CN109985008A - A kind of astaxanthin Solid Self-microemulsion and preparation method thereof - Google Patents

A kind of astaxanthin Solid Self-microemulsion and preparation method thereof Download PDF

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CN109985008A
CN109985008A CN201910357578.5A CN201910357578A CN109985008A CN 109985008 A CN109985008 A CN 109985008A CN 201910357578 A CN201910357578 A CN 201910357578A CN 109985008 A CN109985008 A CN 109985008A
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astaxanthin
microemulsion
solid self
solid
self
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夏强
毛昕宇
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Southeast University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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Abstract

The present invention relates to a kind of astaxanthin Solid Self-microemulsions and preparation method thereof, it is described carrier loaded for astaxanthin, by the way that astaxanthin, grease, emulsifier, assistant for emulsifying agent and solid absorbent are carried out physical mixed absorption, and astaxanthin Solid Self-microemulsion is prepared at normal temperature, the carrier is with good stability and water-soluble, preparation method is simply controllable, reproducible, can be applied in the preparation of the functional food containing astaxanthin.

Description

A kind of astaxanthin Solid Self-microemulsion and preparation method thereof
Technical field
The present invention relates to a kind of astaxanthin Solid Self-microemulsions and preparation method thereof, belong to the load in functional food technology of preparing System system technical field.
Background technique
Astaxanthin is a kind of fat-soluble keto-acid carotenoid in the source non-vitamin A, existing forms be mainly free state and Be esterified state, in molecular structure special conjugated double bond and hydroxyl be it compare vitamin E and beta carotene possess it is stronger Antioxidant activity, it is strongest natural so far in nature.Some researches show that astaxanthin has a variety of lifes Reason activity, such as delaying senility, antitumor, prevention cardiovascular and cerebrovascular disease, treatment diabetes, anti-inflammatory, improvement motion function.Shrimp is green Element can effectively remove interior free yl, while promote antibody tormation, improve animal immunizing power, anti-inflammatory can not only give protection against cancer, and prevent Only ultraviolet radiation can also prevent the disease of cardiovascular, nervous system etc., have in food, health care product, pharmaceuticals industry Considerable practical value and application prospect.
Astaxanthin is to have now been found that the carotenoid that can uniquely penetrate blood-brain, blood-retina barrier, Central nervous System and cerebral function can produce active influence.If being therefore added to astaxanthin as diet function factor in food, It will be with practical meaning to human health is improved.But astaxanthin photostability itself is poor, bioavilability is low, limits it Application in terms of health care product, field of medicaments.
Lipid formulations drug-loading system entered pharmaceutical field in the form of simple oil solution at 1981.Then, lipid Mostly based on self-emulsifiable preparation, self-emulsifying drug-loading system can be used as a kind of effective the product of preparation drug-loading system in the market In order to improve the bioavilability of insoluble medicine, self-emulsifying formulation has highlighted lipid and has improved lipophilic Oral drug absorption means The importance of aspect.But lipid formulations have that dosage form is single few in the market, application range it is narrow apply bottleneck
In order to make up the applied defect that lipid formulations face, solid lipid drug-loading system (solid-state-lipid-based Drug delivery systems, s-LBDDS) research interest of researcher has been caused in recent years.Solid lipid system The preparation process of agent are as follows: liquid fatty preparation is adsorbed onto the stable solid carrier of chemical property using dry technology, thus The sample (such as loose powder, particle and pellet) of solid dosage forms is prepared.The selection of solid pharmaceutical preparation should be conceived to it with outstanding Lipid adsorption capacity, good water-soluble and solid property.
Solid lipid preparation drug-loading system combines the double dominant of lipid formulations formula and solid dosage forms: 1) reducing sample (moisture in conventional lotion or suspension formulation at least containing 50% amount, the volume of sample may be only after solidification for the volume of product There is the specification of a tablet or capsule);2) taking orally dosage can precisely determine;3) liquid dosage form is compared, solid dosage forms is more convenient for The oral medication process of patient;4) small in size without or with a small amount of moisture in solid lipid pharmaceutical formulation, the object stored for a long time Physicochemical stability is high, is easy to transport storage for a long time.
Summary of the invention
The present invention is directed to the deficiencies in the prior art, provides a kind of astaxanthin Solid Self-microemulsion and its preparation side Method, the dissolubility for solving astaxanthin in the prior art is poor, load capacity is low and the shortcoming and defect such as oral administration biaavailability is low place.
To achieve the above object, The technical solution adopted by the invention is as follows:
A kind of astaxanthin Solid Self-microemulsion, is 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%.
As an improvement of the present invention, the grease be coconut oil, corn oil, pungent Triglyceride DDD, grape seed oil, Any one in evening primrose oil or above combination.
As an improvement of the present invention, the emulsifier is polysorbate60, Tween 80, polysorbas20, ten polyglycereol list laurels Dilute (40) stearic acid of acid esters, caprylic/capric LABRAFIL M 1944CS, polyoxy second, the smooth olive oleate of the pure and mild sorb of cetearyl alcohol, Any one in the smooth olive oleate of sorb, -6 olive oleate of ceteareth or above combination.
As an improvement of the present invention, the assistant for emulsifying agent is polyglycerol polyricinoleate, cetyl polyethylene glycol/poly- third - 10/1 dimethyl siloxane of glycol, -30 dimerization hydroxy stearic acid ester of polyethylene glycol, any one in polyethylene glycol-400 or with On combination.
As an improvement of the present invention, the solid absorbent be calcium phosphate dibasic anhydrous, aluminium-magnesium silicate, silica, Any one in gum arabic, lemon isopropyl propionate.
As an improvement of the present invention, the particle size range of the astaxanthin Solid Self-microemulsion is 50-150nm.
As an improvement of the present invention, the preparation method of the astaxanthin Solid Self-microemulsion, 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.
As an improvement of the present invention, a kind of astaxanthin Solid Self-microemulsion is preparing the application in functional food.
It is heretofore described it is carrier loaded be astaxanthin, with anti-oxidant, anti-inflammatory effect, astaxanthin Solid Self-microemulsion Preparation method be physisorphtion, liquid carries out physical mixed absorption from micro emulsion and silica, and is prepared at normal temperature To astaxanthin Solid Self-microemulsion.The carrier is with good stability and water-soluble, and preparation method is simply controllable, reproducible, It can be applied in the preparation of the functional food containing astaxanthin.
Due to using the above technology, the present invention compared with the prior art, is had the advantage that as follows:
(1) astaxanthin Solid Self-microemulsion system of the invention is with good stability;
(2) dissolubility for being insoluble in the astaxanthin of water is improved, to improve its bioavilability;
(3) each component has very high safety in formula, nonirritant to body, non-toxic, can be used as intermediate-type with Food formula is used in compounding, and compatibility is good, can be widely used for food and field of health care products;
(4) preparation method is simply controllable, reproducible.
Detailed description of the invention
Fig. 1 is the preparation method flow chart of astaxanthin Solid Self-microemulsion system of the present invention.
Specific embodiment
The invention will be further described with reference to embodiments.These embodiments are not limited to for illustrating the present invention It limits the scope of the invention.Implementation condition used in the examples can do further adjustment according to the condition of specific producer.
Embodiment 1:
0.2 g astaxanthin and 2.0g corn oil are weighed, is stirred at room temperature after astaxanthin, corn oil are mixed to most of shrimp Green element is dissolved into corn oil, forms the oily phase of system;3g polysorbate60 and 2.0g polyethylene glycol-400 are weighed, by polysorbate60 and is gathered Ethylene glycol -400 is stirred in 50 DEG C of waters bath with thermostatic control in the oily phase of addition, is mixed them thoroughly to form homogeneous phase, is obtained astaxanthin liquid State is from micro emulsion;After being cooled to room temperature, the silica of 5g is added from micro emulsion to astaxanthin liquid as solid absorbent, normal Temperature is lower to carry out physical mixed absorption, is uniformly mixed it, finally obtains astaxanthin Solid Self-microemulsion.
1.0 g astaxanthin Solid Self-microemulsion systems are added in 100g deionized water, after evenly dispersed, utilize particle size analyzer After average grain diameter is 121.2 ± 2.8nm after measuring astaxanthin Solid Self-microemulsion system water dispersion, and 25 DEG C are placed at room temperature for 1 month Its average grain diameter is 130.7 ± 3.0nm, and change of size no significant difference shows that it has good stability.
Embodiment 2:
2 g astaxanthins and 18.5g coconut oil are weighed, is stirred at room temperature after astaxanthin, coconut oil are mixed to most of shrimp Green element is dissolved into coconut oil, forms the oily phase of system;Weigh 30g polysorbas20 and 25g polyglycerol polyricinoleate, by polysorbas20 and Polyglycerol polyricinoleate is stirred in 50 DEG C of waters bath with thermostatic control in the oily phase of addition, mixes them thoroughly to form homogeneous phase, obtains shrimp blueness Plain liquid is from micro emulsion;After being cooled to room temperature, the aluminium-magnesium silicate of 44 g is added from micro emulsion as solid absorption to astaxanthin liquid Agent carries out physical mixed absorption at normal temperature, is uniformly mixed it, finally obtains astaxanthin Solid Self-microemulsion.
1.0g astaxanthin Solid Self-microemulsion system is added in 100g deionized water, after evenly dispersed, utilizes particle size analyzer After average grain diameter is 137.5 ± 3.3nm after measuring astaxanthin Solid Self-microemulsion system water dispersion, and 25 DEG C are placed at room temperature for 1 month Its average grain diameter is 144.7 ± 2.8nm, and change of size no significant difference shows that it has good stability.
Embodiment 3:
0.5 g astaxanthin and the pungent Triglyceride DDD of 7.5g are weighed, in room temperature after astaxanthin, pungent Triglyceride DDD are mixed Lower stirring is dissolved into pungent Triglyceride DDD to most of astaxanthin, forms the oily phase of system;Weigh ten polyglycereol list of 5.0g - 10/1 dimethyl siloxane of laurate and 2.5g cetyl polyethylene/polypropylene glycol, by ten polyglycereol monolaurates and - 10/1 dimethyl siloxane of cetyl polyethylene/polypropylene glycol is stirred in 50 DEG C of waters bath with thermostatic control in the oily phase of addition, fills it Divide and be mixed to form homogeneous phase, obtains astaxanthin liquid from micro emulsion;After being cooled to room temperature, 20 are added from micro emulsion to astaxanthin liquid The calcium phosphate dibasic anhydrous of g carries out physical mixed absorption as solid absorbent at normal temperature, is uniformly mixed it, finally obtains Astaxanthin Solid Self-microemulsion.
1.0 g astaxanthin Solid Self-microemulsion systems are added in 100g deionized water, after evenly dispersed, utilize particle size analyzer After average grain diameter is 105.2 ± 1.9nm after measuring astaxanthin Solid Self-microemulsion system water dispersion, and 25 DEG C are placed at room temperature for 1 month Its average grain diameter is 110.5 ± 1.0 nm, and change of size no significant difference shows that it has good stability.
The foregoing examples are merely illustrative of the technical concept and features of the invention, its object is to allow professional and technical personnel in the field It cans understand the content of the present invention and implement it accordingly, it is not intended to limit the scope of the present invention.It is all smart according to the present invention The changes, modifications, substitutions, combinations, simplifications that refreshing essence is done, should be equivalent substitute mode, are included in guarantor of the invention Within the scope of shield.

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.
CN201910357578.5A 2019-04-29 2019-04-29 A kind of astaxanthin Solid Self-microemulsion and preparation method thereof Pending CN109985008A (en)

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CN111264860A (en) * 2020-01-19 2020-06-12 上海海洋大学 Solid self-microemulsion microcapsule containing astaxanthin and quercetin and preparation method and application thereof
CN112353704A (en) * 2020-11-20 2021-02-12 苏州纳康生物科技有限公司 Preparation method of paeonol nano lipid particle
CN113081870A (en) * 2019-12-23 2021-07-09 嘉兴睿肤丽生物科技有限公司 Preparation method of astaxanthin nano-liposome and application of astaxanthin nano-liposome in cosmetics

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113081870A (en) * 2019-12-23 2021-07-09 嘉兴睿肤丽生物科技有限公司 Preparation method of astaxanthin nano-liposome and application of astaxanthin nano-liposome in cosmetics
CN111264860A (en) * 2020-01-19 2020-06-12 上海海洋大学 Solid self-microemulsion microcapsule containing astaxanthin and quercetin and preparation method and application thereof
CN112353704A (en) * 2020-11-20 2021-02-12 苏州纳康生物科技有限公司 Preparation method of paeonol nano lipid particle

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