CN105963267A - Dimemorfan phosphate preparation and application thereof - Google Patents
Dimemorfan phosphate preparation and application thereof Download PDFInfo
- Publication number
- 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
- Authority
- CN
- China
- Prior art keywords
- dimemorfan phosphate
- purposes
- dimemorfan
- phosphate
- content
- 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.)
- Pending
Links
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
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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610405897.5A CN105963267A (en) | 2016-06-12 | 2016-06-12 | Dimemorfan phosphate preparation and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610405897.5A CN105963267A (en) | 2016-06-12 | 2016-06-12 | Dimemorfan phosphate preparation and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105963267A true CN105963267A (en) | 2016-09-28 |
Family
ID=57010905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610405897.5A Pending CN105963267A (en) | 2016-06-12 | 2016-06-12 | Dimemorfan phosphate preparation and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105963267A (en) |
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 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5053865B2 (en) | Method for producing orally disintegrating solid preparation | |
| KR20180090966A (en) | Capsule formulation comprising montelukast or a pharmaceutically acceptable salt thereof, and levocetirizine or a pharmaceutically acceptable salt thereof | |
| KR20030097892A (en) | Drug preparations | |
| CN105919955A (en) | Ruxolitinib preparation and application thereof | |
| CN107913256A (en) | A kind of macitentan oral disnitegration tablet for treating pulmonary hypertension and preparation method thereof | |
| CN103833712B (en) | The brilliant II type of nicousamide, its method for making and its pharmaceutical composition and purposes | |
| CN106309388A (en) | Medicine composition for treating congestive heart failure and preparation method thereof | |
| US20140163044A1 (en) | Compound Chemical Medicine Acting on Respiratory Disease, Preparation Process and Use Thereof | |
| CN103070865A (en) | Oral solid preparation taking prucalopride succinate as active ingredient and application of oral solid preparation | |
| CN105902506A (en) | Sacubitril/valsartan preparation and application thereof | |
| CN105902507A (en) | Ethanesulfonic acid nintedanib preparation and application thereof | |
| CN106074431A (en) | A kind of Vonoprazan fumarate preparation and application thereof | |
| CN101732312A (en) | Huperzine A oral formulation and a preparation method thereof | |
| CN101152155A (en) | Hydrochloric acid Ivabradine solid pharmaceutical composition and method for preparing the same | |
| CN101099730A (en) | Oral solid preparation containing ambroxol hydrochloride and guaifenesin active components | |
| CN104013589A (en) | Axitinib orally disintegrating tablet and preparation method thereof | |
| CN105919967A (en) | Acotiamide hydrochloride preparation and application thereof | |
| KR101697773B1 (en) | Modified release composition comprising doxofylline | |
| CN101961319B (en) | Silybin meglumine enteric agent with high bioavailability and preparation method thereof | |
| CN105963267A (en) | Dimemorfan phosphate preparation and application thereof | |
| CN107982268A (en) | A kind of tolvaptan preparation and its application | |
| CN114146089A (en) | Pharmaceutical composition containing efavirenz, tenofovir and emtricitabine | |
| CN113908153A (en) | Buvalracetam pharmaceutical composition, preparation method and application thereof | |
| CN101579342A (en) | Desloratadine-contained patulin composition | |
| CN101152187A (en) | Eplerenone pharmaceutical composition |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160928 |
|
| WD01 | Invention patent application deemed withdrawn after publication |