CN109985008A - A kind of astaxanthin solid self-microemulsion and preparation method thereof - Google Patents

Abstract

The invention relates to an astaxanthin solid self-microemulsion and a preparation method thereof, wherein astaxanthin is loaded on a carrier, astaxanthin, grease, an emulsifier, an auxiliary emulsifier and a solid adsorbent are physically mixed and adsorbed, and the astaxanthin solid self-microemulsion is prepared at normal temperature.

Description

A kind of astaxanthin solid self-microemulsion and preparation method thereof

technical field

The invention relates to an astaxanthin solid self-microemulsion and a preparation method thereof, belonging to the technical field of carrier systems in the preparation technology of functional food.

Background technique

Astaxanthin is a non-vitamin A source of fat-soluble keto-carotenoid. It exists in free and esterified forms. The special conjugated double bonds and hydroxyl groups in its molecular structure make it comparable to vitamin E and β- Carotene has stronger antioxidant activity, it is by far the strongest natural antioxidant in nature. Studies have shown that astaxanthin has a variety of physiological activities, such as slowing down aging, anti-tumor, preventing cardiovascular and cerebrovascular diseases, treating diabetes, anti-inflammatory, and improving motor function. Astaxanthin can effectively remove free radicals in the body, at the same time promote the production of antibodies and improve animal immunity. The pharmaceutical industry has considerable practical value and application prospects.

Astaxanthin is the only carotenoid found so far that can penetrate the blood-brain and blood-retina barriers, and can have a positive impact on the central nervous system and brain function. Therefore, if astaxanthin is added to food as a dietary functional factor, it will have practical significance for improving human health. However, astaxanthin itself has poor photostability and low bioavailability, which limit its application in the fields of health care products and medicine.

Lipid drug delivery systems entered the field of pharmacy in 1981 as simple oil solutions. Subsequently, most products on the market of lipid preparation drug-carrying systems are self-emulsifying preparations. Self-emulsifying drug-carrying systems can be used as an effective means to improve the bioavailability of poorly soluble drugs. The importance of quality in enhancing oral absorption of lipophilic drugs. However, there are application bottlenecks in the market of lipid preparations, which have a single dosage form and a narrow application range.

In order to make up for the application defects faced by lipid formulations, solid-state-lipid-based drug delivery systems (s-LBDDS) have attracted the research interest of researchers in recent years. The preparation process of solid lipid preparations is as follows: using drying technology to adsorb liquid lipid preparations into chemically stable solid carriers, so as to prepare samples of solid dosage forms (such as loose powders, granules and pellets, etc.). The selection of solid formulations should focus on their excellent lipid adsorption capacity, good water solubility and solid properties.

The solid lipid preparation drug delivery system combines the dual advantages of lipid preparation formulations and solid dosage forms: 1) The volume of the sample is reduced (conventional emulsion or suspension formulations contain at least 50% moisture, and the sample volume after solidification is at least 50%). The volume may only be the size of a tablet or capsule); 2) The oral dosage can be accurately determined; 3) Compared with the liquid dosage form, the solid dosage form is more convenient for the patient's oral treatment process; 4) The solid lipid formulation does not contain or contains A small amount of water, small size, high physical and chemical stability for long-term storage, easy to transport and store for a long time.

SUMMARY OF THE INVENTION

Aiming at the deficiencies in the prior art, the present invention provides an astaxanthin solid self-microemulsion and a preparation method thereof, and solves the disadvantages of the prior art such as poor solubility, low loading and low oral bioavailability of astaxanthin. and deficiencies.

For achieving the above object, the technical scheme adopted in the present invention is as follows:

An astaxanthin solid self-microemulsion is composed of the following components by mass percentage:

Astaxanthin 1-5%

Grease 10-20%

Emulsifier 20-30%

Co-emulsifier 10-20%

Solid sorbent 10-50%.

As an improvement of the present invention, the oil is any one or a combination of coconut oil, corn oil, caprylic triglyceride, grape seed oil, and evening primrose oil.

As an improvement of the present invention, the emulsifier is Tween 60, Tween 80, Tween 20, ten polyglycerol monolaurate, caprylic/capric acid polyethylene glycol glyceride, polyoxyethylene (40 ) any one or a combination of stearic acid, cetearyl alcohol and sorbitan oleate, sorbitan oleate, and cetearyl oleate-6 oleate.

As an improvement of the present invention, the co-emulsifier is polyglycerol ricinole ester, cetyl polyethylene glycol/polypropylene glycol-10/1 dimethylsiloxane, polyethylene glycol-30 dimer Any one or a combination of hydroxystearate and polyethylene glycol-400.

As an improvement of the present invention, the solid adsorbent is any one of anhydrous calcium hydrogen phosphate, magnesium aluminum silicate, silicon dioxide, gum arabic, and isopropyl citrate.

As an improvement of the present invention, the particle size range of the astaxanthin solid self-microemulsion is 50-150 nm.

As a kind of improvement of the present invention, the preparation method of described astaxanthin solid self-microemulsion, comprises the following steps:

(1) Prepare the following components by weight percentage: astaxanthin 1-5%, oil 10-20%, emulsifier 20-30%, co-emulsifier 10-20%, solid adsorbent 10-50%;

(2) Mix astaxanthin and oil and stir at room temperature until dissolved to form an oil phase system;

(3) After stirring the emulsifier and co-emulsifier in a constant temperature water bath at 50-70°C, add them to the oil phase system and mix to obtain astaxanthin liquid self-microemulsion;

(4) After cooling to normal temperature, adding a solid adsorbent to the astaxanthin liquid self-microemulsion, and performing physical mixing and adsorption at normal temperature to obtain the astaxanthin solid self-microemulsion.

As an improvement of the present invention, an application of astaxanthin solid self-microemulsion in preparing functional food.

In the present invention, the carrier load is astaxanthin, which has antioxidative and anti-inflammatory effects. The preparation method of astaxanthin solid self-microemulsion is a physical adsorption method, and the liquid self-microemulsion and silicon dioxide are physically mixed and adsorbed. And the astaxanthin solid self-microemulsion is prepared at normal temperature. The carrier has good stability and water solubility, the preparation method is simple and controllable, and the repeatability is good, and can be applied to the preparation of functional foods containing astaxanthin.

Owing to having adopted the above technology, compared with the prior art, the present invention has the following beneficial effects:

(1) The astaxanthin solid self-microemulsion system of the present invention has good stability;

(2) Improve the solubility of insoluble astaxanthin, thereby improving its bioavailability;

(3) Each component in the formula has high safety, is non-irritating to the body, non-toxic, can be used as an intermediate type in combination with food formula, has good compatibility, and can be widely used in the field of food and health products;

(4) The preparation method is simple and controllable and has good repeatability.

Description of drawings

Fig. 1 is the flow chart of the preparation method of the astaxanthin solid self-microemulsion system of the present invention.

Detailed ways

The present invention will be further described below in conjunction with the embodiments. These examples are intended to illustrate the invention and not to limit the scope of the invention. The implementation conditions adopted in the embodiments can be further adjusted according to the conditions of specific manufacturers.

Example 1:

Weigh 0.2 g of astaxanthin and 2.0 g of corn oil, mix astaxanthin and corn oil and stir at room temperature until most of the astaxanthin is dissolved in the corn oil to form the oil phase of the system; weigh 3 g of Tween 60 and 2.0 g of polyethylene glycol-400, Tween 60 and polyethylene glycol-400 were stirred in a 50°C constant temperature water bath and added to the oil phase, so that they were fully mixed to form a homogeneous phase to obtain astaxanthin liquid self-microemulsion; After cooling to normal temperature, 5 g of silicon dioxide was added to the astaxanthin liquid self-microemulsion as a solid adsorbent, and physical mixing and adsorption was carried out at normal temperature to make the mixture uniform, and finally the astaxanthin solid self-microemulsion was obtained.

1.0 g of astaxanthin solid self-microemulsion system was added to 100g of deionized water, and after uniform dispersion, the average particle size of astaxanthin solid self-microemulsion system after water dispersion was measured by particle size analyzer was 121.2 ± 2.8nm, and 25 ℃. After being placed at room temperature for 1 month, the average particle size was 130.7±3.0 nm, and there was no significant difference in the particle size change, indicating good stability.

Example 2:

Weigh 2 g of astaxanthin and 18.5 g of coconut oil, mix astaxanthin and coconut oil and stir at room temperature until most of the astaxanthin is dissolved in the coconut oil to form the oil phase of the system; weigh 30 g of Tween 20 and 25g of polyglycerol ricinoleate, Tween 20 and polyglycerol ricinoleate are stirred into the oil phase in a 50° C. constant temperature water bath, and fully mixed to form a homogeneous phase to obtain astaxanthin liquid self-microemulsion; cooling; After reaching room temperature, 44 g of magnesium aluminum silicate was added to the astaxanthin liquid self-microemulsion as a solid adsorbent, and physical mixing and adsorption was carried out at room temperature to make it evenly mixed, and finally astaxanthin solid self-microemulsion was obtained.

1.0g of astaxanthin solid self-microemulsion system was added to 100g of deionized water, and after uniform dispersion, the average particle size of astaxanthin solid self-microemulsion system after water dispersion was measured by particle size analyzer was 137.5±3.3nm, and the temperature was 25°C. After being placed at room temperature for 1 month, the average particle size was 144.7±2.8 nm, and there was no significant difference in the particle size change, indicating good stability.

Example 3:

Weigh 0.5 g of astaxanthin and 7.5 g of caprylic capric triglyceride, mix astaxanthin and caprylic capric triglyceride and stir at room temperature until most of the astaxanthin is dissolved in caprylic capric triglyceride, Form the oil phase of the system; weigh 5.0 g of decaglycerol monolaurate and 2.5 g of cetyl polyethylene glycol/polypropylene glycol-10/1 dimethylsiloxane, decaglycerol monolaurate and Cetyl polyethylene glycol/polypropylene glycol-10/1 dimethyl siloxane was added to the oil phase with stirring in a constant temperature water bath at 50°C to make it fully mixed to form a homogeneous phase to obtain astaxanthin liquid self-microemulsion; cooling After reaching normal temperature, add 20 g of anhydrous calcium hydrogen phosphate to the astaxanthin liquid self-microemulsion as a solid adsorbent, and carry out physical mixing and adsorption at normal temperature to make it mix evenly, and finally obtain astaxanthin solid self-microemulsion.

1.0 g of astaxanthin solid self-microemulsion system was added to 100g of deionized water, and after uniform dispersion, the average particle size of astaxanthin solid self-microemulsion system after water dispersion was measured by particle size analyzer was 105.2±1.9nm, and the temperature was 25 ℃. After being placed at room temperature for 1 month, the average particle size was 110.5±1.0 nm, and there was no significant difference in particle size change, indicating good stability.

The above examples are only to illustrate the technical concept and characteristics of the present invention, and the purpose thereof is to enable those skilled in the art to understand the content of the present invention and implement accordingly, and cannot limit the protection scope of the present invention. All changes, modifications, substitutions, combinations, and simplifications made according to the spirit of the present invention should be equivalent substitution methods, and are included in the protection scope of the present invention.

Claims (8)

1. a kind of astaxanthin Solid Self-microemulsion, which is characterized in that be made of the component of following mass percent:

Astaxanthin 1-5%

Grease 10-20%

Emulsifier 20-30%

Assistant for emulsifying agent 10-20%

Solid absorbent 10-50%.

2. a kind of astaxanthin Solid Self-microemulsion according to claim 1, it is characterised in that: the grease is coconut oil, jade Rice bran oil, pungent Triglyceride DDD, grape seed oil, any one in evening primrose oil or above combination.

3. a kind of astaxanthin Solid Self-microemulsion according to claim 1, it is characterised in that: the emulsifier be polysorbate60, Dilute (40) stearic acid of Tween 80, polysorbas20, ten polyglycereol monolaurates, caprylic/capric LABRAFIL M 1944CS, polyoxy second, The smooth olive oleate of the pure and mild sorb of cetearyl alcohol, sorb smooth olive oleate are appointed in -6 olive oleate of ceteareth The one or more of combination of meaning.

4. a kind of astaxanthin Solid Self-microemulsion according to claim 1, it is characterised in that: the assistant for emulsifying agent is polyglycereol Polyricinoleate, -10/1 dimethyl siloxane of cetyl polyethylene/polypropylene glycol, -30 dimerization hydroxy stearic acid of polyethylene glycol Any one in ester, polyethylene glycol-400 or above combination.

5. a kind of astaxanthin Solid Self-microemulsion according to claim 1, it is characterised in that: the solid absorbent is anhydrous Calcium monohydrogen phosphate, aluminium-magnesium silicate, silica, gum arabic, any one in lemon isopropyl propionate.

6. a kind of astaxanthin Solid Self-microemulsion according to claim 1, it is characterised in that: the astaxanthin Solid Self-microemulsion Particle size range be 50-150nm.

7. a kind of astaxanthin Solid Self-microemulsion according to claim 1, which is characterized in that the astaxanthin Solid Self-microemulsion Preparation method, comprising the following steps:

(1) prepare following components: astaxanthin 1-5%, grease 10-20%, emulsifier 20-30%, assistant for emulsifying agent by weight percentage 10-20%, solid absorbent 10-50%；

(2) stirring forms oil-based system to dissolving at room temperature after mixing astaxanthin, grease；

(3) after stirring emulsifier, assistant for emulsifying agent in 50-70 DEG C of water bath with thermostatic control, addition is mixed into oil-based system, obtains shrimp Green element liquid is from micro emulsion；

(4) after being cooled to room temperature, solid absorbent is added from micro emulsion to astaxanthin liquid, carries out physical mixed suction at normal temperature It is attached, obtain astaxanthin Solid Self-microemulsion.

8. a kind of any one of claim 1-7 astaxanthin Solid Self-microemulsion is preparing the application in functional food.