CN1102567A - Group of drugs with antitussive and expectorant functions - Google Patents
Group of drugs with antitussive and expectorant functions Download PDFInfo
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- CN1102567A CN1102567A CN94110578A CN94110578A CN1102567A CN 1102567 A CN1102567 A CN 1102567A CN 94110578 A CN94110578 A CN 94110578A CN 94110578 A CN94110578 A CN 94110578A CN 1102567 A CN1102567 A CN 1102567A
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- antitussive
- medicine
- chlorphenamine
- expectorant
- cough
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Abstract
The medicine series for stopping cough and dispelling phlegm comprises two drugs. One is made up with chlorpheniramine, probanthine and spiropent for common diseases of respiratory tract and another one for quick treating cold and supervene tracheitis is prepared from chlorpheniramine, probanthine, acetamidophenol, caffeine and artificial bezoar.
Description
The present invention is one group of medicine with antitussive and expectorant using under the different state of an illness.Cloperastine is pounced in invention 1, and to breathe heavily sheet be to be used for the treatment of that to breathe be commonly encountered diseases: chronic tracheitis, bronchial asthma etc. have cough-relieving, expectorant and antiasthmatic effect.Invent 2 quick-acting cold-cough relieving tablets and be the concurrent bronchitis of treatment flu, have the common sympton that had both cured cold, simultaneously again can cough-relieving, expectorant.
Existing antitussive one class is to suppress coughing centre (for example codeine, carbetapentane citrate etc.), when only being suitable for dry cough without phlegm, then should forbid when expectorant is arranged; Another kind of is expelling phlegm for arresting cough medicine (for example ammonium chloride, bromhexine hydrochloride etc.), and its mechanism of action mainly is that the secretion of bronchus body of gland is increased, and makes amount of expectoration increase easy noise made in coughing or vomiting.
The present invention 1 pounces on cloperastine and breathes heavily and both do not had traditional central antitussive in the tablet recipe, does not also have the expelling phlegm for arresting cough medicine.We think the cough reason that above-mentioned disease causes, be mostly since expectorant to due to bronchial stimulation and the factors such as bronchospasm and allergy.Therefore use the anticholinergic agent propantheline and reduce glandular secretion, remove bronchospasm, add chlorphenamine antiallergic (antiinflammatory in case of necessity) again.Prove tangible antitussive and expectorant functions is arranged by experiment, amount of expectoration is reduced, and be easy to noise made in coughing or vomiting and go out with propantheline and chlorphenamine two medicines treatment chronic tracheitis.We once treated chronic simple type tracheitis 500 examples with this two medicine, average medication 10 days, effective percentage 85.4% wherein accounts for 67.8%(and sees Chinese Academy of Medical Sciences's medical information research for details and compile the medical research communication more than the produce effects, 40 pages of 1975 the 5th phases).We treat chronic tracheitis 1750 examples with propantheline, chlorphenamine and sulfamethoxine, and through 1-9 course of therapy, effective percentage reaches 87.9%-99.6%.Be chose as Shandong Province's medical and health scientific and technological achievement (seeing the 53rd page in compilation of the same name for details) in 1978, and prize-winning in Shandong Province's first medical science conference.Test through clinical control, two medicines share cough-relieving, disappear and cough effect significantly, but if respectively single with then curative effect is not good enough, both have the difference (P＜0.01 is seen 12 pages of 290 pages of CHINESE JOURNAL OF INTERNAL MEDICINE 1976 the 5th phases and barefoot doctor's magazine 1977 the 12nd phases for details) of highly significant.Pharmacological evaluation is single does not have obvious antitussive effect (Shandong medicine 1979 o. 11th 12 pages) with chlorphenamine, and chlorphenamine adds propantheline then remarkable antitussive effect (Chinese tuberculosis and respiratory illness magazine, 170 pages of the 3rd phases of nineteen eighty-three).Its mechanism may with relaxing smooth muscle, expansion bronchus, reduce the stimulation of expectorant and cut off certain link of cough opposite arc relevant.But it is relatively poor that above-mentioned two medicines share antiasthmatic effect, so not good enough to asthmatic tracheitis and bronchial asthma curative effect.Existing anti-asthmatic clenbuterol (belongs to β
2Receptor agonist) have good antiasthmatic effect (chief editor such as Lou Fangcen, the physician's prescription handbook, Beijing, Guangming Daily publishing house, 1988 the 1st edition 306 pages).Knowing again that such medicine and anticholinergic agent share may increase its antiasthmatic effect (Bian Rulian: anti-asthmatic progress, practical internal medicine journal, 230 pages of the 5th phases of nineteen eighty-two).The present invention 1 purpose be design a kind of can cough-relieving, expectorant has the medicine of remarkable antiasthmatic effect again.Pounce on cloperastine and breathe heavily sheet and form, obviously can achieve the above object by chlorphenamine, propantheline and clenbuterol three medicines.
The present invention 2 is a kind of medicines for the treatment of the concurrent tracheitis of flu.Most of no antitussive in the medicine (resembling quick-acting cold sheet etc.) of treatment flu at present, the present invention 2 purpose provides a kind of flu of both having treated, and can treat the medicine that it occurs together cough, spits simultaneously again.It is remarkable that known existing quick-acting cold sheet is eliminated flu common sympton effect, knows again and wherein contain chlorphenamine.Prove that according to above-mentioned observation chlorphenamine adds propantheline promptly cough-relieving, expectorant functions,, can reach above-mentioned purpose so in quick-acting cold sheet (or capsule) prescription, add propantheline again.The present invention's 2 quick-acting cold-cough relieving tablets promptly have above-mentioned effect.These two kinds of medicines below are described in detail in detail:
Pounce on cloperastine and breathe heavily sheet (Pu Ke Ping Chuan Pian)
This product contains the 93.0%-107.0% that chlorphenamine (C16 H19 CIN2.C4 H4 O4) should be labelled amount; The total amount that contains bromination Propantheline (C23 H30 Brn) and chlorphenamine (C16 H19 CIN2.C4 H4 O4) should be the 90.0%-110.0% of labelled amount; Hydrochloric clenbuterol (C12 H18 C12 N20.HCI) should be the 90.0%-110.0% of labelled amount.
(prescription) chlorphenamine 2g
Probanthine 7.5g
Clenbuterol hydrochloride 20mg
Right amount of auxiliary materials
Make 1000 altogether
[technology] will write out a prescription Chinese medicine and auxiliary materials and mixing granulated, and beats sheet, wraps yellow sugar-coat, promptly.
[character] this product is yellow coated tablet, removes sugar-coat, bitter in the mouth.
[discriminating] 1, get 20 of this product, remove sugar-coat, porphyrize adds chloroform 20ml, and jolting makes chlorphenamine, probanthine dissolving, filters, and filtrate is put evaporate to dryness in the water-bath, and residue is according to following method test:
(1) get residue a little, add structure rafter vinegar acid anhydride test 1ml, put in the water-bath and heat, be i.e. displaing amaranth.
(2) get residue a little, add dilute hydrochloric acid 1ml, drip the potassium permanganate test, redness promptly disappears.
(3) get residue a little, add sulphuric acid 5ml, promptly show glassy yellow or orange-yellow and micro-green fluorescence.
2, get 20 of this product, porphyrize adds water 10ml, and jolting makes the clenbuterol hydrochloride dissolving, and static several minutes, filter, filtrate is shone following method test:
(1) gets filtrate 1ml, add 20% sulphuric acid system permanganic acid first saturated solution 1ml, behind the jolting number minute, it is an amount of to add the oxalic acid test solution, makes the solution clarification, add 2, the perchloric acid solution of 4-dinitrophenylhydrazine (is got 2,4 dinitrophenyl hydrazine 1.2g, is added 30% perchloric acid solution 50ml and make dissolving, promptly) 10, being heated to boils promptly separates out yellow mercury oxide.
(2) get filtrate 1ml, add dilute hydrochloric acid 1ml, 10% sodium nitrite solution 1ml drips alkaline β-tea phenol experimental liquid number droplet, promptly produces orange-yellow precipitation.
3, will add water by 1 gained residual residue and make dissolving, filter; And, all show the identification (43 pages of two appendix of 90 years versions of Chinese Pharmacopoeia) of bromide by 2 gained filtrates.
[assay] chlorphenamine is got 20 of this product, remove sugar-coat, the accurate title, decide, porphyrize, precision weighs up in right amount (being equivalent to chlorphenamine 4mg approximately), put in the separatory funnel, add sulphuric acid liquid (0.05mol) 20ml, jolting 5 minutes, 20ml adds diethyl ether, layering is placed in jolting (attention prevents emulsifying), divides and gets acid solution, filter is gone in another separatory funnel, the ether layer extracts 2 times with sulphuric acid liquid (0.05mol/l), each 5ml, and acid solution filters, incorporate in the above-mentioned filtrate, filter washs with sulphuric acid liquid (0.05mol/l), and washing liquid is incorporated in the filtrate, and hydro-oxidation sodium test solution makes proper alkalize, repeated hydrogenation sodium oxide 2ml, with ether extraction 2 times, each 25ml, ether liquid divides 3 washings with same water 10ml, ether liquid merges the back and extracts 3 times (20 with sulphuric acid liquid (0.25mol/l), 20,5ml), merge acid solution, put in the 50ml measuring bottle, add sulphuric acid liquid (0.25mol/l) and be diluted to scale, shake up, according to spectrophotography (24 pages of two appendix of 90 years versions of Chinese Pharmacopoeia), measure trap at the wavelength place of 265 ± 1nm, press the absorptance (E of C16 H19 CIN2.C4 H4 O4
1% 1cm) be 217 to calculate promptly.
Chlorphenamine and probanthine total amount; get 20 of this product; porphyrize; add in the chloroform dislocation 100ml measuring bottle; warm and jolting 15 minutes; put coldly add chloroform and are diluted to scale, shake up; filter with dry paper; discard filtrate just, precision is measured subsequent filtrate 50ml, puts in the conical flask; after the evaporation; about 30 minutes of 80 ℃ of dryings, add glacial acetic acid 20ml, with mercuric acetate test solution 10ml dissolving back (can warmly dissolving in case of necessity); add 1 of crystal violet indicator solution; titrating result proofreaies and correct with blank assay with perchloric acid liquid (0.1mol/l), that is, the perchloric acid liquid (0.1mol/l) of every 1ml is equivalent to C16 H19 CIN2.C4 H4 O4 and the C23 H36 Brn of 35.24mg.
The preparation precision of clenbuterol hydrochloride reference substance solution takes by weighing at 105 ℃ of clenbuterol hydrochloride reference substances that are dried to constant weight an amount of, adds hydrochloric acid solution (0.4mol/l) and makes the solution that contains 16ug among every 1ml, shakes up, promptly.
30 of this product are got in the preparation of need testing solution, the accurate title, decide, porphyrize, and precision weighs up in right amount (being equivalent to clenbuterol hydrochloride 400ug approximately), put in the 250ml iodine flask, precision adds hydrochloric acid solution (0.4mol/l) 25ml, and jolting 30 minutes makes the clenbuterol hydrochloride dissolving, filter, discard filtrate just, collect subsequent filtrate, promptly.
The algoscopy precision is measured reference substance solution and each 5ml of need testing solution, put respectively in the 25ml measuring bottle, respectively add hydrochloric acid solution (0.4mol/l) 10ml and 0.1% sodium nitrite solution 1ml, jolting 3 minutes, add 0.5% sulfamic acid ammonium salt solution 1ml, jolting 5 minutes, to there not being nitrogen gas generation, adding hydrochloride naphthodiamide solution 0.5ml(again and get hydrochloric acid naphthylenediamine 0.1g, add 50% ethanol 100ml and make dissolving promptly) shake up after, (0.4mol/l) is diluted to scale with hydrochloric acid solution, shake up,, measure trap respectively at the wavelength place of 500nm according to spectra photometric method (Chinese Pharmacopoeia 90 years version two ones attached 24 pages), calculate, promptly.
[effect and purposes] medicine for the treatment of cough and asthma, and can reduce amount of expectoration, be used for bronchial asthma, chronic tracheitis and emphysema etc.
[usage and consumption] is oral, a 1-2 sheet, and 3 times on the one, the child is cut down according to the circumstance.
[attention] suffers from glaucoma, hyperthyroidism, arrhythmia, hypertension, prostate hyperplasia and lactication phase women forbidding.
[storage] shading, airtight preservation.
Quick-acting cold-cough relieving tablet (Su Xiao Gan Mo zhi Ke Pian)
This product contains the 95.0%-105.0% that acetaminophen (C8 H9 NO2) should be labelled amount; Contain the 93.0%-107% that chlorphenamine (C16 H19 CIN2.C4 H4 O4) should be labelled amount; The total amount that contains bromination Propantheline (C23 H30 Brn) and chlorphenamine (C16 H19 CIN2.C4 H4 O4) should be the 90.0%-110.0% of labelled amount.
[prescription]
Acetaminophen 250g
Chlorphenamine 2g
Probanthine 5g
Caffeine 15g
Artificial Calculus Bovis 10g
Right amount of auxiliary materials
Make 1000 altogether
[technology] will write out a prescription Chinese medicine and auxiliary materials and mixing granulated, and beats sheet, coating, promptly.
[character] this product is yellow coated tablet, removes sugar-coat, bitter in the mouth.
[discriminating] 1, get 1 of this product, porphyrize adds chloroform 20ml, and jolting makes acetaminophen and chlorphenamine, and the probanthine dissolving filters, and filtrate is as need testing solution; Other gets acetaminophen and chlorphenamine, and probanthine, chlorination are copied into and contained acetaminophen 10mg among every 1ml approximately, and the solution of chlorphenamine 0.1mg, probanthine 0.25mg filters, in contrast solution in case of necessity.According to thin layer chromatography (28 pages of two appendix of Chinese Pharmacopoeia nineteen ninety version) test, draw above-mentioned two kinds of each 5ul of solution, put respectively on same silica gel g thin-layer plate, be developing solvent with methanol-liquor ammoniae fortis (20: 0.15), after the expansion, dry, use iodo steam displaing color.Inspect, need testing solution show 2 speckles the position should with the contrast liquid speckle identical.
2, get and differentiate 1 remaining need testing solution down, put evaporate to dryness in the water-bath, residue adds hydrochloric acid 1ml makes dissolving, adds potassium chlorate 0.1g, puts evaporate to dryness in the water-bath again, and residue is met ammonia and promptly shown purple, repeated hydrogenation sodium oxide test solution number droplet, and purple promptly disappears.
3, get 10 of this product, remove sugar-coat, porphyrize, add chloroform 50ml, jolting filters, filtrate is put evaporate to dryness in the water-bath, and residue adds 10% acetum 2ml, stirs, filter, get filtrate 1ml, put in the test tube, furfural solution (1 → 100) 1ml that adds new system, sulfuric acid solution (get sulphuric acid 50ml and water 65ml is mixed and made into) 13ml heats in 70 ℃ of water-baths, and solution shows purple.
[inspection] should be in 5 minutes the disintegrate except that disintegration, and other should meet every regulation relevant under the tablet item (3 pages of two appendix of Chinese Pharmacopoeia nineteen ninety version).
[assay] acetaminophen is got 10 of this product, removes sugar-coat, and accurate the title decides, porphyrize, precision weigh up in right amount (being equivalent to acetaminophen 0.3g approximately), put in the conical flask, add dilute hydrochloric acid 50ml, reflux 1 hour is cooled to room temperature, add water 50ml and potassium bromide 3g, about 2/3 place under the liquid level is inserted at the tip of burette, with sodium nitrite liquid (0.1mol/l) titration rapidly, with dripping with stirring, during to nearly terminal point, the tip of burette is proposed liquid level, with low amounts of water the tip is washed, washing liquid is incorporated in the solution, continue slowly titration, the thin Glass rod of reuse dip in get solution a little, streak and scribble on the white plaque that contains zinc potassium iodide and starch written instructions liquid, promptly show blue streak, stop titration, after 5 minutes, dip in again and get a little and streak once, as still showing blue streak, be terminal point, promptly.The sodium nitrite liquid (0.1mol/l) of every 1ml is equivalent to the C8 H9 NO2 of 15.2mg.
Chlorphenamine (breathing heavily the sheet measurement method) with pouncing on cloperastine
The total quantitative determination of chlorphenamine and probanthine (breathing heavily the sheet measurement method) with pouncing on cloperastine
[effect and purposes] antipyretic-antalgic, antitussive and expectorant, the headache, pantalgia, the rhinorrhea that are used to catch a cold and cause, throat pain is coughed, is spat etc.
[usage and consumption] is oral, one time 1,3 times on the one, the child is cut down according to the circumstance.
[attention] has glaucoma, prostate hyperplasia and lactication phase forbidding.
[storage] is airtight, preserves at shady and cool dry place.
The present invention 1 pounces on cloperastine and breathes heavily sheet treatment chronic tracheitis, and common respiratory disease such as bronchial asthma is when being particularly suitable for expectorant is arranged, because existing central antitussive forbidding when expectorant is arranged.Existing expelling phlegm for arresting cough medicine (ammonium chloride, bromhexine hydrochloride etc.) is amount of expectoration is increased and not reduce.We once did control experiment, with chlorphenamine, propantheline treatment chronic tracheitis, than with ammonium chloride, carbetapentane citrate and peace bitter edible plant alkali effective (P＜0.01), saw CHINESE JOURNAL OF INTERNAL MEDICINE for details, 290 pages of 1976 the 5th phases.Certainly chlorphenamine, propantheline are bound to better if add clenbuterol (promptly pounce on cloperastine and breathe heavily sheet) curative effect again.Also begin to use anticholinergic agent as anti-asthmatic in recent ten years abroad, but do not see that as yet propantheline and chlorphenamine share the enhanced report of antitussive and expectorant functions.Existing medicine is pounced on its antiasthmatic effect of Keling piece, and particularly the quick-acting asthma-relieving effect is poor.The present invention 1 pounces on cloperastine and breathes heavily sheet and can say so to the improvement of this medicine.Used clenbuterol antiasthmatic effect is good, but its antitussive and expectorant functions is poor, treats chronic simple type tracheitis weak curative effect (Guangrao County health bureau tracheitis study on prevention group; The 67 routine brief summaries of Clenbuterol Hydrochloride treatment chronic tracheitis, inside information).From above-mentioned situation, breathe heavily sheet by the cloperastine of pouncing on that propantheline, chlorphenamine and clenbuterol are formed, maximize favourable factors and minimize unfavourable ones, propantheline and chlorphenamine share antitussive and expectorant functions are strengthened, propantheline and clenbuterol share and antiasthmatic effect are strengthened, and have remedied the deficiency that each medicine uses respectively separately.
The present invention's 2 quick-acting cold-cough relieving tablets are compared with existing treatment coldrex commonly used, and seeing from composition has increased the anticholinergic agent propantheline.From therapeutic efficiency, except treatment flu common sympton, antitussive and expectorant functions is arranged still.Be particularly suitable for treating the patient that flu is spat with cough simultaneously.Because of great majority in the medicine of present this type of treatment flu do not contain antitussive, when minority contains central antitussive and is only applicable to dry cough without phlegm.
Claims (3)
1, the present invention is one group of medicine with antitussive and expectorant, is used for the treatment that common respiratory disease and flu and cough are spat.Its composition had not both had traditional antitussive, did not have expectorant yet.It is characterized in that being formed by chlorphenamine and propantheline.
2, a kind of medicine as claimed in claim 1 adds and makes the mutual enhanced clenbuterol of antiasthmatic effect, promptly forms to pounce on cloperastine and breathe heavily sheet.
3, a kind of medicine as claimed in claim 1 adds acetaminophen again, caffeine, and the artificial Calculus Bovis promptly forms quick-acting cold-cough relieving tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN94110578A CN1043302C (en) | 1994-05-03 | 1994-05-03 | Group of drugs with antitussive and expectorant functions |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN94110578A CN1043302C (en) | 1994-05-03 | 1994-05-03 | Group of drugs with antitussive and expectorant functions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1102567A true CN1102567A (en) | 1995-05-17 |
| CN1043302C CN1043302C (en) | 1999-05-12 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN94110578A Expired - Fee Related CN1043302C (en) | 1994-05-03 | 1994-05-03 | Group of drugs with antitussive and expectorant functions |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1043302C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1314399C (en) * | 2004-11-26 | 2007-05-09 | 贵阳高新瑞得科技开发有限公司 | Child metho kahuangmin effervescent granules and its making method |
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1994
- 1994-05-03 CN CN94110578A patent/CN1043302C/en not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN1043302C (en) | 1999-05-12 |
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Granted publication date: 19990512 Termination date: 20090603 |