JP7432255B1 - Pharmaceutical composition for oral administration - Google Patents
Pharmaceutical composition for oral administration Download PDFInfo
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- JP7432255B1 JP7432255B1 JP2022155841A JP2022155841A JP7432255B1 JP 7432255 B1 JP7432255 B1 JP 7432255B1 JP 2022155841 A JP2022155841 A JP 2022155841A JP 2022155841 A JP2022155841 A JP 2022155841A JP 7432255 B1 JP7432255 B1 JP 7432255B1
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- Prior art keywords
- carnitine
- collagen
- oral administration
- content
- powder
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Landscapes
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- General Preparation And Processing Of Foods (AREA)
Abstract
【課題】ＩＩ型コラーゲンを有効に摂取でき、関節への負荷を軽減することが可能で、人間や動物の関節ケアや運動機能改善に有用な経口投与用製剤組成物を提供すること。【解決手段】Ｌ－カルニチンと非変性ＩＩ型コラーゲンとを含有する経口投与用製剤組成物。ここで、Ｌ－カルニチン純分の含有量：非変性ＩＩ型コラーゲン純分の含有量の質量比は、５：１～６０：１の範囲であることが好ましい。本発明の経口投与用製剤組成物はまた、粉体物又は液状物であってもよく、顆粒製剤やカプセル剤とすることもできる。シリカ、さつま芋、りんご及び／又は黒砂糖等を含有していてもよい。【選択図】なしAn object of the present invention is to provide a pharmaceutical composition for oral administration that can effectively ingest type II collagen, reduce the load on joints, and is useful for joint care and motor function improvement in humans and animals. A pharmaceutical composition for oral administration containing L-carnitine and undenatured type II collagen. Here, the mass ratio of the content of pure L-carnitine to the content of pure undenatured type II collagen is preferably in the range of 5:1 to 60:1. The pharmaceutical composition for oral administration of the present invention may also be in the form of powder or liquid, and may also be in the form of granules or capsules. It may contain silica, sweet potato, apple and/or brown sugar. [Selection diagram] None
Description
本発明は、経口投与用製剤組成物に関し、具体的には、人間や動物の関節ケアや運動機能改善に有用な経口投与用製剤組成物に関する。 The present invention relates to a pharmaceutical composition for oral administration, and specifically to a pharmaceutical composition for oral administration that is useful for joint care and improving motor function of humans and animals.
近年、人間や飼育動物の運動機能を改善するための製剤組成物が、重要となっている。人間や、犬、猫、馬のような飼育動物においては、昨今、老化や運動不足、肥満等に起因する、変形性関節症等の関節トラブルが増加傾向にある。こうした関節トラブルの予防及びケア、さらには運動機能全般の改善を目的に、従来より様々な経口投与用製剤組成物が、栄養補助食品、健康補助食品、サプリメント等として供給されている。 In recent years, pharmaceutical compositions for improving the motor function of humans and domestic animals have become important. Recently, in humans and domestic animals such as dogs, cats, and horses, joint problems such as osteoarthritis caused by aging, lack of exercise, obesity, etc. are on the rise. For the purpose of preventing and caring for such joint troubles and improving overall motor function, various orally administered pharmaceutical compositions have been supplied as nutritional supplements, health supplements, supplements, and the like.
例えば、特許文献１には、Ｌ－カルニチン類とグルコサミノグリカン類（コンドロイチン硫酸等の、グルコサミンを成分とするムコ多糖類）とを含む組成物が記載され、また、特許文献２には、グルコサミン類とミルク香料とを含んでなる経口投与用固形製剤が記載されている。さらに、特許文献３には、コラーゲンペプチド及びホエイタンパク質を有効成分とする筋損傷回復促進用組成物が開示され、コラーゲンと関節との関係についても言及されている。加えて、特許文献４には、イミダゾールペプチドとケルセチン配糖体とを含有する組成物、さらにはコラーゲンを含有する組成物が記載されている。 For example, Patent Document 1 describes a composition containing L-carnitines and glucosaminoglycans (mucopolysaccharides containing glucosamine, such as chondroitin sulfate); Solid formulations for oral administration are described comprising glucosamines and milk flavoring. Further, Patent Document 3 discloses a composition for promoting recovery from muscle damage that contains collagen peptides and whey protein as active ingredients, and also mentions the relationship between collagen and joints. In addition, Patent Document 4 describes a composition containing an imidazole peptide and a quercetin glycoside, and further a composition containing collagen.
グルコサミンやコンドロイチン類等は、関節軟骨の主要成分の一つであり、その摂取によって関節障害を予防、治療、又は緩和し得ることが報告されている。しかし、水分を除く関節軟骨成分中で、グルコサミンやコンドロイチン類が占める割合は５～１５質量％程度であるため、特許文献１及び２記載の組成物は、関節のケアのために十分有効とは限らない。しかもグルコサミン等は、体内に吸収され難い短所も有する。関節障害を予防、治療、又は緩和する上では、グルコサミン等よりも、軟骨成分の約８０質量％以上を占めるコラーゲンを摂取する方が有用である。 Glucosamine, chondroitins, and the like are one of the main components of articular cartilage, and it has been reported that ingesting them can prevent, treat, or alleviate joint disorders. However, since the proportion of glucosamine and chondroitin in the articular cartilage components excluding water is about 5 to 15% by mass, the compositions described in Patent Documents 1 and 2 are not sufficiently effective for joint care. Not exclusively. Moreover, glucosamine and the like also have the disadvantage that they are difficult to absorb into the body. In preventing, treating, or alleviating joint disorders, it is more useful to ingest collagen, which accounts for about 80% by mass or more of cartilage components, than glucosamine or the like.
コラーゲンの内でも、脊椎動物中に最も大量に存在するコラーゲンはＩ型であり、関節軟骨に多く含まれるＩＩ型コラーゲンとは構造が異なる。関節を有効にケアするためには、ＩＩ型のコラーゲンを、それも非変性の形で摂取することが望ましい。特許文献３に記載されたような、コラーゲンペプチドを含有する組成物では、たとえＩＩ型コラーゲンを原料に用いても、その構造が加水分解酵素等での処理によって失われてしまっている。そのため、ペプチドが栄養として吸収されるだけでコラーゲンとしては認識されず、関節のケアには必ずしも有効に機能し得ない。特許文献４ではＩＩ型コラーゲンについても言及されてはいるが、コラーゲンペプチドではなく非変性のコラーゲンを摂取することの重要性については、開示されていない。 Among collagens, type I collagen exists in the largest amount in vertebrates, and has a different structure from type II collagen, which is abundantly contained in articular cartilage. In order to effectively care for joints, it is desirable to ingest type II collagen, also in a non-denatured form. In a composition containing a collagen peptide as described in Patent Document 3, even if type II collagen is used as a raw material, its structure is lost by treatment with a hydrolytic enzyme or the like. Therefore, peptides are only absorbed as nutrients and are not recognized as collagen, so they cannot necessarily function effectively in joint care. Although Patent Document 4 also mentions type II collagen, it does not disclose the importance of ingesting non-denatured collagen rather than collagen peptides.
また、関節障害を予防又は治療する上で、関節周辺の筋肉を強化し、加えて体重をできるだけ低減して関節に掛かる負荷を軽減することも重要である。特許文献４で言及されているように、ＩＩ型コラーゲンを含有しているだけでは、筋肉強化や体重低減を含めた総合的な関節ケアを図ることはできない。 Furthermore, in preventing or treating joint disorders, it is important to strengthen the muscles around the joints and to reduce the load on the joints by reducing body weight as much as possible. As mentioned in Patent Document 4, simply containing type II collagen does not provide comprehensive joint care including muscle strengthening and weight reduction.
本発明は、このような実情に鑑みてなされたものであり、関節軟骨の主成分であるＩＩ型コラーゲンを有効に摂取でき、しかも筋肉強化や体重低減を併せて行うことによって、人間や動物の関節障害を予防、治療、又は緩和するとともに、運動機能を改善することができる経口投与用製剤組成物を提供することを目的とする。 The present invention was developed in view of the above circumstances, and it enables humans and animals to effectively ingest type II collagen, which is the main component of articular cartilage, and also strengthens muscles and reduces body weight. The object of the present invention is to provide a pharmaceutical composition for oral administration that can prevent, treat, or alleviate joint disorders and improve motor function.
本発明者は、人間や動物の関節障害や、運動機能の改善を達成するための検討を行ったところ、例えば高齢化すると、関節の軟骨成分が不足する傾向があるとともに、関節周りの筋肉も弱くなりがちであることが判明した。このため、本発明者は、不足しがちな関節の軟骨成分を、非変性ＩＩ型コラーゲンで補給し、また、弱くなりがちな関節周りの筋肉を、Ｌ－カルニチンで補強することによって、人間や動物に発生する関節障害を緩和するとともに、運動機能の改善を図ることができることを見出し、本発明を完成させるに至った。 The present inventor conducted studies to improve joint disorders and motor function in humans and animals, and found that, for example, as people age, cartilage components in the joints tend to become insufficient, and the muscles around the joints also decrease. It turns out that it tends to be weak. For this reason, the present inventor has devised a method for human and human health by replenishing cartilage components in joints, which tend to be deficient, with undenatured type II collagen, and by reinforcing the muscles around joints, which tend to become weak, with L-carnitine. The present inventors have discovered that joint disorders occurring in animals can be alleviated and motor function can be improved, leading to the completion of the present invention.
すなわち、本発明は少なくとも下記の発明を提供する。
［１］Ｌ－カルニチンと非変性ＩＩ型コラーゲンとを含有する経口投与用製剤組成物。
［２］非変性ＩＩ型コラーゲンの含有量に対するＬ－カルニチンの含有量の割合が、質量比で、５～６０の範囲である、［１］に記載の経口投与用製剤組成物。
［３］前記製剤組成物は、粉体物又は液状物である、［１］又は［２］に記載の経口投与用製剤組成物。
［４］前記製剤組成物は、粉体状の前記Ｌ－カルニチンと、粉体状の前記非変性ＩＩ型コラーゲンとを混合した混合物であり、かつ、
前記Ｌ－カルニチンは、酸味抑制剤でマスキングされている、［３］に記載の経口投与用製剤組成物。
［５］前記酸味抑制剤は、シリカ、さつま芋、りんご及び黒砂糖のうちの少なくとも１つの材料で構成されている、［４］に記載の経口投与用製剤組成物。
［６］前記製剤組成物は、前記Ｌ－カルニチンと前記非変性ＩＩ型コラーゲンを水に溶解させて調製した液状物である、［３］に記載の経口投与用製剤組成物。
［７］上記［４］又は［５］に記載の前記製剤組成物からなる顆粒製剤。
［８］上記［６］に記載の前記製剤組成物を充填してなるカプセル剤。
That is, the present invention provides at least the following inventions.
[1] A pharmaceutical composition for oral administration containing L-carnitine and undenatured type II collagen.
[2] The pharmaceutical composition for oral administration according to [1], wherein the ratio of the content of L-carnitine to the content of undenatured type II collagen is in the range of 5 to 60 in terms of mass ratio.
[3] The pharmaceutical composition for oral administration according to [1] or [2], wherein the pharmaceutical composition is a powder or a liquid.
[4] The pharmaceutical composition is a mixture of the powdered L-carnitine and the powdered non-denatured type II collagen, and
The pharmaceutical composition for oral administration according to [3], wherein the L-carnitine is masked with an acidity suppressant.
[5] The pharmaceutical composition for oral administration according to [4], wherein the sour taste suppressant is composed of at least one material selected from silica, sweet potato, apple, and brown sugar.
[6] The pharmaceutical composition for oral administration according to [3], wherein the pharmaceutical composition is a liquid prepared by dissolving the L-carnitine and the undenatured type II collagen in water.
[7] A granule preparation comprising the pharmaceutical composition described in [4] or [5] above.
[8] A capsule filled with the pharmaceutical composition described in [6] above.
本発明によれば、関節軟骨の主成分であるＩＩ型コラーゲンを有効に摂取でき、しかも筋肉強化や体重低減を併せて行うことによって、人間や動物の関節障害を予防、治療、又は緩和するとともに、運動機能を改善することができる経口投与用製剤組成物の提供が可能になった。 According to the present invention, it is possible to effectively ingest type II collagen, which is the main component of articular cartilage, and to strengthen muscles and reduce body weight, thereby preventing, treating, or alleviating joint disorders in humans and animals. Therefore, it has become possible to provide a pharmaceutical composition for oral administration that can improve motor function.
本発明は特定の理論により限定されるものではないが、本発明が効果を奏する理由として、ＩＩ型コラーゲンが非変性の状態で体内に摂取されることの他に、経口免疫寛容が働くことが考えられる。例えば免疫機能が過剰活性化等の異常を来すと、免疫細胞が関節軟骨中のＩＩ型コラーゲンを攻撃してしまう場合がある。ここで非変性のＩＩ型コラーゲンを摂取すると、経口免疫寛容が働き、それまで活性化していた免疫細胞が攻撃を止めるため、関節軟骨の破壊が抑制されると考えられる。コラーゲンにはまた、軟骨細胞を活性化させ、関節のクッションの役割をするヒアルロン酸等の生成を促す機能があり、この機能によっても関節のケアがなされると推定される。 Although the present invention is not limited by any particular theory, the reason why the present invention is effective is that type II collagen is ingested into the body in a non-denatured state and that oral immune tolerance is activated. Conceivable. For example, when immune function becomes abnormal, such as overactivation, immune cells may attack type II collagen in articular cartilage. When non-denatured type II collagen is ingested, oral immune tolerance is activated, and previously activated immune cells stop attacking, which is thought to suppress the destruction of articular cartilage. Collagen also has the function of activating cartilage cells and promoting the production of hyaluronic acid, etc., which acts as a cushion for joints, and it is presumed that this function also provides joint care.
また、本発明の経口投与用製剤組成物によれば、もう一方の主成分であるＬ－カルニチンによって脂肪燃焼が促進されて、体重を適正に制御すると共に、燃焼時のエネルギーによって関節周辺の筋肉を造成することも可能となる。しかもＬ－カルニチンは、肝臓の負担を軽減し、また、血流を改善する機能も有する。そのため、摂取した非変性ＩＩ型コラーゲンの吸収・同化がさらに促進され、関節軟骨の保持・修復に寄与している可能性がある。こうした、非変性ＩＩ型コラーゲンによる関節軟骨自体及び関節周辺の筋肉の強化と、Ｌ－カルニチンによる体重制御、さらにはＬ－カルニチンによる非変性ＩＩ型コラーゲンの吸収・同化の促進等の機能の、いわば相乗効果によって、有効な関節ケア、さらには運動機能の改善がなされると考えられる。 In addition, according to the pharmaceutical composition for oral administration of the present invention, fat burning is promoted by L-carnitine, the other main component, and the body weight is properly controlled, and the energy generated during combustion helps muscles around the joints. It is also possible to create. Furthermore, L-carnitine also has the function of reducing the burden on the liver and improving blood flow. Therefore, the absorption and assimilation of the ingested undenatured type II collagen may be further promoted, contributing to the maintenance and repair of articular cartilage. These functions include strengthening the articular cartilage itself and the muscles around the joint by undenatured type II collagen, controlling body weight by L-carnitine, and promoting the absorption and assimilation of undenatured type II collagen by L-carnitine. It is thought that the synergistic effect results in effective joint care and further improvement in motor function.
以下、本発明の経口投与用製剤組成物について、幾つかの実施形態を例に説明するが、本発明はこれら実施形態に限定されるものではない。 Hereinafter, the pharmaceutical composition for oral administration of the present invention will be described using several embodiments as examples, but the present invention is not limited to these embodiments.
＜経口投与用製剤組成物＞
本発明の経口投与用製剤組成物は、上記のようにＬ－カルニチンと非変性ＩＩ型コラーゲンとを含有する。そして、本発明は、コラーゲンとして非変性のＩＩ型コラーゲンを含有すること、カルニチンとしてＬ－体を含有すること、及びＬ－カルニチンと非変性ＩＩ型コラーゲンとを併用することが必要である。非変性ＩＩ型コラーゲンであれば、関節軟骨中に同化し易く、また、Ｌ－カルニチンの併用によってコラーゲンの吸収・同化がさらに促進されると共に、関節周辺の筋肉の強化や体重の制御等も可能となる。そのため、人間や動物の関節を有効にケアし、さらには運動機能を改善することができる。尚、カルニチンとして、Ｌ－カルニチンではなく、Ｄ－カルニチンを用いた場合には、関節ケア等の効果は発揮され難いため、本発明の経口投与用製剤組成物では、Ｌ－カルニチンを含有させることを必須としている。
<Preparation composition for oral administration>
The pharmaceutical composition for oral administration of the present invention contains L-carnitine and undenatured type II collagen as described above. In the present invention, it is necessary to contain non-denatured type II collagen as collagen, to contain L-form as carnitine, and to use L-carnitine and non-denatured type II collagen in combination. Undenatured type II collagen is easily assimilated into articular cartilage, and combined use of L-carnitine further promotes absorption and assimilation of collagen, strengthening muscles around joints and controlling body weight. becomes. Therefore, it is possible to effectively care for the joints of humans and animals, and even improve motor function. Note that when D-carnitine is used as carnitine instead of L-carnitine, effects such as joint care are unlikely to be exhibited. Therefore, in the pharmaceutical composition for oral administration of the present invention, L-carnitine may be included. is required.
尚、本発明の経口投与用製剤組成物は、非変性ＩＩ型コラーゲンの含有量に対するＬ－カルニチンの含有量の割合が、Ｌ－カルニチン純分の含有量：非変性ＩＩ型コラーゲン純分の質量比で５：１～６０：１の範囲、特に１０：１～５０：１の範囲とするのが好ましい。より好ましくは、後記するように対象とする人間や動物の種類や体重に応じて、Ｌ－カルニチン及び非変性ＩＩ型コラーゲンの含有量、並びに両者の質量比をさらに細かく調整する。こうした調整によって、人間や動物の関節ケアや運動機能の改善を、より効果的に行うことが可能となる。 In addition, in the pharmaceutical composition for oral administration of the present invention, the ratio of the content of L-carnitine to the content of undenatured type II collagen is: content of pure L-carnitine: mass of pure undenatured type II collagen. The ratio is preferably in the range of 5:1 to 60:1, particularly in the range of 10:1 to 50:1. More preferably, the contents of L-carnitine and undenatured type II collagen, as well as the mass ratio of the two, are further finely adjusted depending on the type and body weight of the target human or animal, as described later. These adjustments make it possible to more effectively improve joint care and motor function in humans and animals.
［Ｌ－カルニチン］
Ｌ－カルニチン自体は公知であり、市販もされている。下記式（１）の構造の、室温で固体の物質である。
L-carnitine itself is known and commercially available. It is a substance having the structure of the following formula (1) that is solid at room temperature.
Ｌ－カルニチンはまた、種々の酸との塩の形でも市販されており、本発明の経口投与用製剤組成物においては、これらの塩を使用することもできる。塩の種類に制限はなく、例えば塩酸塩、カルボン酸塩、リン酸塩等を用いることもできるが、これらに限定されない。Ｌ－カルニチンは吸湿性が高いため、取扱容易性の観点からは、カルボン酸等の塩、特にジカルボン酸塩、例えばシュウ酸、クエン酸、酒石酸、フマル酸、マレイン酸との塩が好ましい。例としてＬ－カルニチンフマル酸塩やＬ－カルニチン酒石酸塩等が挙げられるが、これらに限定されない。ナトリウム等の金属イオンや、アンモニウムイオンを含む塩であってもよい。複数種のＬ－カルニチン及び／又はその塩を、併用することもできる。尚、これら塩や混合原料を用いる場合には、Ｌ－カルニチンの含有量は、上記式（１）に相当する純分の量を基に算出するものとする。 L-carnitine is also commercially available in the form of salts with various acids, and these salts can also be used in the pharmaceutical composition for oral administration of the present invention. There is no restriction on the type of salt, and for example, hydrochloride, carboxylate, phosphate, etc. can be used, but the salt is not limited to these. Since L-carnitine is highly hygroscopic, from the viewpoint of ease of handling, salts of carboxylic acids and the like, particularly dicarboxylic acid salts, such as salts with oxalic acid, citric acid, tartaric acid, fumaric acid, and maleic acid, are preferred. Examples include, but are not limited to, L-carnitine fumarate and L-carnitine tartrate. It may also be a salt containing metal ions such as sodium or ammonium ions. Plural types of L-carnitine and/or its salts can also be used in combination. In addition, when using these salts or mixed raw materials, the content of L-carnitine shall be calculated based on the amount of pure content corresponding to the above formula (1).
Ｌ－カルニチンのカルボン酸塩には、一方で酸味を伴う難点もある。こうした難点は、人間用の製剤組成物の場合は、例えばカプセル化や糖衣錠剤化によって解決し得る。しかし、飼育動物の多くはカプセルや糖衣錠を受け付けないため、塩を形成していないほぼ純粋なＬ－カルニチンを経口投与用製剤組成物の成分としてもよい。また、後記するようにＬ－カルニチンを酸味抑制剤、例えばシリカ等のケイ素化合物、又はさつま芋、りんご、黒砂糖等の食物パウダーと複合化（混合、マスキング等）して、その酸味を低減させることもできる。尚、Ｌ－カルニチン等の成分を水に溶解させた、後記するような液状の製剤組成物や、そうした液状製剤組成物を充填したカプセル剤では、吸湿防止の必要がないため、例えばＬ－カルニチンの結晶性粉末も利便性良く使用することができる。 On the other hand, L-carnitine carboxylates have the disadvantage of having a sour taste. These difficulties can be overcome in the case of pharmaceutical compositions for human use, for example, by encapsulation or sugar-coating. However, since many domesticated animals do not accept capsules or sugar-coated tablets, substantially pure L-carnitine without salt formation may be used as a component of the pharmaceutical composition for oral administration. In addition, as described later, L-carnitine can be compounded (mixed, masked, etc.) with an acidity suppressant, such as a silicon compound such as silica, or a food powder such as sweet potato, apple, brown sugar, etc., to reduce its acidity. You can also do it. It should be noted that in liquid pharmaceutical compositions as described below in which components such as L-carnitine are dissolved in water, and in capsules filled with such liquid pharmaceutical compositions, there is no need to prevent moisture absorption. Crystalline powders of can also be conveniently used.
［非変性ＩＩ型コラーゲン］
非変性ＩＩ型コラーゲンも公知であり、市販もされている。また、動物の軟骨等から抽出等によって採取することもできる。ＩＩ型コラーゲンにおいては、α鎖と呼ばれるペプチド鎖３本が集まってコラーゲン細繊維を作り、繊維性のコラーゲンを形成している。本発明の経口投与用製剤組成物において、ＩＩ型コラーゲンは非変性のものであればどのような構造のものでもよく、またどのような製法で得られたものであってもよい。
[Non-denatured type II collagen]
Undenatured type II collagen is also known and commercially available. It can also be collected by extraction from animal cartilage or the like. In type II collagen, three peptide chains called α chains come together to form collagen fibrils, forming fibrous collagen. In the pharmaceutical composition for oral administration of the present invention, type II collagen may have any structure as long as it is undenatured, and may be obtained by any manufacturing method.
ここで、「非変性」とは、ＩＩ型コラーゲンのらせん構造が壊れておらず、例えばコラーゲンペプチドのような低分子量化されたものではない状態、すなわち化学処理や加熱処理による構造の変化を事実上来していない状態を指す。こうした非変性ＩＩ型コラーゲンは、例えば鶏等の動物の軟骨から、温水抽出等によって得ることができる。しかしながら本発明に含まれる非変性ＩＩ型コラーゲンは、他の動物の軟骨や他の抽出方法によって得られたものであってもよい。尚、抽出の際にゼラチンや脂肪分、又はＩ型コラーゲンやＩＩＩ型コラーゲン等の他の構造のコラーゲンが混入する場合もあるが、本発明の経口投与用製剤組成物は、こうした不可避的な混合物を含有していてもよい。 Here, "undenatured" refers to a state in which the helical structure of type II collagen is not broken and is not lowered in molecular weight like collagen peptides, that is, a state in which the structure changes due to chemical treatment or heat treatment. Refers to a state of not rising. Such undenatured type II collagen can be obtained, for example, from the cartilage of animals such as chickens, by hot water extraction or the like. However, the undenatured type II collagen included in the present invention may be obtained from cartilage of other animals or by other extraction methods. Note that during extraction, gelatin, fat, or collagen of other structures such as type I collagen or type III collagen may be mixed in, but the pharmaceutical composition for oral administration of the present invention does not contain such unavoidable mixtures. may contain.
［他成分］
本発明の経口投与用製剤組成物はまた、食品や化粧品、医薬品等に一般に使用される添加剤や成分を含んでいてもよい。例えば、Ｌ－カルニチン及び非変性ＩＩ型コラーゲンに加えて、グルコサミン等のムコ多糖類、例えばヒアルロン酸、ヘパリン、コンドロイチン類；非変性ＩＩ型コラーゲン以外のコラーゲン、例えばＩ型コラーゲン、ＩＩＩ型コラーゲン、コラーゲンペプチド；ビタミン類、例えばビタミンＡ、各種ビタミンＢ、ビタミンＣ、ビタミンＤ；各種タンパク質；炭水化物類、例えば澱粉、デキストリン；脂肪酸塩、例えばステアリン酸カルシウム、パルミチン酸カルシウム、リノール酸ナトリウム等；さらには甘味料、酸味料、香味料、滑剤、界面活性剤、ｐＨ調整剤、賦形剤等を含有していてもよい。
[Other ingredients]
The pharmaceutical composition for oral administration of the present invention may also contain additives and components commonly used in foods, cosmetics, pharmaceuticals, and the like. For example, in addition to L-carnitine and undenatured type II collagen, mucopolysaccharides such as glucosamine, such as hyaluronic acid, heparin, chondroitin; collagens other than undenatured type II collagen, such as type I collagen, type III collagen, collagen Peptides; vitamins such as vitamin A, various vitamin B, vitamin C, vitamin D; various proteins; carbohydrates such as starch, dextrin; fatty acid salts such as calcium stearate, calcium palmitate, sodium linoleate, etc.; and sweeteners. , an acidulant, a flavoring agent, a lubricant, a surfactant, a pH adjuster, an excipient, and the like.
本発明の経口投与用製剤組成物に、例えばシクロデキストリン等のデキストリン、ステアリン酸カルシウム等の脂肪酸塩を配合することにより、賦形効果を得ることができる。また、ビタミン類を配合して、栄養補助剤としての機能を付すこともできる。特に、動物用の経口投与用製剤組成物においては、摂取対象の動物が好む味付け・臭気とするために、各種の炭水化物や、それを含有する食物パウダー、さらには香味料等を配合することが好ましい。 An excipient effect can be obtained by incorporating, for example, a dextrin such as cyclodextrin or a fatty acid salt such as calcium stearate into the pharmaceutical composition for oral administration of the present invention. In addition, vitamins can be added to provide a function as a nutritional supplement. In particular, in pharmaceutical compositions for oral administration to animals, various carbohydrates, food powders containing carbohydrates, flavoring agents, etc. may be added to provide flavors and odors that are preferred by the animals to be ingested. preferable.
［組成物の形状］
本発明の経口投与用製剤組成物はまた、各種成分を水や液糖等に溶解又は分散させた形態であってもよい。例えば、Ｌ－カルニチンと非変性ＩＩ型コラーゲンを水に溶解させて調製した液状物であってもよく、こうした液状の製剤組成物を充填してなるカプセル剤であってもよい。本発明の経口投与用製剤組成物は勿論、粉体物、例えば粉状物や粒状物とすることもできる。製剤組成物から成る顆粒製剤や、錠剤の形状としてもよい。本発明の経口投与用製剤組成物の形状に特に制限はなく、摂取対象及び含有成分に応じて、所望の剤形とすることが可能である。以下では、各種組成及び形状の経口投与用製剤組成物について、具体的な実施形態を幾つか挙げてさらに詳しく説明するが、本発明はこれら実施形態に限定されるものではない。
[Shape of composition]
The pharmaceutical composition for oral administration of the present invention may also be in the form of various components dissolved or dispersed in water, liquid sugar, or the like. For example, it may be a liquid prepared by dissolving L-carnitine and undenatured type II collagen in water, or it may be a capsule filled with such a liquid pharmaceutical composition. The pharmaceutical composition for oral administration of the present invention can of course be in the form of a powder, such as powder or granules. The pharmaceutical composition may be in the form of granules or tablets. There is no particular restriction on the shape of the pharmaceutical composition for oral administration of the present invention, and it is possible to form it into a desired dosage form depending on the subject to be ingested and the ingredients contained. In the following, pharmaceutical compositions for oral administration having various compositions and shapes will be described in more detail by citing some specific embodiments, but the present invention is not limited to these embodiments.
＜人間用経口投与用粉体製剤＞
本発明の経口投与用製剤組成物の実施形態の一つは、主として人間用の、粉体状の経口投与用製剤組成物（人間用経口投与用粉体製剤）である。ここで、粉体製剤とは、細粒剤（一般に８５０μｍふるいを全量通過し、５００μｍふるいに残るものが１０％以下の製剤）等の散剤の他、散剤を粒状に造粒した製剤や顆粒剤等を全て包含する。
<Powder preparation for oral administration for humans>
One embodiment of the pharmaceutical composition for oral administration of the present invention is a powdered pharmaceutical composition for oral administration (powder formulation for human oral administration) mainly for human use. Here, powder preparations include powder preparations such as fine granules (generally preparations that pass through an 850 μm sieve and have 10% or less remaining on a 500 μm sieve), preparations made by granulating powders, and granules. etc. are all included.
人間用の経口投与用粉体製剤は、例えば、純分で３０～１５０ｍｇ、特に６０～１００ｍｇ程度のＬ－カルニチンと、純分で１～２０ｍｇ、特に３～１２ｍｇ程度の非変性ＩＩ型コラーゲンとを含有し、それらを含有する粉体製剤の全量が、例えば１００～１０００ｍｇ、特に２００～５００ｍｇ程度の粉体製剤とすることができる。一般に人間は１日当たり５ｍｇ以上、特に１０ｍｇ程度の非変性ＩＩ型コラーゲンを摂取することが推奨されるため、上記粉体製剤又はこの２倍量の各成分を含む粉体製剤を、例えば１日に１～２包（又は錠）服用してもよい。また、多少の酸味であれば人間は概して忌避しないため、Ｌ－カルニチンの含有量を多めにすることができる。Ｌ－カルニチンを、例えばフマル酸等との塩の形で６０～５００ｍｇ、特に１００～４００ｍｇ程度配合してもよく、結晶性粉末の形で１００～５００ｍｇ、特に２００～４００ｍｇ程度配合してもよい。 A powder preparation for oral administration for humans contains, for example, about 30 to 150 mg of pure L-carnitine, especially about 60 to 100 mg, and about 1 to 20 mg of pure undenatured type II collagen, especially about 3 to 12 mg. The total amount of the powder preparation containing them can be, for example, about 100 to 1000 mg, particularly about 200 to 500 mg. Generally, it is recommended that humans ingest 5 mg or more of undenatured type II collagen per day, especially about 10 mg. You may take 1 to 2 sachets (or tablets). In addition, since humans generally do not dislike a slightly sour taste, the content of L-carnitine can be increased. L-carnitine may be blended in the form of a salt with fumaric acid or the like in an amount of 60 to 500 mg, particularly 100 to 400 mg, or in the form of a crystalline powder of 100 to 500 mg, particularly 200 to 400 mg. .
人間用経口投与用粉体製剤の場合、Ｌ－カルニチンの含有量：非変性ＩＩ型コラーゲンの含有量の比率は、純分の質量比で５：１～５０：１の範囲、中でも１０：１～３０：１の範囲、特に１５：１～２０：１の範囲とするのが好ましい。例えば、純分で１０～５０質量％、特に２０～３０質量％のＬ－カルニチン、及び純分で０．２～５質量％、特に１～２質量％の非変性ＩＩ型コラーゲン、さらには所望により、５～７０質量％、特に１０～５０質量％の炭水化物類、例えばデキストリン、及び／又は０．２～５質量％、特に１～３質量％のステアリン酸カルシウム等の添加剤を含有する組成物であってもよい。 In the case of a powder preparation for oral administration to humans, the ratio of the content of L-carnitine to the content of undenatured type II collagen is in the range of 5:1 to 50:1 in terms of pure mass ratio, especially 10:1. The range is preferably from 15:1 to 20:1, particularly from 15:1 to 20:1. For example, 10 to 50% by mass of pure L-carnitine, especially 20 to 30% by mass, and 0.2 to 5% by mass, especially 1 to 2% by mass of undenatured type II collagen, as well as desired compositions containing 5 to 70% by weight, in particular 10 to 50% by weight of carbohydrates, such as dextrins, and/or 0.2 to 5% by weight, in particular 1 to 3% by weight of additives such as calcium stearate. It may be.
人間用経口投与用粉体製剤においてはまた、Ｌ－カルニチンは、カルボン酸塩、例えばフマル酸塩や酒石酸塩等のジカルボン酸塩であることが好ましい。Ｌ－カルニチンをこうしたジカルボン酸塩とすることにより、吸湿性が抑制されるため、取扱性が良好となる利点が生じる。Ｌ－カルニチン塩の含有によって酸味が多少強くなる場合があるが、人間用製剤においてはこうした酸味が嫌われるケースは少ない。こうした人間用経口投与用粉体製剤は、粉体状や粒体状であってもよく、また、各種成分がゼラチン等のカプセル内に充填された、カプセル剤であってもよい。尚、同様の組成の経口投与用粉体製剤は、人間用に限らず、所望により動物に摂取させてもよい。 In powder formulations for oral administration to humans, L-carnitine is also preferably a carboxylate, for example a dicarboxylate such as fumarate or tartrate. By forming L-carnitine into such a dicarboxylate salt, hygroscopicity is suppressed, resulting in an advantage of improved handling properties. Although the sourness may become somewhat strong due to the inclusion of L-carnitine salt, such sourness is rarely disliked in human preparations. Such powder preparations for oral administration to humans may be in the form of powder or granules, or may be capsules in which various ingredients are filled into capsules such as gelatin. Incidentally, a powder preparation for oral administration having a similar composition is not limited to human use, but may be ingested by animals if desired.
＜人間用経口投与用液状製剤＞
本発明の経口投与用製剤組成物は、上記したように液状であってもよい。例えば、３０～８０質量％、特に５０～６０質量％のＬ－カルニチン、１～１０質量％、特に２～４質量％の非変性ＩＩ型コラーゲン、及び１０～６０質量％、特に２０～３０質量％の水を含有する液状物とすることができる。この液状物はまた、所望により５～４０質量％、特に１０～２０質量％の炭水化物類、例えばデキストリン、及び／又は０．１～５質量％、特に１～３質量％のステアリン酸カルシウム等の添加剤を含有していてもよい。
<Liquid preparation for oral administration for humans>
The pharmaceutical composition for oral administration of the present invention may be in liquid form as described above. For example, 30-80% by weight, especially 50-60% by weight of L-carnitine, 1-10% by weight, especially 2-4% by weight of undenatured type II collagen, and 10-60% by weight, especially 20-30% by weight. % of water. This liquid may optionally also contain the addition of carbohydrates, such as dextrin, in an amount of 5 to 40% by weight, in particular 10 to 20% by weight, and/or calcium stearate, etc., in an amount of 0.1 to 5% by weight, in particular 1 to 3% by weight. It may contain an agent.
こうした人間用経口投与用液状製剤は、液状物として飲用することもできるが、当該液状物をゼラチン等のカプセル内に充填し、上記した人間用経口投与用粉体製剤と同様、カプセル剤として摂取することも可能である。その場合、酸味を感じないで摂取することができるので、Ｌ－カルニチンを比較的多量に含有させ、Ｌ－カルニチン（純分）の含有量：非変性ＩＩ型コラーゲンの含有量の比率を、質量比で例えば１０：１～５０：１の範囲、中でも２０：１～４０：１の範囲、特に２５：１～３０：１の範囲とすることもできる。また、液状のために吸湿性を考慮する必要がないため、Ｌ－カルニチンを、塩ではなく純物質（不可避的不純物を少量含有する物質も含む。）の形で用いることも可能である。例えば、全量３００～７００ｍｇ程度のカプセル剤中に、Ｌ－カルニチンを純度９０％程度の結晶性粉末の形で２００～４００ｍｇ程度、非変性ＩＩ型コラーゲンを３０～６０ｍｇ程度配合してもよい。尚、同様の組成や形状をもつ人間用経口投与用液状製剤は、人間用に限らず、所望により動物に摂取させてもよい。 These liquid preparations for oral administration for humans can be taken as a liquid, but the liquid preparations are filled into capsules such as gelatin and taken as capsules in the same way as the powder preparations for oral administration for humans described above. It is also possible to do so. In that case, since it can be ingested without feeling sour, a relatively large amount of L-carnitine is contained, and the ratio of the content of L-carnitine (pure content) to the content of undenatured type II collagen is adjusted by mass. For example, the ratio may be in the range from 10:1 to 50:1, especially in the range from 20:1 to 40:1, especially in the range from 25:1 to 30:1. Furthermore, since it is liquid, there is no need to consider hygroscopicity, so it is also possible to use L-carnitine in the form of a pure substance (including substances containing small amounts of unavoidable impurities) rather than a salt. For example, in a capsule with a total amount of about 300 to 700 mg, about 200 to 400 mg of L-carnitine in the form of a crystalline powder with a purity of about 90% and about 30 to 60 mg of undenatured type II collagen may be blended. Note that liquid preparations for oral administration to humans having similar compositions and shapes are not limited to those for humans, but may be ingested by animals if desired.
＜動物用経口投与用製剤組成物＞
本発明の経口投与用製剤組成物を動物用、例えば犬や猫等の愛玩動物、あるいは馬や牛等の大型飼育動物用に使用する場合、摂取対象の動物に応じた組成及び摂取量とすることが好ましい。例えば主成分の一つであるＬ－カルニチンは、カルボン酸塩にすると酸味が増して摂取対象の動物が受け付けない場合があるので、塩を形成していないＬ－カルニチンとして配合することが好ましい。また、粉体状のＬ－カルニチン及び／又は非変性ＩＩ型コラーゲンが、炭水化物等の酸味抑制成分と組み合わされていること、特に酸味抑制成分で表面被覆（マスキング）されていることが好ましい。
<Preparation composition for oral administration for animals>
When the pharmaceutical composition for oral administration of the present invention is used for animals, for example pet animals such as dogs and cats, or large domestic animals such as horses and cows, the composition and intake amount should be adjusted according to the animal to be ingested. It is preferable. For example, when L-carnitine, which is one of the main components, is converted into a carboxylic acid salt, it increases the sourness and may not be accepted by the animals to be ingested. Therefore, it is preferable to formulate L-carnitine without forming a salt. Further, it is preferable that the powdered L-carnitine and/or undenatured type II collagen is combined with a sour taste suppressing component such as a carbohydrate, and in particular, the surface is coated (masked) with the sour taste suppressing component.
具体的には、動物用の製剤組成物は例えば、粉体状のＬ－カルニチンと、粉体状の非変性ＩＩ型コラーゲンとを混合した混合物であり、かつ、Ｌ－カルニチンは、粉体化した、シリカ、さつま芋、りんご及び黒砂糖のうちの少なくとも１つの酸味抑制成分で表面被覆（マスキング）されていることが好ましい。尚、こうした動物用経口投与用製剤組成物と同様の配合の製剤組成物は、人間用に使用することも可能である。 Specifically, the pharmaceutical composition for animals is, for example, a mixture of powdered L-carnitine and powdered undenatured type II collagen; It is preferable that the surface is coated (masked) with at least one acidity suppressing component selected from silica, sweet potato, apple, and brown sugar. In addition, a pharmaceutical composition having the same formulation as the pharmaceutical composition for oral administration for animals can also be used for humans.
動物用の経口投与用製剤組成物では、摂取対象の動物がカプセル剤や液状物の剤形を受け付けない場合があるため、粉状物等の粉体状製剤、特にそうした粉状物を加工した顆粒製剤とすることが好ましい。例えば、上記のようにさつま芋等の酸味抑制成分と複合化したＬ－カルニチンの粉体及び非変性ＩＩ型コラーゲンの粉体を、造粒して顆粒製剤とすれば、犬、猫、馬等の種々の動物が嫌がることなく摂取する経口投与用製剤組成物とすることができる。 In the case of pharmaceutical compositions for oral administration to animals, since the target animals may not accept capsules or liquid dosage forms, powdered preparations such as powders, especially those that have been processed A granule formulation is preferred. For example, if L-carnitine powder and undenatured type II collagen powder complexed with an acidity suppressing ingredient such as sweet potato are granulated to form a granule preparation as described above, it can be used for dogs, cats, horses, etc. It can be made into a pharmaceutical composition for oral administration that can be ingested by various animals without objection.
ここで、顆粒製剤を作製する際の造粒方法に特に制限はなく、攪拌造粒、流動層造粒、転動造粒、もしくは押出造粒等の湿式造粒法、又は乾式造粒法、さらには噴霧造粒法等の慣用の方法を採用すればよい。特に、密度が高く、粒度分布の均一な球形粒子が得易い、攪拌造粒法が好ましい。尚、こうした顆粒状や粉状の本発明の動物用経口投与用製剤組成物は、動物の食餌に振りかける、又は混入することによって摂取させることができる。ここで、本発明の動物用経口投与用製剤組成物は、調理後の食餌に振りかけ又は混合することが好ましい。非変性ＩＩ型コラーゲンは熱に弱い傾向があるが、調理後の例えば５０℃以下程度に冷えた食餌であれば分解することなく、効果を発揮し得る。 Here, there is no particular restriction on the granulation method when producing the granule preparation, and wet granulation methods such as stirring granulation, fluidized bed granulation, rolling granulation, or extrusion granulation, or dry granulation methods, Furthermore, conventional methods such as spray granulation may be employed. Particularly preferred is the agitation granulation method, which can easily produce spherical particles with high density and uniform particle size distribution. The granular or powdered pharmaceutical composition for oral administration to animals of the present invention can be ingested by sprinkling or mixing it into animal feed. Here, the pharmaceutical composition for oral administration to animals of the present invention is preferably sprinkled on or mixed with cooked food. Although undenatured type II collagen tends to be sensitive to heat, it can be effective without being decomposed if the food is cooled to, for example, 50° C. or lower after cooking.
動物用経口投与用製剤組成物の１日当たりの使用量等にも特に制限はなく、摂取対象の動物の種類及び体重に応じた所望の量とすることができる。個体差もあるが、１日に摂取させる非変性ＩＩ型コラーゲン量は、小動物の場合で２～１０ｍｇ、例えば５ｍｇ程度、大型動物、例えば体重５００ｋｇ程度の馬の場合は１００～５００ｍｇ程度を目安とすればよい。例えば５０～４００ｍｇ、特に１５０～２５０ｍｇ程度のＬ－カルニチンと、２～１０ｍｇ、特に３～８ｍｇ程度の非変性ＩＩ型コラーゲンとを含有する、１包の全量が０．２～３ｇ、特に０．５～１．５ｇ程度の粉体物又は顆粒製剤を、小型犬や猫、ウサギに対しては半包～１包、中型犬に対しては１～２包程度、体重２０ｋｇ程度以上の大型犬には２包程度以上、馬等の大型動物に対しては体重に応じて５～２００包、特に２０～１００包程度使用することが好ましい。中型動物用に、同様の組成で１包の全量が１～５ｇ、特に１～３ｇ程度の製剤組成物としてもよく、また、大型動物用に１包の全量が１０～１００ｇ程度の製剤組成物とすることもできる。 There is no particular restriction on the daily usage amount of the pharmaceutical composition for oral administration to animals, and it can be set to a desired amount depending on the type and body weight of the animal to be ingested. Although there are individual differences, the amount of undenatured type II collagen to be ingested per day is 2 to 10 mg, for example, 5 mg for small animals, and 100 to 500 mg for large animals, such as horses weighing about 500 kg. do it. For example, one package contains about 50 to 400 mg, especially about 150 to 250 mg of L-carnitine, and about 2 to 10 mg, especially about 3 to 8 mg of undenatured type II collagen, and the total amount of one package is about 0.2 to 3 g, especially about 0. Approximately 5 to 1.5 g of powder or granule preparations are available for half to one package for small dogs, cats, and rabbits, and one to two packages for medium-sized dogs, and for large dogs weighing approximately 20 kg or more. For large animals such as horses, it is preferable to use about 2 or more sachets, and for large animals such as horses, it is preferable to use 5 to 200 sachets, especially about 20 to 100 sachets, depending on the body weight. For medium-sized animals, a pharmaceutical composition with the same composition but a total amount of 1 to 5 g, especially 1 to 3 g may be used, and for large animals, a pharmaceutical composition with a total amount of 10 to 100 g. It is also possible to do this.
動物用経口投与用製剤組成物におけるＬ－カルニチン：非変性ＩＩ型コラーゲンの含有量比にも、特に制限はない。上記のように、小動物であれば１日当たり５ｍｇ程度の非変性ＩＩ型コラーゲン量でも有効なため、その分Ｌ－カルニチンの含有比率が相対的に高まっても構わない。例えばＬ－カルニチンの含有量：非変性ＩＩ型コラーゲンの含有量の比率を、質量比で１０：１～６０：１程度、中でも２０：１～５０：１程度、特に３０：１～４０：１程度としてもよい。 There is also no particular restriction on the content ratio of L-carnitine:undenatured type II collagen in the pharmaceutical composition for oral administration to animals. As mentioned above, in the case of small animals, an amount of undenatured type II collagen of about 5 mg per day is effective, so the content ratio of L-carnitine may be relatively increased accordingly. For example, the ratio of L-carnitine content to undenatured type II collagen content is about 10:1 to 60:1, especially about 20:1 to 50:1, especially about 30:1 to 40:1. It may be a degree.
具体的には、５～４０質量％、特に１５～２０質量％のＬ－カルニチン、０．１～５質量％、特に０．２～２質量％の非変性ＩＩ型コラーゲン、さらには４０～８０質量％、特に６０～７０質量％の酸味抑制成分を含有する動物用経口投与用製剤組成物とすることもできる。ここで、酸味抑制成分としてはシリカ等のケイ素化合物、さつま芋、りんご、及び／又は黒砂糖の粉体等が好ましい。さつま芋やりんごは食物繊維やビタミン、ミネラル等も含むため、整腸作用や血糖値の調整、疲労回復等の効果も奏し得る。特に、糖度の低いさつま芋を、皮をむいた上で乳酸発酵させた後パウダー化することにより、腸内環境の改善効果を発現することも可能となる。 Specifically, 5-40% by weight, especially 15-20% by weight of L-carnitine, 0.1-5% by weight, especially 0.2-2% by weight of undenatured type II collagen, and even 40-80% by weight. It is also possible to prepare a pharmaceutical composition for oral administration to animals containing 60 to 70% by mass of the sour taste suppressing component. Here, as the sour taste suppressing component, silicon compounds such as silica, sweet potato, apple, and/or brown sugar powder, etc. are preferable. Sweet potatoes and apples also contain dietary fiber, vitamins, and minerals, so they can have effects such as regulating the intestines, regulating blood sugar levels, and relieving fatigue. In particular, by peeling sweet potatoes with a low sugar content, subjecting them to lactic acid fermentation, and then turning them into powder, it is possible to improve the intestinal environment.
動物用経口投与用製剤組成物、特に小型～中型動物用の製剤組成物は、より具体的には、例えば全量１ｇ中に、２００～６００ｍｇ、特に３００～４００ｍｇ程度のサツマイモパウダー、１００～５００ｍｇ、特に２００～４００ｍｇ程度のアップルパウダー、及び２～３０ｍｇ、特に５～１５ｍｇ程度の黒砂糖と、５０～４００ｍｇ程度のＬ－カルニチン及び２～１０ｍｇ程度の非変性ＩＩ型コラーゲンとを含有する組成とすることができる。 Pharmaceutical compositions for oral administration to animals, particularly pharmaceutical compositions for small to medium-sized animals, more specifically include, for example, about 200 to 600 mg, especially about 300 to 400 mg of sweet potato powder, 100 to 500 mg, In particular, the composition should contain about 200 to 400 mg of apple powder, 2 to 30 mg, especially about 5 to 15 mg of brown sugar, about 50 to 400 mg of L-carnitine, and about 2 to 10 mg of undenatured type II collagen. be able to.
以下、実施例を通じて本発明の実施形態をより具体的に開示するが、本発明の技術的範囲はこれら実施例に限定されるものではない。 Hereinafter, embodiments of the present invention will be disclosed more specifically through Examples, but the technical scope of the present invention is not limited to these Examples.
［実施例１］
Ｌ－カルニチンフマル酸塩１３７ｍｇ、鶏軟骨抽出物（ロンザ株式会社製のＵＣ－ＩＩ（登録商標）、非変性ＩＩ型コラーゲンを２５質量％含有）２０ｍｇ、シクロデキストリン（賦形剤）１３７ｍｇ、及びステアリン酸カルシウム（賦形剤）６ｍｇを混合して、人間用経口投与用粉体製剤を作製した。本粉体製剤（３００ｍｇ）中のＬ－カルニチン純分量は８０ｍｇ（２７質量％）、非変性ＩＩ型コラーゲン純分量は５ｍｇ（約２質量％）である。この粉体製剤を、７７ｍｇのゼラチン製外皮に封入して、カプセルとした。
[Example 1]
137 mg of L-carnitine fumarate, 20 mg of chicken cartilage extract (UC-II (registered trademark) manufactured by Lonza Corporation, containing 25% by mass of undenatured type II collagen), 137 mg of cyclodextrin (excipient), and calcium stearate. (Excipient) 6 mg was mixed to prepare a powder preparation for oral administration to humans. The pure amount of L-carnitine in this powder preparation (300 mg) is 80 mg (27% by mass), and the pure amount of undenatured type II collagen is 5 mg (about 2% by mass). This powder formulation was encapsulated in a 77 mg gelatin shell to form a capsule.
得られたカプセルを、関節の痛みがあったり、疲労を感じやすい５０歳以上の人の中から任意に選んだ２４名の被験者に毎日２粒ずつ服用してもらい、関節の痛み低減や疲労回復効果が体感されるか否か試験した。尚、ＵＣ－ＩＩ等の摂取によって副作用が観察されないことは、原料メーカーの試験によって確認されている。その結果、１週間後には被験者の６割強が、２週間後には８割近くが、４週間後には９割の被験者が、疲労感の低減等が体感されたと返答した。本願発明の経口投与用製剤組成物は、人間に対して効果を奏することが判明した。 The resulting capsules were randomly selected from among 24 subjects over the age of 50 who were prone to joint pain and fatigue and were asked to take two capsules each day to reduce joint pain and recover from fatigue. A test was conducted to see if the effect could be felt. Furthermore, it has been confirmed through tests by raw material manufacturers that no side effects are observed when ingesting UC-II or the like. As a result, more than 60% of the subjects responded that they felt a reduction in fatigue after one week, nearly 80% after two weeks, and 90% after four weeks. It has been found that the pharmaceutical composition for oral administration of the present invention is effective for humans.
［実施例２］
Ｌ－カルニチン（ロンザ株式会社製のカルニキング（登録商標）、純度５０～６５質量％）粉末３００ｍｇを、サツマイモパウダー３７０ｍｇ、アップルパウダー３００ｍｇ、及び黒砂糖１０ｍｇの混合物で被覆した。この被覆物と、２０ｍｇの鶏軟骨抽出物（ＵＣ－ＩＩ）とを混合し、造粒して顆粒状の動物用経口投与用製剤を作製した。本顆粒状製剤（１０００ｍｇ）中のＬ－カルニチン純分の量は１５０～１９５ｍｇ（約１５～２０質量％）、非変性ＩＩ型コラーゲン純分量は５ｍｇ（０．５質量％）、Ｌ－カルニチン：非変性ＩＩ型コラーゲンの質量比は約３０：１～４０：１である。
[Example 2]
300 mg of L-carnitine (Carniking® manufactured by Lonza Corporation, purity 50-65% by mass) powder was coated with a mixture of 370 mg of sweet potato powder, 300 mg of apple powder, and 10 mg of brown sugar. This coating was mixed with 20 mg of chicken cartilage extract (UC-II) and granulated to prepare a granular preparation for oral administration to animals. The pure amount of L-carnitine in this granular preparation (1000 mg) is 150 to 195 mg (approximately 15 to 20% by mass), the pure amount of undenatured type II collagen is 5 mg (0.5% by mass), L-carnitine: The mass ratio of undenatured type II collagen is about 30:1 to 40:1.
得られた顆粒状製剤を振りかけた食餌を、スムーズに歩けなくなった、犬２３匹及び猫１５匹に食べさせたところ、いずれも嫌がることなく普通に食べた。尚、顆粒状製剤の１日当たりの使用量は、犬又は猫の体重が２０ｋｇ未満の場合１０００ｍｇ（１包）、２０ｋｇ以上の場合は２０００ｍｇ（２包）とした。摂取を１箇月ほど継続すると、７割以上の犬又は猫で歩行状態が改善し、体型もスリムになった。 When the food sprinkled with the obtained granular preparation was fed to 23 dogs and 15 cats who were unable to walk smoothly, all of them ate normally without any objections. The daily usage amount of the granular preparation was 1000 mg (1 package) if the dog or cat weighed less than 20 kg, and 2000 mg (2 packages) if the dog or cat weighed 20 kg or more. After continuing to take it for about a month, more than 70% of dogs and cats improved their walking condition and became slimmer.
［実施例３］
ＵＣ－ＩＩの配合量を５ｍｇとした以外は、実施例２と同様の方法で顆粒状製剤を調製した。実施例３の顆粒状製剤におけるＬ－カルニチン：非変性ＩＩ型コラーゲンの質量比は、約１２０～１６０：１である。この顆粒状製剤を摂取させたところ、体重２０ｋｇ未満の犬では、実施例２と同様の効果が得られた。但し、体重２０ｋｇ以上の犬では、１箇月後に歩行状態が改善された犬の割合が４割程度に止まった。本発明の経口投与用製剤組成物においては、Ｌ－カルニチン：非変性ＩＩ型コラーゲンの質量比を５：１～６０：１の範囲内とするのが好ましいことが、明らかとなった。
[Example 3]
A granular preparation was prepared in the same manner as in Example 2, except that the amount of UC-II was 5 mg. The mass ratio of L-carnitine to undenatured type II collagen in the granular formulation of Example 3 is about 120 to 160:1. When this granular preparation was ingested, the same effects as in Example 2 were obtained in dogs weighing less than 20 kg. However, among dogs weighing 20 kg or more, the percentage of dogs whose walking condition improved after one month was only around 40%. It has become clear that in the pharmaceutical composition for oral administration of the present invention, the mass ratio of L-carnitine to undenatured type II collagen is preferably within the range of 5:1 to 60:1.
尚、カルニキングの代わりにＬ－カルニチンのフマル酸塩（Ｌ－カルニチン純分１５０ｍｇ）を用い、実施例２と同様の方法で顆粒状製剤を調製し、得られた顆粒状製剤を振りかけた食餌を犬に食べさせたところ、犬が摂取したりしなかったりを繰り返したため、歩行状態等の変化を評価することはできなかった。これは、Ｌ－カルニチンフマル酸塩には酸味があり、この酸味を犬が嫌がったためであることが推定される。このため、飼育動物用には、塩の形でないＬ－カルニチンを配合するのが好ましい点が明らかとなった。 Incidentally, a granular preparation was prepared in the same manner as in Example 2 using L-carnitine fumarate (L-carnitine pure content 150 mg) instead of carniking, and the food sprinkled with the obtained granular preparation was fed. When I fed it to a dog, the dog repeatedly ingested and did not ingest it, so it was not possible to evaluate changes in its walking condition, etc. This is presumably because L-carnitine fumarate has a sour taste, and dogs disliked this sour taste. For this reason, it has become clear that it is preferable to incorporate L-carnitine in a non-salt form for domestic animals.
以上のように、本発明に従いＬ－カルニチンと非変性ＩＩ型コラーゲンとを含有する経口投与用製剤組成物は、人間及び飼育動物の関節ケアや運動機能改善に有用である。特に、Ｌ－カルニチン：非変性ＩＩ型コラーゲンの質量比を５：１～６０：１程度とすることにより、運動機能改善効果をさらに高め、かつ飼育動物が嫌がらずに摂取する経口投与用製剤組成物とすることができる。
As described above, the pharmaceutical composition for oral administration containing L-carnitine and undenatured type II collagen according to the present invention is useful for joint care and motor function improvement of humans and domestic animals. In particular, by setting the mass ratio of L-carnitine to undenatured type II collagen to about 5:1 to 60:1, the formulation for oral administration can further enhance the effect of improving motor function and can be ingested by domestic animals without hesitation. It can be a thing.
Claims (6)
前記Ｌ－カルニチンのカルボン酸塩中のＬ－カルニチンの含有量が、前記粉体製剤組成物に対して、純分で１０～５０質量％であり、
前記非変性ＩＩ型コラーゲンの含有量が、前記粉体製剤組成物に対して、純分で０．２～５質量％であり、
前記非変性ＩＩ型コラーゲンの含有量に対する前記Ｌ－カルニチンの含有量の割合が、５～５０の範囲であり、かつ、
酸味抑制成分を含まない、人間への経口投与用粉体製剤組成物。 A powder preparation composition for oral administration to humans , comprising a carboxylate of L-carnitine and undenatured type II collagen ,
The content of L-carnitine in the carboxylate of L-carnitine is 10 to 50% by mass in pure content with respect to the powder formulation composition,
The content of the undenatured type II collagen is 0.2 to 5% by mass of the pure powder formulation composition,
The ratio of the content of L-carnitine to the content of undenatured type II collagen is in the range of 5 to 50, and
A powder formulation composition for oral administration to humans that does not contain an acid taste suppressing ingredient.
前記Ｌ－カルニチンのカルボン酸塩中のＬ－カルニチンの含有量が、前記液状製剤組成物に対して、純分で５０～６０質量％であり、 The content of L-carnitine in the carboxylate of L-carnitine is 50 to 60% by mass in pure content with respect to the liquid preparation composition,
前記非変性ＩＩ型コラーゲンの含有量が、前記液状製剤組成物に対して、１～１０質量％であり、 The content of the undenatured type II collagen is 1 to 10% by mass with respect to the liquid preparation composition,
前記非変性ＩＩ型コラーゲンの含有量に対する前記Ｌ－カルニチンの含有量の割合が、１０～５０の範囲であり、 The ratio of the L-carnitine content to the non-denatured type II collagen content is in the range of 10 to 50,
前記水の含有量が、前記液状製剤組成物に対して、２０～３０質量％であり、かつ、 The water content is 20 to 30% by mass based on the liquid formulation composition, and
酸味抑制成分を含まない、人間への経口投与用カプセル剤。 Capsules for oral administration to humans that do not contain acidity suppressing ingredients.
前記Ｌ－カルニチン粉体は、粉体化した酸味抑制成分で表面被覆されて複合化された複合粉体として形成され、
前記Ｌ－カルニチンの含有量が、前記粉体製剤組成物に対して、純分で５～４０質量％であり、
前記非変性ＩＩ型コラーゲンの含有量が、前記粉体製剤組成物に対して、純分で０．１～５質量％であり、
前記非変性ＩＩ型コラーゲンの含有量に対する前記Ｌ－カルニチンの含有量の割合が、１０～６０の範囲であり、かつ、
前記酸味抑制成分が、前記粉体製剤組成物に対して４０～８０質量％である、動物への経口投与用粉体製剤組成物。 A powder formulation composition for oral administration to animals, which is a mixture of non-salt-forming L-carnitine powder and undenatured type II collagen powder, comprising:
The L-carnitine powder is formed as a composite powder whose surface is coated with a powdered sour taste suppressing component, and
The content of the L-carnitine is 5 to 40% by mass in pure content with respect to the powder formulation composition,
The content of the undenatured type II collagen is 0.1 to 5% by mass of the pure powder formulation composition,
The ratio of the L-carnitine content to the non-denatured type II collagen content is in the range of 10 to 60, and
A powder formulation composition for oral administration to animals, wherein the sour taste suppressing component is 40 to 80% by mass based on the powder formulation composition.
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Citations (3)
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|---|---|---|---|---|
| JP2006129715A (en) | 2004-11-02 | 2006-05-25 | Morishita Jintan Kk | Sugarcoated capsule and method for producing the same |
| US20110218151A1 (en) | 2010-03-04 | 2011-09-08 | Joar Opheim | Substances for promoting healthy joint function comprising omega-3 polyunsaturated fatty acids or drivatives thereof, undenatured type ii collagen and, optionally, glucosamine sulfate |
| JP2017218409A (en) | 2016-06-07 | 2017-12-14 | 株式会社エバーライフ | Cockscomb extract-containing oral composition and method for improving intake difficulty derived from flavor of cockscomb extract |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006129715A (en) | 2004-11-02 | 2006-05-25 | Morishita Jintan Kk | Sugarcoated capsule and method for producing the same |
| US20110218151A1 (en) | 2010-03-04 | 2011-09-08 | Joar Opheim | Substances for promoting healthy joint function comprising omega-3 polyunsaturated fatty acids or drivatives thereof, undenatured type ii collagen and, optionally, glucosamine sulfate |
| JP2017218409A (en) | 2016-06-07 | 2017-12-14 | 株式会社エバーライフ | Cockscomb extract-containing oral composition and method for improving intake difficulty derived from flavor of cockscomb extract |
Non-Patent Citations (1)
| Title |
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| 取扱商品，wayback machine [online]，2022年09月27日，[2023年9月12日検索], <https://web.archive.org/web/20220927053721/https://walky.life/goods/> |
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