CN103006656A - Antitussive and expectorant compound chemical drug - Google Patents
Antitussive and expectorant compound chemical drug Download PDFInfo
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- CN103006656A CN103006656A CN2011102867614A CN201110286761A CN103006656A CN 103006656 A CN103006656 A CN 103006656A CN 2011102867614 A CN2011102867614 A CN 2011102867614A CN 201110286761 A CN201110286761 A CN 201110286761A CN 103006656 A CN103006656 A CN 103006656A
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- carbocisteine
- dimemorfan
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- relieving cough
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Abstract
The invention provides an antitussive and expectorant compound chemical drug, and especially relates to a drug composed of dimemorfan and carbocisteine which are effective components, as well as pharmaceutically acceptable accessories, and a preparation technology. The dimemorfan used in the invention is a non-narcotic central antitussive drug; and compared with central antitussive drugs present on the market, the dimemorfan is equivalent in antitussive effects but low in adverse reaction. Compared with commercially available compound antitussive and expectorant drugs, the compound chemical drug provided by the invention has advantages of relatively good efficacies and low adverse reaction rate, and has quite good social and economic benefits.
Description
Invention field
The invention belongs to chemical medicine field, relate to a kind of compound chemical medicine of relieving cough and expelling phlegm, relate in particular to the compound chemical medicine take dimemorfan and carbocisteine as active ingredient.
Background technology
Because densely populated, smoking population is more and the factor such as environmental pollution, the sickness rate of respiratory system disease and case fatality rate are all high in recent years, data according to U.S.'s statistics yearbook, in all causes of the death are sorted out, with the cause of the death ranking of diseases concerned with respiratory (not comprising tumor) the 10th the 4th (chronic obstructive pulmonary disease) and the 8th (pneumonia, influenza and upper respiratory tract infection thereof) that rises to 1991 from 1970, and the sickness rate of China's respiratory system disease all accounts for first of the various diseases at any age group.This problem causes people's attention day by day, and the exploitation of therefore treating the medicine (be called for short and breathe medicine) of respiratory system disease also becomes the important research and development field of drug research.
Cough, to cough up phlegm be the common symptom of respiratory system disease clinically, play is coughed too frequently, not only increase patient's misery, impact is had a rest and sleep, increase physical demands, even the development of promotion disease, produce other complication, such as pneumonia, chronic pharyngitis, chronic bronchitis, bronchiectasis, pulmonary abscess and cavernous pulmonary tuberculosis etc.Also need suitably to use antisussive and expectorant agent, with relieving cough this moment except the treatment of suiting the remedy to the case for respiratory system disease.Using cough medicine is relief of symptoms, and basic is will be for the etiological treatment of cough.
Most cough is that the medium of excessive release is caused during by diseases such as inflammatory mediator such as tracheitis, asthma, pneumonia and lung tumors; So also need to use expectorant for the state of an illness.
At present mostly antisussive and expectorant agent commonly used is the compound chemical medicine take central antitussive codeine or dextromethorphan hydrobromide and expectorant guaifenesin as active ingredient.The dextromethorphan effect is similar to codeine or stronger, and in June, 2005, U.S. FDA issue bulletin points out that the improper use of dextromethorphan may cause death or other negative effects, such as cerebral lesion, lose consciousness and arrhythmia etc.
Dimemorfan phosphate is the non-addiction sexual centre of a kind of chirality town cough medicine, and three more than ten years of going on the market have no the report of any serious adverse reaction, and determined curative effect is safe and reliable.Selectivity is good, antitussive effect is strong because dimemorfan has, on almost not impact of cental system, without side effect such as drowsiness, respiration inhibition, dependencies, cardiovascular and respiratory system are not produced the advantages such as any obvious effect, still to select in the present invention dimemorfan be cough medicine in the compound preparation.Carbocisteine is the sputum diluent, makes that glandular secretion increases in trachea, the bronchus after oral, and sputum is thinning, thereby makes sputum be easy to expectoration.So dimemorfan and the carbocisteine group of effective components as compound preparation is combined, concerning the patient of respiratory system infection, both played the effect of relieving cough and expelling phlegm, the while less adverse effect, safety is higher, so the present invention will bring certain Gospel to the patient, have certain social meaning.
Summary of the invention
Purpose of the present invention aims to provide a kind of compound chemical medicine of relieving cough and expelling phlegm.
The objective of the invention is to realize by following manner:
Effective medicinal component of compound chemical medicine of the present invention is cough medicine dimemorfan and expectorant carbocisteine.Both are formulated by following weight ratio: 200～300 parts of 5～15 parts of dimemorfans and carbocisteine.
More preferably, described active ingredient dimemorfan and carbocisteine also can be formulated by following weight ratio: 150～350 parts of 1～20 part of dimemorfan and carbocisteine.
More preferably, described active ingredient dimemorfan and carbocisteine also can be formulated by following weight ratio: 230～280 parts of 8～12 parts of dimemorfans and carbocisteine.
Described active ingredient dimemorfan and carbocisteine are best by following weight ratio preparation: 250 parts of 10 parts of dimemorfans and carbocisteine.
Compound chemical medicine of the present invention be with by effective medicinal component dimemorfan of certain weight proportion and carbocisteine by the preparation means of suitable pharmaceutical preparation and rapid release that the acceptable any adjuvant of medicine is made, slow release or common pharmaceutical preparation.
The pharmaceutical preparation that the acceptable any adjuvant of active ingredient of the present invention and medicine is made can be the above oral formulations of any pharmaceutics.
Described oral formulations can be tablet, capsule or oral liquid etc.
Tablet of the present invention is to be prepared from by following weight proportion: take by weighing dimemorfan 10g, carbocisteine 250g, an amount of carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate and PVP K30.Weighed PVP K30 is mixed with 10% solution, other weighed supplementary materials are pulverized respectively, are sieved, then first with sodium lauryl sulphate and carboxymethyl starch sodium mix homogeneously, after adding again dimemorfan and carbocisteine mix homogeneously, PVP K30 solution with 10% is made suitable soft material, granulates, and adds carboxymethyl starch sodium, magnesium stearate mixing again, tabletting namely gets 1000 in tablet of the present invention.
Relieving cough and expelling phlegm compound medicine of the present invention, oral daily dose are dimemorfan 15～200mg and carbocisteine 150～800mg, 1～3 time on the one.
In order to verify the safety and effectiveness of compound chemical medicine of the present invention, 23 smelting Affiliated Hospital have carried out relevant pharmacodynamic study test to the inventor in the Hunan Province, and particular content is as follows:
One, test medicine:
1, medicine group of the present invention is totally three groups, be respectively: every of medicinal tablet A(of the present invention contains dimemorfan 5mg, carbocisteine 300mg), every of medicinal tablet B(of the present invention contains dimemorfan 10mg, carbocisteine 250mg), every of medicinal tablet C(of the present invention contains dimemorfan 20mg, carbocisteine 150mg), control drug: the commercially available U.S. sheet of healing.
Two, test method:
1, case standard: have 4 groups of the outpatient service of the cough symptom that acute upper respiratory tract infection, acute tracheobronchitis, community acquired pneumonia and acute episode of chronic bronchitis cause or inpatients.
2, administrated method: to the patient carry out multicenter, at random, the clinical experimental study of Double-blind double-dummy, masculine parallel comparison.400 patients are divided into three groups for the treatment of groups and one group of comfort group, 100 every group at random.Press the method medication of Double-blind double-dummy masculine parallel comparison, three groups for the treatment of groups are taken respectively medicine A of the present invention, B and C, and another comfort group is taken the control drug U.S. sheet of healing.Each group is oral 3 times of every day, each 2 (comprising the simulation sheet), is 6 days the course for the treatment of.
3, drug combination: look the state of an illness and can merge use antibiotics and antipyretic, but should not add with other cough-relievings, calmness, Claritin.
4, observation index: general data such as blood pressure, pulse frequency, body temperature, breathing etc.; The cough symptom; Breast is saturating; Hematuria is conventional; Hepatic and renal function; The untoward reaction record; Electrocardiogram.
Annotate: to occurring unusual indices in the treatment, should finish to check again in rear 7 days in the course for the treatment of.If persistent anomaly is followed up a case by regular visits to till normal.
5, therapeutic evaluation:
A, cough degree standards of grading: 0 minute: without coughing 1 minute (slightly): be interrupted cough, do not affect orthobiosis and work.2 minutes (moderate): between slight and severe cough.3 minutes (severe): round the clock cough is frequent, affects work and sleep.
B, curative effect judging standard: clinic control: symptom complete obiteration; Produce effects: the cough symptom changed into 1 minute by 3 minutes; Take a turn for the better: the cough symptom changed into 2 minutes by 3 minutes or changed into 1 minute by 2 minutes; Invalid: the cough symptom is without taking a turn for the better or increasing the weight of.
6, result of the test:
The Comparison of therapeutic table:
Above result shows that the cough for the treatment of group and matched group Drug therapy all is effectively, but that curative effect of medication of the present invention contrasts medicine is better.Two medicines all have no significant effect hematuria routine, hepatic and renal function, thyroid function, blood pressure, heart rate and electrocardiogram in addition, adverse reaction rate is lower, sweating due to debility, dizziness, drowsiness, anorexia, xerostomia etc. are wherein arranged, untoward reaction 14 examples occur in treatment group of the present invention three groups altogether, it is adverse reaction rate 4.7%, U.S. sheet group generation untoward reaction 19 examples that heal, namely adverse reaction rate 19%.This shows that drug safety of the present invention is relatively high.
The specific embodiment
Embodiment 1: slow releasing tablet of the present invention
Take by weighing dimemorfan 15g, carbocisteine 200g is an amount of, be prepared into by the following method slow releasing tablet: it is an amount of to take by weighing acroleic acid resin, dextrin, HPMC and magnesium stearate, acroleic acid resin is ground, add 75% appropriate amount of ethanol, with its dissolving, slowly add in the mixture of dimemorfan, carbocisteine, dextrin and HPMC of weighing and mixing, add again the HPMC slurry made from 75% ethanol after grinding well, make soft material, sieve, granulate adds the magnesium stearate mixing again, tabletting, 1000 of preparation cost invention slow releasing tablet.
Embodiment 2: oral liquid of the present invention
Take by weighing dimemorfan 12g, carbocisteine 230g, be prepared into by the following method oral liquid: take by weighing or measure an amount of adjuvant stevioside, xylitol, citric acid and benzyl alcohol sodium, with supplementary material pulverize respectively, sieving is placed in the 800ml purified water, mechanical agitation is dissolved it fully, add purified water to 1000ml, filter, namely get oral liquid 1000ml of the present invention.
Embodiment 3: pellt capsule of the present invention
Take by weighing dimemorfan, carbocisteine is an amount of, is prepared into by the following method pellet capsule:
Take by weighing an amount of starch, dextrin, Icing Sugar, ethyl cellulose, PVP K30, polyvinylpyrrolidone and diethyl phthalate.Weighed starch, dextrin and Icing Sugar are placed coating pan, make wetting agent with Diluted Alcohol, the general ball of molding when ball core circle arrives to a certain degree, takes out, in 50～55 ℃ of bakings 2 hours, and the ball core of screening 20～25 order sizes, for subsequent use.Get an amount of ball core, squirt the ball wicking surface with the Diluted Alcohol liquid of 5% PVP K30, add the mixed powder of a small amount of dimemorfan and carbocisteine (weight ratio is 1:25), make medicated powder stick at the ball wicking surface, 50～55 ℃ were dried by the fire 2 hours, filtered out the pastille micropill of 20～25 order sizes, for subsequent use.It is an amount of to get ethyl cellulose, polyvinylpyrrolidone and diethyl phthalate, uses 95% dissolve with ethanol, and mixing is made ethyl cellulose concentration and is about 2% coating solution, and is for subsequent use.A certain amount of pastille micropill is placed coating pan, carry out spray coating with coating solution, in 50～55 ℃ of bakings 2 hours.Products therefrom is filled into medicinal gelatin capsule, makes every capsules contain dimemorfan 10g, carbocisteine 250g, namely gets 1000 of pellt capsules of the present invention.
Embodiment 4, tablet of the present invention
Take by weighing dimemorfan 20g, carbocisteine 150g, be prepared into by the following method tablet: take by weighing an amount of protein sugar, carboxymethyl starch sodium, microcrystalline Cellulose, magnesium stearate.Weighed supplementary material is pulverized respectively, sieved, first with protein sugar and carboxymethyl starch sodium mix homogeneously, after adding again dimemorfan and carbocisteine mix homogeneously, alcohol granulation with 70%, about 2 hours of 35～40 ℃ of bakings, granulate added microcrystalline Cellulose, magnesium stearate mixing again, tabletting namely gets 1000 in tablet of the present invention.
Embodiment 5, tablet of the present invention
Take by weighing dimemorfan 15g, carbocisteine 200g, be prepared into by the following method tablet: take by weighing an amount of carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate and PVP K30.Weighed PVP K30 is mixed with 10% solution, other weighed supplementary materials are pulverized respectively, are sieved, then first with sodium lauryl sulphate and carboxymethyl starch sodium mix homogeneously, after adding again dimemorfan and carbocisteine mix homogeneously, PVP K30 solution with 10% is made suitable soft material, granulates, and adds carboxymethyl starch sodium, magnesium stearate mixing again, tabletting namely gets 1000 in tablet of the present invention.
Embodiment 6, granule of the present invention
Take by weighing dimemorfan 15g, carbocisteine 200g, be prepared into by the following method granule: take by weighing an amount of anhydrous calcium phosphate, microcrystalline Cellulose, sucrose, arabic gum, gelatin, titanium dioxide and magnesium stearate, to be ground into fine powder after weighed dimemorfan and carbocisteine and the weighed auxiliary materials and mixing, make wetting agent soft material processed with 70% ethanol, cross 18 mesh sieves, granulate, 60 ℃ of forced air drying 30min cross 14 mesh sieve granulate, in 60 ℃ of oven dry, packing namely gets granule 1000 bags of the present invention again.
Embodiment 7, syrup of the present invention
Take by weighing dimemorfan 5g, carbocisteine 350g, be prepared into by the following method syrup: take by weighing the refining white sugar of an amount of nothing, P-hydroxy benzenes methyl, propyl p-hydroxybenzoate, propylene glycol and citric acid, castor sugar is added in the distilled water that 100ml boils, add again the weighed dimemorfan that is ground into fine powder and carbocisteine and other auxiliary materials and mixing things, stirring and dissolving, filtered while hot adds distilled water again to 1000ml, namely gets syrup 1000ml of the present invention.
Embodiment 8, tablet of the present invention
Take by weighing dimemorfan 10g, carbocisteine 250g, be prepared into by the following method tablet: take by weighing an amount of carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate and PVP K30.Weighed PVP K30 is mixed with 10% solution, other weighed supplementary materials are pulverized respectively, are sieved, then first with sodium lauryl sulphate and carboxymethyl starch sodium mix homogeneously, after adding again dimemorfan and carbocisteine mix homogeneously, PVP K30 solution with 10% is made suitable soft material, granulates, and adds carboxymethyl starch sodium, magnesium stearate mixing again, tabletting namely gets 1000 in tablet of the present invention.
Claims (10)
1. the compound chemical medicine of a relieving cough and expelling phlegm, it is characterized in that described medicine by take dimemorfan and carbocisteine as active ingredient and the acceptable adjuvant of medicine form.
2. the chemicals of a kind of relieving cough and expelling phlegm according to claim 1 is characterized in that described active ingredient dimemorfan and carbocisteine are formulated by following weight ratio: 150～350 parts of 1～20 part of dimemorfan and carbocisteine.
3. the compound chemical medicine of a kind of relieving cough and expelling phlegm according to claim 1 is characterized in that described active ingredient dimemorfan and carbocisteine are formulated by following weight ratio: 200～300 parts of 5～15 parts of dimemorfans and carbocisteine.
4. the compound chemical medicine of a kind of relieving cough and expelling phlegm according to claim 1 is characterized in that described active ingredient dimemorfan and carbocisteine are formulated by following weight ratio: 230～280 parts of 8～12 parts of dimemorfans and carbocisteine.
5. the compound chemical medicine of a kind of relieving cough and expelling phlegm according to claim 1 is characterized in that described active ingredient dimemorfan and carbocisteine are formulated by following weight ratio: 250 parts of 10 parts of dimemorfans and carbocisteine.
6. the compound chemical medicine of each described a kind of relieving cough and expelling phlegm is rapid release, slow release or the common drug preparation of being made by described active ingredient and the acceptable any adjuvant of medicine according to claim 1-5.
7. the compound chemical medicine of each described a kind of relieving cough and expelling phlegm according to claim 1-5, described pharmaceutical preparation is oral formulations.
8. the compound chemical medicine of each described a kind of relieving cough and expelling phlegm according to claim 1-5, described oral formulations is tablet, capsule, oral liquid.
9. the compound chemical medicine of a kind of relieving cough and expelling phlegm according to claim 9 is characterized in that described tablet is that 10 parts of effective ingredient with 250 parts of carbocisteine of dimemorfan form with corresponding adjuvant by weight ratio.
10. tablet according to claim 9 is characterized in that being prepared from by following component: take by weighing dimemorfan 10g, carbocisteine 250g, an amount of carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate and PVP K30; Weighed PVP K30 is mixed with 10% solution, other weighed supplementary materials are pulverized respectively, are sieved, then first with sodium lauryl sulphate and carboxymethyl starch sodium mix homogeneously, after adding again dimemorfan and carbocisteine mix homogeneously, PVP K30 solution with 10% is made suitable soft material, granulates, and adds carboxymethyl starch sodium, magnesium stearate mixing again, tabletting namely gets 1000 in tablet of the present invention.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011102867614A CN103006656A (en) | 2011-09-26 | 2011-09-26 | Antitussive and expectorant compound chemical drug |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011102867614A CN103006656A (en) | 2011-09-26 | 2011-09-26 | Antitussive and expectorant compound chemical drug |
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| CN103006656A true CN103006656A (en) | 2013-04-03 |
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| CN2011102867614A Pending CN103006656A (en) | 2011-09-26 | 2011-09-26 | Antitussive and expectorant compound chemical drug |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106109396A (en) * | 2016-07-28 | 2016-11-16 | 北京万全德众医药生物技术有限公司 | A kind of carbocisteine syrup and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1523984A (en) * | 2001-05-25 | 2004-08-25 | ������ҩ��ʽ���� | Drug preparations |
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- 2011-09-26 CN CN2011102867614A patent/CN103006656A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1523984A (en) * | 2001-05-25 | 2004-08-25 | ������ҩ��ʽ���� | Drug preparations |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106109396A (en) * | 2016-07-28 | 2016-11-16 | 北京万全德众医药生物技术有限公司 | A kind of carbocisteine syrup and preparation method thereof |
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Address after: 410005, Hunan, Changsha province Furong Road, No. 368 BOBO world city CTA wealth center, 24 floor Applicant after: HUNAN JIUDIAN PHARMACEUTICAL CO., LTD. Address before: 410005, Hunan, Changsha province Furong Road, No. 368 BOBO world city CTA wealth center, 24 floor Applicant before: Hunan Jiudian Pharmaceutical Co., Ltd. |
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Application publication date: 20130403 |