CN101264080A - Pharmaceutical composition containing dexchlorpheniramine and preparation thereof - Google Patents
Pharmaceutical composition containing dexchlorpheniramine and preparation thereof Download PDFInfo
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- CN101264080A CN101264080A CNA2008101050854A CN200810105085A CN101264080A CN 101264080 A CN101264080 A CN 101264080A CN A2008101050854 A CNA2008101050854 A CN A2008101050854A CN 200810105085 A CN200810105085 A CN 200810105085A CN 101264080 A CN101264080 A CN 101264080A
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- dexchlorpheniramine
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Abstract
The invention discloses a combination containing r-chlorpheniramine, which is formed by the r-chlorpheniramine and the medicine salt and the other or a plurality of active ingredients or pharmaceutical carriers selected from non-steroidal anti-inflammatory drug, ephedrine alkaloids, coffeine, dextromethorphan hydrobromide, carbetapentane citrate, glyceryl guaiacolate, bromhexine hydrochloride, artificial cow-bezoar, amantadine hydrochloride, aminophylline and zinc gluconate. The orally taken preparation developed from the combination comprises granule, tablet, capsule, dispersible tablet, chewable tablet, effervescent tablet, orally disintegrating tablet, buccal tablet, dry suspension and certain solid formulation.
Description
Technical field
The present invention relates to a kind of composition and method of making the same that contains dexchlorpheniramine, belong to medical technical field.
Background technology
Flu is a kind of acute infection rhinitis, is commonly called as " cold ".Being caused by Respirovirus, is main Causative virus with coronavirus and rhinovirus wherein.Virus is discharged from respiratory secretions and is propagated, when Abwehrkraft des Koepers descends, as suffer from cold, malnutrition, overtired, cigarette spills excessively, the chronic disease of systemic disease and nose itself influences respiratory smooth etc., brings out infection easily.Flu outbreak back secondary bacterial infection.Intranasal has dry sensation and gargalesthesia, sneeze, general malaise or low grade fever is arranged during the flu onset, nasal obstruction, cough, hyposmia, a large amount of clear water nasal mucus of stream, nasal mucosa hyperemia, edema is gradually arranged later on, a large amount of clear water samples or purulent secretion etc. are arranged.Because the present specially good effect means of still having the treatment flu add that it has the spontaneous recovery trend, so the purpose of common cold treatment is anti symptom treatment, mitigation symptoms, the shortening course of disease, promotion early recovery.Therapeutic Method comprises non-drug therapy and Drug therapy two aspects.Drug therapy mainly comprises processing, symptomatic treatment and the antiviral to heating.
Along with the going deep into of study of pharmacy work, shown the stereoselective difference of drug enantiomer since nearly 20 years, made its affinity different and cause the very big difference of pharmacological action with each receptor.The curative effect of DL-(+-) suntomycinum only is half of D (-) chloromycetin as the well-known; The pharmaceutically active of Propranolol L-isomer is bigger 100 times than D-isomer." chirality " technology of utilization, people can reject the composition of inoperative in the medicine or toxic side effect effectively, produce the homochiral medicine with single directive construction, thereby make ingredient purer, and curative effect is faster when the treatment disease, the course of treatment is shorter.Therefore, the research of chiral drug has become one of new side of international new drug research at present.
Chlorphenamine is histamine H 1 receptor's antagonist, this product can be to the telangiectasis due to the antianaphylaxis (histamine), reduce the permeability of blood capillary, panting due to the alleviation bronchial smooth muscle shrinks, this product antihistamine effect is more lasting, also have tangible central inhibitory action, can increase the effect of anesthetics, analgesic, hypnotic and local anaesthetics.This product is mainly at liver metabolism.This product is applicable to skin allergy: urticaria, eczema, dermatitis, drug eruption, skin pruritus, neurodermatitis, insect bite disease, solar dermatitis.Also can be used for allergic rhinitis, medicine and food anaphylaxis.The d-isomer of chlorphenamine, the mechanism of action, the same chlorphenamine of purposes.But stress efficacy is strong one times, and consumption is little, few side effects.
Summary of the invention
What the present invention relates to is a kind of dextral chlorphenamine optical isomer.And this optical isomer then exists with the form of maleate usually.
Though because the d-isomer chlorphenamine has identical mechanism of action with the raceme chlorphenamine, its usefulness is then stronger.Therefore, adopting dexchlorpheniramine and other medicine to carry out prescription when forming new compound preparation, can obtain better synergism.
These prescriptions are with dexchlorpheniramine and pharmaceutical salts thereof and another kind of or multiplely are selected from the compositions that NSAID (non-steroidal anti-inflammatory drug), ephedrine, caffeine, dextromethorphan hydrobromide, pentoxyverine citrate, guaifenesin, Bisolvon, artificial Calculus Bovis, amantadine hydrochloride, aminophylline, zinc gluconate etc. be active component and pharmaceutical carrier formation.
The compositions that forms is preferably: maleic acid dexchlorpheniramine+acetaminophen; maleic acid dexchlorpheniramine+pseudoephedrine hydrochloride; maleic acid dexchlorpheniramine+acetaminophen+pseudoephedrine hydrochloride; maleic acid dexchlorpheniramine+acetaminophen+pseudoephedrine hydrochloride+dextromethorphan hydrobromide; maleic acid dexchlorpheniramine+amantadine+acetaminophen+artificial Calculus Bovis+caffeine; maleic acid dexchlorpheniramine+chlorphenamine+zinc gluconate; maleic acid dexchlorpheniramine+guaifenesin+pentoxyverine citrate.
During composing prescription preparation described above was described, ephedrine also comprised its optical isomer, derivant and their pharmaceutical salts thereof.
The preferred acetaminophen of NSAID (non-steroidal anti-inflammatory drug), aminophenazone, benorylate, aspirin, diclofenac sodium etc.
In the composing prescription preparation of these and other compound formation, the unit pharmaceutical dosage of unit dexchlorpheniramine and pharmaceutical salts thereof is 0.5-8mg, preferred 2mg.
This chlorphenamine chemical compound with specificity optically-active carries out prescription when using with other medicines, add the acceptable material of some necessary pharmacy after, it can be prepared into pharmaceutical preparation.These pharmaceutical preparatioies are preferably oral formulations.
These oral formulations comprise any alternative rational solid dosage formss such as granule, tablet, capsule, dispersible tablet, chewable tablet, effervescent tablet, oral cavity disintegration tablet, buccal tablet, dried suspendible.
These compositionss are used for the treatment of various types of flu
The specific embodiment
By following example compositions of the present invention is further specified, but be not limited in this embodiment.
Embodiment 1, maleic acid dexchlorpheniramine+Actamin Extra
Preparation method:
Acetaminophen, microcrystalline Cellulose are crossed 80 mesh sieves respectively, mix homogeneously, standby; It is an amount of that other gets 50% alcoholic solution, add the maleic acid dexchlorpheniramine and make dissolving, with this solution as binding agent system soft material, 24 mesh sieves are granulated, 50 ℃ of dryings, 20 mesh sieve granulate, add micropowder silica gel, CMS-Na, adopt suitable punch die compressed tablets behind the mix homogeneously, promptly.If carry out coating for above-mentioned tablet, then obtain coated tablet, can be Film coated tablets, enteric coatel tablets etc.
Embodiment 2, maleic acid dexchlorpheniramine+acetaminophen+pseudoephedrine hydrochloride+dextromethorphan chewable tablets
Prescription:
Preparation method:
Acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide are all crossed 80 mesh sieves, and behind the sorbitol mix homogeneously, it is an amount of to get 50% alcoholic solution, add the maleic acid dexchlorpheniramine and make it dissolving, as binding agent system soft material, 24 mesh sieves are granulated, 50 ℃ of dryings, 20 mesh sieve granulate.Add Fructus Citri sinensis powdered flavor, micropowder silica gel mix homogeneously, tabletting, promptly.
Embodiment 3, maleic acid dexchlorpheniramine+pseudoephedrine hydrochloride dispersible tablet
Preparation method:
Pseudoephedrine hydrochloride, microcrystalline Cellulose are crossed 80 mesh sieves respectively, adopt equivalent incremental method mix homogeneously, standby; It is an amount of to get 50% alcoholic solution, and add the maleic acid dexchlorpheniramine and make it dissolving, as binding agent system soft material, the granulation of 16 mesh sieves, drying, 20 mesh sieve granulate add other mix homogeneously such as correctives, sweeting agent, fluidizer, disintegrating agent, tabletting, promptly.
Embodiment 4, maleic acid dexchlorpheniramine+amantadine+acetaminophen+artificial Calculus Bovis+caffeine granule
Prescription:
Preparation method:
Amantadine, acetaminophen, artificial Calculus Bovis, caffeine, xylitol are crossed 80 mesh sieves, mix homogeneously respectively; It is an amount of to get 50% alcoholic solution, adds the maleic acid dexchlorpheniramine and makes dissolving, and as binding agent system soft material, 16 mesh sieves are granulated with this solution, 50 ℃ of dryings, and 16 mesh sieve granulate pack behind the adding micropowder silica gel mix homogeneously, promptly
Embodiment 5, maleic acid dexchlorpheniramine+ibuprofen+zinc gluconate capsules
Prescription:
Preparation method:
Zinc gluconate, ibuprofen are all crossed 80 mesh sieves, behind the starch mix homogeneously, standby; It is an amount of that other gets 50% alcoholic solution, adds the maleic acid dexchlorpheniramine and make dissolving, and as binding agent system soft material, 24 mesh sieves are granulated with this solution, 50 ℃ of dryings, and 20 mesh sieve granulate add magnesium stearate, mix homogeneously, packing, promptly.
Used capsule shells can be conventional capsule, also can be enteric coated capsule.
Embodiment 6, maleic acid dexchlorpheniramine+guaifenesin+pentoxyverine citrate oral cavity disintegration tablet
Preparation method:
With mannitol, more create sweet wooden carbolic oil ether, pentoxyverine citrate, microcrystalline Cellulose and cross 60 mesh sieves, mix homogeneously, standby; It is an amount of that other gets 50% alcoholic solution, adds the maleic acid dexchlorpheniramine and make dissolving, and as binding agent system soft material, 24 mesh sieves are granulated with this solution, 50 ℃ of dryings, and 20 mesh sieve granulate, with stevioside, flavoring orange essence, L-HPC mix homogeneously, tabletting gets final product.
Embodiment 7, maleic acid dexchlorpheniramine+acetaminophen drop pill
Preparation method:
Maleic acid dexchlorpheniramine and acetaminophen are crossed 80 mesh sieves, standby; In addition PEG6000, Ploxamer 188 are mixed post-heating and make fusion to about 60 ℃; Maleic acid dexchlorpheniramine and acetaminophen added in the fused solution stirring, move in the dropping funnel, be incubated about 60 ℃, regulate the water dropper size, serves as the cooling phase with-25 ℃ dimethicones, the system of dripping, and ball is washed, selects in filtration, gets final product.
Embodiment 8, maleic acid dexchlorpheniramine+pseudoephedrine hydrochloride dry suspension
Preparation method:
Earlier pseudoephedrine hydrochloride, sucrose, sorbitol etc. are all crossed 80 mesh sieves, and mix homogeneously, the maleic acid dexchlorpheniramine with anhydrous alcohol solution after, as binding agent system soft material, 40 mesh sieves are granulated, drying, adopt 50 mesh sieve granulate, add HPMC, silicon dioxide and mix homogeneously in the gained granula subtilis, the packing of every bag 1 gram gets final product.
Embodiment 9, clinical trial:
1, object of study:
Flu patient 140 examples.Person's standard: 1. 18～65 years old age, male or female; 2. have symptoms (wherein at least 2 kinds of symptoms) such as heating body temperature (37.8～39 ℃), headache, pharyngalgia, nasal obstruction, watery nasal discharge, sneeze, clinical diagnosis is the common cold person; 3. the above-mentioned symptom time occurring is no more than 48 hours persons; 4. leukocyte≤12 * 10./ L; 5. experimenter's pregnancy tests feminine gender (women of child-bearing age); 6. merge severe renal, liver, heart, endocrine, digestion, nerve or psychosis person, suffers from chronic respiratory system diseases acute attack stage person, except thyroid disease, diabetes, coronary heart disease, cardiovascular disease, prostate hyperplasia, hypertension, the intraocular pressure person of increasing.
2, Therapeutic Method:
140 examples are divided into matched group and A, B, C, D, E, F treatment group, every group 20 example at random.Matched group is taken the Paracetamol And Chlorphenamine And Pseudoephedrine sheet, and each 1, every day 3 times, 3～5 days courses of treatment.The treatment group is all taken and is once taken a unit dose, and 3 times on the one, 3～5 days courses of treatment.Have 136 example flu patients and finish clinical research, 118 examples are organized in treatment, matched group 18 examples.
3, efficacy assessment standard:
With reference to " new Chinese medicine clinical research guideline ", quantize rank scores according to the importance of each symptom, see Table 1.Except that the listed standards of grading of table 1, body temperature＜37.1 ℃ are 0 minute, and 37.1～37.9 ℃ is 2 minutes, and 38～38.5 ℃ is 4 minutes, and body temperature＞38.5 ℃ are 6 minutes.Carry out efficacy evaluation with symptom total mark variation before and after the treatment.Recovery from illness: treat 5 days normal with interior temperature recovery, symptom total mark decline 〉=95%.Produce effects: treat 5 days normal with interior temperature recovery, the symptom total mark descends 70～95%.Progressive: as treat and reduced symptom total mark decline 30～70% than before with interior body temperature in 5 days.Invalid: treat and do not reduce with interior body temperature or raise in 5 days, the symptom total mark descends＜30%.
Table 1 is according to symptom rank scores standard
4, result
The clinical efficacy situation is compared with matched group, and each treatment group curative effect and adverse reaction rate comparing difference have statistical significance (P＜0.05), see Table 2
Table 2 treatment group and matched group clinical efficacy and untoward reaction situation analysis
Claims (9)
1. compositions that contains dexchlorpheniramine; it is characterized in that, be with dexchlorpheniramine and pharmaceutical salts thereof and another kind of or multiplely be selected from the compositions that NSAID (non-steroidal anti-inflammatory drug), ephedrine, caffeine, dextromethorphan hydrobromide, pentoxyverine citrate, guaifenesin, Bisolvon, artificial Calculus Bovis, amantadine hydrochloride, aminophylline, zinc gluconate etc. be active component and pharmaceutical carrier formation.
2. the described compositions of claim 1 is characterized in that, the preferred maleate of the pharmaceutical salts of dexchlorpheniramine.
3. the described compositions of claim 1 is characterized in that, the preferred acetaminophen of NSAID (non-steroidal anti-inflammatory drug), aminophenazone, benorylate, aspirin, diclofenac sodium etc.
4. the described compositions of claim 1 is characterized in that, ephedrine also comprises its optical isomer, derivant and their pharmaceutical salts thereof.
5. the described compositions of claim 1 is characterized in that, the unit pharmaceutical dosage of dexchlorpheniramine and pharmaceutical salts thereof is 0.2-10mg, preferred 2mg.
6. the described compositions of claim 1; it is characterized in that; its preferred composition has, maleic acid dexchlorpheniramine+acetaminophen (A); maleic acid dexchlorpheniramine+pseudoephedrine hydrochloride (B); maleic acid dexchlorpheniramine+acetaminophen+pseudoephedrine hydrochloride (C); maleic acid dexchlorpheniramine+acetaminophen+pseudoephedrine hydrochloride+dextromethorphan hydrobromide (D); maleic acid dexchlorpheniramine+amantadine+acetaminophen+artificial Calculus Bovis+caffeine (E); maleic acid dexchlorpheniramine+chlorphenamine+zinc gluconate (F); maleic acid dexchlorpheniramine+guaifenesin+pentoxyverine citrate (G).
7. the described compositions of claim 1 is characterized in that, can be made into oral formulations.
8. the described compositions of claim 1 is characterized in that, oral formulations comprises any solid dosage formss such as granule, tablet, capsule, dispersible tablet, chewable tablet, effervescent tablet, oral cavity disintegration tablet, buccal tablet, dried suspendible.
9. the described compositions of claim 1 is used for the treatment of various types of flu and alleviates its symptom.
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2008101050854A CN101264080A (en) | 2008-04-25 | 2008-04-25 | Pharmaceutical composition containing dexchlorpheniramine and preparation thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2008101050854A CN101264080A (en) | 2008-04-25 | 2008-04-25 | Pharmaceutical composition containing dexchlorpheniramine and preparation thereof |
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| CN101264080A true CN101264080A (en) | 2008-09-17 |
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| CNA2008101050854A Pending CN101264080A (en) | 2008-04-25 | 2008-04-25 | Pharmaceutical composition containing dexchlorpheniramine and preparation thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103212079A (en) * | 2013-04-26 | 2013-07-24 | 陆媛 | Oral medical composition for preventing and/or treating cold and application thereof |
| CN104224765A (en) * | 2014-09-03 | 2014-12-24 | 石家庄开发区博欣医药科技开发有限公司 | Robitussin oral solution composition |
| CN104306376A (en) * | 2014-09-30 | 2015-01-28 | 地奥集团成都药业股份有限公司 | Paracetamol, aminophenazone, caffeine and chlorphenamine maleate tablet and preparation method thereof |
| CN104338133A (en) * | 2013-07-24 | 2015-02-11 | 陆媛 | Chewing medicine composition for preventing and treating mouth, nose and throat upper respiratory infecting and application thereof |
| CN107252426A (en) * | 2017-07-25 | 2017-10-17 | 东莞云森生物医药科技有限公司 | Application of the dexchlorpheniramine in anti-motion sickness field |
| CN109464363A (en) * | 2018-11-30 | 2019-03-15 | 江苏贝塔仕生物科技有限公司 | A kind of formula of novel face washing milk |
-
2008
- 2008-04-25 CN CNA2008101050854A patent/CN101264080A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103212079A (en) * | 2013-04-26 | 2013-07-24 | 陆媛 | Oral medical composition for preventing and/or treating cold and application thereof |
| CN104338133A (en) * | 2013-07-24 | 2015-02-11 | 陆媛 | Chewing medicine composition for preventing and treating mouth, nose and throat upper respiratory infecting and application thereof |
| CN104224765A (en) * | 2014-09-03 | 2014-12-24 | 石家庄开发区博欣医药科技开发有限公司 | Robitussin oral solution composition |
| CN104306376A (en) * | 2014-09-30 | 2015-01-28 | 地奥集团成都药业股份有限公司 | Paracetamol, aminophenazone, caffeine and chlorphenamine maleate tablet and preparation method thereof |
| CN107252426A (en) * | 2017-07-25 | 2017-10-17 | 东莞云森生物医药科技有限公司 | Application of the dexchlorpheniramine in anti-motion sickness field |
| CN109464363A (en) * | 2018-11-30 | 2019-03-15 | 江苏贝塔仕生物科技有限公司 | A kind of formula of novel face washing milk |
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Open date: 20080917 |