the treatment period. Satisfaction with the effectiveness against eye itching was evaluated five days after the start of treatment using the five-point scale shown in Table 3. The percentage of patients who responded at each stage was calculated.

[0032] 3.Results The results are shown in Tables 1 to 3. In Tables 1 to 3, the percentage of people who responded at each stage is shown (rounded to the first decimal place), and "-" indicates no response.

[0033] [Table 1]

[0034] [Table 2]

[0035] [Table 3]

[0036] As shown in Table 1, for the symptoms of non-infectious allergic conjunctivitis, the improvement effect in the 2-dose group (Example) was significantly higher than that in the 3-dose group (Comparative Example 1). Furthermore, among regular contact lens wearers (N=10) in the 2-dose group (Example), satisfaction with the effect on eye itching was 50% "satisfied" and 40% "somewhat satisfied," while satisfaction with the effect on eye redness was 20% "satisfied" and 60% "somewhat satisfied." In contrast, among regular contact lens wearers (N=10) in the 3-dose group (Comparative Example 1), satisfaction with the effect on eye itching was 10% "satisfied" and 10% "somewhat satisfied," while satisfaction with the effect on eye redness was 10% "satisfied" and 10% "somewhat satisfied." In other words, even in cases of regular contact lens wear, which is an aggravating factor for allergic conjunctivitis, the improvement effect in the 2-dose group (Example) was significantly higher than that in the 3-dose group (Comparative Example 1).

[0037] Furthermore, as shown in Table 2, the side effect of increased diuresis frequency was observed at a high rate in the 3-dose group (Comparative Example 1), while it was hardly observed in the 2-dose group (Example), indicating a remarkably significant suppression.

[0038] On the other hand, as shown in Table 2, there was no substantial difference in the improvement effect between the 3-dose group (Comparative Example 3) and the 2-dose group (Comparative Example 2) for the symptoms of infectious bacterial conjunctivitis.

Claims

1. An oral composition for improving allergic conjunctivitis, containing Meirōin extract as the active ingredient, and intended to be taken in two divided doses per day.

2. An oral composition according to claim 1 for improving itchy eyes.

3. An oral composition according to claim 1 for improving eye redness.

4. An oral composition according to claim 1 for improving seasonal allergic conjunctivitis.

5. An oral composition according to claim 1 for improving perennial allergic conjunctivitis.

6. An oral composition according to claim 1, for use by contact lens wearers.

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