CN105963267A - Dimemorfan phosphate preparation and application thereof - Google Patents
Dimemorfan phosphate preparation and application thereof Download PDFInfo
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- CN105963267A CN105963267A CN201610405897.5A CN201610405897A CN105963267A CN 105963267 A CN105963267 A CN 105963267A CN 201610405897 A CN201610405897 A CN 201610405897A CN 105963267 A CN105963267 A CN 105963267A
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- Prior art keywords
- dimemorfan phosphate
- purposes
- dimemorfan
- phosphate
- content
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- 229960001056 dimemorfan Drugs 0.000 title claims abstract description 45
- KBEZZLAAKIIPFK-NJAFHUGGSA-N dimemorfan Chemical compound C1C2=CC=C(C)C=C2[C@@]23CCN(C)[C@@H]1[C@H]2CCCC3 KBEZZLAAKIIPFK-NJAFHUGGSA-N 0.000 title claims abstract description 45
- 238000002360 preparation method Methods 0.000 title abstract description 11
- 206010006451 bronchitis Diseases 0.000 claims abstract description 15
- 239000003814 drug Substances 0.000 claims abstract description 11
- 206010035664 Pneumonia Diseases 0.000 claims abstract description 9
- 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 8
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims abstract description 8
- 206010057190 Respiratory tract infections Diseases 0.000 claims abstract description 8
- 206010006458 Bronchitis chronic Diseases 0.000 claims abstract description 7
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 7
- 206010046306 Upper respiratory tract infection Diseases 0.000 claims abstract description 7
- 208000007451 chronic bronchitis Diseases 0.000 claims abstract description 7
- 239000008101 lactose Substances 0.000 claims abstract description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 7
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 7
- 229940079593 drug Drugs 0.000 claims abstract description 5
- 229960001375 lactose Drugs 0.000 claims abstract 2
- 239000000203 mixture Substances 0.000 claims description 23
- 230000000954 anitussive effect Effects 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 229940124584 antitussives Drugs 0.000 claims description 10
- 239000002775 capsule Substances 0.000 claims description 8
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims description 8
- 208000008128 pulmonary tuberculosis Diseases 0.000 claims description 7
- 239000013543 active substance Substances 0.000 claims description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 3
- 239000000945 filler Substances 0.000 claims description 3
- 229920000881 Modified starch Polymers 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 241001289435 Astragalus brachycalyx Species 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 239000004375 Dextrin Substances 0.000 claims 1
- 229920001353 Dextrin Polymers 0.000 claims 1
- 235000002917 Fraxinus ornus Nutrition 0.000 claims 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 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- 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 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 1
- 239000001506 calcium phosphate Substances 0.000 claims 1
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 1
- 235000011010 calcium phosphates Nutrition 0.000 claims 1
- 235000019425 dextrin Nutrition 0.000 claims 1
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 235000001727 glucose Nutrition 0.000 claims 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 1
- 238000006116 polymerization reaction Methods 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
- 239000000811 xylitol Substances 0.000 claims 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 1
- 229960002675 xylitol Drugs 0.000 claims 1
- 235000010447 xylitol Nutrition 0.000 claims 1
- 206010011224 Cough Diseases 0.000 abstract description 10
- 201000010099 disease Diseases 0.000 abstract description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 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 abstract 1
- 206010013453 Disseminated tuberculosis Diseases 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000000890 drug combination Substances 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 208000020029 respiratory tract infectious disease Diseases 0.000 abstract 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 12
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 10
- 238000000034 method Methods 0.000 description 9
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 7
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 6
- 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 description 6
- 235000019359 magnesium stearate Nutrition 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000008187 granular material Substances 0.000 description 5
- 239000008213 purified water Substances 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 4
- 230000002354 daily effect Effects 0.000 description 4
- 239000000314 lubricant Substances 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 239000011159 matrix material Substances 0.000 description 4
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 4
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 4
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 4
- 239000000377 silicon dioxide Substances 0.000 description 4
- 235000012239 silicon dioxide Nutrition 0.000 description 4
- 239000000853 adhesive Substances 0.000 description 3
- 230000001070 adhesive effect Effects 0.000 description 3
- -1 fluidizer Substances 0.000 description 3
- MKXZASYAUGDDCJ-SZMVWBNQSA-N LSM-2525 Chemical compound C1CCC[C@H]2[C@@]3([H])N(C)CC[C@]21C1=CC(OC)=CC=C1C3 MKXZASYAUGDDCJ-SZMVWBNQSA-N 0.000 description 2
- 206010044302 Tracheitis Diseases 0.000 description 2
- 239000003434 antitussive agent Substances 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
- 229960001985 dextromethorphan Drugs 0.000 description 2
- 229920000609 methyl cellulose Polymers 0.000 description 2
- 239000001923 methylcellulose Substances 0.000 description 2
- 235000010981 methylcellulose Nutrition 0.000 description 2
- 230000002093 peripheral effect Effects 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000000741 silica gel Substances 0.000 description 2
- 229910002027 silica gel Inorganic materials 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 206010010774 Constipation Diseases 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- DBLHYLDWZSNRBI-UHFFFAOYSA-N N=NC=NN.N=NC=NN.P(=O)(O)(O)O Chemical compound N=NC=NN.N=NC=NN.P(=O)(O)(O)O DBLHYLDWZSNRBI-UHFFFAOYSA-N 0.000 description 1
- MHQJUHSHQGQVTM-HNENSFHCSA-N Octadecyl fumarate Chemical compound CCCCCCCCCCCCCCCCCCOC(=O)\C=C/C(O)=O MHQJUHSHQGQVTM-HNENSFHCSA-N 0.000 description 1
- 206010036790 Productive cough Diseases 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 150000001335 aliphatic alkanes Chemical class 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 229960004126 codeine Drugs 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 208000017574 dry cough Diseases 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 239000003172 expectorant agent Substances 0.000 description 1
- 230000003419 expectorant effect Effects 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
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 210000001767 medulla oblongata Anatomy 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 210000001034 respiratory center Anatomy 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 210000001533 respiratory mucosa Anatomy 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 210000000582 semen Anatomy 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- 210000003802 sputum Anatomy 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 229940071138 stearyl fumarate Drugs 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a dimemorfan phosphate preparation and application thereof. The dimemorfan phosphate preparation is prepared from dimemorfan phosphate, lactose, microcrystalline cellulose and a pharmaceutically acceptable carrier. The dimemorfan phosphate preparation with the good flowability, stability and dissolution rate can be obtained, and therefore the dimemorfan phosphate preparation is suitable for industrial mass production. The dimemorfan phosphate preparation is a cough relief drug combination which can treat upper respiratory infection, acute bronchitis, pneumonia and tuberculosis, lung cancer and chronic bronchitis, the compatibility is reasonable, drugs can be rapidly released, and the good curative effect can be generated on diseases.
Description
Technical field
The present invention relates to Dimemorfan phosphate for preparing the purposes of medicine, be suitable to the sheet being administered orally in particular for preparation
Agent and capsule.
Dimemorfan phosphate (Dimemorfan Phosphate), molecular formula: C18H25N.H3O4P, molecular weight: 353.39
It is for treating upper respiratory tract infection, acute bronchitis, pneumonia and pulmonary tuberculosis, pulmonary carcinoma, the antitussive of chronic bronchitis
Three kind new medicines, currently carry out preclinical study.
Background technology
Cough, is a kind of strong respiratory movement that happens suddenly, and this action is owing to the respiratory center irriate of oblongata causes
's.The cough that respiratory mucosa is upset (such as foreign body, inflammation) and causes, Main Function is to discharge foreign body and sputum, has
Important Protection significance.The main cause causing cough mostly is respiratory system disease, as flu, tracheitis, pneumonia, asthma etc. are normal
See disease.Cough medicine is divided into central antitussive and peripheral antitussive drugs by its site of action difference.Central antitussive is by pressing down
Oblongata coughing centre processed and play antitussive effect, this type of medicine is applicable to the dry cough without expectorant.Peripheral antitussive drugs is coughed by suppression
The coughre flex arc coughed outside maincenter plays antitussive effect to coughing link.
Dimemorfan phosphate is a kind of upper respiratory tract infection, acute bronchitis, pneumonia and pulmonary tuberculosis, pulmonary carcinoma, chronic
Country three kind new medicine of the antitussive effect of tracheitis；Pharmaceutical research shows: this product suppression medulla oblongata coughing centre, for non-additive
Maincenter town cough medicine, it is structurally and functionally similar to dextromethorphan, and antitussive effect is slightly better than 2 times of dextromethorphan, about codeine.
Advantage is that toxicity is low, and safety is big, and therapeutic dose does not suppress to breathe, and does not has constipation side effect.
Summary of the invention
The present invention relates to the pharmaceutical composition containing Dimemorfan phosphate and this based composition for safely and effectively treatment
Respiratory tract infection, acute bronchitis, pneumonia and pulmonary tuberculosis, pulmonary carcinoma, the application of the antitussive of chronic bronchitis.
The invention still further relates to the pharmaceutical composition containing Dimemorfan phosphate Yu the oral administration of other drug active substance.
Said composition is to be obtained by the surface making the granule of pharmaceutically active substance adhere to carrier matrix.Pharmaceutically active substance is made to sink
The method on carrier matrix of is minimum in order to make the gathering of active substance/carrier substrate particles be reduced to.
The present invention relates to the pharmaceutical composition containing about 3mg--300 mg Dimemorfan phosphate, said composition is given daily
It is used for treating upper respiratory tract infection, acute bronchitis, pneumonia and pulmonary tuberculosis, pulmonary carcinoma, the antitussive of chronic bronchitis for three times.Excellent
The pharmaceutical composition of choosing contains the Dimemorfan phosphate of about 10mg--200 mg, and most preferred pharmaceutical composition contains about 10mg--
The Dimemorfan phosphate of 150 mg.Further, this kind of preferred and most preferred pharmaceutical composition is given daily three times for treating
Upper respiratory tract infection, acute bronchitis, pneumonia and pulmonary tuberculosis, pulmonary carcinoma, the antitussive of chronic bronchitis.
Above-mentioned Dimemorfan phosphate pharmaceutical composition for being given daily also can be the most regular to some patient to
Medicine.Such as, make their upper respiratory tract infection to being treated by daily Dimemorfan phosphate pharmaceutical composition, anxious
Property bronchitis, pneumonia and pulmonary tuberculosis, pulmonary carcinoma, the antitussive of chronic bronchitis obtain control patient can implement maintaining treatment side
Case is to protect it from further infecting.This maintaining treatment scheme include every day not enough once take Dimemorfan phosphate medicine
Compositions.Such as, just within every three or four days, being administered once, it is enough.
The Dimemorfan phosphate pharmaceutical composition of the present invention can be configured to the form through any suitable administration, the most excellent
The oral administration combination of choosing can be tablet, capsule, granule or powder type.According to method well known in the art, phosphoric acid diformazan
Coffee alkane pharmaceutical composition can be to be configured to the form that parenteral, rectum or via intranasal application are administered.This kind of preparation can include pharmaceutically acceptable
Excipient, described excipient includes in this based composition conventional filler, fluidizer, lubricant, disintegrating agent, binding agent etc..
Present invention additionally comprises slow releasing preparation.
Tablet and capsule preparations containing about 10mg 100mg Dimemorfan phosphate can be prepared by the following method,
To guarantee the efficient of product and good uniformity.First Dimemorfan phosphate calmness is made on the surface of carrier matrix
Standby compositions.This step is completed by following operation: form Dimemorfan phosphate and the solution of adhesive material, then at carrier
Matrix granule applies this solution while keeping motion in the way of spraying.Control condition is so that the gathering of granule is preferably minimized.
Any other composition that will comprise in granule and compositions after drying, such as disintegrating agent/fluidizer/lubricant mix
Close.Then the powder obtained it is pressed into sheet or is filled into capsule.
Preferred solvent in said method is the ethanol of water or variable concentrations.
Adhesive material preferably has the polymer of high-consistency.The material being suitable for includes polyvidone, methylcellulose, hydroxyl
Methylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, polyvidone, hydroxymethyl cellulose are preferred
's.In whole compositions, the content of adhesive material is preferably the about 1%--about 10%(weight of compositions gross weight).
The disintegrant content that whole compositions includes is preferably the about 1%--7% of compositions gross weight.The disintegrating agent being suitable for includes
Polyvinylpolypyrrolidone, cross-linked carboxymethyl cellulose, low-substituted hydroxypropyl methylcellulose, Explotab, pregelatinized Starch and Semen Maydis
Starch, polyvinylpolypyrrolidone is preferred.
The lubricant content that whole compositions includes is preferably the about 1%--5% of compositions gross weight.The lubricant being suitable for includes
Micropowder silica gel, magnesium stearate, stearic acid, stearyl fumarate and sodium lauryl sulfate, micropowder silica gel, magnesium stearate are preferred
's.
Detailed description of the invention
The Dimemorfan phosphate compositions of the following example explanation present invention
Embodiment 1
Said method is used to prepare 25 milligrams of Dimemorfan phosphate capsules
| Composition | Amount %(w/w) | Amount/grain |
| Dimemorfan phosphate | 5 | 10mg |
| Microcrystalline Cellulose | 47.00 | 94 mg |
| Lactose | 30.00 | 60 mg |
| Polyvidone | 5.00 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 10.00 | 20.0mg |
| Magnesium stearate | 0.90 | 1.8mg |
| Silicon dioxide | 2.1 | 4.0 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 200.00 mg |
Embodiment 2
Said method is used to prepare 50 milligrams of Dimemorfan phosphate capsules
| Composition | Amount %(w/w) | Amount/grain |
| Dimemorfan phosphate | 16.03 | 50 mg |
| Microcrystalline Cellulose | 32.05 | 100 mg |
| Lactose | 32.05 | 100 mg |
| Polyvidone | 9.60 | 30mg |
| Polyvinylpolypyrrolidone | 9.60 | 30.0mg |
| Silicon dioxide | 0.60 | 2.00mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 312.00 mg |
Embodiment 3
Said method is used to prepare 10 milligrams of Dimemorfan phosphate capsules
| Composition | Amount %(w/w) | Amount/piece |
| Dimemorfan phosphate | 5.26 | 10 mg |
| Microcrystalline Cellulose | 26.32 | 50 mg |
| Lactose | 52.63 | 100 mg |
| Polyvidone | 4.47 | 8.5 mg |
| Polyvinylpolypyrrolidone | 5.26 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 5.26 | 10 mg |
| Magnesium stearate | 0.79 | 1.5 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 190 mg |
Embodiment 4
Said method is used to prepare 100 milligrams of Dimemorfan phosphate sheets
| Composition | Amount %(w/w) | Amount/piece |
| Dimemorfan phosphate | 25.00 | 100 mg |
| Microcrystalline Cellulose | 25.00 | 100 mg |
| Lactose | 37.50 | 150 mg |
| Polyvidone | 2.50 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 5.00 | 20 mg |
| Magnesium stearate | 2.5 | 10 mg |
| Silicon dioxide | 2.5 | 10 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 401.50 mg |
Embodiment 5
Said method is used to prepare 10 milligrams of Dimemorfan phosphate sheets
| Composition | Amount %(w/w) | Amount/piece |
| Dimemorfan phosphate | 5.00 | 10 mg |
| Microcrystalline Cellulose | 40.00 | 80 mg |
| Lactose | 50.00 | 100 mg |
| Polyvidone | 3.00 | 6mg |
| Low-substituted hydroxypropyl methylcellulose | 1.50 | 3 mg |
| Magnesium stearate | 0.5 | 1 mg |
| Silicon dioxide | 0.5 | 1 |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 200.00 mg |
Claims (10)
1. Dimemorfan phosphate is used for preparing oral administration three times a day for treating upper respiratory tract infection, acute bronchitis, lung
Inflammation and pulmonary tuberculosis, pulmonary carcinoma, the purposes of the antitussive of chronic bronchitis pharmaceutical composition in the form of tablets or capsules, wherein said
Pharmaceutical composition contains the Dimemorfan phosphate of 3mg 300mg.
2. the purposes of claim 1, the content of wherein said Dimemorfan phosphate is 3mg 250mg.
3. the purposes of claim 1, the content of wherein said Dimemorfan phosphate is 3mg 200mg.
4. the purposes of claim 3, the content of wherein said Dimemorfan phosphate is 10mg.
5. the purposes of claim 3, the content of wherein said Dimemorfan phosphate is 25mg.
6. the purposes of claim 3, the content of wherein said Dimemorfan phosphate is 50mg.
7. the purposes of claim 3, the content of wherein said Dimemorfan phosphate is 100mg.
8. the purposes of claim 3, the content of wherein said Dimemorfan phosphate is 150mg.
9. the purposes of claim 1, described compositions therein contains one or more other drug active substances.
10. the purposes of claims 1, wherein said filler is selected from lactose, xylitol, microcrystalline Cellulose, dextrin, manna
Alcohol, sorbitol, sucrose, starch, pregelatinized Starch, glucose, calcium phosphate, calcium hydrogen phosphate, calcium carbonate, and mixture, and
Described Dimemorfan phosphate be by have enough stickiness polymerization emplastic stick together on described filler.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610405897.5A CN105963267A (en) | 2016-06-12 | 2016-06-12 | Dimemorfan phosphate preparation and application thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610405897.5A CN105963267A (en) | 2016-06-12 | 2016-06-12 | Dimemorfan phosphate preparation and application thereof |
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| Publication Number | Publication Date |
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| CN105963267A true CN105963267A (en) | 2016-09-28 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201610405897.5A Pending CN105963267A (en) | 2016-06-12 | 2016-06-12 | Dimemorfan phosphate preparation and application thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756919A (en) * | 2008-12-24 | 2010-06-30 | 北京利乐生制药科技有限公司 | Orally disintegrating tablet containing dimemorfan and preparation method thereof |
| CN102746227A (en) * | 2012-07-09 | 2012-10-24 | 浙江保灵药业有限公司 | Dimemorfan phosphate crystal form II and preparation method thereof, and pharmaceutical composition |
| CN105596312A (en) * | 2016-01-08 | 2016-05-25 | 珠海联邦制药股份有限公司 | Dimemorfan phosphate capsule composition and preparing method thereof |
-
2016
- 2016-06-12 CN CN201610405897.5A patent/CN105963267A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756919A (en) * | 2008-12-24 | 2010-06-30 | 北京利乐生制药科技有限公司 | Orally disintegrating tablet containing dimemorfan and preparation method thereof |
| CN102746227A (en) * | 2012-07-09 | 2012-10-24 | 浙江保灵药业有限公司 | Dimemorfan phosphate crystal form II and preparation method thereof, and pharmaceutical composition |
| CN105596312A (en) * | 2016-01-08 | 2016-05-25 | 珠海联邦制药股份有限公司 | Dimemorfan phosphate capsule composition and preparing method thereof |
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