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CN-116212034-B - Sustained release preparation of beta-hydroxybutyric acid or salt thereof

CN116212034BCN 116212034 BCN116212034 BCN 116212034BCN-116212034-B

Abstract

The invention provides a sustained release preparation of beta-hydroxybutyric acid or a salt thereof, which comprises the following components, by weight, 40-50% of beta-hydroxybutyric acid or a salt thereof, 40-60% of a sustained release skeleton matrix material and 1-3% of auxiliary materials. The product of the invention has excellent water dispersion performance, can realize the slow release of beta-hydroxybutyric acid or salt, can keep stable and effective blood concentration for a long time in vivo, and has very important significance for the practical application of the beta-hydroxybutyric acid and the salt.

Inventors

  • TANG JUN
  • WANG WEI
  • LIAO QILIN

Assignees

  • 南京纽邦生物科技有限公司

Dates

Publication Date
20260508
Application Date
20221207

Claims (5)

  1. 1. A slow release preparation of beta-hydroxybutyric acid or a salt thereof is characterized by comprising, by weight, 40-50% of beta-hydroxybutyric acid or a salt thereof, 40-60% of a slow release skeleton matrix material and 1-3% of an auxiliary material, wherein the slow release skeleton matrix material comprises an erodable skeleton material, the erodable skeleton material is any one or a mixture of two of hydrogenated vegetable oil and stearic acid, the slow release skeleton material further comprises one or a plurality of hydrophilic gel skeleton materials and water-insoluble skeleton materials, the hydrophilic gel skeleton material is any one or a mixture of more than two of hydroxypropyl methyl cellulose, sodium alginate, inulin, konjac glucomannan, carrageenan, locust bean gum and zein, and the water-insoluble skeleton material is any one or a mixture of more than two of ethyl cellulose, methyl cellulose and zein.
  2. 2. The sustained-release preparation according to claim 1, wherein the β -hydroxybutyrate or a salt thereof is selected from the group consisting of β -hydroxybutyrate, sodium β -hydroxybutyrate, potassium β -hydroxybutyrate, calcium β -hydroxybutyrate and magnesium β -hydroxybutyrate.
  3. 3. The sustained release preparation of claim 1, wherein the auxiliary material comprises an adhesive material or a suspending material.
  4. 4. The sustained-release preparation according to claim 3, wherein the binding material is one or a mixture of two or more of guar gum, gum arabic and pectin, and the suspending material is one or a mixture of two or more of xanthan gum, guar gum, pectin and agar.
  5. 5. A method of preparing a sustained release formulation as claimed in any one of claims 1 to 4 comprising wet granulation, hot melt granulation or dry granulation.

Description

Sustained release preparation of beta-hydroxybutyric acid or salt thereof Technical Field The invention belongs to the field of dietary supplements, and particularly relates to a sustained release preparation of beta-hydroxybutyric acid or a salt thereof. Background Beta-hydroxybutyrate (beta-hydroxybutyrate), also known as 3-hydroxybutyrate, is a hydroxy acid of the formula CH 3CH(OH)CH2CO2 H. Beta-hydroxybutyric acid is chiral and has two enantiomers, D-3-hydroxybutyric acid and L-3-hydroxybutyric acid. The compound plays an important role in the physiological response of hypoglycemia in hunger. Ketogenic diet (ketogenic-diet, KD for short) is a high fat, low carbohydrate, protein and other nutrient-suitable formula diet that produces ketone bodies by biological metabolism in humans. It is used for treating epilepsy initially, and has obvious effects of reducing weight (ketone body has appetite suppressing effect) and improving athletic performance. In addition to the fact that the body itself produces ketone bodies by changing the structure of food, there is a more direct way to ingest ketone body material directly, and the ketone ingested from outside the body is an exogenous ketone that replaces carbohydrates to power muscles and the brain. Common exogenous ketone forms are, in addition to β -hydroxybutyrate, also the salt forms thereof such as sodium, magnesium, calcium and potassium β -hydroxybutyrate. However, exogenous ketones are easily metabolized by the body, and the ketone bodies in the human body return to the original basal state after perhaps 1 hour at the very least. The common application forms of the beta-hydroxybutyric acid and the salt thereof in the market at present are powder and capsules, the existing commercial dosage forms only maintain the nutritional blood ketone concentration (0.5-3.0 mmol/L) for 30-40 min once, the blood ketone concentration in the body is required to be maintained by taking more than 2-3 times per day, and meanwhile, the preparation products are easy to absorb moisture and harden in the production, preparation, storage, transportation and use processes. Therefore, development of a slow release preparation technology and a product of the beta-hydroxybutyric acid and the salt thereof is needed to solve the problems of the application of the beta-hydroxybutyric acid and the salt preparation product thereof, and the dietary supplement product has very broad market prospect. Disclosure of Invention In order to solve the problems, the invention provides a sustained-release preparation containing beta-hydroxybutyric acid or salt thereof, which can effectively wrap the beta-hydroxybutyric acid or salt, can slowly and continuously release the beta-hydroxybutyric acid and salt thereof for human body to absorb within 0-5 h after being taken, has simple preparation process, stable dispersion in water, good sustained-release effect and can well improve the defect that the beta-hydroxybutyric acid and salt thereof can be metabolized rapidly after being taken orally. In a first aspect, the invention provides a sustained release preparation of beta-hydroxybutyric acid or a salt thereof, which comprises the following components, by weight, 40-50% of beta-hydroxybutyric acid or a salt thereof, 40-60% of a sustained release skeleton matrix material, and 1-3% of auxiliary materials. In some embodiments, the beta-hydroxybutyric acid or salt thereof is selected from the group consisting of beta-hydroxybutyric acid, sodium beta-hydroxybutyrate, potassium beta-hydroxybutyrate, calcium beta-hydroxybutyrate, and magnesium beta-hydroxybutyrate in any one or more of any combination of proportions. In some embodiments, the slow release matrix material is selected from one or more of a hydrophilic gel matrix material, an erodible matrix material, a water insoluble matrix material. In some embodiments, the hydrophilic gel matrix material is any one or a mixture of two or more of hydroxypropyl methylcellulose, sodium alginate, inulin, konjac glucomannan, carrageenan, locust bean gum and tragacanth in any proportion. In some embodiments, the erodable backbone material is any one or a mixture of two or more of hydrogenated vegetable oil, stearic acid, beeswax, carnauba wax, and glyceryl behenate in any proportion. In some embodiments, the water insoluble matrix material is any one or a mixture of two or more of ethylcellulose, methylcellulose and zein in any proportion. In some embodiments, the adjunct comprises a binding material or a suspending material. In some embodiments, the binding material is any one or a mixture of more than two of guar gum, acacia and pectin in any proportion, and the suspending material is any one or a mixture of more than two of xanthan gum, guar gum, pectin and agar in any proportion. In some embodiments, the sustained release formulation may be prepared by wet granulation, hot melt granulation, or dry granulation. In some embodiments, the sustained release formu