CN109985012A - A kind of Co-Q10 chewable tablets of high bioavilability and preparation method thereof - Google Patents
A kind of Co-Q10 chewable tablets of high bioavilability and preparation method thereof Download PDFInfo
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- CN109985012A CN109985012A CN201711480212.4A CN201711480212A CN109985012A CN 109985012 A CN109985012 A CN 109985012A CN 201711480212 A CN201711480212 A CN 201711480212A CN 109985012 A CN109985012 A CN 109985012A
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- CN
- China
- Prior art keywords
- preparation
- hydrophilic
- coenzyme
- chewable tablets
- dry
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- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 title claims abstract description 151
- 238000002360 preparation method Methods 0.000 title claims abstract description 31
- 239000007910 chewable tablet Substances 0.000 title claims abstract description 30
- 239000000839 emulsion Substances 0.000 claims abstract description 23
- 230000000694 effects Effects 0.000 claims abstract description 10
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- 239000008107 starch Substances 0.000 claims abstract description 7
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 6
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000000853 adhesive Substances 0.000 claims abstract description 6
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- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims abstract description 6
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims abstract description 6
- 229960002675 xylitol Drugs 0.000 claims abstract description 6
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims abstract description 5
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 10
- 238000010438 heat treatment Methods 0.000 claims description 9
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 8
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- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 230000001055 chewing effect Effects 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
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- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims description 3
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- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 2
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- QNTNKSLOFHEFPK-UPTCCGCDSA-N ubiquinol-10 Chemical compound COC1=C(O)C(C)=C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)C(O)=C1OC QNTNKSLOFHEFPK-UPTCCGCDSA-N 0.000 description 6
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- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 5
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- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
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Classifications
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- 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
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
- A23L2/52—Adding ingredients
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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
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- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2063—Proteins, e.g. gelatin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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Abstract
The present invention provides a kind of high bioavilability Co-Q10 chewable tablets and preparation method thereof, the preparation method includes mixing fat-soluble Co-Q10 with hydrophilic gel liquid solution, after high speed shearing emulsification, drop is crushed under high-pressure situations to obtain the emulsion droplet of nano-dispersed, the hydrophilic coenzyme q 10 dry containing high level is obtained by spray drying or spray congealing-starch bed dry technology again, by obtained coenzyme q 10 dry and xylitol, lactose, other adhesives, the mixed pressuring plates such as glidant, it finally obtains in good taste, the high Co-Q10 chewable tablets of bioavilability.Co-Q10 is in unformed state in the Co-Q10 chewable tablets that the present invention obtains, and nano-dispersed, stability is good, and oral administration biaavailability is excellent, has anti-oxidant, strengthen immunity effect well, suitable for applying in health food, cosmetics or drug etc..
Description
Technical field
The present invention relates to a kind of high bioavilability Co-Q10 chewable tablets and preparation method thereof, belong to field of health care products.
Background technique
Co-Q10 is the fat-soluble compound being widely present in organism, it is widely distributed in nature, is primarily present
It is one of most important coenzyme of human body in the cell of yeast, plant leaf, seed and the heart of animal, liver and kidney.
Co-Q10, also known as ubiquinone, (Ubiquinone) is yellow crystal under normal circumstances, and fusing point is insoluble at 48 DEG C
Yu Shui is a kind of liposoluble substance.The structural formula of Co-Q10 is as follows:
Co-Q10 is the natural that biological cell itself generates, and can prevent the formation of free radical, help to safeguard
The regular event of immune system and anti-aging have good strengthen immunity, alleviate a variety of lifes such as physical fatigue, anti-oxidant
Object effect has remarkable result to prevention coronary heart disease, alleviation periodontitis, treatment diabetes etc., in hypertension, congested hair
Important role is also play in terms of the treatment of force failure and angina pectoris, the nervous system disease and Cutaneous illness, while also
Antitumor action clinically has certain curative effect for the transfer of cancer cell.
Co-Q10 is a kind of important endogenous biostearin in human body, and Co-Q10 content is with respect to highest in heart.Body
Portion of Coenzyme Q10 necessary to body is provided by being endogenously synthesized, and other parts are absorbed from food.The mankind exist
At 20 years old, the Co-Q10 ability independently synthesized reaches peak, maintains to 50 years old or so.It can decline year by year later, because deposit is auxiliary
The cell mitochondrial DNA material of enzyme Q10 is destroyed by oxygen radical, and autonomous synthesizing coenzyme Q 10 is caused to reduce.As a result make human body thin
The metabolic function of born of the same parents, especially heart cell declines, and " senile " just displays.
There is good anti-oxidant, strengthen immunity and other effects just because of Co-Q10, but with the increasing at human body age
Greatly, the content of internal Co-Q10 is fewer and fewer, declines quickly, so in order to supplement the mesh for the amount for being endogenously synthesized Co-Q10
, the universal Co-Q10 in the form of dietary supplements or health care product or food outside supplementary quota now, only China just
There are tens kinds of health care products or dietary supplements containing Co-Q10, these health care products or the dietary supplements overwhelming majority are
Existing in the form of soft capsule, i.e., mainly Co-Q10 crystal is dispersed or dissolved in vegetable fat, or will be described
Crystal powder is directly loadable into capsule, then is aided with other vitamins or biostearin, is taken with soft gelatin capsules.
But due to Co-Q10 be it is fat-soluble, be substantially insoluble in, and be crystalline state, which has limited its biology benefit
The raising of expenditure, the Co-Q10 for generally requiring overdose can be only achieved expected effect.Moreover, being taken in soft gelatin capsules
When Co-Q10, Co-Q10 need to be dispersed or dissolved in vegetable fat or other sweet three esters, will cause additional grease intake,
This resistance by some consumers.On the other hand, Co-Q10 is a kind of unstable substance, oxidizable and reduce its life
Object potency, so certain safeguard measure for preventing Co-Q10 from aoxidizing is necessary when being made into the preparation that can be taken
's.
In order to overcome crystal Co-Q10 poorly water-soluble, the low defect of bioavilability, many people are dedicated to researching and developing oral life
The better product of object availability, as Chen Yujun et al. is (" raw in " method and thinking that improve coenzyme Q 10 oral bioavilability "
Object technological world " 2015 the 3rd phases) in mention using Gemini as the bioadhesive material of Co-Q10, adhered to by electrostatic interaction
In gastrointestinal tract surface, increase the time of contact of preparation and gastrointestinal tract, to improve the bioavilability of Q10.
PCT international application no PCT/JP2007/057954 discloses a kind of for improving Co-Q10 stripping property in the oral cavity
The method of energy, Co-Q10 is wrapped in cyclodextrin, especially cyclodextrin, then the cyclodextrin encapsulated product is used as coenzyme
Q10 ingredient is mixed and made into chewing composition with other auxiliary materials, wherein the biology benefit in order to guarantee Co-Q10 in chewing composition
Expenditure, the lower Co-Q10 content the more advantageous in cyclodextrin encapsulated product.
Chinese patent application publication number CN106177227A refer to it is a kind of have effects that strengthen immunity containing Co-Q10
Composition, it is believed that Co-Q10 and grape seed extract are used in compounding the bioavilability that can improve Co-Q10.
Chinese patent application publication number CN104983697A, which is disclosed through the adjustment of formula of chewable tablets, enhances Co-Q10
Bioavilability in human body, but do not see from document disclosed in it reinforcing effect of its bioavilability.
The benzoquinones combination that PCT international application no PCT/US2006/029821 describe solubility and bioavilability improve
Object, after mainly dissolving the polymer that benzoquinones such as Co-Q10 and at least one solubility improve in a solvent, removing solvent is formed
Amorphous benzoquinones, to improve its bioavilability.
In above-mentioned various raising the Co-Q10s in human body method of bioavilability, or by allow Co-Q10 and its
Its substance is used in combination, and by the measures such as terminal formulation products formula is adjusted, bioavilability reinforcing effect is unobvious, and
Lack necessary theoretical basis.Alternatively, dissolve Co-Q10 in organic solvent together with other polymer, after will be organic molten
Agent removing, is adsorbed in Co-Q10 in polymer with amorphous form, so that its bioavilability in human body is improved, but
On the one hand this method will use the more virose organic solvent of tool, it cannot be guaranteed that the safety of terminal formulation products, another
The stability of aspect Co-Q10 does not obtain necessary improvement, moreover, the application of number of polymers, to the mouthfeel shadow of finished product
Sound is larger, when these being especially adsorbed in the Co-Q10 on polymer being used for oral taking chewy piece, has a kind of beastly
Mouthfeel, consumption experience when mouthfeel takes orally consumer are very crucial.Alternatively, Co-Q10 is made by the inclusion of cyclodextrin
With improving its dissolving out capability, to improve bioavilability, but in order to reach preferable inclusion effect, Co-Q10 in inclusion compound
Content it is more lower better, this is unfavorable to the economy of finished product.
In short, due to the fat-soluble feature of crystal Co-Q10, bioavilability in human body is not high, in order to improve
Its bioavilability is had to and grease compounded use, is perhaps changed Co-Q10 crystalline structure by some measures or is changed
The dissolution properties of Co-Q10, but there is various defects, such as Co-Q10 in finished product in these methods of early period
Bioavilability raising is unobvious, and the use of organic solvent brings safety issue, acts on not the stability improvement of Co-Q10
It is big etc..
In conventional Co-Q10 chewing machining process, usually Co-Q10 crystal powder is mixed with auxiliary material, it is auxiliary
Material includes but is not limited to dextrin, starch, sucrose or other glycitols, glidant silica, stearic acid release agent magnesium, adhesive
Other vitamins or plant extracts is added, through tablet press in cellulose derivative, povidone, starch derivatives etc. when necessary
It is made after technique.
There is the defect of the following aspects by the conventional Co-Q10 chewing obtained chewable tablets of machining process: firstly,
Co-Q10 bioavilability in human body is low in chewable tablets.It is water-soluble very poor since Co-Q10 is existed with crystal state, with
Co-Q10 existing forms are the same in soft capsule, and bioavilability is very poor in human body, in order to achieve the desired results require supplementation with it is more
The Co-Q10 of amount, it is less economical.With also being mentioned in document by Co-Q10 microencapsulation in the past, but often complex process,
Nano-dispersed is not achieved, bioavilability is relatively low when tablet is made.Secondly as Co-Q10 is through any protective effect, easily
Oxygen in ingress of air and be oxidized degradation, further reduced its biological value.Again, due to crystal Co-Q10 resistance to pressure
Difference, in order to make its molding, it has to it is fine that a large amount of auxiliary material such as microcrystalline cellulose, povidone, magnesium stearate, hydroxypropyl methyl be added
Element etc. is tieed up, the mouthfeel for easilying lead to last chewable tablets in this way is very poor, reduces the consumption experience effect of consumer.Finally, due to
The fusing point of crystal Co-Q10 is at 48 DEG C, so in production, especially in continuous high speed high pressure tabletting production process, due to
Equipment heating, it is easy to melt portion of Coenzyme Q10 and sticking, cause the difficulty in production.
Therefore, it is highly desirable to find a kind of effective method and is improving the same of Co-Q10 bioavilability in human body
When, improve its stability, and can by it is a kind of easily and effectively in a manner of eat.
Summary of the invention
In order to overcome the defect of prior art, the present invention provides a kind of the auxiliary of the high bioavilability of energy industrialized production
Enzyme Q10 chews tablet composition, to solve above-mentioned all problems.In order to overcome crystal Co-Q10 these defects in direct tablet compressing,
Simultaneously in the various defects for considering the prior art, the present invention provides a kind of Co-Q10 chewable tablets of high bioavilability
Preparation method, the preparation method comprises the following steps: (a) heating melting crystal Co-Q10, by the Co-Q10 of molten with
Hydrophilic gel liquid solution is mixed under high speed shear, to form oil-in-water type emulsion droplet；(b) it will be walked by high-pressure homogeneous effect
Suddenly the oil-in-water type emulsion droplet of (a) is crushed, to obtain the emulsion droplet of nano-dispersion；(c) using spray drying or by spraying
Condensation-starch bed fluidized drying technology shapes the emulsion droplet of the nano-dispersion of step (b), to obtain hydrophilic coenzyme
Q10 dry powder or particle；And (d) the hydrophilic coenzyme q 10 dry or particle of step (c) are mixed with filler
It closes, direct tablet compressing after mixing, to obtain the Co-Q10 chewable tablets of high bioavilability.
In the technical solution of preparation method of the present invention, it is preferable that in step (a), the hydrophilic colloid be gelatin,
Arabic gum, starch Sodium Octenyl Succinate etc. have the colloid of emulsion stability effect.
In the technical solution of preparation method of the present invention, it is preferable that in step (a), the hydrophilic colloid is dissolved in 60
In~80 DEG C of water, to obtain hydrophilic gel liquid solution.Preferably, in the colloidal solution solid content in 10-80%.
In the technical solution of preparation method of the present invention, it is preferable that in step (a), heating melting crystal Co-Q10
Temperature is the Co-Q10 of 50 DEG C of moltens formed above.
In the technical solution of preparation method of the present invention, it is preferable that in step (a), the Co-Q10 of the molten with
The hydrophilic gel liquid solution is mixed under high speed shear, shear rate 5000-20000rpm.
In the technical solution of preparation method of the present invention, it is preferable that in step (a), emulsion droplet average grain diameter is after shearing
0.5-4.0μm。
In the technical solution of preparation method of the present invention, it is preferable that in step (b), will be walked by high-pressure homogeneous effect
Suddenly the oil-in-water type emulsion droplet of (a) is crushed to obtain the emulsion droplet of nano-dispersion, and the high-pressure homogeneous pressure is 8000-
30000psi；The average grain diameter of the emulsion droplet of nano-dispersion after high-pressure homogeneous is 100-1000nm.
In the technical solution of preparation method of the present invention, it is preferable that in step (c), the hydrophilic Co-Q10 is dry
Co-Q10 content is 5-60wt.% in powder or particle.
In the technical solution of preparation method of the present invention, it is preferable that in step (d), the filler is xylitol, mountain
Pears alcohol, mannitol or lactose.
In the technical solution of preparation method of the present invention, it is preferable that as needed, can add in Co-Q10 chewable tablets
Enter a small amount of release agent, glidant, adhesive, flavoring agent, nutrient.Wherein, the release agent is magnesium stearate, the glidant
For silica, the pico- crystalline cellulose of described adhesive or low-substituted hydroxypropyl cellulose, the flavoring agent are citric acid, apple
Acid, essence, fruit powder, the nutrient are vitamin E, vitamin A, vitamin C.
The present invention also provides the Co-Q10 chewable tablets of the high bioavilability using the method preparation, the coenzyme
Q10 chewable tablets includes hydrophilic coenzyme q 10 dry or particle and filler；Wherein, the hydrophilic coenzyme q 10 dry or
Particle includes the internal layer containing coenzyme q 10 dry or particle and the outer layer containing hydrophilic colloid.
In the technical solution of Co-Q10 chewable tablets of the present invention, it is preferable that the hydrophilic colloid be gelatin, I
Primary glue or starch Sodium Octenyl Succinate, the filler are xylitol, sorbierite, mannitol or lactose.
Co-Q10 is in the obtained Co-Q10 chewable tablets of the present invention with amorphous form, and nano-dispersed is in hydrophilic colloid
In, release can be dissolved quickly into after in oral cavity, in human body bioavilability with higher.Simultaneously because Co-Q10 is received
Rice is scattered in hydrophilic colloid, these hydrophilic colloids have good protective effect to Co-Q10 molecule, it is made to be not easy oxygen
Change degradation, ensure that the stability of Co-Q10.
In addition, the Co-Q10 for being scattered in the amorphous state in hydrophilic colloid has more relative to crystal Co-Q10
Good compressibility does not have to or only uses a small amount of auxiliary material in tableting processes to form, and not only formula is succinct, but also mouthfeel is more
Easily adjustment improves the consumption experience impression of consumer.The Co-Q10 being scattered in hydrophilic colloid also overcomes crystal coenzyme
Sticking phenomenon caused by Q10 is melted since temperature raises in tableting processes, improves the operability in production.
In short, obtaining Co-Q10 chewable tablets by the present invention, higher bioavilability is not only shown in vivo,
And stability improves, and formula is succinct, good mouthfeel, strong operability in production.Other than chewing sheet form, obtained in technique
Hydrophily dry powder containing Co-Q10 or particle can also food, nutrient and healthcare products, cosmetics, in terms of with it
The forms such as its dosage form such as hard capsule, emulsion, electuary, drinks are applied.
Other than Co-Q10 chewable tablets, the invention technology applies also for reduced coenzyme Q 10 similar in chewable tablets.
Specific embodiment
The present invention is further illustrated with embodiment below, the embodiment of the present invention is merely to illustrate technical side of the invention
Case, and the non-limiting present invention.
All Test Materials and all commercial product of chemical reagent.
Embodiment 1
100g Co-Q10 (source: Zhejiang Medicine Co) is heated to 50 DEG C of formation molten liquids.
1900g Arabic gum is mixed with 2000mL water, and heating is kept for 1 hour at 60 DEG C under stirring state, keeps Arabic gum completely molten
Solution obtains gumwater.Co-Q10 molten liquid is added in gumwater, while keeping high speed shear state,
Shear rate keeps 5000rpm, obtains oil-in-water type Co-Q10 lotion, mean droplet size passes through MasterSizer in lotion
3000 laser diffraction granularity distribution instruments are detected as 4.0 μm.
By oil-in-water type Co-Q10 lotion, by PhD-TECH high pressure homogenizer, that high pressure is carried out under 30000psi pressure is equal
After matter, emulsion droplet average grain diameter reaches 1000nm.Lotion is dry by obtaining hydrophilic Co-Q10 after spray drying after high-pressure homogeneous
Powder, Co-Q10 content is 5% in dry powder, has good dispersibility in water.
Above-mentioned hydrophilic coenzyme q 10 dry is taken, obtains Co-Q10 chewable tablets by direct tablet compressing after following table 1 proportion mixing.
Table 1
Embodiment 2
400g Co-Q10 (source: Zhejiang Medicine Co) is heated to 50 DEG C of formation molten liquids.
600g starch Sodium Octenyl Succinate is mixed with 150mL water, and heating is kept for 0.5 hour at 80 DEG C under stirring state, makes octene
Base succinic acid starch sodium is completely dissolved to obtain starch Sodium Octenyl Succinate solution.Co-Q10 molten liquid is added to octenyl
In succinic acid starch sodium solution, while high speed shear state is kept, shear rate keeps 10000rpm, obtains oil-in-water type coenzyme
Q10 lotion, mean droplet size is detected as 0.5 μm by 3000 laser diffraction granularity distribution instrument of MasterSizer in lotion.
By oil-in-water type Co-Q10 lotion, by PhD-TECH high pressure homogenizer, that high pressure is carried out under 8000psi pressure is equal
After matter, emulsion droplet average grain diameter reaches 500nm.Lotion after high-pressure homogeneous is close by obtaining after spray congealing-starch bed liquefaction drying
Aqueous Co-Q10 particle, Co-Q10 content is 40% in particle, has good dispersibility in water.
Above-mentioned hydrophilic Co-Q10 particle is taken, obtains Co-Q10 chewable tablets by direct tablet compressing after following table 2 proportion mixing.
Table 2
| Title | Mg/ piece | Remarks |
| Co-Q10 particle 40% | 120 | / |
| Synthesize VE 50%CWS | 100 | Zhejiang Medicine Co |
| Mannitol (powder) | 525 | Xi'an good harvest biotechnology company |
| Lactose (particle) | 300 | Bioengineering Co., Ltd, Changzhou nangzan |
| Vitamin C | 25 | Shi Yao group |
| Low-substituted hydroxypropyl cellulose | 106 | Anhui mountains and rivers pharmaceutic adjuvant |
| Strawberry essence | 12 | Tangchao Food Industry Co., Ltd., Tianjin |
| Magnesium stearate | 12 | Anhui mountains and rivers pharmaceutic adjuvant |
| It amounts to | 1200 | / |
Embodiment 3
600g Co-Q10 (source: Zhejiang Medicine Co) is heated to 50 DEG C of formation molten liquids.
400g gelatin is mixed with 3600mL water, under stirring state heating kept for 1.5 hours at 70 DEG C, make gelatin be completely dissolved to obtain it is bright
Sol solution.Co-Q10 molten liquid is added in gelatin solution, while keeping high speed shear state, shear rate is kept
20000rpm obtains oil-in-water type Co-Q10 lotion, and mean droplet size is spread out by 3000 laser of MasterSizer in lotion
It penetrates particles distribution instrument and is detected as 2.0 μm.
By oil-in-water type Co-Q10 lotion, by PhD-TECH high pressure homogenizer, that high pressure is carried out under 15000psi pressure is equal
After matter, emulsion droplet average grain diameter reaches 100nm.Lotion after high-pressure homogeneous is dry by obtaining hydrophilic Co-Q10 after spray drying
Powder, Co-Q10 content is 60% in dry powder, has good water dispersible.
Above-mentioned hydrophilic coenzyme q 10 dry is taken, obtains Co-Q10 chewable tablets by direct tablet compressing after following table 3 proportion mixing.
Table 3
Embodiment 4
400g reduced coenzyme Q 10 (source: Zhejiang Medicine Co) is heated to 50 DEG C of formation
Molten liquid.600g gelatin is mixed with 1000mL water, and heating is kept for 1.5 hours at 70 DEG C under stirring state, keeps gelatin completely molten
Solution obtains gelatin solution.Co-Q10 molten liquid is added in gelatin solution, while keeping high speed shear state, shear rate
12000rpm is kept, obtains oil-in-water type reduced coenzyme Q 10 lotion, mean droplet size passes through MasterSizer in lotion
3000 laser diffraction granularity distribution instruments are detected as 2.4 μm.
Oil-in-water type reduced coenzyme Q 10 lotion is carried out under 12000psi pressure by PhD-TECH high pressure homogenizer
After high-pressure homogeneous, emulsion droplet average grain diameter reaches 180nm.Lotion after high-pressure homogeneous is by obtaining hydrophilic reduction after spray drying
Type coenzyme q 10 dry, reduced coenzyme Q 10 content is 40% in dry powder, has good water dispersible.
Above-mentioned hydrophilic coenzyme q 10 dry is taken, obtains Co-Q10 chewable tablets by direct tablet compressing after following table 4 proportion mixing.
Table 4
| Title | Mg/ piece | Remarks |
| Coenzyme q 10 dry 40% | 650 | / |
| VC powder | 175 | Rivers and mountains pharmacy |
| Sorbierite | 200 | Xi'an good harvest biotechnology company |
| Xylitol (particle) | 210 | Shandong Longli Biology Science and Technology Co., Ltd |
| Malic acid | 15 | Xi'an good harvest biotechnology company |
| Magnesium stearate | 16 | Anhui mountains and rivers pharmaceutic adjuvant |
| Flavoring apple essence | 18 | Tangchao Food Industry Co., Ltd., Tianjin |
| Silica | 16 | Anhui mountains and rivers pharmaceutic adjuvant |
| It amounts to | 1300 | / |
Take above-mentioned reduced coenzyme Q 10 dry powder filling hard capsule, can also be mixed to get electuary with dextrin etc., and with it is other
Water dispersant is mixed to get emulsion, may be added to and prepares drinks in beverage.
Comparing embodiment 5
Co-Q10 crystal powder is taken, obtains Co-Q10 chewable tablets by direct tablet compressing after following table 5 proportion mixing.
Table 5
It is not easily molded in tableting processes, it is easy sliver, the later period is easy sticking, and obtained chewable tablets darkens, and mouthfeel is not
It is good, there is a kind of " dregs " sense.
Embodiment 6: bioavilability comparative test
Example 1, embodiment 2, sample carries out bioavilability comparative test in comparing embodiment 5, is implemented with comparing
Sample is as control in example 5.Dosage is based on Co-Q10 weight, 1 time a day, each 48mg.60 people of health volunteer, male
Female is fifty-fifty, every group of 20 people, and the age 40 ± 8 years old, 165 ± 4cm of height, 63 ± 8 kilograms of weight.Subject is through comprehensive physical examination, liver kidney
Function is normal, Pass Test requirement, and during test and test does not take other medicines in first 2 months, unified diet during test.
Testing program and data processing reference literature: Xiao Shuhua, Wei Guangli etc., the human bioavailability of coenzyme-Q _10 tablet
Research, Chinese Clinical pharmacology and acology, 2000,5 (1), 39-41.Test result shows compared with the control group, to press
AUC(0-t)It counts, the bioavilability of sample is respectively to be higher by 47% and 64% in embodiment 1 and embodiment 2, has conspicuousness poor
It is different.The bioavilability of sample also has same significant difference in embodiment 3 and embodiment 4.
The present invention is illustrated by above embodiments, it is not limited to above-described particular example and implementation
Scheme is the purpose that it is enumerated at this those of skill in the art is helped to practice the present invention.Skill in any this field
Art personnel can be further improved and perfect without departing from the spirit and scope of the present invention.The present invention is only sent out by this
The limitation of the content and range of bright claim, intention, which covers, all is included in the present invention as defined by appendix claim
Alternative and equivalent program in spirit and scope.
Claims (12)
1. a kind of preparation method of the Co-Q10 chewable tablets of high bioavilability, the preparation method comprises the following steps:
(a) heating melting crystal Co-Q10 carries out the Co-Q10 of molten with hydrophilic gel liquid solution under high speed shear
Mixing, to form oil-in-water type emulsion droplet；
(b) the oil-in-water type emulsion droplet of step (a) is crushed by high-pressure homogeneous effect, to obtain nano-dispersion
Emulsion droplet；
(c) utilize spray drying or spray congealing-starch bed fluidized drying technology by the cream of the nano-dispersion of step (b)
Shape is titrated, to obtain hydrophilic coenzyme q 10 dry or particle；And
(d) the hydrophilic coenzyme q 10 dry or particle of step (c) are mixed with filler, is directly pressed after mixing
Piece, to obtain the Co-Q10 chewable tablets of high bioavilability.
2. preparation method as described in claim 1, wherein in step (a), the hydrophilic colloid be gelatin, Arabic gum,
Or starch Sodium Octenyl Succinate.
3. preparation method as claimed in claim 2, wherein in step (a), the hydrophilic colloid is dissolved in 60~80 DEG C of water
In, to obtain hydrophilic gel liquid solution.
4. preparation method as described in claim 1, wherein in step (a), the temperature of heating melting crystal Co-Q10 is 50
The Co-Q10 of DEG C molten formed above.
5. preparation method as described in claim 1, wherein in step (a), the Co-Q10 of the molten with it is described hydrophilic
Property colloidal solution is mixed under high speed shear, shear rate 5000-20000rpm.
6. preparation method as claimed in claim 5, wherein in step (a), emulsion droplet average grain diameter is 0.5-4.0 μm after shearing.
7. preparation method as described in claim 1, wherein in step (b), acted on by high-pressure homogeneous by the institute of step (a)
It states oil-in-water type emulsion droplet to be crushed to obtain the emulsion droplet of nano-dispersion, the high-pressure homogeneous pressure is 8000-30000psi；
The average grain diameter of the emulsion droplet of nano-dispersion after high-pressure homogeneous is 100-1000nm.
8. preparation method as described in claim 1, wherein in step (c), the hydrophilic coenzyme q 10 dry or particle
Middle Co-Q10 content is 5-60wt.%.
9. preparation method as described in claim 1, wherein in step (d), the filler is xylitol, sorbierite, sweet dew
Sugar alcohol or lactose.
10. the preparation method as described in claim 1~9 is any, wherein further include release agent, glidant, adhesive, seasoning
Agent, nutrient；The release agent be magnesium stearate, the glidant be silica, the pico- crystalline cellulose of described adhesive or
Low-substituted hydroxypropyl cellulose, the flavoring agent are citric acid, malic acid, essence, fruit powder, and the nutrient is vitamin E, dimension life
Plain A, vitamin C.
11. a kind of Co-Q10 chewing of the high bioavilability using the method preparation as described in claim 1~10 is any
Piece, the Co-Q10 chewable tablets include hydrophilic coenzyme q 10 dry or particle and filler；Wherein, described hydrophilic auxiliary
Enzyme Q10 dry powder or particle include the internal layer containing coenzyme q 10 dry or particle and the outer layer containing hydrophilic colloid.
12. Co-Q10 chewable tablets as claimed in claim 11, wherein the hydrophilic colloid be gelatin, Arabic gum or
Starch Sodium Octenyl Succinate, the filler are xylitol, sorbierite, mannitol or lactose.
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| CN113396979A (en) * | 2021-06-30 | 2021-09-17 | 华南理工大学 | Milk containing coenzyme Q10 and preparation method thereof |
| CN114504557A (en) * | 2021-11-05 | 2022-05-17 | 南京德瑞源医药科技有限公司 | Water-soluble composite vitamin dry powder and preparation method and application thereof |
| CN114504103A (en) * | 2021-11-05 | 2022-05-17 | 南京德瑞源医药科技有限公司 | Preparation method of rapidly-dispersed particles containing nano-scale coenzyme Q10 |
| CN115812971A (en) * | 2021-12-13 | 2023-03-21 | 浙江康恩贝集团医疗保健品有限公司 | Chewable tablet rich in zinc and selenium elements and preparation method thereof |
| CN117837754A (en) * | 2024-03-08 | 2024-04-09 | 中国农业大学 | Amorphous coenzyme Q10 with improved solubility and preparation method thereof |
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| CN1961869A (en) * | 2006-11-30 | 2007-05-16 | 重庆市力扬医药开发有限公司 | Orally disintegrating tablet of coenzyme Q10 and preparation method thereof |
| US20090060993A1 (en) * | 2007-09-04 | 2009-03-05 | Joseph Schwarz | Solid pharmaceutical composition for enhanced delivery of coenzyme q-10 and ubiquinones |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113396979A (en) * | 2021-06-30 | 2021-09-17 | 华南理工大学 | Milk containing coenzyme Q10 and preparation method thereof |
| CN114504557A (en) * | 2021-11-05 | 2022-05-17 | 南京德瑞源医药科技有限公司 | Water-soluble composite vitamin dry powder and preparation method and application thereof |
| CN114504103A (en) * | 2021-11-05 | 2022-05-17 | 南京德瑞源医药科技有限公司 | Preparation method of rapidly-dispersed particles containing nano-scale coenzyme Q10 |
| CN115812971A (en) * | 2021-12-13 | 2023-03-21 | 浙江康恩贝集团医疗保健品有限公司 | Chewable tablet rich in zinc and selenium elements and preparation method thereof |
| CN117837754A (en) * | 2024-03-08 | 2024-04-09 | 中国农业大学 | Amorphous coenzyme Q10 with improved solubility and preparation method thereof |
| CN117837754B (en) * | 2024-03-08 | 2024-05-28 | 中国农业大学 | Amorphous coenzyme Q10 with improved solubility and preparation method thereof |
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