CN109453130A - Buccal tablet and preparation method thereof containing caffeine - Google Patents
Buccal tablet and preparation method thereof containing caffeine Download PDFInfo
- Publication number
- CN109453130A CN109453130A CN201811588987.8A CN201811588987A CN109453130A CN 109453130 A CN109453130 A CN 109453130A CN 201811588987 A CN201811588987 A CN 201811588987A CN 109453130 A CN109453130 A CN 109453130A
- Authority
- CN
- China
- Prior art keywords
- buccal tablet
- caffeine
- vitamin
- stearate
- sugar alcohol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 title claims abstract description 196
- 239000006189 buccal tablet Substances 0.000 title claims abstract description 99
- 229940046011 buccal tablet Drugs 0.000 title claims abstract description 97
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 title claims abstract description 95
- 229960001948 caffeine Drugs 0.000 title claims abstract description 95
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 title claims abstract description 95
- 238000002360 preparation method Methods 0.000 title claims abstract description 11
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 claims abstract description 80
- 150000005846 sugar alcohols Chemical class 0.000 claims abstract description 42
- 229960003080 taurine Drugs 0.000 claims abstract description 40
- 229940088594 vitamin Drugs 0.000 claims abstract description 25
- 229930003231 vitamin Natural products 0.000 claims abstract description 25
- 235000013343 vitamin Nutrition 0.000 claims abstract description 25
- 239000011782 vitamin Substances 0.000 claims abstract description 25
- 150000003722 vitamin derivatives Chemical class 0.000 claims abstract description 25
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims abstract description 24
- 102000040350 B family Human genes 0.000 claims abstract description 20
- 108091072128 B family Proteins 0.000 claims abstract description 20
- 239000000203 mixture Substances 0.000 claims description 57
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 36
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 34
- DFPAKSUCGFBDDF-UHFFFAOYSA-N nicotinic acid amide Natural products NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims description 33
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- 239000011570 nicotinamide Substances 0.000 claims description 29
- 229960003966 nicotinamide Drugs 0.000 claims description 29
- 229940114926 stearate Drugs 0.000 claims description 23
- 239000000463 material Substances 0.000 claims description 20
- 235000019359 magnesium stearate Nutrition 0.000 claims description 18
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 claims description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 5
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- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims description 4
- 229930003779 Vitamin B12 Natural products 0.000 claims description 4
- 229930003537 Vitamin B3 Natural products 0.000 claims description 4
- FDJOLVPMNUYSCM-WZHZPDAFSA-L cobalt(3+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+3].N#[C-].N([C@@H]([C@]1(C)[N-]\C([C@H]([C@@]1(CC(N)=O)C)CCC(N)=O)=C(\C)/C1=N/C([C@H]([C@@]1(CC(N)=O)C)CCC(N)=O)=C\C1=N\C([C@H](C1(C)C)CCC(N)=O)=C/1C)[C@@H]2CC(N)=O)=C\1[C@]2(C)CCC(=O)NC[C@@H](C)OP([O-])(=O)O[C@H]1[C@@H](O)[C@@H](N2C3=CC(C)=C(C)C=C3N=C2)O[C@@H]1CO FDJOLVPMNUYSCM-WZHZPDAFSA-L 0.000 claims description 4
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims description 4
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- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 claims description 4
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- 229940011671 vitamin b6 Drugs 0.000 claims description 4
- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 claims description 3
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 3
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- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 3
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- 239000008116 calcium stearate Substances 0.000 claims description 3
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 3
- 239000000845 maltitol Substances 0.000 claims description 3
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims description 3
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- 229940114930 potassium stearate Drugs 0.000 claims description 3
- ANBFRLKBEIFNQU-UHFFFAOYSA-M potassium;octadecanoate Chemical compound [K+].CCCCCCCCCCCCCCCCCC([O-])=O ANBFRLKBEIFNQU-UHFFFAOYSA-M 0.000 claims description 3
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- 235000019164 vitamin B2 Nutrition 0.000 claims description 3
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- GHOKWGTUZJEAQD-UHFFFAOYSA-N Chick antidermatitis factor Natural products OCC(C)(C)C(O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-UHFFFAOYSA-N 0.000 claims description 2
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- FAPWYRCQGJNNSJ-UBKPKTQASA-L calcium D-pantothenic acid Chemical compound [Ca+2].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O.OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O FAPWYRCQGJNNSJ-UBKPKTQASA-L 0.000 claims description 2
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- DCXXMTOCNZCJGO-UHFFFAOYSA-N tristearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 4
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Abstract
The invention discloses a kind of buccal tablet and preparation method thereof containing caffeine.Every buccal tablet includes 4~7mg of caffeine, 0.7~1.6mg of B family vitamin, 3.5~8mg of 3.5~8.0mg of taurine, 338~773mg of sugar alcohol and stearate.Caffeine in buccal tablet of the invention instant in the oral cavity can absorb.
Description
Technical field
The present invention relates to a kind of buccal tablet and preparation method thereof containing caffeine.
Background technique
Caffeine is the white bitter taste powder for belonging to the alkaloid of methyl xanthine, chemical formula C8H10N4O2, chemical name
It is 1,3,7- trimethyl xanthines or 3,7- dihydro -1,3,7 trimethyl -1H- purine -2,6- diketone, molecular weight 194.19.Coffee
Coffee can be improved the content of intracellular adenosine cyclophosphate, excitement is big because being a kind of alkaloid extracting from tealeaves, coffee berry
Cortex is inspired enthusiasm, and attention, self-confidence and working efficiency and enthusiasm are improved；Enhance alertness and reduce tired sense,
The ability that enhancing your vigilance property and maintenance persistently work；Enhance recognition capability, shorten the reaction time, and instantaneous oral memory can be improved
Power moderately using dispelling tired excitor nerve, therefore is widely used as adjuvant is refreshed oneself.
CN108402363A discloses a kind of pick-me-up, selects 16 carbamide of N- benzyl, caffeine, taurine, flesh
Alcohol, niacinamide, vitamin B1, vitamin B6 etc. are formulated as primary raw material, wherein content of caffeine be 0.01~
0.04%.Pick-me-up is absorbed in a manner of taking orally and being absorbed by stomach, and it is irritating to stomach to take caffeine for a long time
Effect.
A kind of chewing gum with refreshing function is disclosed in CN101595933A, each component accounts for chewing gum weight ratio such as
Under: taurine 2~20%, caffeine 0.1~1%, sweetener 30~50% and matrix 20~50%, can relieve fatigue,
Excited spirit.Main refreshing function ingredient is taurine in the chewing gum, and content of caffeine is lower；Chewing gum component release time
It is short and uneven, cause effective component to discharge absorption in the big concentration of initial chew, and middle and later periods concentration significantly reduces until being
Zero, influence the refresh oneself stability and duration of effect.
A kind of candy containing caffeine is disclosed in CN1242686C, wherein containing the coffee of 50~100mg in every candy
Coffee can play restoring consciouness, refresh oneself, resist because of, the Radix Glycyrrhizae of 20~100mg, the lily of the ginseng of 25~150mg and 25~100mg
Effect of fatigue.The candy contains the caffeine of large dosage, and a large amount of caffeines enter gastrointestinal tract absorption, aggravate GI irritation,
Damage health.
A kind of anti-fatigue candy with natural coffeine (in terms of 1 ton of product), including 30~150g are disclosed in CN1168233A
Natural caffeine, 4.5~7.6kg of Radix Astragali, 1.8~3.1kg of mulberry fruit, 2.2~6.7kg of American Ginseng, pine nut 6.3~10kg is white
3.4~5.1kg of art, 2.1~5.2kg of lily have restoring consciouness, eliminate fatigue, regain one's strength, inspire enthusiasm and improve ability to work
Effect.Main active is medicinal material, especially Radix Astragali in the candy；And the content of caffeine is very low, effect is very
It is limited.
Summary of the invention
In view of this, the caffeine contained can it is an object of that present invention to provide a kind of buccal tablet containing caffeine
Rapidly by buccal absorption in buccal tablet course of dissolution.
Another object of the present invention is to provide the preparation methods of the buccal tablet containing caffeine.
On the one hand, the present invention provides a kind of buccal tablet containing caffeine, and every buccal tablet includes 4~7mg of caffeine, B
0.7~1.6mg of family vitamin, 3.5~8mg of 3.5~8.0mg of taurine, 338~773mg of sugar alcohol and stearate.
Buccal tablet according to the present invention, it is preferable that the sugar alcohol is selected from maltitol, D-sorbite, xylitol, lactose
One of alcohol, antierythrite or mannitol are a variety of.
Buccal tablet according to the present invention, it is preferable that the stearate is selected from magnesium stearate, calcium stearate, odium stearate
With one of potassium stearate or a variety of.
Buccal tablet according to the present invention, it is preferable that the weight ratio of the sugar alcohol and stearate is 70~110:1.
Buccal tablet according to the present invention, it is preferable that every buccal tablet also includes 0.5~5mg of auxiliary material, and the auxiliary material is selected from color
One of element and essence are a variety of.
Buccal tablet according to the present invention, it is preferable that the B family vitamin is selected from vitamin B1, vitamin B2, vitamin
At least one of B3, niacinamide, vitamin B5, vitamin B6, Vitamin B9 and vitamin B12.
Buccal tablet according to the present invention, it is preferable that every buccal tablet include 5~6mg of caffeine, niacinamide 0.9~
1.3mg, 5~7mg of 4.5~6.5mg of taurine, 480~550mg of D-sorbite and magnesium stearate.
Buccal tablet according to the present invention, it is preferable that every buccal tablet is only grouped as by following group: 5~6mg of caffeine, cigarette
0.9~1.3mg of amide, 4.5~6.5mg of taurine, 480~550mg of D-sorbite, 5~7mg of magnesium stearate and essence 0.5~
1mg。
On the other hand, the present invention provides a kind of preparation method of buccal tablet containing caffeine, includes the following steps:
(1) raw material comprising caffeine, B family vitamin, taurine and part sugar alcohol is crushed and is uniformly mixed, obtained
First mixture, the first mixture partial size are 30 mesh or less；
(2) first mixture and remaining sugar alcohol and stearate are mixed to get the second mixture, the residue
The partial size of sugar alcohol is 16~60 mesh；
(3) the second mixture compression molding is obtained into buccal tablet, pressure needed for tabletting is 15~25kgf.
Preparation method according to the present invention, it is preferable that in step (3), required pressure is 18~22kgf.
Containing the caffeine of given dose in buccal tablet of the present invention, at the same be added in buccal tablet a certain amount of sugar alcohol and
Stearate can further control the dissolution rate of caffeine, and such caffeine, which dissolves, to be fully absorbed by oral cavity.Mouth containing
During piece is containing changing, not extra caffeine enters gastrointestinal tract substantially, avoids stimulating gastrointestinal road.
Specific embodiment
The present invention is further illustrated combined with specific embodiments below, but protection scope of the present invention is not limited to
This.
< contains the buccal tablet > of caffeine
Research has shown that the absorption rate of caffeine in the oral cavity is 0.65mg/min.The present invention passes through to coffee in buccal tablet
Coffee because content and sugar alcohol and stearate content control, make caffeine oral cavity it is buccal during it is instant i.e. absorption.This
Sample can avoid damage to stomach.
Buccal tablet for the every present invention containing caffeine, comprising caffeine, B family vitamin, taurine, sugar alcohol and
Stearate.The weight of every buccal tablet is 350~800mg, preferably 400~700mg, more preferably 450~600mg.This
The content of caffeine is 4~7mg, preferably 5~6mg in invention.Containing the caffeine of given dose in buccal tablet of the present invention,
It, can be by stabilization, equably dissolve when including of oral cavity.And caffeine is dissolved and is fully absorbed by oral cavity, can quickly be sent out
Wave the effect of refreshing the mind.
Sugar alcohol in the present invention is selected from maltitol, D-sorbite, xylitol, lactitol, antierythrite or mannitol
One of or a variety of, preferably one of D-sorbite, xylitol or mannitol or a variety of, more preferably sorbose
Alcohol.The weight of sugar alcohol described in every buccal tablet can for 338~773mg, preferably 480~550mg, more preferably 500~
530mg.Sugar alcohol can control the dissolution rate of caffeine in buccal tablet, so that caffeine is inhaled by oral cavity while dissolution
It receives.
According to the preferred embodiment of the present invention, the stearate be selected from magnesium stearate, calcium stearate, odium stearate and
One of potassium stearate is a variety of, preferably magnesium stearate.The weight of stearate in every buccal tablet is 3.5~8mg,
Preferably 4~7.5mg, more preferably 4~6mg.Stearate can further control the dissolution rate of caffeine in buccal tablet,
So that caffeine is while dissolution i.e. by buccal absorption.
It is an unexpected discovery of the invention that by caffeine, sugar alcohol and stearate combination can control in buccal tablet well
Caffeine dissolution rate.In the present invention, it is preferable that the weight ratio of the sugar alcohol and stearate be 70~110:1, preferably 75
~100:1, more preferably 80~97:1.
B family vitamin in the present invention can be selected from vitamin B1, vitamin B2, vitamin B3, niacinamide, vitamin
At least one of B5, vitamin B6, Vitamin B9 or vitamin B12, such as vitamin B1, vitamin B3, niacinamide, dimension life
At least one of plain B6 or vitamin B12, preferably niacinamide.In every buccal tablet the weight of B family vitamin be 0.7~
1.6mg, preferably 0.8~1.3mg, more preferably 0.9~1.1mg.Caffeine can be assisted to play a role in this way, raising is refreshed oneself
The effect of restoring consciouness.
The weight of taurine is 3.5~8mg, preferably 4.5~7mg, more preferably 5~6.5mg in the present invention.The present invention
In taurine there is auxiliary caffeine the effect of playing a role, refreshing the mind.
It finds of the inventionly, by caffeine, B family vitamin and taurine combination can promote caffeine to play well
Refresh the mind effect, and improves the caffeine dissolution rate in buccal tablet.In the present invention, it is preferable that the B family vitamin and ox
The weight ratio of sulfonic acid is 1:3~7, preferably 1:4~6, more preferably 1:5.
Buccal tablet of the present invention can also include auxiliary material, and the auxiliary material is selected from one of pigment and essence or a variety of.Every
The weight for the auxiliary material that buccal tablet contains is 0.5~5mg, preferably 1~4mg, more preferably 2~3mg.Pigment is preferably Natural Food
With pigment, the natural food colour is preferably shellac color, carthamin yellow, beet red, capsorubin, turmeric, β carrot
One of element, copper chlorophyllin sodium salt, dark reddish brown element are a variety of, more preferably carthamin yellow, beet red, turmeric, β carrot
Element is further preferably turmeric, bata-carotene.Essence can be in fruit essence, Mint Essence, flavoring rose essence and osmanthus flower fragrance
It is any.As a preferred embodiment of the invention, the auxiliary material only includes essence, and every buccal tablet contains essence
0.5~5mg, preferably 0.5~1.5mg, more preferably 1mg.
According to embodiment of the present invention, the every buccal tablet of the invention containing caffeine includes following component:
5~6mg of caffeine, 0.9~1.3mg of niacinamide, 4.5~6.5mg of taurine, 480~550mg of D-sorbite and magnesium stearate 5
~7mg.According to the preferred embodiment of the present invention, the every buccal tablet of the invention containing caffeine includes following component: coffee
Coffee because 5~6mg, 0.9~1.3mg of niacinamide, 4.5~6.5mg of taurine, 480~550mg of D-sorbite, magnesium stearate 5~
1~4mg of 7mg and essence.
According to another implementation of the invention, the buccal tablet of the invention containing caffeine, and every buccal tablet is only
It is grouped as by following group: 5~6mg of caffeine, 0.9~1.3mg of niacinamide, 4.5~6.5mg of taurine, D-sorbite 480~
5~7mg of 550mg and magnesium stearate.According to the preferred embodiment of the present invention, the buccal tablet of the invention containing caffeine, and
Every buccal tablet is only grouped as by following group: 5~6mg of caffeine, 0.9~1.3mg of niacinamide, 4.5~6.5mg of taurine, mountain
480~550mg of pears sugar alcohol, 1~4mg of 5~7mg of magnesium stearate and essence.
< preparation method >
The preparation method of buccal tablet containing caffeine of the invention includes the following steps:
(1) by the raw material comprising caffeine, B family vitamin, taurine and part sugar alcohol be crushed to partial size be 30 mesh with
Under, it is uniformly mixed, obtains the first mixture；
(2) first mixture and remaining sugar alcohol and stearate are mixed to get the second mixture；The residue
The partial size of sugar alcohol is 16~60 mesh；
(3) the second mixture compression molding is obtained into buccal tablet, pressure needed for compression molding is 15~25kgf.
In the present invention, auxiliary material can also be contained in raw material.B family vitamin, taurine, auxiliary material, sugar alcohol and stearate
As described above, which is not described herein again.
In step (1), first by each crushing material to partial size be 30 mesh hereinafter, preferably 25 mesh hereinafter, more preferably 20
Below mesh.Using above-mentioned partial size, is conducive to each material and is uniformly mixed.The part sugar alcohol is can be sugar alcohol total weight 1/5
~4/5, preferably 1/3~3/5, more preferably 1/2.It can be by smashed caffeine, B family vitamin, taurine, optional
Auxiliary material and part sugar alcohol conventional method are uniformly mixed；Can also by smashed caffeine, B family vitamin, taurine and
Optional auxiliary material is uniformly mixed, and then gradient mixing method, such as equivalent gradient mixing method is used to be uniformly mixed with part sugar alcohol.Root
According to an embodiment of the invention, caffeine, B family vitamin, taurine and optional auxiliary material are uniformly mixed first, obtained
To primary mix；Then by the primary mix with etc. the sugar alcohols of quality be uniformly mixed, repeat 2~5 times, obtain the first mixing
Object.Above-mentioned equivalent gradient mixing method is conducive to caffeine, B family vitamin, taurine, auxiliary material and is uniformly mixed with sugar alcohol.
In step (2), the partial size of remaining sugar alcohol is 16~60 mesh, preferably 20~50 mesh, also preferably 25~45 mesh, more
Preferably 30~40 mesh.Remaining sugar alcohol uses above-mentioned partial size, is conducive to the dissolution rate for controlling caffeine.
It is 15~25kgf, preferably 18~22kgf to the pressure that second mixture applies in step (3).Using
The tablet that above-mentioned pressure obtains is conducive to the dissolution rate for further improving caffeine.Buccal tablet can be conventional sheet in the present invention
Type, or the shape of Special-shaped sheet, the buccal tablet is selected from one of circle, pentalpha, triangle, rectangular.
According to embodiment of the present invention, include the following steps:
(1) caffeine and B family vitamin, taurine, optional auxiliary material and part sugar alcohol are crushed to partial size is 25 mesh
Below；Caffeine is uniformly mixed with B family vitamin, taurine and optional auxiliary material, primary mix is obtained, by the primary
Mixture is uniformly mixed with the part sugar alcohol using equivalent gradient mixing method, and the first mixture is obtained；The part sugar alcohol is
The 1/3~3/5 of sugar alcohol total weight；
(2) remaining sugar alcohol is crushed to partial size is 25~45 mesh, and by first mixture and the remaining sugar
Alcohol, stearate are uniformly mixed, and obtain the second mixture；
(3) the pressure compression molding that second mixture is imposed to 18~22kgf, obtains buccal tablet.
In the above-mentioned methods, B family vitamin is preferably niacinamide, and sugar alcohol is D-sorbite, and the auxiliary material is essence.
Embodiment 1
The formula of buccal tablet is as follows:
Caffeine 5g, niacinamide 1g, taurine 5g, D-sorbite 483g, essence 1g and magnesium stearate 5g.
It is prepared as follows buccal tablet:
(1) 5g caffeine, 1g niacinamide, 5g taurine, 1g essence and 241.5g D-sorbite are crushed to 25 mesh.It will
5g caffeine, 1g niacinamide, 5g taurine and 1g essence are uniformly mixed and obtain primary mix, then by the primary mix
It is uniformly mixed with the 241.5g D-sorbite using equivalent gradient mixing method, obtains the first mixture；
(2) remaining 241.5g D-sorbite is crushed to partial size is 30 mesh, and hard with first mixture and 5g
Fatty acid magnesium is uniformly mixed, and obtains the second mixture；
(3) the pressure tabletting that second mixture imposes 20kgf is obtained into buccal tablet, every 500mg.The buccal tablet
Dissolution rate test result referring to table 1.
Embodiment 2
The formula of buccal tablet is as follows:
Caffeine 3.5g, niacinamide 0.8g, taurine 4g, D-sorbite 431g, essence 1g and magnesium stearate 4.5g.
It is prepared as follows buccal tablet:
(1) 3.5g caffeine, 0.8g niacinamide, 4g taurine, 1g essence and 215.5g D-sorbite are crushed to 30
The 3.5g caffeine, 0.8g niacinamide, 4g taurine and 1g essence are uniformly mixed obtain primary mix first, so by mesh
The primary mix is uniformly mixed with the 215.5g D-sorbite using equivalent gradient mixing method afterwards, obtains the first mixing
Object；
(2) by remaining 215.5g D-sorbite be crushed to partial size be 25 mesh, and with first mixture and 4.5g
Magnesium stearate is uniformly mixed, and obtains the second mixture；
(3) the pressure tabletting that second mixture imposes 20kgf is obtained into buccal tablet, every 750mg.The buccal tablet
Dissolution rate test result referring to table 1.
Embodiment 3
The formula of buccal tablet is as follows:
Caffeine 5g, niacinamide 1g, taurine 4g, D-sorbite 533g, essence 1g and magnesium stearate 6g.
It is prepared as follows buccal tablet:
(1) 5g caffeine, 1g niacinamide, 4g taurine, 1g essence and 266.5g D-sorbite are crushed to 28 mesh, it is first
First the 5g caffeine, 1g niacinamide, 4g taurine and 1g essence are uniformly mixed and obtain primary mix, it then will be described first
Grade mixture is uniformly mixed with the 266.5g D-sorbite using equivalent gradient mixing method, and the first mixture is obtained；
(2) remaining 266.5g D-sorbite is crushed to partial size is 35 mesh, and hard with first mixture and 6g
Fatty acid magnesium is uniformly mixed, and obtains the second mixture；
(3) the pressure tabletting that second mixture imposes 18kgf is obtained into buccal tablet, every 600mg.The buccal tablet
Dissolution rate test result referring to table 1.
Embodiment 4
The formula of buccal tablet is as follows:
Caffeine 7g, niacinamide 2g, lysine 6g, D-sorbite 577g, essence 1g and magnesium laurylsulfate 7g.
It is prepared as follows buccal tablet:
(1) 7g caffeine, 2g niacinamide, 6g lysine, 1g essence and 288.5g D-sorbite are crushed to 26 mesh, it is first
First the 7g caffeine, 2g niacinamide, 6g lysine and 1g essence are uniformly mixed and obtain primary mix, it then will be described first
Grade mixture is uniformly mixed with the 288.5g D-sorbite using equivalent gradient mixing method, and the first mixture is obtained；
(2) by remaining 288.5g D-sorbite be crushed to partial size be 20 mesh, and with first mixture and the 7g month
Cinnamic alcohol magnesium sulfate is uniformly mixed, and obtains the second mixture；
(3) the pressure tabletting that second mixture imposes 22kgf is obtained into buccal tablet, every 400mg.The buccal tablet
Dissolution rate test result referring to table 1.
Embodiment 5
The formula of buccal tablet is as follows:
Caffeine 6g, niacinamide 1.5g, taurine 6.5g, D-sorbite 474g, Aspartame 3g, essence 1g and tristearin
Sour magnesium 6g.
It is prepared as follows buccal tablet:
(1) by 6g caffeine, 1.5g niacinamide, 6.5g taurine, 3g Aspartame, 1g essence and 237g D-sorbite
21 mesh are crushed to, are first mixed the 6g caffeine, 1.5g niacinamide, 6.5g taurine, 3g Aspartame and 1g essence equal
It is even to obtain primary mix, then the primary mix is mixed with the 237g D-sorbite using equivalent gradient mixing method
Uniformly, the first mixture is obtained；
(2) remaining 237g D-sorbite is crushed to partial size is 55 mesh, and stearic with first mixture and 6g
Sour magnesium is uniformly mixed, and obtains the second mixture；
(3) the pressure tabletting that second mixture imposes 20kgf is obtained into buccal tablet, every 498mg.The buccal tablet
Dissolution rate test result referring to table 1.
Embodiment 6
The formula of buccal tablet is as follows:
Caffeine 4g, vitamin B3 1g, methionine 4g, xylitol 433g, Aspartame 2g, essence 0.5g and tristearin
Sour magnesium 5.5g.
It is prepared as follows buccal tablet:
(1) by 4g caffeine, 1g vitamin B3,4g methionine, 2g Aspartame, 0.5g essence and 216.5g xylitol
15 mesh are crushed to, are first mixed the 4g caffeine, 1g vitamin B3,4g methionine, 2g Aspartame and 0.5g essence equal
It is even to obtain primary mix, then the primary mix is mixed with the 216.5g xylitol using equivalent gradient mixing method
Uniformly, the first mixture is obtained；
(2) remaining 216.5g xylosic alcohol powder is broken to partial size is 40 mesh, and hard with first mixture and 5.5g
Fatty acid magnesium is uniformly mixed, and obtains the second mixture；
(3) the pressure Tablet compression Compression that second mixture imposes 20kgf is obtained into buccal tablet, every 500mg.The mouth
The dissolution rate test result of lozenge is referring to table 1.
Comparative example 1
The D-sorbite 483g and magnesium stearate 5g in embodiment 1 are omitted, remaining condition is same as Example 1, institute
The dissolution rate test result of buccal tablet is obtained referring to table 1.
Comparative example 2
The D-sorbite 483g in embodiment 1 is omitted, remaining condition is identical as embodiment, the dissolution rate of gained buccal tablet
Test result is referring to table 1.
Comparative example 3
The magnesium stearate 5g in embodiment 1 is omitted, remaining condition is identical as embodiment, and the dissolution rate of gained buccal tablet is surveyed
Test result is referring to table 1.
Experimental example 1
1, experimental method
Using RC8MD intelligence digestion instrument respectively to the buccal tablet of the buccal tablet A of 6 embodiments 1,6 comparative examples 1,6 it is right
The buccal tablet of ratio 2, the buccal tablet of 6 comparative examples 3,6 comparative examples 4 buccal tablet carry out dissolution rate test respectively, intelligence is molten
500mL water is accommodated in the stripping rotor of instrument out, the revolving speed of intelligent digestion instrument is 200rpm, when reaching 37 ± 0.5 DEG C in stripping rotor,
Buccal tablet A is put into stripping rotor, carries out the dissolution of caffeine in buccal tablet from taking-up partially liq in stripping rotor every 1min
The test of degree takes the average value of 6 built-in testing results.
2, test result
Caffeine dissolution data is shown in Table 1.
Table 1, caffeine dissolution rate test result
As known from Table 1, the dissolution rate of the caffeine of embodiment 1 when reaching 10min dissolution rate be 98.92%, 12min when
Dissolution rate is 99.77%, is almost dissolved out.It is 0.65mg/min according to the absorption rate of caffeine in the oral cavity, it is seen that every
Caffeine in piece buccal tablet A is completely absorbed in complete dissolution.By comparative example 1 to 3 it is found that sugar alcohol and stearate
Play a significant role to the dissolution rate of control caffeine.
Present invention is not limited to the embodiments described above, without departing from the essence of the present invention, this field skill
Any deformation, improvement, the replacement that art personnel are contemplated that each fall within the scope of the present invention.
Claims (10)
1. a kind of buccal tablet containing caffeine, which is characterized in that every buccal tablet includes 4~7mg of caffeine, B family vitamin
0.7~1.6mg, 3.5~8mg of 3.5~8.0mg of taurine, 338~773mg of sugar alcohol and stearate.
2. buccal tablet according to claim 1, which is characterized in that the sugar alcohol is selected from maltitol, D-sorbite, xylose
One of alcohol, lactitol, antierythrite or mannitol are a variety of.
3. buccal tablet according to claim 1, which is characterized in that the stearate be selected from magnesium stearate, calcium stearate,
One of odium stearate and potassium stearate are a variety of.
4. buccal tablet according to claim 1, which is characterized in that the weight ratio of the sugar alcohol and stearate be 70~
110:1。
5. buccal tablet according to claim 1, which is characterized in that every buccal tablet also includes 0.5~5mg of auxiliary material, described
Auxiliary material is selected from one of pigment and essence or a variety of.
6. described in any item buccal tablets according to claim 1~5, which is characterized in that the B family vitamin is selected from vitamin
At least one in B1, vitamin B2, vitamin B3, niacinamide, vitamin B5, vitamin B6, Vitamin B9 and vitamin B12
Kind.
7. buccal tablet according to claim 1, which is characterized in that every buccal tablet includes 5~6mg of caffeine, niacinamide
0.9~1.3mg, 5~7mg of 4.5~6.5mg of taurine, 480~550mg of D-sorbite and magnesium stearate.
8. buccal tablet according to claim 1, which is characterized in that every buccal tablet is only grouped as by following group: caffeine 5
~6mg, 0.9~1.3mg of niacinamide, 4.5~6.5mg of taurine, 480~550mg of D-sorbite, 5~7mg of magnesium stearate and perfume (or spice)
0.5~1mg of essence.
9. the preparation method of described in any item buccal tablets according to claim 1~8, which comprises the steps of:
(1) raw material comprising caffeine, B family vitamin, taurine and part sugar alcohol is crushed and is uniformly mixed, it is mixed to obtain first
Object is closed, the first mixture partial size is 30 mesh or less；
(2) first mixture and remaining sugar alcohol and stearate are mixed to get the second mixture, the residue sugar alcohol
Partial size be 16~60 mesh；
(3) the second mixture compression molding is obtained into buccal tablet, pressure needed for tabletting is 15~25kgf.
10. preparation method according to claim 9, which is characterized in that in step (3), required pressure is 18~22kgf.
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