CN107126421A - A kind of dextromethorphan chewable tablets - Google Patents
A kind of dextromethorphan chewable tablets Download PDFInfo
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- CN107126421A CN107126421A CN201710295538.3A CN201710295538A CN107126421A CN 107126421 A CN107126421 A CN 107126421A CN 201710295538 A CN201710295538 A CN 201710295538A CN 107126421 A CN107126421 A CN 107126421A
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- dextromethorphan
- chewable tablets
- magnesium stearate
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- 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
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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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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Abstract
A kind of dextromethorphan chewable tablets, it is characterized in that the prescription of the chewable tablets is：It is used as the parts by weight of dextromethorphan hydrobromide 15~30 of active component, phosphatidyl choline, the parts by weight of citric acid 1~2, the parts by weight of lactose 40~50, the parts by weight of hydroxypropyl methyl cellulose 100~150, the parts by weight of PVPP 57, the parts by weight of magnesium stearate 0.5~1,20~30 parts of mannitol, 20 30 parts of sucrose, the weight ratio of the phosphatidyl choline and dextromethorphan hydrobromide is 2.5~3:1.
Description
Technical field
The present invention relates to a kind of dextromethorphan hydrobromide oral formulations.
Background technology
Dextromethorphan hydrobromide (Dextromethorphan Hydrobromid) belongs to the local anaesthetics of amide-type, is maincenter
Property antitussive, act on, but analgesia without codeine and sedation suitable with codeine, without additive, therapeutic dose will not press down
Respiratory center processed and respiratory mucosa secretion.Significantly, adverse reaction rate is low, and clinical practice is extremely for clinical practice antibechic effect
Safety, has the advantages that taking dose is few and antibechic effect is good, is increasingly widely used in antibechic treatment.But normal oral system
Biological half-life of the agent in human body is only 2.3 hours, need within one day administration 3-4 times, and common oral preparation action speed compared with
Slowly, the requirement of quick antibechic can not be met.Therefore provide one kind can quick acting, and can sustained release active ingredient
Dextromethorphan hydrobromide oral formulations turn into urgent problem to be solved in the prior art.
The content of the invention
To solve aforementioned technical problem, the invention provides a kind of dextromethorphan chewable tablets, it is characterized in that described
The prescription of chewable tablets is：It is used as the parts by weight of dextromethorphan hydrobromide 15~30 of active component, phosphatidyl choline, citric acid 1~2
Parts by weight, the parts by weight of lactose 40~50, the parts by weight of hydroxypropyl methyl cellulose 100~150, PVPP (is handed over
Join PVP) 5-7 parts by weight, the parts by weight of magnesium stearate 0.5~1,20~30 parts of mannitol, 20-30 parts of sucrose, the phosphatidyl courage
The weight ratio of alkali and dextromethorphan hydrobromide is 2.5~3:1.
Described a kind of dextromethorphan chewable tablets, it is characterized in that the prescription of the chewable tablets is preferably that hydrobromic acid is right
The parts by weight of dextromethorphan 30, the parts by weight of phosphatidyl choline 75, the parts by weight of citric acid 1~2, the parts by weight of lactose 40~50, hydroxypropyl first
The parts by weight of base cellulose 150, the parts by weight of PVPP 7, the parts by weight of magnesium stearate 0.5~1, mannitol 20~30
Part, 20-30 parts of sucrose.
Described a kind of dextromethorphan chewable tablets, it is characterized in that the dextromethorphan hydrobromide content of the chewable tablets
Specification is 30mg/ pieces.
A kind of dextromethorphan chewable tablets, it is characterized in that preparing in the following manner
1) ethanol solution of dextromethorphan hydrobromide is rapidly injected in the phosphatidyl choline aqueous solution, vacuum after stirring
Revolving to dry,
2) then add appropriate 95% ethanol it is scattered after, add other auxiliary materials except for magnesium stearate, make softwood,
And wet granulation is carried out, dry and magnesium stearate progress tabletting is added after whole grain.
It is many using addition hydroxypropyl methyl fiber in the prior art when making dextromethorphan hydrobromide oral slow-releasing preparation
The mode of plain (HPMC), makes medicine form the dextromethorphan hydrobromide hydrophilic gel based on HPMC, experimental study after oral administration
Show, the release of medicine mainly determines that lactose is as water-soluble filler to medicine by framework material HPMC viscosity and consumption
Release there is also influence.Sustained-release tablet forms gel layer running into digestive juice on its surface first, and the medicine on its surface is to disappearing
Change in liquid and spread, gel layer continues aquation, skeleton is swelled, and thickening for gel layer can delay the release of medicine；Tablet skeleton is same
When there is corrosion, digestive juice infiltrates into the complete corrosion of skeleton to the piece heart, and medicine all discharges.But it is due to carry out antibechic treatment
When need active ingredient quick acting, and sustained release preparation prepare turn into oral disnitegration tablet or chewable tablets when, the drug release of its oral cavity
Performance can not meet needs.Based on drawbacks described above of the prior art, we are found surprisingly that in research and development, using phosphatidyl courage
Alkali to being handled as the dextromethorphan hydrobromide of active component, add after the auxiliary material such as citric acid and lactose, mannitol with
HPMC is made after chewable tablets, the sustained release after can not only realizing orally, and rapid release can be had when carrying out oral cavity chewing
Effect composition reaches the effect of quick antibechic.And the realization of the effect above depends on phosphatidyl choline, citric acid, lactose, sweet dew
The synergy of the auxiliary materials such as alcohol and HPMC, and and if only if when active component is dextromethorphan hydrobromide, obtained chewable tablets can
Produce the effect above.
Embodiment
Dextromethorphan chewable tablets in the embodiment of the present invention, it is characterized in that preparing in the following manner
1) ethanol solution of dextromethorphan hydrobromide is rapidly injected in the phosphatidyl choline aqueous solution, vacuum after stirring
Revolving to dry,
2) then add appropriate 95% ethanol it is scattered after, add other auxiliary materials except for magnesium stearate, make softwood,
And wet granulation is carried out, dry and magnesium stearate progress tabletting is added after whole grain.
The formula of embodiment 1~3 and reference examples see the table below (unit g feeds intake by 1000)
Reference examples 1~3 are added without citric acid, and reference examples 4~9 are added without lactose or mannitol respectively.
Pharmacological Examples 1
Experimental animal every group 6, is divided into 13 groups, experimental group using healthy new zealand white rabbit, 2.0 ± 0.5kg of body weight
1~3 gives the chewable tablets of embodiment 1~3 respectively, and experimental group 4~12 gives the chewable tablets of reference examples 1~9, and control group gives commercially available hydrogen
Bromic acid dextromethorphan chewable tablets (Harbin Kedi Pharmaceutical Co., Ltd, 15mg/ pieces), fasting 12h before medication, in after administration
0.25h, 0.5h, 0.75h, 1.0h, 1.5h, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h take blood in rabbit auricular vein, detect blood medicine
Concentration data simultaneously carries out statistical analysis.Experimental result such as following table (dosage is in terms of dextromethorphan hydrobromide)
Above-mentioned as shown by data, the preparation provided using the present invention, when experimental animal is administered orally, is reachable in 0.25h
To higher blood concentration, illustrate in experimental animal mastication processes can by mucous membrane of mouth to the activity that absorbs the drug into
Point, so as to realize the effect of quick acting, after the completion of medication, peak plasma concentrations are reduced, but high blood concentration is held time
It is longer.Illustrate also play a part of sustained release, and in comparative example, although slow releasing function is also played, but it can not be realized soon
Speed improves the effect of blood concentration.
Claims (4)
1. a kind of dextromethorphan chewable tablets, it is characterized in that the prescription of the chewable tablets is：It is used as the hydrogen bromine of active component
The sour parts by weight of dextromethorphan 15~30, phosphatidyl choline, the parts by weight of citric acid 1~2, the parts by weight of lactose 40~50, hydroxypropyl first
The parts by weight of base cellulose 100~150, PVPP 5-7 parts by weight, the parts by weight of magnesium stearate 0.5~1, sweet dew
20~30 parts of alcohol, 20-30 parts of sucrose, the weight ratio of the phosphatidyl choline and dextromethorphan hydrobromide is 2.5~3:1.
2. a kind of dextromethorphan chewable tablets as claimed in claim 1, it is characterized in that the prescription of the chewable tablets is preferred
For the parts by weight of dextromethorphan hydrobromide 30, the parts by weight of phosphatidyl choline 75, the parts by weight of citric acid 1~2, the weight of lactose 40~50
Part, the parts by weight of hydroxypropyl methyl cellulose 150, the parts by weight of PVPP 7, the parts by weight of magnesium stearate 0.5~1,
20~30 parts of mannitol, 20-30 parts of sucrose.
3. a kind of dextromethorphan chewable tablets as claimed in claim 1, it is characterized in that a kind of described right U.S. of hydrobromic acid
Husky sweet smell chewable tablets, it is characterized in that the dextromethorphan hydrobromide content specification of the chewable tablets is 30mg/ pieces.
4. a kind of dextromethorphan chewable tablets as described in claims 1 to 3, it is characterized in that preparing in the following manner
1) ethanol solution of dextromethorphan hydrobromide is rapidly injected in the phosphatidyl choline aqueous solution, vacuum is rotated after stirring
It is extremely dry,
2) then add appropriate 95% ethanol it is scattered after, add other auxiliary materials except for magnesium stearate, make softwood, go forward side by side
Row wet granulation, dries and magnesium stearate progress tabletting is added after whole grain.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710295538.3A CN107126421A (en) | 2017-04-28 | 2017-04-28 | A kind of dextromethorphan chewable tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710295538.3A CN107126421A (en) | 2017-04-28 | 2017-04-28 | A kind of dextromethorphan chewable tablets |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107126421A true CN107126421A (en) | 2017-09-05 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710295538.3A Pending CN107126421A (en) | 2017-04-28 | 2017-04-28 | A kind of dextromethorphan chewable tablets |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108836943A (en) * | 2018-07-24 | 2018-11-20 | 江苏金丝利药业股份有限公司 | A kind of injection dextromethorphan hydrobromide and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1589789A (en) * | 2003-09-03 | 2005-03-09 | 吕宝光 | Preparation of hydrobromic acid dextro methaphen and beta cyclodeatrin compounding object |
| CN101658500A (en) * | 2008-08-26 | 2010-03-03 | 北京科信必成医药科技发展有限公司 | Dextromethorphan hydrobromide sustained- release tablets and preparation method thereof |
| CN102028222A (en) * | 2009-09-29 | 2011-04-27 | 烟台鸿瑞集团生物科技园有限公司 | Soya bean lecithin chewable tablets |
| CN102258489A (en) * | 2010-05-24 | 2011-11-30 | 重庆医科大学 | Dextromethorphan chewing gum tablets and preparation method thereof |
| CN104490813A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Dextromethorphan hydrobromide composition chewable tablets and preparation method thereof |
-
2017
- 2017-04-28 CN CN201710295538.3A patent/CN107126421A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1589789A (en) * | 2003-09-03 | 2005-03-09 | 吕宝光 | Preparation of hydrobromic acid dextro methaphen and beta cyclodeatrin compounding object |
| CN101658500A (en) * | 2008-08-26 | 2010-03-03 | 北京科信必成医药科技发展有限公司 | Dextromethorphan hydrobromide sustained- release tablets and preparation method thereof |
| CN102028222A (en) * | 2009-09-29 | 2011-04-27 | 烟台鸿瑞集团生物科技园有限公司 | Soya bean lecithin chewable tablets |
| CN102258489A (en) * | 2010-05-24 | 2011-11-30 | 重庆医科大学 | Dextromethorphan chewing gum tablets and preparation method thereof |
| CN104490813A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Dextromethorphan hydrobromide composition chewable tablets and preparation method thereof |
Non-Patent Citations (4)
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| 刘娟等: "新型右美沙芬咀嚼胶给药***的药代动力学研究", 《南方医科大学学报》 * |
| 吴琳华等: "氢溴酸右美沙芬咀嚼片在正常人体内的生物利用度", 《中国药学杂志》 * |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108836943A (en) * | 2018-07-24 | 2018-11-20 | 江苏金丝利药业股份有限公司 | A kind of injection dextromethorphan hydrobromide and preparation method thereof |
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20170905 |
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| RJ01 | Rejection of invention patent application after publication |