JP2009184967A - Solid preparation for oral administration containing glucosamine - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a safe glucosamine-containing solid preparation having excellent palatability, and enabling daily successive ingestion. <P>SOLUTION: The solid preparation for the oral administration, containing the glucosamine, and having improved foreign taste originated from the glucosamine, and improved palatability is provided by formulating a milk perfume with a solid preparation for the oral administration containing the glucosamine. The invention is especially suitable for the solid preparation for oral administration for a pet. <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

  The present invention relates to a solid preparation for oral administration in which a unique flavor attributed to glucosamine is improved.

  In recent years, osteoarthritis such as knee osteoarthritis and hip osteoarthritis has been increasing in middle-aged and older people due to obesity due to aging and lack of exercise and overuse of joints. Osteoarthritis is a disease in which the cartilage of the joint is worn away and the ends of the bones are rubbed together. As the symptoms progress, pain augmentation, gait disturbance, restriction of daily living activities, etc. become prominent.

  Osteoarthritis tends to increase not only in humans but also in pets (pet animals) such as dogs and cats due to aging and increased obesity. Major symptoms of osteoarthritis in pet animals include lameness, joint pain, joint instability, and the like. Such a symptom in a pet animal is a big problem not only for the pet animal but also for the owner because it causes a mental and / or physical burden on the owner.

  Conventionally, steroids and non-steroidal anti-inflammatory drugs have been commonly used as therapeutic agents for osteoarthritis, but they are more safe because serious side effects such as immune disorders and gastrointestinal disorders may occur. High treatment and prevention methods are desired. Under such circumstances, for example, glucosamine, chondroitin (for example, shark cartilage powder), enzyme-treated rutin (for example, quercetin glycoside), etc. are taken as a safer countermeasure using components derived from natural products. It has been studied to treat, prevent, and relieve arthropathy.

  However, functional components such as glucosamine have a unique flavor, and their ingestion often becomes a problem when ingested. Especially when orally administered to pets, pets will not sense and take the smell of the functional ingredient, or even if it is taken at first, it will refuse to take it repeatedly because it will remember its flavor. In some cases, there is a need to develop a preparation with good palatability.

  Patent Document 1 discloses a feed composition made from shark cartilage as a raw material. By subjecting shark cartilage to softening, pulverization, or flaky processing, a dog and An improved feed formulation is described that is easily consumed by cats.

  Patent Document 2 describes a pet palatability preparation in which a fragrance preferred by animals is coated on the surface, and improves palatability by coating the fragrance, and meat flavor or fish flavor is given as a flavor preferred by animals. Is disclosed.

Patent Document 3 discloses a pet supplement molded in a stick jelly shape, and describes that an animal taste is improved by combining a flavoring agent with a flavoring agent.
JP 2005-58191 A JP 2004-194514 A JP 2007-306848 A

  In the glucosamine-containing composition, masking for a unique flavor of glucosamine is required. The subject of this invention is providing the glucosamine containing composition which is excellent in palatability, and is safe and can be continuously ingested on a daily basis.

  As a result of diligent research to achieve the above object, the present inventor has improved the flavor of a composition for oral administration containing glucosamine by using a milk fragrance to form a solid preparation without using a flavoring agent. The present invention has been completed by finding that palatability can be improved. In particular, in glucosamine-containing compositions for pets such as dogs and cats, pets bite the formulation in the mouth, and therefore, there has been a need to improve palatability regardless of the method of coating or the like. However, the solid preparation for oral administration of the present invention is suitable for use in a dosage form such as a tablet (especially a chewable tablet) and is particularly desirable for a pet animal.

That is, according to the present invention, the present invention is not limited to this, but the following invention is provided.
1. A solid preparation for oral administration comprising glucosamines and a milk flavor.
2. 2. The solid preparation for oral administration according to 1 above, wherein the glucosamine is one or more selected from the group consisting of glucosamine, glucosamine salts, or N-acetylglucosamine.
3. 3. The solid preparation for oral administration according to 1 or 2 above, wherein the solid preparation is a tablet.
4). 4. The solid preparation for oral administration according to 3 above, wherein the tablet is a chewable tablet.
5. 5. The solid preparation for oral administration according to any one of 1 to 4 above, which is for a pet animal.
6). 6. The solid preparation for oral administration according to 5 above, wherein the pet animal is a dog.
7). 7. The solid preparation for oral administration according to any one of 1 to 6 above, wherein the blending ratio of glucosamines and milk flavor is in the range of 4: 1 to 30: 1.
8). 8. The solid preparation for oral administration according to any one of 1 to 7 above, further comprising chondroitin and / or enzyme-treated rutin.
9. A method for producing a solid preparation for oral administration containing glucosamines, comprising blending a milk flavor.
10. A method for improving the flavor of a solid preparation for oral administration containing glucosamines, comprising blending a milk flavor.

  An unpleasant flavor derived from glucosamine is masked by blending a milk fragrance with a solid preparation containing glucosamine, which is a physiologically active ingredient having a different taste, and continuous intake of the glucosamine-containing composition becomes possible. In particular, since the glucosamine-containing solid preparation of the present invention can be formulated as a tablet, for example, a chewable tablet, it is suitable as a preparation for pets that bites the tablet in the mouth.

BEST MODE FOR CARRYING OUT THE INVENTION

The solid preparation for oral administration of the present invention comprises glucosamine and milk flavor, and can be used for pharmaceutical use including veterinary use and food use including supplements.
(Dosage form)
The present invention contains glucosamine as an active ingredient and milk flavor as its flavor improving agent. The solid preparation for oral administration according to the present invention preferably takes the form for oral administration, for example, tablet, capsule, granule, powder or lozenge. The solid preparation of the present invention is particularly suitable for an oral preparation since the flavor improving effect is exhibited by the milk flavor. Especially, since it contains glucosamine which is an off-flavor component, it is preferable that it is a tablet.

  The solid preparation of the present invention is particularly suitable for a so-called chewable type tablet that can be chewed in the mouth. In general, crushing tablets should be avoided because it impairs the masking effect of odors and tastes of coated tablets and the like, as well as sustained release and enteric properties, but the present invention masks the savory taste of glucosamine with milk flavor. Therefore, the effect of the invention can be sufficiently exerted as a dosage form of a chewable tablet. In particular, the chewable tablet of the present invention is suitable for administration to animals that chew tablets in the mouth.

(Glucosamine)
The solid preparation of the present invention contains glucosamine as an active ingredient. Glucosamine is 2-aminoglucose in which the hydroxyl group at the 2-position of glucose is substituted with an amino group, and is a natural amino sugar widely distributed in nature as a constituent sugar molecule such as glycoproteins, glycolipids, and mucopolysaccharides that are biological components. . Industrially, it can be obtained by hydrolyzing, separating, and purifying chitin contained in crustaceans such as crabs, shrimps, and krill and squid cartilage.

  In recent years, glucosamine has been confirmed not only as an essential component of biological components but also as a health food for the purpose of treatment and prevention of osteoarthritis, beauty and other effects. Widely used.

  Glucosamine that can be used in the present invention is not particularly limited in terms of its origin, production method, and the like. Moreover, glucosamine can also be used as a salt and various derivatives, and there is no restriction | limiting in particular also about those kinds, When a glucosamine is only used in this invention, a salt and a derivative are also included. Examples of glucosamine salts and derivatives include glucosamine hydrochloride, glucosamine sulfate, glucosamine lactate, N-acetylglucosamine, and the like.

  The amount of glucosamine to be added to the solid preparation can be determined based on the fact that the intake of glucosamine is 100 mg to 5000 mg, preferably 300 mg to 2000 mg per person per day. Moreover, the intake per 1 kg of body weight can be 1.5-85.0 mg / kg, for example, More preferably, it can be set to 5.0-60.0 mg / kg. For example, the blending ratio of glucosamine to the tablet can be 0.1 to 95% by weight, preferably 10 to 80% by weight, based on the whole tablet.

(Milk flavor)
The solid preparation of the present invention comprises a milk flavor and has an improved taste unique to glucosamine. The milk flavor in the present invention means a food flavor (flavor) having a milk-like flavor, that is, a flavor similar to milk, butter, cheese, or yogurt. In the present invention, as long as the effect of the present invention is not hindered, the kind of milk flavor is not particularly limited, and any of natural flavor and synthetic flavor can be used. The milk flavor (milk flavor) in the present invention affects not only the fragrance but also the overall mouth sensation felt until the food enters the mouth and is swallowed, and can improve the flavor of the solid preparation containing glucosamine. .

  The method of adding the fragrance is not particularly limited, and examples thereof include a method of mixing the powder fragrance or a method of spraying it by adding it to the binder liquid. The compounding quantity in the solid preparation of milk fragrance | flavor can be suitably set in the range by which the flavor derived from glucosamine is eased. For example, 0.1 to 10% by weight, preferably 1 to 5% by weight can be employed as the blending ratio in the tablet.

  In the solid preparation of the present invention, the blending ratio of glucosamine and milk flavor can be appropriately set within a range in which the flavor derived from glucosamine is relaxed. Especially, it is desirable that it is the range of 4: 1-30: 1.

(Other ingredients)
In addition to glucosamine and milk flavor, the solid preparation of the present invention contains other in vivo functional materials such as chondroitin (for example, chondroitin derived from shark cartilage), enzyme-treated rutin, collagen, hyaluronic acid, vitamins, etc. May be included. Furthermore, additives or auxiliary components generally used in foods may be included, and for example, sweeteners, acidulants, starches, dextrins and the like may be included.

(Chondroitin)
Chondroitin is widely distributed in the human body as chondroitin sulfate, and since it is abundantly contained in the cartilage and skin of joints, it is a healthy food aimed at improving osteoarthritis and skin beauty. It's being used. As understood in the art, the term “chondroitin” in the present invention is meant to include chondroitin sulfate or a salt thereof. Chondroitin sulfate is contained in cartilage and skin, but in particular, cartilage is contained in a high concentration. Shark cartilage powder is widely used as a health food material containing chondroitin at a high concentration, and its main component is sodium chondroitin sulfate which is a polysaccharide having a molecular weight of about 100,000 to several hundred thousand. However, chondroitin produced from raw materials other than shark cartilage, such as squid and salmon, can also be used in the present invention.

  The shark cartilage powder that can be used in the present invention is not limited with respect to the type of shark derived from the shark cartilage, and examples thereof include abalone shark and blue shark. Furthermore, there is no restriction | limiting about the origin part of a cartilage, For example, a head, a fin, etc. are mentioned. Further, it may be a shark cartilage pulverized product obtained by directly pulverizing shark cartilage, or a shark cartilage extract treated for efficiently extracting polysaccharides. Shark cartilage extract is, for example, chopped shark cartilage, extracted by treatment with proteolytic enzyme in a solvent such as water, purified by a method such as adsorption or filtration, and added with excipients such as dextrin Powdered by a method such as spray drying.

  The amount of shark cartilage powder to be blended can be determined with reference to the intake amount of shark cartilage powder per individual being 10 mg to 3000 mg, preferably 50 mg to 1000 mg per day. Moreover, the intake per 1 kg of body weight can be 0.15-50.0 mg / kg, for example, More preferably, it can be 0.80-20.0 mg / kg.

(Enzyme-treated rutin)
Enzyme-treated rutin is obtained by glycosylation of rutin and rutin analogs by enzymatic treatment, and examples of rutin analogs include quercetin, isoquercitrin, morin, myricitrin, and myricetin. Enzyme-treated rutin is known to have a variety of physiological functions such as platelet aggregation and adhesion inhibition, vasodilation, and anticancer in addition to strong antioxidant activity, improving inflammation and promoting blood circulation. It is used in health foods for the purpose of such effects.

  The origin and production method of the enzyme-treated rutin that can be used in the present invention are not particularly limited. The enzyme-treated rutin can be obtained, for example, by treating an extract such as Enju or buckwheat with a glycosyltransferase. Specifically, it can be obtained by the methods described in JP-A-7-10898 and JP-A-2003-33164, and may contain not only enzyme-treated rutin but also pharmaceutically acceptable additives.

  The compounding amount of the enzyme-treated rutin can be determined with reference to a daily intake of enzyme-treated rutin of 1 mg to 500 mg, preferably 5 mg to 300 mg per individual. Moreover, the intake per 1 kg of body weight can be 0.015-8.5 mg / kg, for example, More preferably, it can be 0.080-5.0 mg / kg.

(Subject of administration)
The administration target of the solid preparation of the present invention is not particularly limited. For example, when targeting humans, it may be difficult to swallow tablets in middle-aged and elderly people who have a high risk of developing arthritis, and it is particularly preferable to administer the solid preparation of the present invention as a chewable tablet. In addition, in animals other than humans, palatability greatly affects the ease of administration, and therefore, the solid preparation of the present invention with an improved taste unique to glucosamine is suitable for animal administration. Among them, the present invention suitable for formulation as chewable tablets is particularly preferable for pets (especially dogs and cats) that tend to chew tablets in the mouth.

(Production method)
Moreover, from another viewpoint, this invention can be evaluated with the manufacturing method of the solid preparation for oral administration containing a glucosamine characterized by mix | blending milk fragrance | flavor. Furthermore, from another viewpoint, it can also be understood as a method for improving the flavor of a solid preparation for oral administration containing glucosamine, which comprises blending a milk flavor.

(Example 1)
In a composition containing glucosamine hydrochloride and the like, a composition for suitably masking a flavor peculiar to glucosamine was examined.

  Glucosamine (D-glucosamine hydrochloride, F-50, manufactured by Protein Chemical), chondroitin (shark cartilage powder [KSCP-S], manufactured by Kyowa Technos), or enzyme-treated rutin (San-Emic P15, manufactured by San-Ei Gen FFI) A milk flavor (milk flavor powder SAB-8042, manufactured by Hasegawa Fragrance) was blended with the powder containing, and the effect of the milk flavor was evaluated. 10 g of sample powder was prepared according to the formulation shown in Table 1.

  Six prepared panelists orally ingested the prepared mixed powder, and sensory evaluation was carried out about the flavor. As for the flavor of the mixed powder, the masking effect of the milk flavor was evaluated according to the following criteria for each of glucosamine, chondroitin, and enzyme-treated rutin.

3 points: I do not feel bitterness 2 points: I feel somewhat bitterness 1 point: I feel quite bitterness 0 points: I feel bitterness The total of the evaluation of 6 panelists, the average score of 3 points or less, more than 2 points ○, Two points or less and more than one point were evaluated as Δ, and one point or less and 0 point were set as ×. The results are shown in Table 1.

As is clear from the results in Table 1, it was found that the milk fragrance specifically masks the flavor of glucosamine hydrochloride.
(Example 2)
A glucosamine-containing composition was formulated and the masking effect of the milk flavor was evaluated.

According to the formulation shown in Table 2, milk flavor (sample 1 only), glucosamine hydrochloride, lactose (Freund Sangyo), cellulose (Asahi Kasei Chemicals), silicon oxide (DSL. Japan), sucrose fatty acid ester (Mitsubishi Chemical) About 30 kg of mixed powder was prepared. To mix each component, powder other than sucrose fatty acid ester is put into a blender (Kotobuki Mixwell V-100, manufactured by Tokuju Kosakusho) and mixed at 22 rpm for 5 minutes, and then the same amount of sucrose fatty acid ester is mixed. The powder was triturated and put into a mixer and mixed at 22 rpm for 2 minutes. The obtained mixed powder was beaten using a mortar (HT-AP15SS-II, manufactured by Hata Iron Works), about 2000 kgf, rotation speed about
Tableting was performed directly under the conditions of 20 rpm and a diameter of 10 mm to obtain tablets.
6 panelists orally ingested, sensuously tasted when they were swallowed for 10 seconds after swallowing, and when they were swallowed and swallowed immediately after being swallowed. Therefore, it was evaluated.

3 points: I do not feel bitterness 2 points: I feel somewhat bitterness 1 point: I feel quite bitterness 0 point: The evaluation of 6 panelists who feel bitterness is aggregated, the average of the score is less than 3 points and more than 2 points ○, Two points or less and more than one point were evaluated as Δ, and one point or less and 0 point were set as ×. The results are shown in Table 2.

As shown in Table 2, the masking effect of the milk flavor was confirmed for the unique flavor of glucosamine.
(Example 3)
A glucosamine-containing composition was formulated and the palatability of the dog was evaluated.

  According to the composition shown in Table 3, milk flavor (sample 1 only), glucosamine hydrochloride, chondroitin sulfate-containing shark cartilage powder, enzyme-treated rutin, cellulose, silicon oxide, and sucrose fatty acid ester are mixed to prepare approximately 30 kg of mixed powder. did. To mix each component, powder other than sucrose fatty acid ester is put into a blender (Kotobuki Mixwell V-100, manufactured by Tokuju Kosakusho) and mixed at 22 rpm for 5 minutes, and then the same amount of sucrose fatty acid ester is mixed. The powder was triturated and put into a mixer and mixed at 22 rpm for 2 minutes.

The obtained mixed powder was beaten using an mortar (HT-AP15SS-II, manufactured by Hata Iron Works), about 2000 kgf,
Tableting was performed directly under the conditions of a rotational speed of about 20 rpm and a diameter of 10 mm.

The two prepared tablets were placed about 10 cm apart from each other on the floor, and 21 dogs were allowed to eat freely. The taste of the tablet was evaluated by the owner according to the following evaluation criteria.
3 points: ate well 2 points: ate normally 1 point: not easy to eat but ate 0 points: did not eat The evaluation results of 21 heads were tabulated, and the average score was 3 points or less and more than 2 points ○ 2 points or less, 1 point or more, Δ, 1 point or less, 0 point.

  As a result, it was confirmed that all dogs chewed the tablets and ingested them. Moreover, as shown in Table 3, the palatability in the dog of the glucosamine containing composition improved by setting it as the tablet which mix | blended the milk fragrance | flavor.

Example 4
Milk fragrance or pork fragrance (manufactured by Takasago fragrance) was blended with the glucosamine-containing solid preparation, and a blend suitable for dog taste was examined.

  According to the formulation shown in Table 4, milk flavor (sample 1) or pork flavor (sample 2), glucosamine hydrochloride, chondroitin sulfate-containing shark cartilage powder, enzyme-treated rutin, cellulose, silicon oxide, sucrose fatty acid ester, About 30 kg of mixed powder was prepared. To mix each component, powder other than sucrose fatty acid ester is put into a blender (manufactured by Kotobuki Mixwell V-100 Tokuju Kosakusho) and mixed for 5 minutes at 22 rpm, then the same amount of sucrose fatty acid ester is mixed. And the mixture was put into a mixer and mixed at 22 rpm for 2 minutes.

The obtained mixed powder was beaten using an mortar (HT-AP15SS-II, manufactured by Hata Iron Works), about 2000 kgf,
Tableting was performed directly under the conditions of a rotational speed of about 20 rpm and a diameter of 10 mm.

Two prepared tablets were placed about 10 cm apart from each other and placed on the floor, and 21 dogs were allowed to eat freely, and the owner evaluated the palatability.
As a result, it was confirmed that all dogs chewed the tablets and consumed them. As for the presence or absence of ingestion, 14 of 21 animals were eaten both and 2 were not eaten for 2 kinds of tablets. As shown in Table 3 below, the remaining 6 dogs were 5 dogs that particularly preferred to eat Sample 1 (with milk flavor), and 1 dog that particularly preferred to eat Sample 2 (with pork flavor). .

  As shown in Table 4, the sample blended with the milk flavor had better palatability than the sample blended with the pork flavor.

Claims (10)

  A solid preparation for oral administration comprising glucosamines and a milk flavor.   The solid preparation for oral administration according to claim 1, wherein the glucosamine is one or more selected from the group consisting of glucosamine, a glucosamine salt, or N-acetylglucosamine.   The solid preparation for oral administration according to claim 1 or 2, wherein the solid preparation is a tablet.   The solid preparation for oral administration according to claim 3, wherein the tablet is a chewable tablet.   The solid preparation for oral administration according to any one of claims 1 to 4, which is for a pet animal.   The solid preparation for oral administration according to claim 5, wherein the pet animal is a dog.   The solid preparation for oral administration according to any one of claims 1 to 6, wherein the blending ratio of glucosamines and milk flavor is in the range of 4: 1 to 30: 1.   The solid preparation for oral administration according to any one of claims 1 to 7, further comprising chondroitin and / or enzyme-treated rutin.   A method for producing a solid preparation for oral administration containing glucosamines, comprising blending a milk flavor.   A method for improving the flavor of a solid preparation for oral administration containing glucosamines, comprising blending a milk flavor.