CN100496496C - Compound metformin glipidide preparation for treating diabetes type II, and its preparation method - Google Patents
Compound metformin glipidide preparation for treating diabetes type II, and its preparation method Download PDFInfo
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- CN100496496C CN100496496C CNB2005102005848A CN200510200584A CN100496496C CN 100496496 C CN100496496 C CN 100496496C CN B2005102005848 A CNB2005102005848 A CN B2005102005848A CN 200510200584 A CN200510200584 A CN 200510200584A CN 100496496 C CN100496496 C CN 100496496C
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- Prior art keywords
- metformin hydrochloride
- metformin
- cortex cinnamomi
- glipizide
- mixing
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- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 title claims abstract description 104
- 150000001875 compounds Chemical class 0.000 title claims abstract description 4
- 238000002360 preparation method Methods 0.000 title claims description 48
- 229960003105 metformin Drugs 0.000 title claims description 27
- 206010012601 diabetes mellitus Diseases 0.000 title abstract description 13
- 239000000284 extract Substances 0.000 claims abstract description 86
- ZJJXGWJIGJFDTL-UHFFFAOYSA-N glipizide Chemical compound C1=NC(C)=CN=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZJJXGWJIGJFDTL-UHFFFAOYSA-N 0.000 claims abstract description 57
- 229960001381 glipizide Drugs 0.000 claims abstract description 57
- 239000003814 drug Substances 0.000 claims abstract description 32
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 96
- 229960004329 metformin hydrochloride Drugs 0.000 claims description 76
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims description 76
- 238000002156 mixing Methods 0.000 claims description 65
- 238000000605 extraction Methods 0.000 claims description 58
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Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
Tested number | Concentration of alcohol | System soft material situation | |
1 | 40~50 | % ethanol | Soft material easily bonds |
2 | 20~30 | % ethanol | Soft material is moderate |
3 | 10~20 | % ethanol | Soft material viscosity |
Tested number | The soybean oil consumption | The pill situation |
1 | 20~30% ethanol, 0.5~1.0% soybean oil | Soft material viscosity is not enough, can't pill |
2 | 20~30% ethanol, 1.2~1.5% soybean oils | Soft material is moderate, suitable pill |
3 | 20~30% ethanol, 1.6~2.5% soybean oils | Soft material easily bonds, the pill difficulty |
Numbering | Coating pan rotating speed (r/min) | The molten diffusing time (min) | Mouldability |
1 | 20~30 | 6.93 | Relatively poor |
2 | 35~45 | 7.12 | Better |
3 | 50~65 | 12.35 | Harder |
4 | 70~85 | 14.38 | Hard |
5 | 90~100 | 15.49 | Hard |
Claims (12)
- [claim 1] a kind of compounding metformin glipidide for the treatment of type 2 diabetes mellitus, it is characterized in that: according to listed as parts by weight, it is with 75~225 parts of 62~188 parts of metformin hydrochloride, 1~4 part of glipizide and Cortex Cinnamomi extracts, and in addition right amount of auxiliary materials is made into: coated tablet, dispersible tablet, hard capsule, soft capsule, granule, powder, pellet, drop pill or oral liquid; Wherein Cortex Cinnamomi extract is such preparation: get cinnamomic dry branch, leaf vapor distillation extraction method extraction 2~4 times, and each 1~3 hour, merge volatile oil, when being 20 ℃, temperature measures relative density, and its relative density is 1.0~1.1, promptly.
- [claim 2] is according to the compounding metformin glipidide of the described treatment type 2 diabetes mellitus of claim 1, it is characterized in that: according to listed as parts by weight, it is with 100~200 parts of 90~160 parts of metformin hydrochloride, 2~3 parts of glipizide and Cortex Cinnamomi extracts, and in addition right amount of auxiliary materials is made into coated tablet, dispersible tablet, hard capsule, soft capsule, granule, powder, pellet, drop pill or oral liquid.
- [claim 3] is according to the compounding metformin glipidide of the described treatment type 2 diabetes mellitus of claim 1, it is characterized in that: according to listed as parts by weight, it is with 150 parts of 125 parts of metformin hydrochloride, 2.5 parts of glipizide and Cortex Cinnamomi extracts, and in addition right amount of auxiliary materials is made into coated tablet, dispersible tablet, hard capsule, soft capsule, granule, powder, pellet, drop pill or oral liquid.
- [claim 4] is according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, the starch that adds the 40%-60% of metformin hydrochloride weight, the dextrin of the 40%-60% of metformin hydrochloride weight, mixing, ethanol system wet granular with 10~30%, dry, granulate, packing promptly gets granule.
- [claim 5] is characterized in that according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, mixing; Other gets 15%~25% low-substituted hydroxypropyl cellulose of metformin hydrochloride weight, the carboxymethyl starch sodium of the 10%-20% of metformin hydrochloride weight, mixing, get 3/5 with the mixed powder mix homogeneously of metformin hydrochloride, glipizide and Cortex Cinnamomi extract, starch slurry with 5~15% is made binding agent, 40 order system material, granulate, mixed powder and 0.5~1% part of magnesium stearate of adding residue 2/5 low-substituted hydroxypropyl cellulose and carboxymethyl starch sodium are added in the granule that makes, mixing, tabletting promptly gets dispersible tablet.
- [claim 6] is according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, the starch that adds the 20%-30% of metformin hydrochloride weight, mixing, with 20~30% ethanol and 1.2~1.5% soybean oil system soft materials, the soft material that makes micropill mechanism ball, wet feed pushed the 0.8mm sieve aperture, the wet grain of strip cuts off round as a ball, 50~60 ℃ of drying and mouldings are crossed 16~20 mesh sieves and are selected ball or spray drying, wet-milling granulation molding, mould placed add the great achievement ball in the coating pan, medicated powder: water is 1:1.2~1.5, and the coating pan rotating speed is 35~45r/min, capping, select ball, promptly get pellet.
- [claim 7] is according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, the PEG400 that adds the 5%-15% of metformin hydrochloride weight, the sorbitol of the 10%-20% of metformin hydrochloride weight, mixing; Press medication amount: substrate amount=1:1.2~1.5 add soybean oils, mixing; The prescription of rubber is a gelatin: glycerol: water: titanium dioxide=100:45:100:2, batchingization adhesive tape part is: weigh batching, in the inputization glue jar, merceration is warming up to 65 ± 5 ℃ gradually after 30~60 minutes, stirred 2~4 hours and simultaneously evacuation remove bubble, treat evenly back blowing of sizing material, incapsulate after the filtration in the sizing material bucket of machine; The debugging pellet press, 65 ± 5 ℃ of gelatin box temperature controls, mould rotating speed 1.0~3.0 is rolled in 45 ± 5 ℃ of sprinkler body temperature controls, rubber thickness 0.7~0.8mm, 18~25 ℃ of indoor temperatures, relative humidity is less than 40%, pelleting; The dry typing drying of rolling that adopts combined with two steps of tray dried, dry 1~3 hour of the typing of rolling, and 25 ± 5 ℃ of baking temperatures, dry relative humidity should be lower than 40%, and promptly got soft capsule at 24~48 hours drying time.
- [claim 8] is characterized in that according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract mixing; Get the said mixture portion, two parts of Macrogol 4000s, polyoxyethylene monostearate S-40 portion, mix homogeneously, dissolve in the water-bath, stir evenly, drip and in dimethicone, to become ball, drip apart from 3~7cm, drip footpath 2.5mm/2mm, mix 80 ± 5 ℃ of ointment temperature, liquid coolant height 70 ± 5cm promptly gets drop pill.
- [claim 9] is according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, the starch that adds the 15%-25% of metformin hydrochloride weight, the carboxymethyl starch sodium of the 10%-20% of metformin hydrochloride weight, mixing, with 10~50% alcohol granulations, dry, granulate adds 1~5% part carboxymethyl starch sodium, 0.5~1% part magnesium stearate, mixing, tabletting, coating promptly gets coated tablet.
- [claim 10] is according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, mixing, add distilled water, 2~5% aspartame, sterilization promptly gets oral liquid.
- [claim 11] is according to the preparation method of the two 17 guanidine glipizide preparations of compound recipe diformazan of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, the starch that adds the 20%-30% of metformin hydrochloride weight, mixing, drying and crushing is sieved, divided dose, packing promptly gets powder.
- [claim 12] is according to the preparation method of the compounding metformin glipidide of any described treatment type 2 diabetes mellitus among the claim 1-3, it is characterized in that: get metformin hydrochloride, glipizide, Cortex Cinnamomi extract, mixing, 15%~40% the starch that adds metformin hydrochloride weight, mix homogeneously, use 80% alcohol granulation, filling promptly gets hard capsule.
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CN102274285B (en) * | 2011-07-20 | 2014-07-02 | 天津市聚星康华医药科技有限公司 | Pharmaceutical composition for treating type 2 diabetes and complications thereof |
CN102266388B (en) * | 2011-07-20 | 2014-08-27 | 天津市聚星康华医药科技有限公司 | Pharmaceutical composition for preventing and treating type 2 diabetes and complication thereof |
CN102274514B (en) * | 2011-07-20 | 2014-08-27 | 天津市聚星康华医药科技有限公司 | Medicinal composition for preventing and treating type-II diabetes and complications thereof |
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