CN101161240A - Levodropropizine medicinal composition for oral cavity use - Google Patents
Levodropropizine medicinal composition for oral cavity use Download PDFInfo
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- CN101161240A CN101161240A CNA200610032393XA CN200610032393A CN101161240A CN 101161240 A CN101161240 A CN 101161240A CN A200610032393X A CNA200610032393X A CN A200610032393XA CN 200610032393 A CN200610032393 A CN 200610032393A CN 101161240 A CN101161240 A CN 101161240A
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- CN
- China
- Prior art keywords
- levodropropizine
- pharmaceutical composition
- oral cavity
- mixture
- correctives
- 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.)
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- PTVWPYVOOKLBCG-ZDUSSCGKSA-N levodropropizine Chemical compound C1CN(C[C@H](O)CO)CCN1C1=CC=CC=C1 PTVWPYVOOKLBCG-ZDUSSCGKSA-N 0.000 title claims abstract description 38
- 229960002265 levodropropizine Drugs 0.000 title claims abstract description 36
- 210000000214 mouth Anatomy 0.000 title claims abstract description 10
- 239000000203 mixture Substances 0.000 title claims description 11
- 229940046011 buccal tablet Drugs 0.000 claims abstract 2
- 239000006189 buccal tablet Substances 0.000 claims abstract 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 16
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 235000019359 magnesium stearate Nutrition 0.000 claims description 8
- 239000001828 Gelatine Substances 0.000 claims description 6
- 229920002472 Starch Polymers 0.000 claims description 6
- 229930006000 Sucrose Natural products 0.000 claims description 6
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- 229920000159 gelatin Polymers 0.000 claims description 6
- 235000019322 gelatine Nutrition 0.000 claims description 6
- 239000008107 starch Substances 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- 229960004793 sucrose Drugs 0.000 claims description 6
- 239000003085 diluting agent Substances 0.000 claims description 5
- NOOLISFMXDJSKH-UHFFFAOYSA-N p-menthan-3-ol Chemical compound CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
- 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
- 239000004375 Dextrin Substances 0.000 claims description 4
- 229920001353 Dextrin Polymers 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 239000011230 binding agent Substances 0.000 claims description 4
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 4
- 235000019425 dextrin Nutrition 0.000 claims description 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 4
- 239000000314 lubricant Substances 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 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 description 3
- -1 correctives Substances 0.000 claims description 3
- 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 description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 3
- 239000008101 lactose Substances 0.000 claims description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
- 102000004169 proteins and genes Human genes 0.000 claims description 3
- 108090000623 proteins and genes Proteins 0.000 claims description 3
- 239000004925 Acrylic resin Substances 0.000 claims description 2
- 229920000178 Acrylic resin Polymers 0.000 claims description 2
- 229920000858 Cyclodextrin Polymers 0.000 claims description 2
- 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 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- 229920000881 Modified starch Polymers 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 2
- 239000001095 magnesium carbonate Substances 0.000 claims description 2
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 2
- 235000014380 magnesium carbonate Nutrition 0.000 claims description 2
- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims description 2
- 239000000395 magnesium oxide Substances 0.000 claims description 2
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims description 2
- 235000012245 magnesium oxide Nutrition 0.000 claims description 2
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims description 2
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 claims description 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
- 239000002002 slurry Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 4
- 239000006185 dispersion Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 16
- 238000002360 preparation method Methods 0.000 abstract description 10
- 230000002035 prolonged effect Effects 0.000 abstract 1
- 238000012360 testing method Methods 0.000 description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 239000002671 adjuvant Substances 0.000 description 6
- 206010011224 Cough Diseases 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 230000000694 effects Effects 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- 239000002775 capsule Substances 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- 206010002091 Anaesthesia Diseases 0.000 description 2
- 238000001949 anaesthesia Methods 0.000 description 2
- 230000037005 anaesthesia Effects 0.000 description 2
- 229940124584 antitussives Drugs 0.000 description 2
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 description 2
- 230000003902 lesion Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000007937 lozenge Substances 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- 235000011837 pasties Nutrition 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- RUZIUYOSRDWYQF-HNNXBMFYSA-N (S)-glaucine Chemical compound CN1CCC2=CC(OC)=C(OC)C3=C2[C@@H]1CC1=C3C=C(OC)C(OC)=C1 RUZIUYOSRDWYQF-HNNXBMFYSA-N 0.000 description 1
- JTUQXGZRVLWBCR-UHFFFAOYSA-N 1-[1-[2-(phenylmethyl)phenoxy]propan-2-yl]piperidine Chemical compound C1CCCCN1C(C)COC1=CC=CC=C1CC1=CC=CC=C1 JTUQXGZRVLWBCR-UHFFFAOYSA-N 0.000 description 1
- CFJMRBQWBDQYMK-UHFFFAOYSA-N 1-phenyl-1-cyclopentanecarboxylic acid 2-[2-(diethylamino)ethoxy]ethyl ester Chemical compound C=1C=CC=CC=1C1(C(=O)OCCOCCN(CC)CC)CCCC1 CFJMRBQWBDQYMK-UHFFFAOYSA-N 0.000 description 1
- PTVWPYVOOKLBCG-UHFFFAOYSA-N 3-(4-phenyl-1-piperazinyl)propane-1,2-diol Chemical compound C1CN(CC(O)CO)CCN1C1=CC=CC=C1 PTVWPYVOOKLBCG-UHFFFAOYSA-N 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- DABPOQZSGVNAAS-UHFFFAOYSA-N Glaucocalactone Natural products O=CC12C3C(C4)OC(=O)C2C(C)(C)CCC1OC(=O)C13CC4C(=C)C1OC(=O)C DABPOQZSGVNAAS-UHFFFAOYSA-N 0.000 description 1
- 102000006386 Myelin Proteins Human genes 0.000 description 1
- 108010083674 Myelin Proteins Proteins 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 239000003434 antitussive agent Substances 0.000 description 1
- 230000007885 bronchoconstriction Effects 0.000 description 1
- 210000000748 cardiovascular system Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229960004126 codeine Drugs 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000011981 development test Methods 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 229960004722 dropropizine Drugs 0.000 description 1
- 206010013663 drug dependence Diseases 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000013401 experimental design Methods 0.000 description 1
- 229940113086 glaucine Drugs 0.000 description 1
- 229930004041 glaucine Natural products 0.000 description 1
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 210000005012 myelin Anatomy 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000007830 nerve conduction Effects 0.000 description 1
- 229940127240 opiate Drugs 0.000 description 1
- 229960003436 pentoxyverine Drugs 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000011514 reflex Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
- 239000007779 soft material Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Abstract
A levodropropizine novel preparation is provided in the present invention, a buccal tablet capable of buccal administration and releasing slowly in oral cavity composed of levodropropizine and corresponding supplementary. The present invention leads active component levodropropizine medicine to remain at focal part to act, in oral cavity local range medicine concentration is relative heightened, so working time is prolonged relatively.
Description
Invention field
The invention belongs to the chemical drugs invention field, relate to the pharmaceutical composition that a kind of main component is a levodropropizine, promptly a kind of novel form of the levodropropizine that in the oral cavity, uses.
Background technology
Cough is a kind of common clinical, and the common anti-tussitives multiaction is in maincenter, as opiates narcoticness cough medicine morphine, codeine etc. at present; Non-narcotic analgesics such as dromethan, Glaucine, pentoxyverine, ASA-158/5 etc.; Though suchlike cough medicine kind is many, how unsatisfactory curative effect is, and side effect is very big.Someone thinks, comparatively ideal cough medicine should reduce sensorineural sensitivity in the lung, and blocking-up has the sensory nerve conduction (as the local anaesthesia medicine) in myelin or the nonmedullated nerve, but the local anaesthesia medicine has the lung of inhibition protective reflex and brings out side effect such as bronchoconstriction.
By gondola Dompe company (commodity be called Levotuss) and Mediolanum company (trade name Danka) exploitation, in Italy go on the market the earliest by in October, 1988 for levodropropizine, is used for the treatment of all kinds cough, is a kind of peripheral antitussive drugs.Levodropropizine is a chipal compounds, does not almost have the maincenter sedation of its raceme dropropizine and analog antitussive thereof, and the cardiovascular system respiratory system of unifying is not produced any obvious effect, its better tolerance, and no drug dependence and stability are high.The domestic levodropropizine preparation that has gone on the market has conventional tablet, capsule, oral liquid etc. at present.Yet conventional tablet and capsule are unfavorable for old man or child and swallow, though oral liquid taking convenience but character are not very stable relatively and store trouble, dosage and pharmacokinetics character are not as capsule and tablet, so the inventor has invented a kind of new dosage form at this Study of Defects, i.e. buccal or the levodropropizine pharmaceutical composition chewed in the oral cavity, can make medicine be stranded in lesions position, drug level increases relatively, prolong action time relatively, thereby reach the minimizing drug dose, be easy to absorb, the holding time is long and improve the purpose of therapeutic effect.
Summary of the invention
Purpose of the present invention aims to provide a kind of pharmaceutical composition of levodropropizine, and a kind of novel form of the levodropropizine that can use in the oral cavity has and can make medicine be stranded in lesions position, and drug level increases relatively, and action time is advantage such as prolongation relatively.
Levodropropizine pharmaceutical composition of the present invention is by levodropropizine and be used to suck the chemical medicine thing and prepare required corresponding adjuvant and form.
The weight ratio of levodropropizine pharmaceutical composition levodropropizine of the present invention and adjuvant is a levodropropizine 5～20%, and adjuvant is 95～80%.
The used adjuvant of levodropropizine pharmaceutical composition of the present invention is made up of in diluent, correctives, binding agent, the lubricant one or more.
Diluent can be one or more the mixture in cane sugar powder, mannitol, calcium sulfate two water things, lactose, starch, pregelatinized Starch, dextrin, microcrystalline Cellulose, magnesium oxide, magnesium carbonate, the calcium carbonate.
Correctives can be one or more the mixture in Mentholum, protein sugar, cane sugar powder, mannitol, citric acid, cyclodextrin glucose oligomer, the various natural or artificial essence.
Binding agent can be one or more the mixture in starch slurry, dextrin, hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose, polyvinylpyrrolidone, acrylic resin, mucialga of arabic gummy, gelatine size, the microcrystalline Cellulose.
Lubricant can be one or more the mixture in magnesium stearate, Pulvis Talci, micropowder silica gel, Macrogol 4000, the magnesium laurylsulfate.
Above-mentioned various adjuvant and consumption thereof are selected according to preparation method and subjective demand, with reference to open source information and use the prior art of this professional field can obtain the pharmaceutical composition of gratifying levodropropizine, this medicine uses in the oral cavity, every day three times, twice medication interval should be more than 6 hours.
The specific embodiment
Embodiment 1:
Supplementary material g
Levodropropizine 60
Protein sugar 120
Cane sugar powder 900
Hydroxypropyl methylcellulose (15cp) 5
Mentholum 15
Magnesium stearate 5
70% ethanol is an amount of
With the supplementary material pulverize separately, sieve, standby.Take by weighing supplementary material by recipe quantity.With adjuvant (except magnesium stearate and the Mentholum) mixing, add the levodropropizine mixing more earlier.Ethanol system soft material with 70% is granulated, and 50～55 ℃ were toasted about 2 hours, and the granulate that sieves adds the magnesium stearate mixing, sprays into Mentholum 95% alcoholic solution, seals about 6 hours promptly.1000 of tablettings.
Test example 1: Bioavailability of Human Body development test
Test objective: the relative bioavailability that is intended to study Levodropropizine lozenge.
Content of the test: adopt binary cycle to intersect (2 * 2) EXPERIMENTAL DESIGN at random, 18 experimenters are divided into 2 groups at random, every group 9 people.Every group of experimenter takes the Levodropropizine lozenge sample of embodiment 1 gained according to testing program and as the levodropropizine sheet that has gone on the market (specification is the conventional tablet of 60mg/ sheet) of reference preparation in different tests.
Result of the test: the main pharmacokinetic parameter C of reference preparation and test preparation
Max, T
Max, AUC
0 → 12And AUC
0 → ∞(mean ± standard deviation) is respectively: 200.1 ± 25.9 and 228.4 ± 31.7ng/ml; 0.67 ± 0.18 and 0.76 ± 0.23h; 624.8 ± 134.6 and 654.4 ± 128.0ng.h/ml; 674.2 ± 151.8 and 687.2 ± 156.2ng.h/ml.T
MaxThrough the Mann-Whitney check, different preparation differences do not have significance, C
Max, AUC
0 → 12And AUC
0 → ∞After to number conversion, carry out variance analysis, the result shows that both do not have the significance meaning with the different cycles differences between different preparations.Test preparation to the relative bioavailability F of reference preparation (with AUC
0 → 12As estimating foundation) be 101% ± 6%, this shows that both have bioequivalence when dosage is identical.
Embodiment 2
Supplementary material g
Levodropropizine 60
Beta-schardinger dextrin-200
Lactose 30
Steviosin 8
Magnesium stearate 4
5% gelatine size is an amount of
With the supplementary material pulverize separately, sieve, standby; Take by weighing supplementary material by recipe quantity; Beta-schardinger dextrin-adding levodropropizine soluble in water is ground to form pasty state, and oven dry is pulverized, and sieves; With said mixture and all the other auxiliary materials and mixing (except the magnesium stearate), add gelatine size, granulate, baking, granulate adds magnesium stearate, mixing; 1000 of tablettings.
Embodiment 3
Supplementary material g
Levodropropizine 60
Starch 360
Sucrose 60
Polyvinylpyrrolidone 5
Pulvis Talci 5
5% gelatine size is an amount of
With the supplementary material pulverize separately, sieve, standby; Take by weighing supplementary material by recipe quantity; Starch adding levodropropizine soluble in water is ground to form pasty state, and oven dry is pulverized, and sieves; With said mixture and all the other auxiliary materials and mixing, add gelatine size, granulate baking, granulate, 1000 of tablettings.
Claims (6)
1. pharmaceutical composition that contains levodropropizine, can be in the oral cavity buccal and slowly dissolving is perhaps chewed by the oral cavity and made its dispersion and slowly dissolving.It is characterized in that it contains the necessary pharmaceutic adjuvant of the levodropropizine and 95%～80% (weight) of 5%～20% (weight).
2. a kind of pharmaceutical composition that contains levodropropizine according to claim 1, the dosage form that it is characterized in that it is a buccal tablet.
3. a kind of pharmaceutical composition that contains levodropropizine according to claim 2 is characterized in that described pharmaceutic adjuvant comprises diluent, correctives, binding agent, lubricant.
4. a kind of pharmaceutical composition that contains levodropropizine according to claim 2 is characterized in that described pharmaceutic adjuvant comprises diluent, correctives.
5. according to the described a kind of pharmaceutical composition that contains levodropropizine of claim 1～4, it is characterized in that described pharmaceutic adjuvant comprises correctives.
6. a kind of pharmaceutical composition that contains levodropropizine according to claim 3 is characterized in that:
A, diluent can be one or more the mixture in cane sugar powder, mannitol, calcium sulfate two water things, lactose, starch, pregelatinized Starch, dextrin, microcrystalline Cellulose, magnesium oxide, magnesium carbonate, the calcium carbonate.
B, correctives can be one or more the mixture in Mentholum, protein sugar, cane sugar powder, mannitol, citric acid, cyclodextrin glucose oligomer, the various natural or artificial essence.
C, binding agent can be one or more the mixture in starch slurry, dextrin, hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose, polyvinylpyrrolidone, acrylic resin, mucialga of arabic gummy, gelatine size, the microcrystalline Cellulose.
D, lubricant can be one or more the mixture in magnesium stearate, Pulvis Talci, micropowder silica gel, Macrogol 4000, the magnesium laurylsulfate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB200610032393XA CN100544722C (en) | 2006-10-12 | 2006-10-12 | The levodropropizine pharmaceutical composition that uses in a kind of oral cavity |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB200610032393XA CN100544722C (en) | 2006-10-12 | 2006-10-12 | The levodropropizine pharmaceutical composition that uses in a kind of oral cavity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101161240A true CN101161240A (en) | 2008-04-16 |
| CN100544722C CN100544722C (en) | 2009-09-30 |
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| CNB200610032393XA Active CN100544722C (en) | 2006-10-12 | 2006-10-12 | The levodropropizine pharmaceutical composition that uses in a kind of oral cavity |
Country Status (1)
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101766583B (en) * | 2008-12-29 | 2012-11-28 | 北京德众万全药物技术开发有限公司 | Medicinal effervescent tablet for treating cough and preparation method thereof |
| CN103381145A (en) * | 2012-05-03 | 2013-11-06 | 贵州大学 | Method for improving levodropropizine taste by solid dispersion |
| CN103381272A (en) * | 2012-05-03 | 2013-11-06 | 贵州大学 | Method for improving levodropropizine taste by cyclodextrin clathration |
| CN108904460A (en) * | 2012-02-19 | 2018-11-30 | 奥拉黑尔斯公司 | Alkalization wattle viscose binder for oral cavity adhesion disk |
| WO2019132823A1 (en) * | 2017-12-27 | 2019-07-04 | Biofarma Ilac Sanayi Ve Ticaret A.S. | A pharmaceutical product comprising levodropropizine |
-
2006
- 2006-10-12 CN CNB200610032393XA patent/CN100544722C/en active Active
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101766583B (en) * | 2008-12-29 | 2012-11-28 | 北京德众万全药物技术开发有限公司 | Medicinal effervescent tablet for treating cough and preparation method thereof |
| CN108904460A (en) * | 2012-02-19 | 2018-11-30 | 奥拉黑尔斯公司 | Alkalization wattle viscose binder for oral cavity adhesion disk |
| CN103381145A (en) * | 2012-05-03 | 2013-11-06 | 贵州大学 | Method for improving levodropropizine taste by solid dispersion |
| CN103381272A (en) * | 2012-05-03 | 2013-11-06 | 贵州大学 | Method for improving levodropropizine taste by cyclodextrin clathration |
| WO2019132823A1 (en) * | 2017-12-27 | 2019-07-04 | Biofarma Ilac Sanayi Ve Ticaret A.S. | A pharmaceutical product comprising levodropropizine |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100544722C (en) | 2009-09-30 |
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