CN108836943A - A kind of injection dextromethorphan hydrobromide and preparation method thereof - Google Patents
A kind of injection dextromethorphan hydrobromide and preparation method thereof Download PDFInfo
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- CN108836943A CN108836943A CN201810821148.XA CN201810821148A CN108836943A CN 108836943 A CN108836943 A CN 108836943A CN 201810821148 A CN201810821148 A CN 201810821148A CN 108836943 A CN108836943 A CN 108836943A
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- parts
- injection
- dextromethorphan hydrobromide
- preparation
- water
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Classifications
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- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
Abstract
The invention discloses a kind of injection dextromethorphan hydrobromide and preparation method thereof, dextromethorphan hydrobromide, excipient and waters for injection.Mannitol is chosen in the preparation method of dextromethorphan hydrobromide of the present invention as excipient, weigh the dextromethorphan hydrobromide of recipe quantity, water for injection is added to stir to being completely dissolved, addition needle-use activated carbon, which stirs evenly, afterwards is heated to 55-60 DEG C, heat preservation 30 minutes, it is cooled to room temperature, when aseptic filtration, selecting aperture is the filter membrane of 0.22mm, during pre-freeze and drying, pre-freezing temperature is -40 DEG C, the pre-freeze time is 2 hours, vacuum degree is 20Pa, condenser temperature is -50 DEG C, sublimation time is 10 hours, products temperature is 35 DEG C, drying time is 4 hours, solve the problems, such as the formation problems and solubility of preparation injection dextromethorphan hydrobromide, simple process, it is easy to operate.
Description
Technical field
The present invention relates to pharmaceutical field, in particular to a kind of injection dextromethorphan hydrobromide and preparation method thereof.
Background technique
Dextromethorphan hydrobromide (Dextromethorphan Hydrobromide) is opened by Switzerland's Roche (Roche) company
Hair.The states such as the U.S., Britain, Japan and Italy pharmacopeia is recorded.Dextromethorphan hydrobromide is classified as non-prescription drugs by U.S. FDA,
It is decided to be non-narcotic drug in world's arcotic meeting, the World Health Organization thinks that " dextromethorphan hydrobromide is that replace can be to
The antitussive medicine of cause ".This product is non-habituation sexual centre antitussive, by inhibiting oblongata coughing centre to work.Its antibechic is made
It is similar to narcoticness antitussive codeine with intensity.Without analgesic activity without additive, therapeutic dose will not inhibit in breathing this product
Pivot, toxicity are low.Suitable for the infection of the upper respiratory tract (flu, sphagitis, nasosinusitis etc.), acute or chronic bronchitis, bronchus
The control of cough symptom caused by asthma, bronchiectasis, pneumonia, pulmonary tuberculosis etc., it can also be used to thoracentesis, branch
Cause the treatment of cough when Tracheography and bronchoscopy.It is particularly suitable for the cough that can not be fed after dry cough and operation
Cough patient.Past this product applies peroral dosage form clinically more tablet, capsule, syrup, granule or sustained release preparation etc.,
Also it is chiefly used in compound preparation.American Drug Index (American Drug Index) records dextromethorphan hydrobromide folk prescription system
Agent 9, compound preparation 67, be oral preparation.In recent years dextromethorphan hydrobromide injection listing is had approved in Japan,
National Drug Administration ratifies Tianjin medicine company Lianshui Co., Ltd dextromethorphan hydrobromide injection (lml within 2001:
It 5mg) produces, for domestic exclusive product.There is Shanghai new Asia pharmaceutical factory production and selling in the dextromethorphan hydrobromide raw material country.Note
It penetrates with the 5th kind new medicine of dextromethorphan hydrobromide category drug registration, change dosage form but does not change administration route, injection works
Fastly, it can quickly relieve symptoms, release patient suffering.It is freeze-dried compared with injection, it is high except having rapid-action and bioavilability
The advantages of outside, also have property stability good, be readily transported and store, winter and low temperature use unaffected feature.
But in the prior art, although since dextromethorphan hydrobromide is soluble in water, excipient is being not added
In the case of be difficult to form, only at concentration shape, will appear loosely frangible situation excipient is added.In addition, figuration is added
The bad situation of the solubility of product happens occasionally after agent.Therefore, it is necessary to make a kind of forming and the good hydrobromic acid of solubility
Dextromethorphan.
Summary of the invention
The technical problem to be solved in the present invention is to provide a kind of injection dextromethorphan hydrobromides and preparation method thereof, solve
Dextromethorphan hydrobromide is difficult to the problem formed and solubility is not strong.
In order to solve the above-mentioned technical problem, the technical scheme is that：
A kind of injection dextromethorphan hydrobromide is provided, is comprised the following components in parts by weight：
Dextromethorphan hydrobromide：2-10 parts；Mannitol：10-200 parts；Water for injection：500-1500 parts.
It is furthermore preferred that comprising the following components in parts by weight：
Dextromethorphan hydrobromide：5 parts；Mannitol：50 parts；Water for injection：1000 parts.
Preferably, injection dextromethorphan hydrobromide provided by the invention, preparation method mainly include the following steps that：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 55-60 DEG C, keeps the temperature 30 minutes, then cool down
To room temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, through filter membrane aseptic filtration, packing；
S6：It is sent into pre-freeze and drying in freeze drying box；
S7：Tamponade is rolled lid and is made after drying.
By adopting the above technical scheme, due to using the mannitol of zone of reasonableness dosage as figuration dosage, so that injection
Dextromethorphan hydrobromide molding is easy and skeleton is secured and solubility is strong.
Specific embodiment
Specific embodiments of the present invention will be further explained below.It should be noted that for these implementations
The explanation of mode is used to help understand the present invention, but and does not constitute a limitation of the invention.In addition, this hair disclosed below
Technical characteristic involved in bright each embodiment can be combined with each other as long as they do not conflict with each other.
Embodiment 1
The injection dextromethorphan hydrobromide, comprises the following components in parts by weight：
Dextromethorphan hydrobromide：5 parts；Lactose：10 parts；Water for injection：1000 parts.
Preparation method mainly includes the following steps that：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, about 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 60 DEG C, 30 minutes is kept the temperature, is cooled to
Room temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, and via hole diameter is the filter membrane degerming of 0.22mm
Filter, packing；
S6：- 40 DEG C are set in freeze drying box, and pre-freeze 2 hours, vacuum degree transported 20Pa, and -50 DEG C of condenser temperature, distillation 10 is small
When, products temperature transports 35 DEG C, drying 4 hours, until residual moisture content is within 3%.
S7：Tamponade is rolled lid and is made after drying.
Embodiment 2
The injection dextromethorphan hydrobromide, comprises the following components in parts by weight：
Dextromethorphan hydrobromide：5 parts；Sodium chloride：9 parts；Water for injection：1000 parts.
Preparation method mainly includes the following steps that：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, about 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 60 DEG C, 30 minutes is kept the temperature, is cooled to
Room temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, and via hole diameter is the filter membrane degerming of 0.22mm
Filter, packing；
S6：- 40 DEG C are set in freeze drying box, and pre-freeze 2 hours, vacuum degree transported 20Pa, and -50 DEG C of condenser temperature, distillation 10 is small
When, products temperature transports 35 DEG C, drying 4 hours, until residual moisture content is within 3%.
S7：Tamponade is rolled lid and is made after drying.
Embodiment 3
The injection dextromethorphan hydrobromide, comprises the following components in parts by weight：
Dextromethorphan hydrobromide：5 parts；Mannitol：50 parts；Water for injection：1000 parts.
Preparation method mainly includes the following steps that：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, about 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 60 DEG C, 30 minutes is kept the temperature, is cooled to
Room temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, and via hole diameter is the filter membrane degerming of 0.22mm
Filter, packing；
S6：- 40 DEG C are set in freeze drying box, and pre-freeze 2 hours, vacuum degree transported 20Pa, and -50 DEG C of condenser temperature, distillation 10 is small
When, products temperature transports 35 DEG C, drying 4 hours, until residual moisture content is within 3%.
S7：Tamponade is rolled lid and is made after drying.
Embodiment 4
The injection dextromethorphan hydrobromide, comprises the following components in parts by weight：
Dextromethorphan hydrobromide：5 parts；Glucose：50 parts；Water for injection：1000 parts.
Preparation method mainly includes the following steps that：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, about 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 60 DEG C, 30 minutes is kept the temperature, is cooled to
Room temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, and via hole diameter is the filter membrane degerming of 0.22mm
Filter, packing；
S6：- 40 DEG C are set in freeze drying box, and pre-freeze 2 hours, vacuum degree transported 20Pa, and -50 DEG C of condenser temperature, distillation 10 is small
When, products temperature transports 35 DEG C, drying 4 hours, until residual moisture content is within 3%.
S7：Tamponade is rolled lid and is made after drying.
Embodiment 5
The injection dextromethorphan hydrobromide, comprises the following components in parts by weight：
Dextromethorphan hydrobromide：5 parts；Dextran-40：10 parts；Sodium hydrogensulfite：2 parts；Water for injection：2000 parts
Preparation method mainly includes the following steps that：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, about 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 60 DEG C, 30 minutes is kept the temperature, is cooled to
Room temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, and via hole diameter is the filter membrane degerming of 0.22mm
Filter, packing；
S6：- 40 DEG C are set in freeze drying box, and pre-freeze 2 hours, vacuum degree transported 20Pa, and -50 DEG C of condenser temperature, distillation 10 is small
When, products temperature transports 35 DEG C, drying 4 hours, until residual moisture content is within 3%.
S7：Tamponade is rolled lid and is made after drying.
The preparation effect of 1-5 of the embodiment of the present invention shows, the right beauty of injection hydrobromic acid that the embodiment of the present invention 3 is prepared
The skeleton of Sha Fen is most secured and solubility is strong.
Table 1：The preparation effect of the preparation-obtained injection dextromethorphan hydrobromide of embodiment 1-5
As seen from the experiment：The mannitol of sufficient dosage is added in the preparation process of injection dextromethorphan hydrobromide
As excipient, the molding of dextromethorphan hydrobromide is promoted, while also guaranteeing that the secured and solubility of its skeleton is good.
Above the embodiments of the present invention are described in detail, but the present invention is not limited to described embodiments.It is right
For those skilled in the art, in the case where not departing from the principle of the invention and spirit, these embodiments are carried out more
Kind change, modification, replacement and modification, still fall within protection scope of the present invention.
Claims (7)
1. a kind of injection dextromethorphan hydrobromide, it is characterised in that：Its composition includes dextromethorphan hydrobromide, figuration
Agent and water for injection.
2. injection dextromethorphan hydrobromide according to claim 1, it is characterised in that：The excipient be mannitol,
Lactose, low molecule dextrose be intoxicated -40, common salt or glucose one of which.
3. injection dextromethorphan hydrobromide according to claim 1, it is characterised in that：Group including following parts by weight
Point：Dextromethorphan hydrobromide：2-10 parts；Mannitol：10-100 parts；Water for injection：500-1500 parts.
4. injection dextromethorphan hydrobromide according to claim 1, it is characterised in that：Group including following parts by weight
Point：Dextromethorphan hydrobromide：5 parts；Mannitol：50 parts；Water for injection：1000 parts.
5. a kind of method for preparing injection dextromethorphan hydrobromide as described in claim 1, it is characterised in that：Mainly include
Following steps：
S1：The dextromethorphan hydrobromide and mannitol for weighing recipe quantity, are placed in container；
S2：According to parts by weight, 800 parts of water for injection are added, stirring is to being completely dissolved；
S3：According to parts by weight, 5 parts of needle-use activated carbon are added, stirs evenly and is heated to 55-60 DEG C, 30 minutes is kept the temperature, is cooled to room
Temperature；
S4：Initial filter decarburization is carried out with stud；
S5：According to parts by weight, filtrate is settled to 1000 parts with water for injection, through filter membrane aseptic filtration, packing；
S6：It is sent into pre-freeze and drying in freeze drying box；
S7：Tamponade is rolled lid and is made after drying.
6. the method for preparation injection dextromethorphan hydrobromide according to claim 5, it is characterised in that：The preparation side
The step S6 of method carries out aseptic filtration using the filter membrane that aperture is 0.22mm.
7. the method for preparation injection dextromethorphan hydrobromide according to claim 5, it is characterised in that：The preparation side
The step S6 of method, pre-freezing temperature are -40 DEG C, and the pre-freeze time is 2 hours, vacuum degree 20Pa, and condenser temperature is -50 DEG C, distillation
Time is 10 hours, and products temperature is 35 DEG C, and drying time is 4 hours, remains moisture control within 3%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810821148.XA CN108836943A (en) | 2018-07-24 | 2018-07-24 | A kind of injection dextromethorphan hydrobromide and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810821148.XA CN108836943A (en) | 2018-07-24 | 2018-07-24 | A kind of injection dextromethorphan hydrobromide and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108836943A true CN108836943A (en) | 2018-11-20 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810821148.XA Pending CN108836943A (en) | 2018-07-24 | 2018-07-24 | A kind of injection dextromethorphan hydrobromide and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090215810A1 (en) * | 2005-12-13 | 2009-08-27 | Trinity Laboratories, Inc. | Method to Treat Premature Ejaculation in Humans |
| CN103536527A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide injection and preparation method thereof |
| CN107126421A (en) * | 2017-04-28 | 2017-09-05 | 北京茗泽中和药物研究有限公司 | A kind of dextromethorphan chewable tablets |
-
2018
- 2018-07-24 CN CN201810821148.XA patent/CN108836943A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090215810A1 (en) * | 2005-12-13 | 2009-08-27 | Trinity Laboratories, Inc. | Method to Treat Premature Ejaculation in Humans |
| CN103536527A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide injection and preparation method thereof |
| CN107126421A (en) * | 2017-04-28 | 2017-09-05 | 北京茗泽中和药物研究有限公司 | A kind of dextromethorphan chewable tablets |
Non-Patent Citations (1)
| Title |
|---|
| 侯惠民等主编: "《药用辅料应用技术》", 31 July 2002, 中国医药科技出版社 * |
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