CN107049978A - Gliclazid in tablets and preparation method thereof - Google Patents
Gliclazid in tablets and preparation method thereof Download PDFInfo
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- CN107049978A CN107049978A CN201710118068.3A CN201710118068A CN107049978A CN 107049978 A CN107049978 A CN 107049978A CN 201710118068 A CN201710118068 A CN 201710118068A CN 107049978 A CN107049978 A CN 107049978A
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- gliclazid
- tablets
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- 229960000346 gliclazide Drugs 0.000 title claims abstract description 72
- BOVGTQGAOIONJV-UHFFFAOYSA-N gliclazide Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1CC2CCCC2C1 BOVGTQGAOIONJV-UHFFFAOYSA-N 0.000 title claims abstract description 42
- 238000002360 preparation method Methods 0.000 title claims abstract description 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 49
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 36
- BOVGTQGAOIONJV-BETUJISGSA-N 1-[(3ar,6as)-3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl]-3-(4-methylphenyl)sulfonylurea Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1C[C@H]2CCC[C@H]2C1 BOVGTQGAOIONJV-BETUJISGSA-N 0.000 claims abstract description 31
- 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 30
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims abstract description 30
- 239000008101 lactose Substances 0.000 claims abstract description 30
- 229920000881 Modified starch Polymers 0.000 claims abstract description 29
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 28
- 239000000741 silica gel Substances 0.000 claims abstract description 21
- 229910002027 silica gel Inorganic materials 0.000 claims abstract description 21
- 239000002245 particle Substances 0.000 claims description 57
- 238000001035 drying Methods 0.000 claims description 24
- 235000020985 whole grains Nutrition 0.000 claims description 20
- 238000002156 mixing Methods 0.000 claims description 19
- 238000005469 granulation Methods 0.000 claims description 10
- 230000003179 granulation Effects 0.000 claims description 10
- 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 description 7
- 239000002994 raw material Substances 0.000 claims description 5
- 238000004806 packaging method and process Methods 0.000 claims description 3
- 239000008213 purified water Substances 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 229920002472 Starch Polymers 0.000 claims 1
- 239000003292 glue Substances 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 210000004369 blood Anatomy 0.000 abstract description 7
- 239000008280 blood Substances 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 6
- 238000001727 in vivo Methods 0.000 abstract description 6
- 230000000857 drug effect Effects 0.000 abstract description 5
- 230000007774 longterm Effects 0.000 abstract description 3
- 238000005507 spraying Methods 0.000 abstract description 3
- 238000013268 sustained release Methods 0.000 abstract description 3
- 239000012730 sustained-release form Substances 0.000 abstract description 3
- 238000000034 method Methods 0.000 description 8
- 239000003814 drug Substances 0.000 description 7
- 239000000499 gel Substances 0.000 description 7
- 239000000377 silicon dioxide Substances 0.000 description 7
- 239000003643 water by type Substances 0.000 description 7
- 235000013339 cereals Nutrition 0.000 description 6
- 230000002218 hypoglycaemic effect Effects 0.000 description 4
- DCXXMTOCNZCJGO-UHFFFAOYSA-N tristearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 4
- 229940079593 drug Drugs 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 230000036470 plasma concentration Effects 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 229910052749 magnesium Inorganic materials 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 210000000496 pancreas Anatomy 0.000 description 2
- 210000002381 plasma Anatomy 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 206010018873 Haemoconcentration Diseases 0.000 description 1
- 241000282414 Homo sapiens Species 0.000 description 1
- 208000013016 Hypoglycemia Diseases 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 229940100389 Sulfonylurea Drugs 0.000 description 1
- JLRGJRBPOGGCBT-UHFFFAOYSA-N Tolbutamide Chemical compound CCCCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 JLRGJRBPOGGCBT-UHFFFAOYSA-N 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 description 1
- 238000003353 bioavailability assay Methods 0.000 description 1
- 230000023555 blood coagulation Effects 0.000 description 1
- 238000010241 blood sampling Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 229960004580 glibenclamide Drugs 0.000 description 1
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 230000009191 jumping Effects 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000575 pesticide Substances 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 229960005371 tolbutamide Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
-
- 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
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of gliclazid in tablets and preparation method thereof, the gliclazid in tablets includes the gliclazide of 60~100 parts by weight, the lactose of 30~55 parts by weight, the pregelatinized starch of 20~45 parts by weight, the anhydrous silica gel of 0.5~1.5 parts by weight, the talcum powder of 1~4 parts by weight, the magnesium stearate of 0.5~2.5 parts by weight.Gliclazid in tablets had good sustained release effect in the present invention, its active component can slowly discharge in vivo, and gliclazide blood concentration is on effective treatment concentration in keeping body, it is ensured that drug effect；In addition, the gliclazid in tablets that the present invention is provided has long-term effect, so as to reduce times for spraying, treatment cost is greatly reduced；Gliclazid in tablets preparation cost is low in the present invention, efficacy stability.
Description
Technical field
The present invention relates to gliclazide field, more particularly to a kind of gliclazid in tablets and preparation method thereof.
Background technology
Gliclazide is second generation sulfonylureas oral hypoglycemic, has hypoglycemic work to normal person and diabetic
With.Its hypoglycemic intensity is between tolbutamide and glibenclamide.The direct effect of this product mainly to pancreas, promotes Ca++ to pancreas
The transhipment of island β cells, and stimulate the secretion of insulin.Meanwhile, metabolism of the surrounding tissue to glucose can be also improved, so that
Reduce blood glucose.
After existing gliclazid in tablets is oral can rapidly bungee jumping into uniform stickiness suspension, with it is convenient to take, inhale
Receive the features such as fast, bioavilability is high.But it is due to that gliclazid in tablets disintegration time is fast, the features such as absorbing fast also result in medicine
Thing can reach very high blood concentration in vivo the short time, and the problem of cause hypoglycemia.
The content of the invention
In view of this, it is an object of the invention to provide a kind of gliclazid in tablets and preparation method thereof, its drug ingedient can
Gliclazide blood concentration is on effective treatment concentration in slow release in vivo, keeping body, it is ensured that drug effect.
A kind of gliclazid in tablets, includes the raw material of following parts by weight：
Preferably, the raw material of following parts by weight is included：
Preferably, in addition to PLA, the parts by weight of the PLA are 2~5 parts.
Present invention also offers a kind of preparation method of gliclazid in tablets, comprise the following steps：
A) it is gliclazide, lactose, pregelatinized starch, anhydrous silica gel, talcum powder, Magnesium Stearate is standby；
B) gliclazide, lactose and pregelatinized starch are added to dry-mixed in efficient wet granulator, 10~20min of mixing
Afterwards, purified water is added, particle is made in granulation；
C) particle made from step b) is added in drying machine and dried；
D) dry particle made from step c) is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then general
Grain is put into Mixers with Multi-direction Movement, adds anhydrous silica gel, talcum powder and magnesium stearate, and mixing obtains midbody particle；
E) intermediate particle made from step d) is subjected to tabletting packaging, produces gliclazid in tablets.
Preferably, drying temperature is 45~55 DEG C in step c), and drying time is 10~20min, in dried particle
Moisture is less than 2%.
Preferably, the lactose crosses 80 mesh sieves, the gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, tristearin
Sour magnesium crosses 30 mesh sieves.
Preferably, also include adding PLA into efficient wet granulator in step b).
A kind of gliclazid in tablets that the present invention is provided and preparation method thereof, the gliclazid in tablets includes 60~100 weight
Part gliclazide, the lactose of 30~55 parts by weight, the pregelatinized starch of 20~45 parts by weight, 0.5~1.5 parts by weight it is anhydrous
Silica gel, the talcum powder of 1~4 parts by weight, the magnesium stearate of 0.5~2.5 parts by weight.Gliclazid in tablets slow release effect in the present invention
Good, its active component can slowly be discharged in vivo, and gliclazide blood concentration is protected on effective treatment concentration in keeping body
Demonstrate,prove drug effect；In addition, the gliclazid in tablets that the present invention is provided has long-term effect, so as to reduce times for spraying, treatment cost
Substantially reduce；Gliclazid in tablets preparation cost is low in the present invention, efficacy stability.
Embodiment
The invention discloses a kind of gliclazid in tablets and preparation method thereof, those skilled in the art can be used for reference in herein
Hold, be suitably modified technological parameter realization.In particular, the similar replacement and change are to those skilled in the art
For be it will be apparent that they are considered as being included in the present invention.The method of the present invention and reference are by preferably implementing
Example is described, related personnel substantially can not departing from present invention, in spirit and scope to method described herein and
Using being modified or suitably changing with combining, to realize and apply the technology of the present invention.
A kind of gliclazid in tablets that the present invention is provided, includes the raw material of following parts by weight：
In above-mentioned technical proposal, gliclazid in tablets had good sustained release effect, its active component can slowly discharge in vivo, keep
Internal gliclazide blood concentration is on effective treatment concentration, it is ensured that drug effect；In addition, the gliclazid in tablets tool that the present invention is provided
There is long-term effect, so as to reduce times for spraying, treatment cost is greatly reduced；Gliclazid in tablets prepares cost in the present invention
It is low, efficacy stability.
In the present invention, the parts by weight of gliclazide are 60~100 parts；In an embodiment of the present invention, gliclazide
Parts by weight be 70~90 parts；In other embodiments, the parts by weight of gliclazide are 75~85 parts.
Lactose primarily serves filling effect as filler.In the present invention, the parts by weight of lactose are 30~55 parts；
In an embodiment of the present invention, the parts by weight of lactose are 35~50 parts；In other embodiments, the parts by weight of lactose are 40
~45 parts.
Pregelatinized starch plays adhesive effect.In the present invention, the parts by weight of pregelatinized starch are 20~45 parts；At this
In the embodiment of invention, the parts by weight of pregelatinized starch are 25~40 parts；In other embodiments, the weight of pregelatinized starch
Number is 30~35 parts.
In the present invention, the parts by weight of anhydrous silica gel are 0.5~1.5 part；In an embodiment of the present invention, anhydrous silica gel
Parts by weight be 0.8~1.2 part；In other embodiments, the parts by weight of anhydrous silica gel are 0.9~1.1 part.
Talcum powder can enable to medicine slowly to discharge in vivo as slow-release material, maintain steady state plasma concentration.
In the present invention, the parts by weight of talcum powder are 1~4 part；In an embodiment of the present invention, the parts by weight of talcum powder be 1.5~
3.5 part；In other embodiments, the parts by weight of talcum powder are 2~3 parts.
Magnesium stearate can play lubrication.In the present invention, the parts by weight of magnesium stearate are 0.5~2.5 part；
In embodiments of the invention, the parts by weight of magnesium stearate are 1~2 part；In other embodiments, the parts by weight of magnesium stearate
For 1.3~1.7 parts.
In order to control the rate of release of medicine.In an embodiment of the present invention, in addition to PLA, the parts by weight of PLA
Number is 2~5 parts.
In an embodiment of the present invention, the parts by weight of PLA are 2~5 parts；In other embodiments, the weight of PLA
It is 3~4 parts to measure number.
Present invention also offers a kind of preparation method of gliclazid in tablets, comprise the following steps：
A) it is gliclazide, lactose, pregelatinized starch, anhydrous silica gel, talcum powder, Magnesium Stearate is standby；
B) gliclazide, lactose and pregelatinized starch are added to dry-mixed in efficient wet granulator, 10~20min of mixing
Afterwards, purified water is added, particle is made in granulation；
C) particle made from step b) is added in drying machine and dried；
D) dry particle made from step c) is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then general
Grain is put into Mixers with Multi-direction Movement, adds anhydrous silica gel, talcum powder and magnesium stearate, and mixing obtains midbody particle；
E) intermediate particle made from step d) is subjected to tabletting packaging, produces gliclazid in tablets.
Wherein, gliclazide, lactose, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate are same as above, herein
Repeat no more.
In above-mentioned technical proposal, the production technology of gliclazid in tablets is more stable, controllable, be easy to industrialization.Work of the present invention
Skill is simply operable, and process controllability is high, is adapted to the big production of industrialization.
In order that obtaining moisture in dried particle is less than 2%, in an embodiment of the present invention, drying temperature in step c)
For 45~55 DEG C, drying time is 10~20min.
In order to ensure the release of product stable homogeneous, product property stable homogeneous is good simultaneously, and differences between batches are small, reappearance
It is excellent.In an embodiment of the present invention, lactose crosses 80 mesh sieves, gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, tristearin
Sour magnesium crosses 30 mesh sieves.
In order to control also to include to efficient wet granulator in the rate of release of active component in gliclazid in tablets, step b)
Middle addition PLA.
The gliclazid in tablets provided to further illustrate the present invention with reference to embodiment the present invention and its preparation side
Method is described in detail.
Embodiment 1
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；60g gliclazides, 30g lactose, 25g pregelatinized starch is taken to be added to dry-mixed in efficient wet granulator, after mixing 10min,
40g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 45 DEG C, is done
The dry time is 10min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add 1.1g anhydrous silica gels, 2g talcum powder and 0.5g magnesium stearates, mixing obtains intermediate
Grain；Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazid in tablets.
Embodiment 2
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；70g gliclazides, 50g lactose, 30g pregelatinized starch is taken to be added to dry-mixed in efficient wet granulator, after mixing 20min,
52g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 50 DEG C, is done
The dry time is 15min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add 0.9g anhydrous silica gels, 3g talcum powder and 2.5g magnesium stearates, mixing obtains intermediate
Grain；Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazid in tablets.
Embodiment 3
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；75g gliclazides, 40g lactose, 40g pregelatinized starch is taken to be added to dry-mixed in efficient wet granulator, after mixing 15min,
53g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 50 DEG C, is done
The dry time is 15min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add 0.8g anhydrous silica gels, 1.5g talcum powder and 2g magnesium stearates, mixing obtains intermediate
Grain；Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazid in tablets.
Embodiment 4
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；85g gliclazides, 45g lactose, 35g pregelatinized starch is taken to be added to dry-mixed in efficient wet granulator, after mixing 15min,
56g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 55 DEG C, is done
The dry time is 10min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add 1.2g anhydrous silica gels, 1g talcum powder and 1g magnesium stearates, mixing obtains midbody particle；
Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazid in tablets.
Embodiment 5
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；Take 100g gliclazides, 35g lactose, 45g pregelatinized starch to be added to dry-mixed in efficient wet granulator, mix 15min
Afterwards, 62g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 45 DEG C,
Drying time is 20min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then by particle
It is put into Mixers with Multi-direction Movement, adds 1.5g anhydrous silica gels, 4g talcum powder and 1.3g magnesium stearates, mixing obtains intermediate
Particle；Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazide
Piece.
Embodiment 6
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；90g gliclazides, 55g lactose, 20g pregelatinized starch is taken to be added to dry-mixed in efficient wet granulator, after mixing 15min,
57g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 50 DEG C, is done
The dry time is 20min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add 0.5g anhydrous silica gels, 3.5g talcum powder and 1.7g magnesium stearates, mixing obtains intermediate
Particle；Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazide
Piece.
Embodiment 7
Lactose crosses 80 mesh sieves, and gliclazide, pregelatinized starch, anhydrous silica gel, talcum powder, magnesium stearate cross 30 mesh sieves, standby
With；80g gliclazides, 43g lactose, 32g pregelatinized starch is taken to be added to dry-mixed in efficient wet granulator, after mixing 15min,
53g purified waters are added, particle is made in granulation；Obtained particle is added in drying machine and dried, drying temperature is 55 DEG C, is done
The dry time is 20min；Dried particle is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add 1g anhydrous silica gels, 2.5g talcum powder and 1.5g magnesium stearates, mixing obtains intermediate
Grain；Obtained intermediate particle is subjected to tabletting so that the piece weight after tabletting is 80mg, then is packed, and produces gliclazid in tablets.
First, the detection of dissolution rate is carried out to gliclazid in tablets made from embodiment 1~7
According to《Chinese Pharmacopoeia》Dissolution determination method specified in second C of annex Ⅹ of version in 2010, respectively to implementing
The gliclazid in tablets of 1~7 kind of production of example is detected that testing result is as shown in table 1 below：
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Embodiment 7 | |
| 1h | 17.2 | 17.6 | 17.5 | 16.9 | 17.1 | 17.3 | 17.4 |
| 2h | 32.5 | 33.1 | 32.9 | 33.4 | 32.8 | 33.0 | 33.2 |
| 4h | 47.7 | 48.2 | 48.6 | 49.0 | 48.1 | 48.3 | 48.2 |
| 6h | 63.1 | 63.4 | 63.7 | 63.7 | 63.0 | 63.3 | 64.1 |
| 8h | 79.1 | 78.4 | 78.6 | 78.4 | 79.4 | 78.9 | 79.2 |
| 12h | 98.6 | 97.9 | 98.7 | 99.0 | 98.9 | 98.3 | 98.4 |
2nd, the evaluation of pesticide effectiveness is carried out by taking gliclazid in tablets made from embodiment 7 as an example
Using the product of the embodiment of the present invention 7, the Bioavailability Determination of product pharmaceutical active composition, specific side are carried out
Method is delivered with reference to Liu Zhao equalitys《The relative bioavailability assay method of Gliciazide Tabiets After A Single Oral Administration In Healthy Subjects》(China faces
Bed pharmacology magazine, 1991,7 (3)：166-168)：Healthy volunteer 20 is chosen, blank blood sample is taken after early morning fasted conditions
Lower to take this product 1 (being had meal on time after medicine) respectively, (second day clear by 1,2,4,8,12,24 hours arm venous blood sampling 3ml after medication
Morning takes this product 1 again, and the 3rd day early morning took this product 1 again), separate serum after blood coagulation.Serum is obtained to preserve after freezer,
Detect, average by literature method, be as a result recorded in table 2 below.
| Time (h) | Mean blood plasma concentration (ng/mL) | Time (h) | Mean blood plasma concentration (ng/mL) |
| 1 | 389.6 | 32 | 1745.2 |
| 2 | 601.3 | 36 | 1312.5 |
| 4 | 1301.6 | 48 | 634.5 |
| 8 | 1452.1 | 49 | 876.4 |
| 12 | 1156.4 | 50 | 1122.0 |
| 24 | 456.7 | 52 | 1689.1 |
| 25 | 765.4 | 56 | 1823.6 |
| 26 | 1123.8 | 60 | 1345.1 |
| 28 | 1563.4 | 72 | 602.3 |
After patient takes, internal gliclazide haemoconcentration maintains more than 1000ng/ml for a long time, but is no more than
2000ng/ml, substantially increases the compliance of patient's medication, effectively realizes：15%~20% active component, 2 are discharged in 1 hour
30~35% active components of release in hour, discharge 40~50% active components in 4 hours, 60~70% are discharged in 6 hours and is lived
Property composition, 75~85% active components are discharged in 8 hours, release reaches 100% in 12 hours, had good sustained release effect, efficacy stability,
And can persistently ensure drug effect.
The foregoing description of the disclosed embodiments, enables professional and technical personnel in the field to realize or public to institute using this
The described above for the embodiment opened, enables professional and technical personnel in the field to realize or using the present invention.To these embodiments
A variety of modifications will be apparent for those skilled in the art, and generic principles defined herein can be
In the case of not departing from the spirit or scope of the present invention, realize in other embodiments.Therefore, the present invention is not intended to be limited to
The embodiments shown herein, and it is to fit to the most wide model consistent with novel features with principles disclosed herein
Enclose.
Claims (7)
1. a kind of gliclazid in tablets, it is characterised in that include the raw material of following parts by weight：
2. gliclazid in tablets as claimed in claim 1, it is characterised in that include the raw material of following parts by weight：
3. gliclazid in tablets as claimed in claim 1 or 2, it is characterised in that also including PLA, the weight of the PLA
Number is 2~5 parts.
4. a kind of preparation method of gliclazid in tablets as claimed in claim 1 or 2, it is characterised in that comprise the following steps：
A) it is gliclazide, lactose, pregelatinized starch, anhydrous silica gel, talcum powder, Magnesium Stearate is standby；
B) gliclazide, lactose and pregelatinized starch are added to it is dry-mixed in efficient wet granulator, mixing 10~20min after,
Purified water is added, particle is made in granulation；
C) particle made from step b) is added in drying machine and dried；
D) dry particle made from step c) is added in shaking screen, carried out with 14 mesh sieves after whole grain, whole grain, then particle is put
Enter in Mixers with Multi-direction Movement, add anhydrous silica gel, talcum powder and magnesium stearate, mixing obtains midbody particle；
E) intermediate particle made from step d) is subjected to tabletting packaging, produces gliclazid in tablets.
5. preparation method as claimed in claim 4, it is characterised in that drying temperature is 45~55 DEG C in step c), when drying
Between be 10~20min, moisture is less than 2% in dried particle.
6. preparation method as claimed in claim 4, it is characterised in that the lactose crosses 80 mesh sieves, the gliclazide, pre- glue
Change starch, anhydrous silica gel, talcum powder, magnesium stearate and cross 30 mesh sieves.
7. preparation method as claimed in claim 4, it is characterised in that also include adding into efficient wet granulator in step b)
Enter PLA.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102440972A (en) * | 2011-09-16 | 2012-05-09 | 浙江众益药业有限公司 | Gliclazide tablet (II) and preparation method thereof |
| CN105193758A (en) * | 2014-06-30 | 2015-12-30 | 南京瑞尔医药有限公司 | Gliclazide sustained release tablets and preparation method thereof |
-
2017
- 2017-03-01 CN CN201710118068.3A patent/CN107049978A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102440972A (en) * | 2011-09-16 | 2012-05-09 | 浙江众益药业有限公司 | Gliclazide tablet (II) and preparation method thereof |
| CN105193758A (en) * | 2014-06-30 | 2015-12-30 | 南京瑞尔医药有限公司 | Gliclazide sustained release tablets and preparation method thereof |
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| Title |
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| 张纪兴等: "格列齐特缓释片的研制", 《广东药学院学报》 * |
| 邢树礼等: "格列齐特缓释片的制备及其释药因素考察", 《西北药学杂志》 * |
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