CN101411715B - Pharmaceutical composition containing acarbose - Google Patents
Pharmaceutical composition containing acarbose Download PDFInfo
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- CN101411715B CN101411715B CN2007101561380A CN200710156138A CN101411715B CN 101411715 B CN101411715 B CN 101411715B CN 2007101561380 A CN2007101561380 A CN 2007101561380A CN 200710156138 A CN200710156138 A CN 200710156138A CN 101411715 B CN101411715 B CN 101411715B
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- acarbose
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- agent
- medicine composition
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- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 title claims abstract description 33
- 229960002632 acarbose Drugs 0.000 title claims abstract description 33
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 title claims abstract description 33
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 8
- 210000000214 mouth Anatomy 0.000 claims abstract description 18
- 239000003814 drug Substances 0.000 claims abstract description 10
- 239000000203 mixture Substances 0.000 claims abstract description 8
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 18
- 239000003795 chemical substances by application Substances 0.000 claims description 16
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 10
- 239000000945 filler Substances 0.000 claims description 9
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 claims description 8
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 8
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 8
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 7
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 7
- 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 6
- 229930195725 Mannitol Natural products 0.000 claims description 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 6
- 235000015165 citric acid Nutrition 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 239000000594 mannitol Substances 0.000 claims description 6
- 235000010355 mannitol Nutrition 0.000 claims description 6
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 6
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 6
- 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 claims description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 5
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 5
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 5
- 238000004132 cross linking Methods 0.000 claims description 5
- 235000019359 magnesium stearate Nutrition 0.000 claims description 5
- 239000000741 silica gel Substances 0.000 claims description 5
- 229910002027 silica gel Inorganic materials 0.000 claims description 5
- 239000011734 sodium Substances 0.000 claims description 5
- 229910052708 sodium Inorganic materials 0.000 claims description 5
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 5
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 4
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- 239000005434 MCC/mannitol excipient Substances 0.000 claims description 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 2
- 239000001530 fumaric acid Substances 0.000 claims description 2
- 239000001630 malic acid Substances 0.000 claims description 2
- 235000011090 malic acid Nutrition 0.000 claims description 2
- 150000007524 organic acids Chemical class 0.000 claims description 2
- 239000011975 tartaric acid Substances 0.000 claims description 2
- 235000002906 tartaric acid Nutrition 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 abstract description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 7
- 239000002775 capsule Substances 0.000 abstract description 3
- 238000012216 screening Methods 0.000 abstract description 3
- 230000007547 defect Effects 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 239000002671 adjuvant Substances 0.000 description 10
- 238000007907 direct compression Methods 0.000 description 7
- 238000012360 testing method Methods 0.000 description 6
- 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 description 5
- 238000005516 engineering process Methods 0.000 description 5
- 239000008101 lactose Substances 0.000 description 5
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 239000002994 raw material Substances 0.000 description 4
- 238000005303 weighing Methods 0.000 description 4
- 229940079593 drug Drugs 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 235000012054 meals Nutrition 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 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 1
- 102000001554 Hemoglobins Human genes 0.000 description 1
- 108010054147 Hemoglobins Proteins 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 description 1
- 230000023852 carbohydrate metabolic process Effects 0.000 description 1
- 235000021256 carbohydrate metabolism Nutrition 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000013467 fragmentation Methods 0.000 description 1
- 238000006062 fragmentation reaction Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 238000011031 large-scale manufacturing process Methods 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000000291 postprandial effect Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 230000014860 sensory perception of taste Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to a medicine composition containing acarbose. The composition can be made into orally disintegrated ablets through screening each minor ingredient and dosage thereof. Therefore, the invention overcomes the defect of inconvenient taken existing in the prior tablet and capsule, and provides an acarbose preparation which can be disintegrated quickly in oral cavity, and can be taken more easily without water.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, more specifically say so and contain the pharmaceutical composition of acarbose.
Background technology
Acarbose (Acarbose), chemical name: O-4, two deoxidation-4-[(1S of 6-; 4R, 5S, 6S) 4; 5,6-trihydroxy-3-(methylol)-2-cyclohexenyl group-1-is amino]-a-D-glucopyranosyl-(1 4)-O-a-D-glucopyranosyl-(1 4)-D-Glucopyranose..Be a kind of novel OHA, it is an alpha-glucosidase inhibitor, and the clinical research result proves that acarbose is a kind of medicine of controlling carbohydrate metabolism safely and effectively.Can reduce post-prandial glycemia, fasting glucose and glycolated hemoglobin value effectively.
The present clinical dosage form of using is ordinary tablet and capsule, and the instructions of taking of tablet is for before the meal or chew with former mouthfuls of foods in the meal and take.For the patient of elderly patients and the inconvenience of medication during the journey, there are the defective of taking inconvenience in tablet and capsule.Therefore need a kind of can disintegrate fast in the oral cavity, do not need the dosage form that is easier to take of water to replace, to have better patient's compliance.
The characteristics of oral cavity disintegration tablet are taking conveniences, do not need water, can take whenever and wherever possible, and rapid-action.Medicine places and need not in the oral cavity to chew, disintegrate fast, be dispersed or dissolved in the saliva, the patient do not need water or only need little water just can with medicine smoothly clothes down, onset rapidly.
But acarbose is processed oral cavity disintegration tablet in industry, exist certain difficulty: the preparation oral cavity disintegration tablet can adopt methods such as lyophilization or direct compression to realize; And freeze-drying is realized large-scale production and the employing of rarer producer owing to production technology is complicated, difficult; Another kind of direct compression process is used owing to production technology simply and widely; But the compressibility of acarbose raw material, disintegrative are all undesirable; Can't satisfy supplementary material in the direct compression process should have good compressibility and have the good disintegrating property and the requirement of some other parameter again; That is to say that must add the suitable excipients of q.s, the slice, thin piece that acarbose is suppressed meets each item index of oral cavity disintegration tablet.But; The adjuvant that adds is too many, certainly will influence the disintegration rate that makes slice, thin piece again and the index that does not reach oral cavity disintegration tablet, moreover the preparation specification of acarbose itself bigger (50mg/ sheet); Therefore, never have the report of the suitability for industrialized production of acarbose oral cavity disintegration tablet.Must select the combination of the kind and the amount of carrying out of adjuvant meticulously.
Summary of the invention
The present invention will solve is that existing ordinary tablet is taken this technical problem of inconvenience, and a kind of pharmaceutical composition that contains acarbose is provided, but this compositions industrialization process the acarbose oral cavity disintegration tablet.
The invention provides a kind of pharmaceutical composition that contains acarbose, by weight percentage, comprising:
Acarbose 8-32%,
Filler 50-70%,
Disintegrating agent 2-12%,
Help and collapse agent 5-20%,
Lubricant 0.5-5%;
Wherein said filler is selected from one or more in microcrystalline Cellulose, mannitol and the copolyvidone; Described disintegrating agent is one or more in polyvinylpolypyrrolidone, carboxymethylstach sodium and the cross-linking sodium carboxymethyl cellulose; Describedly help that to collapse agent be organic acid and sodium bicarbonate; Described lubricant is micropowder silica gel and/or magnesium stearate.
Be preferably:
Acarbose 13-20%,
Filler 55-67%,
Disintegrating agent 6-12%,
Help and collapse agent 5-12%,
Lubricant 1-2%.
Wherein said filler preferably microcrystalline cellulose and mannitol share.
Wherein said helping collapsed agent and is preferably in citric acid, tartaric acid, malic acid or the fumaric acid one or more and sodium bicarbonate.
This pharmaceutical composition is suitable for being prepared into oral cavity disintegration tablet.
From the conventional knowledge of preparation, lactose is good a kind of filler, but considers that acarbose is the diabetics medication, should avoid selecting for use to the uncomfortable adjuvant of diabetics as far as possible.So the present invention does not select lactose for use.
In adjuvant of the present invention was selected, all adjuvants were except taking into full account its cost, and it is chosen all through testing preferably; Even if some adjuvant very conventional in oral cavity disintegration tablet does not adopt because of not accomplishing technical scheme of the present invention yet; Just can not select for use like starch, Icing Sugar and dextrin etc., because after finding to have used these adjuvants through test, preparation that makes or disintegrate are too slow; Compressibility is undesirable, can't industrialization.
Below be a part of prescription screening (added amount is for by weight percentage):
According to the characteristics of oral cavity disintegration tablet, choose 5 main indexs such as friability of appearance character, powder flowbility, disintegration time, mouthfeel and the slice, thin piece of slice, thin piece above prescription is estimated, investigated, the result is as shown in the table:
| Prescription 1 | Prescription 2 | Prescription 3 | Prescription 4 | Prescription 3 | Prescription 6 | Prescription 7 | Prescription 8 | Prescription 9 | Prescription 10 | Prescription 11 | Prescription 12 | |
| The slice, thin piece outward appearance | Very loose | Loose | Loose | Loose | Loose | Still can | Still can | Slice, thin piece is bigger | Better | Better | Loose | Still can |
| Powder flowbility | Still can | Still can | Still can | Still can | Still can | Still can | Better | Better | Better | Better | Better | Still can |
| Friability | Bad | Bad | Bad | Bad | Still can | Still can | Better | Better | Better | Poorer slightly than prescription 9 | Still can | Still can |
| Disintegration time (second) | 70 | 90 | 70 | 100 | Less than 60 | Less than 60 | Less than 60 | 47 | 45 | 47 | Less than 60 | Less than 60 |
| Mouthfeel | Better | Not fine | Relatively poor | Relatively poor | Relatively poor | Better | Better | Good | Good | Good | Relatively poor | Better |
| Overall merit | Difference | Difference | Difference | Difference | Qualified | Qualified | Qualified | Better | Best | Good | Qualified | Qualified |
The standard of wherein said judge is following:
The standard of slice, thin piece outward appearance is: very loose: hands is pinched, and is slightly firmly promptly broken;
Loose: hardness is 1-3kg
Still can: hardness is 3-4kg
Better: hardness is 4-6kg;
The standard of powder flowbility is: still can: during manual tabletting,, cause sheet heavy not enough because of the powder flowbility difference is difficult to fill up; During the machine tabletting,, feasible reluctantly because of vibration is arranged;
Better: manual tabletting is feasible reluctantly; Feasible during the machine tabletting;
Friability: very bad: slice, thin piece is just broken in (regulation 100 circles) in friabilator transfer 5 circles;
Bad: as to change just broken (stipulating 4 minutes) in 2 minutes;
Better: do not have any breakage in 1 minute, going to did not still have obviously fragmentation in 4 minutes.
Disintegration time inspection described in this test is adopted and is sucked method and external disintegrating method method, wherein
Suck method: slice, thin piece is put in the mouth, picks up counting, and melts fully to slice, thin piece.Allow tongue to do slight and stirring slowly during this time.
External disintegrating method method: with the teat glass of the about 12mm of diameter, place 37 ℃ water bath with thermostatic control, contain the water of 37 ℃ of about 1.8ml in the test tube, slice, thin piece is put into test tube, pick up counting, till complete disintegrate, and must be all through 50 mesh sieves.
Analytically the reason of table is following simultaneously:
Prescription 1: lactose and copolyvidone influence its disintegration rate.
Prescription 2: lactose and copolyvidone influence its disintegration rate.The low-substituted hydroxypropyl cellulose mouthfeel is not good.
Prescription 3: the low-substituted hydroxypropyl cellulose mouthfeel is not good.Cross-linking sodium carboxymethyl cellulose disintegrate power is not enough.
Prescription 4: the low-substituted hydroxypropyl cellulose mouthfeel is not good.Cross-linking sodium carboxymethyl cellulose disintegrate power is not enough.Carboxymethylstach sodium does not play and improves the friability effect.
Prescription 5: raw material ratio is great, and difficulty collapses; With mannitol, it is bad to distinguish the flavor of.
Prescription 6: it is more reasonable to write out a prescription, but because the raw material proportion is higher, has influenced disintegrate a little.
Prescription 7: it is more reasonable to write out a prescription, but because list uses carboxymethylstach sodium as disintegrating agent, effect influences its disintegrate and taste not as polyvinylpolypyrrolidone.
Prescription 8: have higher rating, but copolyvidone is not brought into play positive effect.
Prescription 9: each item index is the most desirable.
Prescription 10: the consumption that microcrystalline Cellulose in the prescription 9 is described is more suitable.Strengthen, it is neither suitable to reduce consumption.
Prescription 11: this prescription is still reasonable.
Prescription 12: raw material ratio is great, and difficulty collapses.
Visible by above result, prescription 1,2,3,4, evaluation all relatively poor, though prescription 5,6,7,11,12 can be qualified, also not ideal enough, particularly two key indexs of disintegration time and friability are not ideal.And 8,9,10 overall merits of writing out a prescription are better.
Result of the test is analyzed visible, lactose is inapplicable to diabetics except waiting, and also can influence the disintegration rate of slice, thin piece, and low-substituted hydroxypropyl cellulose can cause that the mouthfeel of slice, thin piece is not good, so the equal the present invention of these adjuvants does not adopt; Copolyvidone also has certain influence to the disintegration rate of slice, thin piece.Though super-disintegrant such as cross-linking sodium carboxymethyl cellulose, carboxymethylstach sodium can be used, effect is good not as polyvinylpolypyrrolidone, and mouthfeel is also good not as polyvinylpolypyrrolidone.
For the better sense of taste is arranged, can also add correctives in the pharmaceutical composition of acarbose provided by the present invention, like citric acid, A Siba is sweet and other sweeting agent etc.
The compositions that contains acarbose provided by the invention has good compressibility, and has good disintegrating property.Through the screening of adjuvant, reduce the addition of adjuvant widely simultaneously, guaranteed the disintegration rate of slice, thin piece.Thereby can in industry, realize the preparation oral cavity disintegration tablet.In addition, the acarbose oral cavity disintegration tablet of the present invention's preparation has improved the compliance of particular patients ' greatly, and convenient patient takes, and onset speed is faster.
The method for preparing of acarbose oral cavity disintegration tablet provided by the present invention can adopt direct compression technology.Preparation technology: each material is crossed 80 mesh sieves all in advance, by prescription weighing, mixing, tabletting.
The specific embodiment
Embodiment 1
Acarbose: 50g
Microcrystalline Cellulose: 130g
Mannitol: 67g
Polyvinylpolypyrrolidone: 33g
Citric acid: 17g
Sodium bicarbonate: 12g
Micropowder silica gel: 3.3g
Magnesium stearate: 1.7g
By the prescription weighing, each material is crossed 80 mesh sieves all in advance, mixing, and direct compression is processed 1000.
Embodiment 2
Acarbose: 50g
Microcrystalline Cellulose: 180g
Mannitol: 67g
Copolyvidone: 5g
Polyvinylpolypyrrolidone: 33g
Citric acid: 17g
Sodium bicarbonate: 12g
Micropowder silica gel: 3.3g
Magnesium stearate: 1.7g
By the prescription weighing, each material is crossed 80 mesh sieves all in advance, mixing, and direct compression is processed 1000.
Embodiment 3
Acarbose: 50g
Microcrystalline Cellulose: 90g
Mannitol: 67g
Polyvinylpolypyrrolidone: 33g
Citric acid: 17g
Sodium bicarbonate: 12g
Micropowder silica gel: 3.3g
Magnesium stearate: 1.7g
By the prescription weighing, each material is crossed 80 mesh sieves all in advance, mixing, and direct compression is processed 1000.
Embodiment is verified the result sees the following form:
Claims (4)
1. the pharmaceutical composition that contains acarbose by weight percentage, comprising:
Acarbose 8-32%,
Filler 50-70%,
Disintegrating agent 2-12%,
Help and collapse agent 5-20%,
Lubricant 0.5-5%;
Wherein said filler is selected from one or more in microcrystalline Cellulose, mannitol and the copolyvidone; Described disintegrating agent is one or more in polyvinylpolypyrrolidone, carboxymethylstach sodium and the cross-linking sodium carboxymethyl cellulose; Describedly help that to collapse agent be organic acid and sodium bicarbonate; Described lubricant is micropowder silica gel and/or magnesium stearate; The wherein said Acarbose medicine composition that contains is used to process oral cavity disintegration tablet.
2. the Acarbose medicine composition that contains according to claim 1 by weight percentage, comprising:
Acarbose 8-32%,
Filler 55-67%,
Disintegrating agent 6-12%,
Help and collapse agent 5-12%,
Lubricant 1-2%.
3. the Acarbose medicine composition that contains according to claim 1 and 2, wherein said filler is selected from microcrystalline Cellulose and mannitol.
4. the Acarbose medicine composition that contains according to claim 1 and 2 wherein saidly helps that to collapse agent be one or more and sodium bicarbonate in citric acid, tartaric acid, malic acid or the fumaric acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007101561380A CN101411715B (en) | 2007-10-19 | 2007-10-19 | Pharmaceutical composition containing acarbose |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007101561380A CN101411715B (en) | 2007-10-19 | 2007-10-19 | Pharmaceutical composition containing acarbose |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101411715A CN101411715A (en) | 2009-04-22 |
| CN101411715B true CN101411715B (en) | 2012-03-28 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2007101561380A Active CN101411715B (en) | 2007-10-19 | 2007-10-19 | Pharmaceutical composition containing acarbose |
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Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20130403A1 (en) * | 2010-04-27 | 2013-04-13 | Bayer Ip Gmbh | ORAL DISINTEGRATION TABLET CONTAINING ACARBOSE |
| WO2012055066A1 (en) * | 2010-10-25 | 2012-05-03 | 北京北大维信生物科技有限公司 | Acarbose composition with effect of lowering blood glucose and preparation method thereof |
| TR201100150A2 (en) * | 2011-01-06 | 2012-07-23 | Bi̇lgi̇ç Mahmut | Water soluble dosage forms |
| CN103230594A (en) * | 2013-04-07 | 2013-08-07 | 深圳奥萨医药有限公司 | Medicine composition of alpha-glucosidase inhibitor and vitamin B |
| CN103315971B (en) * | 2013-06-13 | 2015-03-04 | 海南葫芦娃制药有限公司 | Acarbose tablets and preparation method thereof |
| CN104940164B (en) * | 2015-06-30 | 2016-08-24 | 四川绿叶宝光药业股份有限公司 | A kind of Acarbose capsules agent medicine compositions and preparation method thereof |
| US11786471B2 (en) * | 2016-07-11 | 2023-10-17 | Wuhan Ll Science And Technology Development Co. Ltd. | Complex disintegrant system for oral solid preparation and oral solid preparation comprising said complex disintegrant system |
| CN113081984B (en) * | 2021-04-19 | 2023-06-02 | 北京阳光诺和药物研究股份有限公司 | Acarbose orally disintegrating tablet and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101019874A (en) * | 2007-03-12 | 2007-08-22 | 杭州中美华东制药有限公司 | Acarbose medicine composition and its prepn |
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2007
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101019874A (en) * | 2007-03-12 | 2007-08-22 | 杭州中美华东制药有限公司 | Acarbose medicine composition and its prepn |
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