JP6153436B2 - Oral composition - Google Patents

Description

  The present invention relates to an oral composition containing willow extract powder, which has a masked flavor and / or a change with time. The present invention also relates to an oral composition containing willow extract powder that has improved fluidity as compared with the willow extract powder itself.

  Willow extract is an extract obtained by decocting willow leaves or bark. In ancient Greece, willow extract has been used as a pain relieving ingredient for pain such as ventilation and labor. Salicin, which is an active ingredient of the willow extract, is similar in chemical structure to aspirin. Therefore, the willow extract is said to have antipyretic analgesic action as well as aspirin. In particular, it has been found that salicin is not as fast-acting as aspirin, but does not cause gastric damage, a significant side effect of aspirin. For this reason, willow extract is still being taken as a countermeasure against migraine and back pain, mainly in Europe and America (see Non-Patent Document 1 above).

  However, the willow extract has a unique strong bitterness and smell, and it is painful to take continuously. Further, the willow extract changes with time to cause discoloration, consolidation, etc., and therefore products containing it are very difficult to handle such as production and distribution.

  For this reason, in order to mask the bitterness and odor of the willow extract, many methods have been tried to offset and suppress the specific bitterness by adding an additive having a strong taste such as a sweetener. However, there are disadvantages such as an increase in taste and an increase in cost, and a masking method using an additive is not always a useful solution.

  On the other hand, glucosamine is a component contained in various tissues such as animal skin, bone, and cartilage. In recent years, it has been reported that glucosamine is effective for knee joint pain due to a decrease in cartilage (see Non-Patent Document 2, etc.).

  Boswellic acid is a component extracted and refined from the resin of Boswellia serrata, which is a deciduous tree of the orchidaceae that grows naturally mainly in West Asia. Ayurveda, a traditional Indian medicine, has long been used as an analgesic ingredient. It is also known to have an anti-inflammatory action (see Non-Patent Document 3, Patent Document 1, etc.).

Special table 2012-502901 gazette

B. Meier et al., “Functionality of medicinal herbs and their use XII Western willow resin (Willow Bark) Use as an analgesic and anti-rheumatic drug – reviving?”, Food and Development VOL.36, NO.12, pp.52-56, 2001 Shuji Enomoto et al., “Therapeutic effect of glucosamine hydrochloride on knee osteoarthritis”, Journal of Japanese Society of Clinical Nutrition, 20 (1): 41-47, 1998, G.B.SINGH et al., `` Pharmacology of an extract of salai suggal ex-Boswellia serrata, a new non-steroidal anti-inflammatory agent '', Agent and Actions, vol. 18, 3/4, pp. 407-412, 1986

  An object of the present invention is to provide an oral composition containing willow extract powder, in which the bitterness and smell (flavor) peculiar to willow extract are masked. Another object of the present invention is to provide an oral composition containing willow extract powder in which changes over time (discoloration and / or consolidation) of the willow extract are suppressed. Furthermore, the present invention provides a method for producing an oral composition containing willow extract powder, in which bitterness, smell (flavor) and / or change over time is suppressed, in other words, bitterness and smell (flavor) of willow extract powder. Another object of the present invention is to provide a method for suppressing changes over time.

  The present inventor has been diligently studying to solve the above-mentioned problems, and by covering the surface of the willow extract powder by attaching a complex of glucosamine or a salt thereof and boswellic acid to the surface of the willow extract powder. We found that the bitterness and smell peculiar to willow extract can significantly mask. In addition, the willow extract extract-containing composition obtained by the method has significantly suppressed the time-dependent discoloration and caking that is found in the willow extract powder, and this method not only masks the flavor but also the willow extract. It was found that it is effective in significantly suppressing the time-dependent change (discoloration and / or consolidation) of the powder. Furthermore, the composition obtained by the method has greatly improved fluidity compared to the raw willow extract powder, and may be useful as a granule or as a raw material for preparing tablets. found.

  The present invention has been completed based on these findings, and includes the following embodiments.

(I) Oral composition containing willow extract powder (I-1) Boswellic acid, glucosamine or a salt thereof, and an oral composition containing willow extract powder, comprising boswellic acid and glucosamine or a salt thereof An oral composition, characterized in that the product is present on the surface of the willow extract powder.
(I-2) The oral composition described in (I-1), wherein the composite contains glucosamine or a salt thereof (total amount) at a ratio of 0.5 to 100 parts by weight with respect to 1 part by weight of boswellic acid. .
(I-3) 0.5 to 1 part by weight of boswellic acid and 0.5 to 100 parts by weight of glucosamine or a salt thereof (total amount), preferably 1 to 50 parts by weight, based on 1 part by weight of willow extract powder More preferably, the oral composition according to (I-1) or (I-2) is contained at a ratio of 1 to 20 parts by weight.
(I-4) The oral composition according to any one of (I-1) to (I-3), which has a granulated form such as a granule, tablet or pill.

(II) Method for producing oral composition containing willow extract powder (II-1) Boswellic acid and glucosamine or a salt thereof are mixed with powder to prepare a composite of boswellic acid and glucosamine. A method for producing an oral composition comprising a step of granulating and sizing powder by mixing powder.
(II-2) The production method according to (II-1), which is a dry granulation method or a wet granulation method.

(III) Method for suppressing flavor masking and / or change over time of willow extract powder powder (III-1) A compound of boswellic acid and glucosamine is prepared by mixing powder of boswellic acid and glucosamine or a salt thereof. A method for suppressing flavor masking and / or change over time of a willow extract powder, comprising a step of mixing the willow extract powder and granulating and adjusting the size.
(III-2) The method according to (III-1), wherein the composite contains glucosamine or a salt thereof (total amount) at a ratio of 0.5 to 100 parts by weight with respect to 1 part by weight of boswellic acid.
(III-3) 0.5 to 1 part by weight of boswellic acid and 0.5 to 100 parts by weight, preferably 1 to 50 parts by weight, more preferably 1 part by weight of boswellic acid with respect to 1 part by weight of willow extract powder The method according to (III-1) or (III-2), which is prepared so as to be a ratio of 1 to 20 parts by weight.

(IV) Fluidity improvement method of willow extract powder (IV-1) Boswellic acid and glucosamine are mixed in powder to prepare a composite of boswellic acid and glucosamine or a salt thereof. A method for improving the fluidity of willow extract powder, comprising the steps of granulating and sizing.
(IV-2) The method according to (IV-1), wherein the composite contains glucosamine or a salt thereof (total amount) at a ratio of 0.5 to 100 parts by weight with respect to 1 part by weight of boswellic acid.
(IV-3) 0.5 to 1 part by weight of boswellic acid and 0.5 to 100 parts by weight of glucosamine or a salt thereof (total amount), preferably 1 to 50 parts by weight, based on 1 part by weight of the willow extract powder The method according to (IV-1) or (IV-2), wherein the preparation is more preferably performed at a ratio of 1 to 20 parts by weight.

  Since the bitterness and smell (flavor) peculiar to the willow extract are masked significantly, the oral composition of the present invention manufactures and sells products containing the willow extract powder without worrying about the flavor of the willow extract. can do. In addition, the oral composition of the present invention has significantly reduced temporal changes (discoloration or consolidation) of the willow extract powder, so that it has stable properties (color and shape) while containing the willow extract powder. Products can be manufactured and sold.

  Furthermore, according to the method of the present invention, a granular willow extract-containing composition can be obtained in which the fluidity of the willow extract powder is significantly improved as compared with the raw willow extract powder. Such a willow extract powder-containing composition can be effectively used as a granule or as a raw material for tablet preparation.

The image which observed each component and composition shown below with the microscope (VHX-D510, Keyence Corporation) is shown. (A) Willow extract powder (lens magnification Z50 × 200) (B) Boswellic acid powder (lens magnification Z50 × 50) (C) Glucosamine powder (lens magnification Z50 × 200). The image which observed each component and composition shown below with the microscope (VHX-D510, Keyence Corporation) is shown. (A) Powder mixture of boswellic acid and glucosamine (lens magnification Z50 × 150) (B) Mixture of willow extract powder and powder mixture of boswellic acid and glucosamine (lens magnification Z50 × 250) (C) Willow Powder mixture of extract powder and glutamine (lens magnification Z50 × 250) (D) Powder mixture of willow extract powder and boswellic acid (lens magnification Z50 × 250).

(1) Boswellic acid As described above, boswellic acid is a component extracted and purified from the resin of Boswellia Serrate, which is a deciduous tree of the Orchidaceae family that grows mainly in West Asia (especially India). . It is known that Boswellia Serata resin contains six types of Boswellic acids. The boswellic acid targeted by the present invention includes these six types of boswellic acid, specifically, α-boswellic acid, β-boswellic acid, 11-keto-β-boswellic acid, 3-O-acetyl. Mention may be made of 11-keto-β-boswellic acid, 3-O-acetyl-α-boswellic acid, and 3-O-acetyl-β-boswellic acid. Β-Boswellic acid is preferred. In addition, these may be used individually by 1 type and can also be used in combination of 2 or more types arbitrarily.

  The boswellic acid used in the present invention may be a pure product made of 100% boswellic acid, or may be an impurity as long as it contains boswellic acid. Examples of such impurities include an extract of a Boswellia serrata resin containing the above boswellic acid and a crudely purified product thereof. It should be noted that powder products containing a high content of boswellic acid and resin extracted products of boswellia serrata (containing about 37.5 to 65% of boswellic acid) can be obtained commercially. For example, the former can be obtained from Nippon Shinyaku Co., Ltd. and TS Trading Co., Ltd., and the latter can be obtained from Mona Co., Ltd.

  The boswellic acid (including pure product and boswellia serrata resin extract) used in the present invention preferably has a powder form. As an average particle diameter of powder, 1-20 micrometers can be mentioned normally. In addition, the average particle diameter here means the average particle diameter measured with a sieve.

(2) Glucosamine or a salt thereof Glucosamine is an amino acid having a molecular weight of 180 in which a hydroxyl group of a part of glucose is substituted with an amino group, such as animal skin, bone, cartilage, and shells of shellfish such as shrimp and crab, Included in various organizations. Glucosamine used in the present invention is not particularly limited by its origin or production method. For example, the glucosamine targeted by the present invention includes fermented glucosamine produced by fermentation using a plant as a raw material. The glucosamine targeted by the present invention also includes N-acetylglucosamine.

  In the present invention, glucosamine can also be used in the form of a salt. Here, the salt may be a pharmaceutically acceptable salt, and specific examples thereof include glucosamine inorganic acids such as glucosamine hydrochloride and sulfate. Preferably, it is glucosamine or hydrochloride or sulfate of glucosamine.

  Glucosamine or a salt thereof (hereinafter collectively referred to as “glucosamines”) used in the present invention may be a pure product composed of 100% glucosamines, but may be an impurity as long as it contains these. . Examples of such impurities include crude purified products of glucosamines produced from shells of shellfish such as shrimps and crabs. Glucosamines can be obtained commercially, for example, glucosamic acid or its salt (hydrochloride) is from Protein Chemical Co., Ltd., Koyo Chemical Co., Ltd., N-acetylglucosamine is fermented from Yaizu Suisan Chemical Co., Ltd. Glucosamine can be obtained from Kyowa Hakko Bio Co., Ltd.

  The glucosamines used in the present invention preferably have a powder form. As an average particle diameter of powder, 1-300 micrometers can be mentioned normally. In addition, the average particle diameter here means the average particle diameter measured with a sieve.

(3) Willow extract powder Willow extract is an extract prepared by decocting willow leaves or bark. The willow extract targeted by the present invention is not particularly limited as long as it contains salicin, which is an active ingredient, and the type of willow to be used and its production method (extraction method, etc.) are not particularly limited. In general, as the willow to be used as a raw material, Salix daphnoides, Salix purpurea, and Salix fragilis, as well as other varieties with a total salicin content of 1.5% by weight or more in dry crude drugs Can do.

  The willow extract powder preferably has a total salicin content of 10% by weight or more, more preferably a total salicin content of 15% by weight or more. Such willow extract powder is commercially available, and examples thereof include Indena Japan Co., Ltd.

  As for the willow extract extract used by this invention, 1-200 micrometers can be mentioned normally as the average particle diameter. In addition, the average particle diameter here means the average particle diameter measured with a sieve.

(4) Oral composition of the present invention The oral composition of the present invention comprises the aforementioned three components. More specifically, these three components are contained in a state where a complex of glucosamines and boswellic acid (hereinafter referred to as “GB complex”) is attached to the surface of the willow extract powder. The state of the presence of the GB complex in the oral composition of the present invention is not limited as long as it is attached to the surface of the willow extract powder, but it is preferably attached to the entire surface of the willow extract powder. More preferably, it is in a state where it uniformly adheres to the entire surface of the willow extract powder to the extent that the surface of the willow extract powder becomes invisible.

  The GB composite is a mixture (granulated product) in which glucosamines and boswellic acid are attached to each other, and has a form in which boswellic acid is attached to the surface of the glucosamines. The mode of attachment is not particularly limited, and may be partially or mottled attached to a part of the surface of glucosamines, or may be uniformly attached to the entire periphery of the surface. The GB composite can be prepared by powder mixing glucosamines and boswellic acid. The GB composite is not particularly limited, but usually 1 part by weight of boswellic acid (powder) and 0.5 to 100 parts by weight, preferably 1 to 50 parts by weight, more preferably 1 to 20 parts by weight of glucosamines ( Powder) can be obtained by dry granulation or wet granulation.

  The GB composite is applied to the surface of the willow extract powder at a ratio of 1 to 120 parts by weight, preferably 1 to 55 parts by weight, more preferably 1 to 25 parts by weight per 1 part by weight of the willow extract powder. By adhering, it is possible to prepare a willow extract extract-containing composition (granulated product, particularly granular product) having improved fluidity compared to the willow extract powder itself, that is, having good fluidity. The composition can be provided as a granular preparation in which the flavor (bitter taste and odor) and change with time (discoloration or solidification) of the willow extract powder are suppressed, and by further molding this , Pills or tablets having the same effect (inhibition of flavor and changes over time).

  In preparation of the oral composition of the present invention, first, boswellic acid (powder) and glucosamines (powder) are mixed with powder, and the GB composite having a form in which boswellic acid adheres to the surface of glucosamines. Prepare the product. The GB composite thus prepared can then be mixed with the willow extract powder and granulated by a known method (dry granulation method, wet granulation method, etc.).

  Here, as a method of powder mixing the GB composite and willow extract powder (powder) is not particularly limited, if dry granulation method, diffusion mixing method and moving mixing method, etc. can be mentioned, Examples of the wet granulation method include extrusion granulation method, stirring granulation method, fluidized bed granulation method, rolling granulation method, and spray granulation method. After granulation, it can be sized (sized) by lightly pulverizing or sieving. The opening of the sieve used for sizing can be appropriately selected according to the desired size of the granule to be prepared, but is usually 1 to 10 mm, preferably 3 to 8 mm, more preferably 4 to 5 mm. be able to.

  In the oral composition of the present invention, in addition to willow extract powder, glucosamines and boswellic acid, other components such as amino acids, vitamins and inorganic salts may be contained. These components are preferably added after the preparation of the oral composition of the present invention, but may be added at any stage of the manufacturing process as long as it does not inhibit the adhesion of the GB complex to the surface of the willow extract powder. Good.

  Although the aspect in particular will not be limited if the oral composition of this invention is taken orally, For example, a food composition, a pharmaceutical composition etc. are mentioned, for example.

(Food composition)
If the oral composition of the present invention is used as a food composition, the flavor of the willow extract powder can be masked and / or the change over time can be suppressed, and it can be stored for a longer period of time, etc. High quality stability can be maintained. Moreover, by taking the oral composition of the present invention, the analgesic effect and anti-inflammatory (anti-inflammatory) effect of the willow extract powder, and the action effect of glucosamines and boswellic acid, to arthropathy and rheumatoid arthritis. Can be expected.

  When the oral composition of the present invention is used as a food composition, the above-described composition of the present invention may be used as it is as a food composition, and usually in various food forms together with carriers and additives that are acceptable in the field of food. It may be prepared. The contents of the willow extract powder, glucosamines and boswellic acid in the food composition can also be appropriately set according to the oral composition of the present invention described above.

  The form of the food is not particularly limited, and examples thereof include various foods such as confectionery and bread. These various foods are produced according to conventional methods used for the production of various foods by blending a granulated product having a form in which the GB composite is adhered to the surface of the willow extract powder together with other ingredients. can do.

  In addition to the foods described above, the food composition of the present invention can also be prepared as functional foods such as health foods (nutrient functional foods, foods for specified health use, etc.), supplements, foods for the sick, and the like. When preparing as such a food, it is desirable to prepare it in the form of granules, tablets, capsules, tablets (including chewable agents, etc.), etc. so that continuous ingestion is easy. From the standpoint of maximizing the effects of the present invention, the form of granules and tablets is preferred, but not particularly limited thereto.

  The food composition prepared in the above-described form can also be appropriately prepared according to a conventional method using the above-described carrier acceptable in the field of food. Moreover, even when preparing in other forms, conventional methods may be followed, and the production method is not particularly limited as long as it does not impair the effects of the present invention, and is used by those skilled in the art for each application. It is sufficient to follow the method.

  In addition, foods for specified health use (including foods for specified health use with conditions) can show the function / effect of the food, such as displaying that the packaging container has an effect of imparting anti-inflammatory analgesic action. Food.

  In preparing the above-mentioned foods, functional foods and the like, they can be added together with auxiliary materials and additives usually used.

  The daily intake of the food composition of the present invention is not particularly limited, but it may be usually about 100 to 1000 mg in terms of the amount of willow extract powder. Such an intake can be taken 1 to several times a day, and an effective amount can be taken efficiently.

(Oral pharmaceutical composition)
If the oral composition of the present invention is used as an oral pharmaceutical composition, the flavor of the willow extract powder can be masked and / or the change over time can be suppressed, and it can be stored for a longer period of time. For example, high quality stability can be maintained. Further, by taking the oral composition of the present invention, from the analgesic effect and anti-inflammatory (anti-inflammatory) effect of the willow extract powder, and the action effect of glucosamines and boswellic acid, arthropathy, rheumatoid arthritis, etc. It can be expected to work as a therapeutic or preventive agent.

  Here, prevention means preventing the onset of the disease, specifically, preventing the onset of such a disease by acting on the onset mechanism of the disease in advance, It can be understood that a function higher than that at the time of normal or remission is acquired, and physiological damage of a lesion caused after the onset of the disease is reduced.

  When the oral composition of the present invention is used as an oral pharmaceutical composition, the composition of the present invention described above may be used as it is as an oral pharmaceutical composition, and various dosage forms are usually used together with carriers and additives that are acceptable in the pharmaceutical field. May be prepared. The contents of willow extract powder, glucosamines and boswellic acid in the oral pharmaceutical composition can also be appropriately set according to the oral composition of the present invention described above.

  The dosage form of the oral pharmaceutical composition of the present invention is not particularly limited, and examples thereof include powders, tablets, granules, pills, capsules (soft capsules or hard capsules), troches, chewable tablets and the like. Moreover, you may have a formulation form which controlled the release | release property of the medicinal component (for example, immediate release formulation, sustained release formulation, etc.). Also preferred are tablets, granules, pills, and capsules (soft capsules or hard capsules). Formulations having such dosage forms can be prepared according to conventional methods in the art.

  The oral pharmaceutical composition may be formulated with various carriers and additives that are pharmaceutically acceptable for oral administration in order to formulate the oral dosage form described above and to stabilize the oral dosage form (for example, Japan). (See Pharmacopoeia, “Pharmaceutical Additives Encyclopedia” (published by Yakuji Nippo).

  In addition to the above components, as long as the effect of the present invention is not diminished, stabilizers, dispersants, fluidizing agents, buffering agents, wetting agents, thickening agents, preservatives, and the like, which are usually acceptable as additives for pharmaceuticals, Optional components such as a pH adjuster, a solvent, a solubilizing agent and the like can be added as desired.

  The dose of the above oral pharmaceutical composition depends on the patient's age, sex, degree of symptom to be treated, and administration method, but it is converted into the amount of willow extract powder contained in the oral pharmaceutical composition. Thus, the daily dose for an adult may be usually about 100 to 1000 mg. If it is this administration range, it can also administer in 1 to several times a day.

  The oral pharmaceutical composition of the present invention can be used in combination with pharmaceuticals for known diseases in order to provide a better preventive or therapeutic effect.

  Hereinafter, based on an Example and an experiment example, this invention is demonstrated in detail. However, these examples and experimental examples are examples for explaining the present invention, and the present invention is not limited to these examples and experimental examples. In the following examples, “%” means “% by weight” and “parts” means “parts by weight” unless otherwise specified.

Examples 1-8 and Comparative Examples 1-3
Granules containing willow extract powder were prepared according to the composition described in Table 1 described later using the following materials.

[1] Raw material (1) Willow extract powder:
Willow dried extract (containing 15% salicin) formulation (powder), average particle size 100 μm
(2) Glucosamine:
Glucosamine 100% formulation (powder), average particle size 200μm
(3) Boswellic acid:
Preparation containing 90% boswellic acid (powder), average particle size 10 μm.

  In addition, the image which observed each raw material with the microscope (VHX-D510, Keyence Corporation) is shown in FIG. 1 (A: Willow extract powder (lens magnification Z50 × 200), B: Boswellic acid powder (lens magnification Z50 × 50) , C: Glucosamine powder (lens magnification Z50 × 200)).

[2] Manufacturing method (1) Dry granulation method (Examples 1 to 8)
According to the ratio shown in Table 1, glucosamine and boswellic acid were diffused and mixed and granulated to prepare GB composites. The prepared GB composite was granulated by adding willow extract and stirring and mixing (temperature: 25 ° C., relative humidity 60%). The granulated material thus prepared was passed through a sieve (aperture 4-5 mm) to obtain a granular composition.

(Comparative Example 2 or 3)
In accordance with the ratio shown in Table 1, willow extract was added to glucosamine or boswellic acid and granulated by stirring and mixing (temperature: 25 ° C., relative humidity 60%). The granulated material thus prepared was passed through a sieve (aperture 4-5 mm) to obtain a granular composition.

(2) Wet granulation method (Examples 1-8)
According to the ratio shown in Table 1, glucosamine and boswellic acid and water (purified water of 5% of the total weight) are added and mixed uniformly to granulate, and then the resulting granulated product has a moisture content of 2%. It dried with the warm air drying apparatus until it became the following, it passed through the sieve (opening 4-5mm), and the GB composite was prepared. Thereafter, willow extract and water (purified water of 5% of the total weight) are added to the prepared GB composite and mixed uniformly, and the resulting granulated product is warm-air dried until the water content is 2% or less. And passed through a sieve (opening 4 to 5 mm) to obtain a granular composition (temperature: 25 ° C., relative humidity 60%).

(Comparative Example 2 or 3)
Depending on the proportions shown in Table 1, glucosamine or boswellic acid is added with willow extract and water (purified water of 5% of the total weight) and mixed uniformly and granulated. Was dried with a hot air drying apparatus until it became 2% or less, and passed through a sieve (opening 4 to 5 mm) to obtain a granular composition (temperature: 25 ° C., relative humidity 60%).

  In addition, the image which observed the powder mixture of the boswellic acid and glucosamine, and the mixture of the powder mixture of the boswellic acid and glucosamine, and the willow extract powder with a microscope (VHX-D510, Keyence Corporation) is respectively FIG. ) And (B). In addition, for comparison, images of a powder mixture of willow extract powder and glutamine, and a powder mixture of willow extract powder and boswellic acid, which were similarly observed with a microscope, are shown in FIGS. 2 (C) and (D), respectively. Show.

[3] Physical property evaluation (1) Flavor (bitterness, smell)
The sensory test of flavor (bitterness, smell) was performed by 10 panelists. Specifically, 300 mg of each prepared granular sample (Examples 1 to 8, Comparative Examples 1 to 3) was smelled and then included in the mouth as it was, and then 50 ml of water was placed in the mouth. After crushing twice, they were exhaled with water and evaluated the bitterness and smell of each sample. In addition, only water was used as a blank, and willow extract itself was also included in the mouth as a positive control.

[Evaluation criteria]
The willow-specific flavor was evaluated by Visual Analogue Scale (hereinafter referred to as VAS). A 10 cm long black line (the left end was “no flavor” and the right end was “flavored”) was shown to the monitor, and the level of the sample flavor was checked. The distance from the left end was measured, and the average value of 10 monitor persons was calculated. 0 to 2.5 cm is “◎ (no flavor)”, 2.5 cm to 5 cm is “◯ (slightly unflavored)”, 5 cm to 7.5 cm is “Δ (somewhat flavored)”, 7.5 cm to 10 cm Was “× (flavored)”.

(2) Change over time (discoloration, consolidation)
Changes over time (discoloration, consolidation) of the prepared samples (Examples 1 to 8, Comparative Examples 1 to 3) were evaluated by a sensory test by 10 panelists.

  Specifically, the prepared sample was first left for 24 hours under dark conditions at 25 ° C. and a relative humidity of 60%. Next, let the 10 monitors monitor the sample state (appearance color and form) before standing (immediately after preparation) and compare the sample state (appearance color and form) with the naked eye. The presence or absence of (discoloration and consolidation) was evaluated.

[Evaluation criteria]
The evaluation was performed by Visual Analogue Scale (hereinafter referred to as VAS) in comparison with the appearance of the sample before being left standing. Show the black line of 10 cm in length (the left end is “no change to sample” and the right end is “discolored and / or solidified”) to the monitor to check how much the sample has changed. It was. The distance from the left end was measured, and the average value of 10 monitor persons was calculated. 0 to 2.5 cm is “◎ (no change)”, 2.5 cm to 5 cm is “◯ (slightly no change)”, 5 cm to 7.5 cm is “Δ (slightly change)”, 7.5 cm to 10 cm Was “× (changed)”.

(3) Fluidity The fluidity of the obtained test sample was confirmed visually. 10g of each test sample is put into a 50ml glass bottle, and the powder in the bottle is moved by changing the tilt of the bottle, and compared with the powder (Powder willow extract powder), the adhesion to the bottle and the scattering property are small. Was evaluated as “◯”, and the same or larger one was evaluated as “x”.

[4] Physical property evaluation results Table 1 shows the compositions of the granular samples (Examples 1 to 8 and Comparative Examples 1 to 3) prepared above. Moreover, the physical-property evaluation result of the granular sample prepared by the wet granulation method is also shown.

  As shown in Table 1, three kinds of mixtures (granular samples) of the present invention prepared by adding and mixing the willow extract to Boswellia and glucosamine powder mixture (GB composite) It was confirmed that the flavor (bitter taste, smell) was significantly masked, and that changes over time (discoloration, consolidation) could be suppressed (Examples 1 to 8). Furthermore, it was confirmed that the three-type mixture (granular sample) (Examples 1 to 8) of the present invention has improved fluidity as compared with the fluidity of the willow extract powder used as a raw material. . From this, it is confirmed that the three-type mixture (granular sample) of the present invention is suitable as a granule or as a granule for tableting, and can be tableted and prepared into a tablet form. It was done.

  From the results shown in Table 1 above, in the GB composite, it is desirable that glucosamine is 0.5 to 100 parts, preferably 1 to 50 parts, more preferably 1 to 20 parts, with respect to 1 part of boswellic acid. Moreover, it turned out that it is desirable that 1 to 120 parts, preferably 1 to 55 parts, more preferably 1 to 25 parts, of the GB composite with respect to 1 part of the willow extract. Moreover, as a compounding ratio of 3 components, 0.5 to 1 part of boswellic acid and 0.5 to 100 parts of glucosamine, preferably 1 to 50 parts, more preferably 1 to 1 part of willow extract It turned out to be desirable to be 20 parts.

  In addition, although the physical property of the granular sample prepared by the dry granulation method was slightly inferior to the above, a comparable result was obtained. More specifically, the granular sample prepared by the wet granulation method has a more uniform glucosamine and boswellic acid complex on the surface of the willow extract powder than the granular sample prepared by the dry granulation method. The effect of suppressing the flavor and time-dependent change of the willow extract was high.

Comparative Example 4
A glucosamine extract was further added to and mixed with the sample obtained in Comparative Example 2 (two mixtures of willow extract and boswellic acid) to prepare a three-component mixture. The blending amount of glucosamine was 0.5 parts with respect to 1 part of a mixture of willow and boswellic acid (willow: boswellic acid: glucosamine = 1: 1: 1, weight ratio).

  In the two-type mixture obtained in Comparative Example 2, the willow extract was attached to the surface of the boswellic acid (the willow was exposed on the surface), and thus glucosamine was hardly attached.

  This three-type mixture was subjected to the physical property evaluation described above, and each physical property (flavor, change with time, fluidity) was evaluated. As a result, although the three-type mixture of Comparative Example 4 has a relatively high fluidity (evaluation: ◯), the change with time (discoloration / consolidation) is not suppressed (evaluation: x), and moreover, it is characteristic of willow The flavor (bitterness / smell) was not masked (evaluation: x).

Comparative Example 5
Boswellic acid was further added to the sample obtained in Comparative Example 3 (two mixtures of willow extract and glucosamine) and mixed to prepare a three-mixture. The compounding amount of boswellic acid was 0.5 parts with respect to 1 part of a mixture of willow and glucosamine (willow: boswellic acid: glucosamine = 1: 1: 1, weight ratio).

  When boswellic acid was added to the two mixtures obtained in Comparative Example 4, the majority became a composite in which boswellic acid was attached to the surface of glucosamine, and a composite in which willow extract was attached to the surface of boswellic acid, The surface of the willow extract could not be effectively covered.

  This three-type mixture was subjected to the physical property evaluation described above, and each physical property (flavor, change with time, fluidity) was evaluated. As a result, although the three-type mixture of Comparative Example 5 has fluidity (evaluation: ◯), the change over time (discoloration, consolidation) is not suppressed (evaluation: ×), and a willow peculiar flavor ( The bitterness and smell were not masked (evaluation: x).

Claims (4)

  An oral composition containing boswellic acid, glucosamine or a salt thereof, and willow extract powder, wherein a complex of boswellic acid and glucosamine or a salt thereof is present on the surface of the willow extract powder. An oral composition.   The oral composition according to claim 1, wherein the composite contains glucosamine or a salt thereof (total amount) at a ratio of 0.5 to 100 parts by weight with respect to 1 part by weight of boswellic acid.   The oral composition according to claim 1 or 2, which has a granulated form of granules, tablets or pills.   An oral composition having a step of powder mixing boswellic acid and glucosamine or a salt thereof to prepare a composite of boswellic acid and glucosamine or a salt thereof, and mixing and granulating and regulating the size of willow extract powder. Production method.

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