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CN-117143164-B - Adenosine eutectic, preparation method and application thereof

CN117143164BCN 117143164 BCN117143164 BCN 117143164BCN-117143164-B

Abstract

The invention provides an adenosine eutectic, a preparation method and application thereof, and belongs to the technical field of biological medicines. The adenosine eutectic is formed by adenosine and ectoine or nicotinamide according to the molar ratio of 1:0.2-16.9, and the problem of poor bioavailability of the adenosine in the prior art is solved. Compared with adenosine, the adenosine eutectic provided by the invention has significantly higher solubility, can be used as a medicament to improve the blood concentration in organisms so as to exert more effective treatment effect, can be used as a skin care product or a cosmetic to avoid the influence of horny layer hydrophobicity so as to improve the skin permeability of the product, can be used as a hair-growing product to improve the dissolving dosage of active ingredients in the product, and can better exert the hair-growing effect, thus having wide application potential.

Inventors

  • FAN YUMEI
  • TENG CHANG
  • XIE YU
  • LI JINHUA
  • SUN PEIWEN

Assignees

  • 时垠(上海)生物科技有限公司

Dates

Publication Date
20260505
Application Date
20230831

Claims (8)

  1. 1. An adenosine eutectic is characterized in that the adenosine eutectic is formed by adenosine and a eutectic forming agent according to a molar ratio of 1:0.2-16.9; the eutectic forming agent is ectoine or nicotinamide; When the co-crystal former is ectoin, the adenosine co-crystal is an adenosine ectoin co-crystal; The PXRD pattern of the adenosin-ectoin co-crystal has characteristic peaks at least at 2 θ = 18.99, 23.02, 23.83, 25.56 and 39.93; when the co-crystal former is nicotinamide, the adenosine co-crystal is an adenosine nicotinamide co-crystal; The PXRD pattern of the co-crystal of adenylamine has characteristic peaks at least at 2 θ = 22.09, 22.90, 23.68 and 28.46; the preparation method of the adenosine eutectic comprises the following steps: Mixing adenosine and a eutectic forming agent, and mechanically grinding to obtain an adenosine eutectic; The molar ratio of the adenosine to the eutectic forming agent is 1:0.2-16.9.
  2. 2. The adenosine co-crystal of claim 1, wherein the adenosine ectoin co-crystal is characterized by a PXRD pattern as shown in figure 2.
  3. 3. The adenosine co-crystal of claim 1, wherein the adenosine nicotinamide co-crystal is characterized by a PXRD pattern as shown in figure 4.
  4. 4. A method for producing an adenosine co-crystal according to any one of claims 1 to 3, comprising the steps of: Mixing adenosine and a eutectic forming agent, and mechanically grinding to obtain an adenosine eutectic; the molar ratio of the adenosine to the eutectic forming agent is 1:0.2-16.9; The co-crystal former is ectoin or nicotinamide.
  5. 5. The method of producing an adenosine eutectic according to claim 4, wherein the molar ratio of the adenosine to the eutectic forming agent is 1:0.8 to 2.
  6. 6. The method for producing an adenosine eutectic according to claim 4, wherein the mechanical grinding time is 10min or longer.
  7. 7. Use of an adenosine co-crystal according to any one of claims 1 to 3 or obtained by the preparation method according to any one of claims 4 to 6 in the preparation of an analgesic, anti-inflammatory, anti-arrhythmic, antihypertensive or wound repair promoting drug.
  8. 8. Use of the adenosine co-crystal according to any one of claims 1 to 3 or the adenosine co-crystal obtained by the preparation method according to any one of claims 4 to 6 for preparing a moisturizing cosmetic, an anti-aging cosmetic, an anti-oxidation product, an anti-wrinkle cosmetic, a repair cosmetic or a hair-growing product.

Description

Adenosine eutectic, preparation method and application thereof Technical Field The invention relates to the technical field of biological medicine, in particular to an adenosine eutectic, a preparation method and application thereof. Background Adenosine, also known as adenine nucleoside, is a compound formed by connecting N-9 of adenine and C-1 of D-ribose through beta glycosidic bond, and is a water-soluble small molecule. Adenosine has various pharmacological activities including analgesia, anti-inflammation, antiarrhythmic, antihypertensive, wound repair promotion, immunity improvement, etc., and can exert various effects in cosmetics and daily chemical products, such as promotion of collagen production by human dermal fibroblasts, improvement of skin elasticity, reduction of periocular and intereyebrow wrinkles, moisturizing, repair, and stimulation of hair growth, etc. However, the short half-life and duration of action of adenosine in vivo, the hydrophobic nature of the stratum corneum results in relatively poor permeability of hydrophilic adenosine, and low solubility of adenosine in water (less than 1% at room temperature), all of which limit the effectiveness of adenosine. If the problem of adenosine solubility can be solved, the anti-aging effect of the product can be effectively improved. To overcome the above problems, there is a great deal of attention to the selection of suitable formulations and modes of administration to improve the bioavailability of adenosine. In the prior art, a face cream using an adenosine-carrying microneedle has been disclosed which is superior to a face cream directly comprising adenosine as a component in improving skin elasticity, dermis density and wrinkles, and is also capable of reducing the dosage of adenosine. However, during daily skin care, the presence of microneedles affects consumer use and does not promote the solubility of adenosine in water/ethanol. Chinese patent CN115337283a discloses a nano-encapsulation of adenosine encapsulated with molecular motor vesicles, a method for preparing the same, a composition and use of the composition. According to the technical scheme, the molecular motor vesicle is used for processing the adenosine preparation into the nano-encapsulation object, so that the bioavailability of the adenosine and the use convenience of the adenosine are effectively improved, but the solubility of the adenosine in water/ethanol is not improved, the preparation process is complex, the cost is high, and the preparation method is not suitable for industrial application. Disclosure of Invention The invention aims to provide an adenosine eutectic, a preparation method and application thereof, so as to solve the problem of poor bioavailability of adenosine in the prior art. In order to achieve the above object, the present invention provides the following technical solutions: The invention provides an adenosine eutectic, which is formed by adenosine and a eutectic forming agent according to the molar ratio of 1:0.2-16.9; the co-crystal former is ectoine or nicotinamide. Preferably, the co-crystal former is ectoin, and the adenosine co-crystal is ectoin co-crystal; The PXRD pattern of the adenosin-ectoin co-crystal has characteristic peaks at least at 2 θ = 18.99, 23.02, 23.83, 25.56 and 39.93. Preferably, the adenosin-ectoin co-crystal is characterized by a PXRD pattern as shown in figure 2. Preferably, the co-crystal former is nicotinamide and the adenosine co-crystal is an adenosine nicotinamide co-crystal; the PXRD pattern of the co-crystal of adenylamine has characteristic peaks at least at 2 θ = 22.09, 22.90, 23.68 and 28.46. Preferably, the adenylamide co-crystal is characterized by a PXRD pattern as shown in figure 4. The invention also provides a preparation method of the adenosine eutectic, which comprises the following steps: Mixing adenosine and a eutectic forming agent, and mechanically grinding to obtain an adenosine eutectic; the molar ratio of the adenosine to the eutectic forming agent is 1:0.2-16.9; The co-crystal former is ectoin or nicotinamide. Preferably, the molar ratio of the adenosine to the eutectic forming agent is 1:0.8-2. Preferably, the mechanical grinding time is 10min or more. The invention also provides the application of the adenosine eutectic or the adenosine eutectic obtained by the preparation method in preparing analgesic drugs, anti-inflammatory drugs, antiarrhythmic drugs, antihypertensive drugs and drugs for promoting wound repair. The invention also provides application of the adenosine eutectic or the adenosine eutectic obtained by the preparation method in preparing moisturizing cosmetics, anti-aging cosmetics, antioxidant products, anti-wrinkle cosmetics, repairing cosmetics or hair-growing products. The invention has the beneficial effects that: Compared with adenosine, the adenosine eutectic provided by the invention has significantly higher solubility, can be used as a medicament to improve the