WO2021212995A1 - 抗衰老组合物、包含其的药物和保健品、及其应用 - Google Patents
抗衰老组合物、包含其的药物和保健品、及其应用 Download PDFInfo
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- WO2021212995A1 WO2021212995A1 PCT/CN2021/077542 CN2021077542W WO2021212995A1 WO 2021212995 A1 WO2021212995 A1 WO 2021212995A1 CN 2021077542 W CN2021077542 W CN 2021077542W WO 2021212995 A1 WO2021212995 A1 WO 2021212995A1
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- aging
- aging composition
- adenosylmethionine
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/30—Foods or foodstuffs containing additives; Preparation or treatment thereof containing carbohydrate syrups; containing sugars; containing sugar alcohols, e.g. xylitol; containing starch hydrolysates, e.g. dextrin
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Definitions
- the invention belongs to the field of biomedicine, and specifically relates to anti-aging compositions, medicines and health products containing them, and applications thereof.
- Nicotinamide mononucleotide ( ⁇ -Nicotinamide mononucleotide, NMN) is a substance inherent in the human body.
- NMN is the precursor of intracellular nicotinamide adenine dinucleotide (NAD + ), and its function is embodied by NAD +.
- NAD + also known as Coenzyme I, is a coenzyme for hundreds of redox reactions. Its functions include catalyzing the production of more than 95% of the energy required for life activities and regulating hundreds of metabolic reactions in the human body.
- NAD + is also the key to maintaining seven long-lived proteins, repairing DNA, and maintaining the normal function of the immune system.
- NMN has important physiological functions to human cells. It can be synthesized naturally in cells and can also be derived from a variety of foods, including broccoli, cabbage, cucumber, edamame, avocado, etc.
- NAD + decreases drastically, only a fraction of that when young, which triggers various symptoms of aging in the body, such as memory decline, weakened cardiovascular function, immune imbalance, poor sleep quality, Decreased energy, increased blood sugar, constipation, hair loss, loss of appetite, and degeneration of various neurons.
- scientists have repeatedly confirmed that supplementing with NMN can effectively increase and restore NAD + levels in the body.
- NMN NMN will be converted into the metabolite nicotinamide (NAM) and accumulate in the body, which may induce liver fibrosis or fatty liver.
- NAM nicotinamide
- the present invention provides an anti-aging composition, medicines and health products containing the same, and applications thereof.
- the present invention provides:
- An anti-aging composition characterized in that the active ingredients of the anti-aging composition are nicotinamide mononucleotide and a salt of S-adenosylmethionine, and wherein the nicotinamide mononucleotide
- the molar ratio with the salt of S-adenosylmethionine is 1:(0.2-3.0).
- auxiliary material is selected from one or more of fillers, disintegrants, lubricants, and coating agents.
- the total weight, the amount of the filler is 10%-70% (w/w).
- An anti-aging drug comprising the anti-aging composition described in any one of (1) to (12).
- An anti-aging health product comprising the anti-aging composition described in any one of (1) to (12).
- the present invention has the following advantages and positive effects:
- the present invention provides a new anti-aging combination and its application. It is proposed to simply add a salt of S-adenosylmethionine to NMN and meet the molar ratio of 1:(0.2-3.0), that is, it can be NMN
- the decomposition provides sufficient source of methyl to reduce or solve the accumulation of NAM, and at the same time can provide sufficient anti-aging effects.
- the salt of NMN and S-adenosylmethionine is safe as a medicine or health care product.
- the present invention can also increase the level of longevity protein (Sirt1) at the same time, and can also bring positive effects on insulin resistance and height and body mass index.
- Sirt1 longevity protein
- the present invention proposes to simply add a salt of S-adenosylmethionine to NMN and meet the molar ratio of 1:(0.2-3.0).
- the present invention provides a new anti-aging composition, which is characterized in that the active ingredients of the anti-aging composition are nicotinamide mononucleotide and S-adenosylmethionine salt, and wherein smoke
- the molar ratio of the amide mononucleotide to the salt of S-adenosylmethionine is 1:(0.2-3.0).
- SAMe S-adenosylmethionine
- SAMe has an activated methyl group, which is the main coenzyme involved in the methyl transfer reaction. After losing this activated methyl group, SAMe becomes S-adenosyl-L-homocysteine (SAH).
- SAH S-adenosyl-L-homocysteine
- Most of the SAMe in the human body is mainly produced in the liver, and it participates in more than 40 chemical reactions of anabolic or catabolism. Although its precursor methionine is abundant in many protein diets, SAMe is not sufficient in the diet.
- SAMe can be synthesized from methionine by the liver, methionine supplementation cannot effectively increase the amount of SAMe synthesized by the body.
- SAMe is sold as a nutritional supplement under the name of SAMe, which has the effect of improving mood, maintaining liver and comforting joints.
- NAM uses Nicotinamide N-methyltransferase (NNMT) in the human body to be converted into methyl nicotinamide (MNA) through the methyl transfer reaction of SAMe. Excreted from the body.
- NNMT Nicotinamide N-methyltransferase
- MNA methyl nicotinamide
- MNA can induce an increase in the level of longevity protein (Sirt1) and produce a synergistic effect with NMN.
- MNA also has a positive effect on insulin resistance and body mass index (BMI).
- nicotinamide mononucleotide When the molar ratio of nicotinamide mononucleotide to the salt of S-adenosylmethionine is less than 1:3.0, it is easy to exceed the upper limit of the recommended daily dose of S-adenosylmethionine; when nicotinamide mononucleotide When the molar ratio to the salt of S-adenosylmethionine is greater than 1:0.2, NAM begins to accumulate in the body, which may induce diseases such as non-alcoholic fatty liver, hepatitis, or cirrhosis.
- the amount of the nicotinamide mononucleotide is 5%-20% (w/w) based on the total weight of the anti-aging composition.
- the amount of the salt of S-adenosylmethionine is 9%-65% (w/w), preferably 9%-35% (w/ w) or 18%-65% (w/w).
- the amount of the S-adenosylmethionine p-toluenesulfonic acid sulfate is 9%-35% (w/w) based on the total weight of the anti-aging composition.
- the amount of S-adenosylmethionine 1,4-butanedisulfonate is 18%-65% (w/w)
- the anti-aging composition further includes excipients.
- the auxiliary material can be selected from one or more of fillers, disintegrants, lubricants, and coating agents.
- the filler may be selected from one or more of microcrystalline cellulose, lactose, starch, and mannitol. Based on the total weight of the anti-aging composition, the amount of the filler may be 10%-70% (w/w).
- the disintegrant is selected from one or more of croscarmellose sodium, crospovidone, and sodium starch glycolate. Based on the total weight of the anti-aging composition, the amount of the disintegrant may be 0.5%-5% (w/w).
- the lubricant is selected from one or more of magnesium stearate, micronized silica gel, and talc. Based on the total weight of the anti-aging composition, the amount of the lubricant may be 0.1%-3% (w/w).
- the daily dosage of nicotinamide mononucleotide is preferably 1-5000 mg/day, more preferably 300-3000 mg/day, and more preferably 600-1500 mg/day.
- the anti-aging composition of the present invention may include nicotinamide mononucleotide at a dose of 1-5000 mg/day, or nicotinamide mononucleotide at a dose of 300-3000 mg/day, or a dose of 600-1500 mg/day. Nicotinamide mononucleotide.
- the daily dosage of the salt of S-adenosylmethionine is 1-5000 mg/day, more preferably 400-4000 mg/day, more preferably 800-3200 mg/day.
- the anti-aging composition of the present invention may include a salt of S-adenosylmethionine at a dose of 1-5000 mg/day, or a salt of S-adenosylmethionine at a dose of 400-4000 mg/day, or Contains the salt of S-adenosylmethionine at a dose of 800-3200 mg/day.
- the content of nicotinamide mononucleotide in the single-dose pharmaceutical composition is 100-150 mg, and the content of the salt of S-adenosylmethionine in the single-dose pharmaceutical composition is 30-300 mg, for example, 150 mg.
- the invention also provides the application of the anti-aging composition in the preparation of anti-aging medicines or health care products.
- the present invention also provides an anti-aging medicine, which comprises the anti-aging composition of the present invention.
- the anti-aging drug is in the form of an oral preparation or an injection.
- the oral preparations include solid preparations such as tablets, capsules (such as soft capsules), granules, and powders, and liquid preparations.
- the oral preparations are enteric-coated preparations.
- the dosage form can be prepared from the pharmaceutical composition of the present invention by a method known in the art using known materials.
- the anti-aging drug is a tablet
- the content of nicotinamide mononucleotide in a single-dose tablet is 100-150 mg
- the salt of S-adenosylmethionine is in a single-dose tablet.
- the content in the agent is 30-300 mg, for example 150 mg.
- the invention also provides an anti-aging health care product, which comprises the anti-aging composition of the invention.
- the anti-aging health care product is in the form of an oral preparation; wherein the oral preparation includes solid preparations such as tablets, capsules (such as soft capsules), granules, powders, and liquid preparations; preferably, the oral preparations are Enteric-coated preparations.
- the dosage form can be prepared from the pharmaceutical composition of the present invention by a method known in the art using known materials.
- the anti-aging health care product is a tablet
- the content of nicotinamide mononucleotide in a single-dose tablet is 100-150 mg
- the salt of S-adenosylmethionine in a single-dose is 30-300 mg, for example 150 mg.
- Food-grade ⁇ -nicotinamide mononucleotide (white dry powder; purity>99%): produced by GeneHarbor (Hong Kong) Biotechnologies Ltd;
Abstract
一种抗衰老组合物、包含其的药物和保健品、及其应用，其中的活性成分为烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐，并且二者的摩尔比为1: (0.2-3.0)。
Description
本发明属于生物医药领域，具体而言，涉及抗衰老组合物、包含其的药物和保健品、及其应用。
烟酰胺单核苷酸(β-Nicotinamide mononucleotide，NMN)是人体内固有的物质。在人体中，NMN是细胞内烟酰胺腺嘌呤二核苷酸(Nicotinamide adenine dinucleotide，NAD
+)的前体，其功能通过NAD
+体现。NAD
+又称辅酶Ⅰ，是数百种氧化还原反应的辅酶，功能包括催化产生95％以上生命活动所需的能量，并调控人体数百项代谢反应。而近几年的科学研究更加进一步揭示除了作为几百种酶的辅酶之外，NAD
+还是维持7种长寿蛋白、修复DNA和维持免疫体系正常功能的关键。NMN对人体细胞有重要的生理功能，能在细胞中天然合成，也可以来源于多种食物，包括西兰花、卷心菜、黄瓜、毛豆、鳄梨等。
步入中年后，NAD
+的数量急剧减少，仅为年青时的数分之一，由此触发体内各种衰老的症状，如记忆力衰退、心血管功能弱化、免疫力失调、睡眠质量差、精力下降、血糖增加、便秘、脱发、食欲不振和各种神经元之退化等。科学家反复证实补充NMN可有效地增加和恢复体内NAD
+水平。
然而，NMN经使用后会转化成代谢物烟酰胺(NAM)并于体内积聚，有机会诱发肝纤维化或脂肪肝。
发明内容
为解决上述现有技术中所存在的问题，本发明提供了抗衰老组合物、包含其的药物和保健品、及其应用。
具体而言，本发明提供了：
(1)一种抗衰老组合物，其特征在于，所述抗衰老组合物的活性成分为烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐，并且其中烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐的摩尔比为1:(0.2-3.0)。
(2)根据(1)所述的抗衰老组合物，其中所述S-腺苷甲硫氨酸的盐选自S-腺苷甲硫氨酸对甲苯磺酸硫酸盐、S-腺苷甲硫氨酸1,4-丁二磺酸盐中的一种或多种。
(3)根据(1)所述的抗衰老组合物，其中基于所述抗衰老组合物的总重量，所述烟酰胺单核苷酸的量为5％-20％(w/w)。
(4)根据(1)所述的抗衰老组合物，其中基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸的盐的量为9％-65％(w/w)。
(5)根据(2)所述的抗衰老组合物，其中基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸对甲苯磺酸硫酸盐的量为9％-35％(w/w)，所述S-腺苷甲硫氨酸1,4-丁二磺酸盐的量为18％-65％(w/w)。
(6)根据(1)所述的抗衰老组合物，其中所述抗衰老组合物还包含辅料。
(7)根据(6)所述的抗衰老组合物，其中所述辅料选自填充剂、崩解剂、润滑剂、包衣剂中的一种或多种。
(8)根据(7)所述的抗衰老组合物，其中所述填充剂选自微晶纤维素、乳糖、淀粉、甘露醇中的一种或多种，并且基于所述抗衰老组合物的总重量，所述填充剂的量为10％-70％(w/w)。
(9)根据(7)所述的抗衰老组合物，其中所述崩解剂选自交联羧甲基纤维素钠、交联聚维酮、羧甲淀粉钠中的一种或多种，并且基于所述抗衰老组合物的总重量，所述崩解剂的量为0.5％-5％(w/w)。
(10)根据(7)所述的抗衰老组合物，其中所述润滑剂选自硬脂酸镁、微粉硅胶、滑石粉中的一种或多种，并且基于所述抗衰老组合物的总重量，所述润滑剂的量为0.1％-3％(w/w)。
(11)根据(1)所述的抗衰老组合物，其中所述抗衰老组合物包含1-5000mg/天剂量的所述烟酰胺单核苷酸。
(12)根据(1)所述的抗衰老组合物，其中所述抗衰老组合物包含1-5000mg/天剂量的所述S-腺苷甲硫氨酸的盐。
(13)根据(1)-(12)中任一项所述的抗衰老组合物在制备抗衰老药物或保健品中的应用。
(14)一种抗衰老药物，其包含(1)-(12)中任一项所述的抗衰老组合物。
(15)根据(14)所述的抗衰老药物，其中该抗衰老药物为口服制剂或注射剂的形式；其中所述口服制剂包括片剂、胶囊、颗粒剂、粉剂和液体制剂；优选地，所述口服制剂为肠溶制剂。
(16)一种抗衰老保健品，其包含(1)-(12)中任一项所述的抗衰老组合物。
(17)根据(16)所述的抗衰老保健品，其中该抗衰老保健品为口服制剂的形式；其中所述口服制剂包括片剂、胶囊、颗粒剂、粉剂和液体制剂；优选地，所述口服制剂为肠溶制剂。
本发明与现有技术相比具有以下优点和积极效果：
本发明提供了一种新的抗衰老组合及其应用，提出简单地在NMN中加入S-腺苷甲硫氨酸的盐，并且满足1:(0.2-3.0)的摩尔比，即能够为NMN的分解提供足够的甲基来源，从而减轻或解决NAM之积聚，同时能够提供足够的抗衰老效果。
NMN和S-腺苷甲硫氨酸的盐作为药物或保健品的安全性良好。
本发明还能同时提高长寿蛋白(Sirt1)的水平，亦能为胰岛素抵抗和身高体重指数带来正面影响。
以下通过具体实施方式的描述对本发明作进一步说明，但这并非是对本发明的限制，本领域技术人员根据本发明的基本思想，可以做出各种修改或改进，但是只要不脱离本发明的基本思想，均在本发明的范围之内。
为了解决NMN所导致的NAM在体内积聚的问题，本发明提出 简单地在NMN中加入S-腺苷甲硫氨酸的盐，并满足1:(0.2-3.0)的摩尔比。
因此，本发明提供了一种新的抗衰老组合物，其特征在于，所述抗衰老组合物的活性成分为烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐，并且其中烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐的摩尔比为1:(0.2-3.0)。
S-腺苷甲硫氨酸的盐在人体内以S-腺苷甲硫氨酸(S-adenosylmethionine，SAMe)形式存在。SAMe带有一个活化了的甲基，是参与甲基转移反应的主要辅酶，在失去该活化甲基后，SAMe变为S-腺苷-L-高半胱氨酸(SAH)。人体内大部分的SAMe主要在肝脏生成，其参与超过40种以上合成代谢或分解代谢的化学反应。尽管其前体甲硫氨酸(methionine)在许多蛋白质饮食中含量丰富，但SAMe在饮食中并不充足。SAMe虽然可由肝脏从甲硫氨酸合成而来，但补充甲硫氨酸并不能有效增加身体合成SAMe的量。研究发现，定期食用SAMe可抗抑郁，肝脏疾病，和关节炎/关节疼痛。在美国市场上用SAMe的名字按营养补品销售，有改善情绪、保养肝脏和舒适关节的功效。随着营养补充品在大众消费中的增长，用于治疗目的的SAMe亦有增加。
本发明不受理论的束缚，但认为NAM利用人体内烟酰胺N-甲基转移酶(Nicotinamide N-methyltransferase，NNMT)，通过SAMe的甲基转移反应，被转化为甲基烟酰胺(MNA)从而排出体外。
另外，MNA能诱发长寿蛋白(Sirt1)水平的增加，和NMN产生协同效应。此外，MNA对胰岛素抵抗(insulin resistance)和身高体重指数(BMI)也有正面影响。
当烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐的摩尔比小于1:3.0时，容易超出S-腺苷甲硫氨酸每日建议剂量上限；当烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐的摩尔比大于1:0.2时，NAM在身体中开始积聚，可能诱发非酒精性脂肪肝、肝炎或肝硬化等疾病。
优选地，基于所述抗衰老组合物的总重量，所述烟酰胺单核苷酸的量为5％-20％(w/w)。
优选地，基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸的盐的量为9％-65％(w/w)，优选为9％-35％(w/w)或18％-65％(w/w)。
优选地，基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸对甲苯磺酸硫酸盐的量为9％-35％(w/w)。
优选地，基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸1,4-丁二磺酸盐的量为18％-65％(w/w)
在本发明的一些实施方案中，所述抗衰老组合物还包含辅料。辅料可以选自填充剂、崩解剂、润滑剂、包衣剂中的一种或多种。
所述填充剂可以选自微晶纤维素、乳糖、淀粉、甘露醇中的一种或多种。基于所述抗衰老组合物的总重量，所述填充剂的量可以为10％-70％(w/w)。
所述崩解剂选自交联羧甲基纤维素钠、交联聚维酮、羧甲淀粉钠中的一种或多种。基于所述抗衰老组合物的总重量，所述崩解剂的量可以为0.5％-5％(w/w)。
所述润滑剂选自硬脂酸镁、微粉硅胶、滑石粉中的一种或多种。基于所述抗衰老组合物的总重量，所述润滑剂的量可以为0.1％-3％(w/w)。
烟酰胺单核苷酸的每天使用剂量优选为1-5000mg/天，更优选300-3000mg/天，更优选600-1500mg/天。
因此，本发明的抗衰老组合物可以包含1-5000mg/天剂量的烟酰胺单核苷酸，或者包含300-3000mg/天剂量的烟酰胺单核苷酸，或者包含600-1500mg/天剂量的烟酰胺单核苷酸。
S-腺苷甲硫氨酸的盐的每天使用剂量为1-5000mg/天，更优选400-4000mg/天，更优选800-3200mg/天。
因此，本发明的抗衰老组合物可以包含1-5000mg/天剂量的S-腺苷甲硫氨酸的盐，或者包含400-4000mg/天剂量的S-腺苷甲硫氨酸的盐，或者包含800-3200mg/天剂量的S-腺苷甲硫氨酸的盐。
优选地，烟酰胺单核苷酸在单剂药物组合物中的含量为100-150mg，S-腺苷甲硫氨酸的盐在单剂药物组合物中的含量为30-300mg，例如150mg。
本发明还提供了所述的抗衰老组合物在制备抗衰老药物或保健品中的应用。
本发明还提供了一种抗衰老药物，其包含本发明所述的抗衰老组合物。优选地，该抗衰老药物为口服制剂或注射剂的形式。所述口服制剂包括片剂、胶囊(如软胶囊)、颗粒剂、粉剂等固体制剂、和液体制剂，优选地，所述口服制剂为肠溶制剂。
在本发明中，所述剂型可以通过本领域已知的方法采用已知的材料由本发明所述的药物组合物进行制备。
在本发明优选的实施方案中，抗衰老药物为片剂，并且烟酰胺单核苷酸在单剂片剂中的含量为100-150mg，S-腺苷甲硫氨酸的盐在单剂片剂中的含量为30-300mg，例如150mg。
本发明还提供了一种抗衰老保健品，其包含本发明所述的抗衰老组合物。优选地，该抗衰老保健品为口服制剂的形式；其中所述口服制剂包括片剂、胶囊(如软胶囊)、颗粒剂、粉剂等固体制剂、和液体制剂；优选地，所述口服制剂为肠溶制剂。
在本发明中，所述剂型可以通过本领域已知的方法采用已知的材料由本发明所述的药物组合物进行制备。
在本发明优选的实施方案中，抗衰老保健品为片剂，并且烟酰胺单核苷酸在单剂片剂中的含量为100-150mg，S-腺苷甲硫氨酸的盐在单剂片剂中的含量为30-300mg，例如150mg。
以下通过实施例的方式进一步解释或说明本发明内容，但这些实施例不应被理解为对本发明保护范围的限制。
实施例
以下除非特别说明，否则以下例子均使用本领域的常规流程、操作、材料和条件进行，或按照制造商的建议进行。
实施例中所用材料和设备的描述如下
食品级β-烟酰胺单核苷酸(白色干粉末；纯度>99％)：产自基因港(香港)生物科技有限公司(GeneHarbor(Hong Kong) Biotechnologies Ltd)；
食品级S-腺苷甲硫氨酸对甲苯磺酸硫酸盐：白色干粉末；纯度>99％)：产自基因港(香港)生物科技有限公司(GeneHarbor(Hong Kong)Biotechnologies Ltd)。
食品级S-腺苷甲硫氨酸1,4-丁二磺酸盐：白色干粉末；纯度>98％)：产自基因港(香港)生物科技有限公司(GeneHarbor(Hong Kong)Biotechnologies Ltd)。
实施例1
(1)称取：16g食品级NMN；7.6g食品级S-腺苷甲硫氨酸对甲苯磺酸硫酸盐；15g D-甘露醇；30g淀粉；10g微晶纤维素；3.5g交联聚维酮；0.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀，压片。
实施例2
(1)称取：7g食品级NMN；8.1g食品级S-腺苷甲硫氨酸对甲苯磺酸硫酸盐；12g乳糖；10g淀粉；2g羧甲淀粉钠；0.8g微晶纤维素；0.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀，压片。
实施例3
(1)称取：7g食品级NMN；8.1g食品级S-腺苷甲硫氨酸对甲苯磺酸硫酸盐；12g乳糖；10g淀粉；1g羧甲淀粉钠；0.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀，压片。
实施例4
(1)称取：3.3g食品级NMN；22.5g食品级S-腺苷甲硫氨酸对 甲苯磺酸硫酸盐；13g D-甘露醇；20g淀粉；2.5g交联聚维酮；0.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀，压片。
实施例5
(1)称取：5g食品级NMN；17.2g食品级S-腺苷甲硫氨酸对甲苯磺酸硫酸盐；15g D-甘露醇；30g淀粉；10g微晶纤维素；3.5g交联聚维酮；1.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀，压片。
实施例6
(1)称取：7g食品级NMN；8.1g食品级S-腺苷甲硫氨酸对甲苯磺酸硫酸盐；12g乳糖；10g淀粉；2g羧甲淀粉钠；0.8g微晶纤维素；0.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀；
(3)用2.5克隔离包衣(2.4g羟丙甲纤维素和0.1g聚乙二醇)和7.3克肠溶包衣(6.2g尤特奇和1.1g滑石粉)进行包衣，得到胶囊。
实施例7
(1)称取：19g食品级NMN；17g食品级S-腺苷甲硫氨酸1,4-丁二磺酸盐；8g D-甘露醇；30g淀粉；15g微晶纤维素；3.5g交联聚维酮；1.5g微粉硅胶；
(2)在不锈钢容器中搅拌均匀，再加入0.5g硬脂酸镁，混匀，压片。
Claims (17)
- 一种抗衰老组合物，其特征在于，所述抗衰老组合物的活性成分为烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐，并且其中烟酰胺单核苷酸和S-腺苷甲硫氨酸的盐的摩尔比为1:(0.2-3.0)。
- 根据权利要求1所述的抗衰老组合物，其中所述S-腺苷甲硫氨酸的盐选自S-腺苷甲硫氨酸对甲苯磺酸硫酸盐、S-腺苷甲硫氨酸1,4-丁二磺酸盐中的一种或多种。
- 根据权利要求1所述的抗衰老组合物，其中基于所述抗衰老组合物的总重量，所述烟酰胺单核苷酸的量为5％-20％(w/w)。
- 根据权利要求1所述的抗衰老组合物，其中基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸的盐的量为9％-65％(w/w)。
- 根据权利要求2所述的抗衰老组合物，其中基于所述抗衰老组合物的总重量，所述S-腺苷甲硫氨酸对甲苯磺酸硫酸盐的量为9％-35％(w/w)，所述S-腺苷甲硫氨酸1,4-丁二磺酸盐的量为18％-65％(w/w)。
- 根据权利要求1所述的抗衰老组合物，其中所述抗衰老组合物还包含辅料。
- 根据权利要求6所述的抗衰老组合物，其中所述辅料选自填充剂、崩解剂、润滑剂、包衣剂中的一种或多种。
- 根据权利要求7所述的抗衰老组合物，其中所述填充剂选自微晶纤维素、乳糖、淀粉、甘露醇中的一种或多种，并且基于所述抗衰老组合物的总重量，所述填充剂的量为10％-70％(w/w)。
- 根据权利要求7所述的抗衰老组合物，其中所述崩解剂选自交联羧甲基纤维素钠、交联聚维酮、羧甲淀粉钠中的一种或多种，并且基于所述抗衰老组合物的总重量，所述崩解剂的量为0.5％-5％(w/w)。
- 根据权利要求7所述的抗衰老组合物，其中所述润滑剂选自硬脂酸镁、微粉硅胶、滑石粉中的一种或多种，并且基于所述抗衰老组合物的总重量，所述润滑剂的量为0.1％-3％(w/w)。
- 根据权利要求1所述的抗衰老组合物，其中所述抗衰老组合物包含1-5000mg/天剂量的所述烟酰胺单核苷酸。
- 根据权利要求1所述的抗衰老组合物，其中所述抗衰老组合物包含1-5000mg/天剂量的所述S-腺苷甲硫氨酸的盐。
- 根据权利要求1-12中任一项所述的抗衰老组合物在制备抗衰老药物或保健品中的应用。
- 一种抗衰老药物，其包含权利要求1-12中任一项所述的抗衰老组合物。
- 根据权利要求14所述的抗衰老药物，其中该抗衰老药物为口服制剂或注射剂的形式；其中所述口服制剂包括片剂、胶囊、颗粒剂、粉剂和液体制剂；优选地，所述口服制剂为肠溶制剂。
- 一种抗衰老保健品，其包含权利要求1-12中任一项所述的抗衰老组合物。
- 根据权利要求16所述的抗衰老保健品，其中该抗衰老保健品为口服制剂的形式；其中所述口服制剂包括片剂、胶囊、颗粒剂、 粉剂和液体制剂；优选地，所述口服制剂为肠溶制剂。
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| TAO MIN, GAN XIN: "Current Research and Application Expectation of S-Adenosyl-L-Methionine", AMINO ACIDS & BIOTIC RESOURCES, vol. 27, no. 3, 30 September 2005 (2005-09-30), CN, pages 49 - 51, XP055859839, ISSN: 1006-8376 * |
| ZHAO JUAN;ZHANG JIAN;YU ZHI-JIAN;CAO YONG-QIANG;CHEN CHAO;YANG ZHEN-NA: "Progress on research and application of nicotinamide mononucleotides", FOOD SCIENCE AND TECHNOLOGY, vol. 43, no. 04, 20 April 2018 (2018-04-20), CN, pages 257 - 262, XP055859833, ISSN: 1005-9989, DOI: 10.13684/j.cnki.spkj.2018.04.047 * |
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