CN1546147A - Effervescence tablet for treating children's cough and asthma and its preparation - Google Patents

Abstract

A children's cough relieving effervescent tablet and preparation process, the preparation is prepared from Chinese ephedra, honeysuckle flower, bitter apricot seed, isatic root, gupse, licorice root, and pericarpium trichosanthis through the steps of water grilling, alcohol separating, cold storage, centrifuging, charging Chinese ephedra, extracting concrete, drying and disintegrating, granulation, drying and tabletting.

Description

Infantile asthma effervescent tablet and preparation method thereof

Technical field: the present invention relates to a kind of Chinese medicine, especially relate to infantile asthma effervescent tablet of a kind of child's of treatment tracheitis, cough, upper respiratory tract infection and preparation method thereof.

Background technology: tracheitis, cough, upper respiratory tract infection are usual diseases of childhood, frequently-occurring disease, also be anxious, the serious symptom of department of pediatrics in clinical, at present, the Chinese medicine of treatment children with tracheal inflammation, cough, upper respiratory tract infection is generally oral liquid, because the extraction process of oral liquid is that simple water is carried, spissated method is prepared from, the finished product precipitation is many, and the loss of effective components of medicine is bigger when refining, affects the treatment, transport in addition, carry equal inconvenience, limited clinical practice.

Summary of the invention: in order to solve the problem of above-mentioned existence, it is good to the invention provides a kind of therapeutic effect, taking convenience, steady quality, and transportation, infantile asthma effervescent tablet easy to carry and preparation method thereof.

Concrete technical scheme is as follows: a kind of infantile asthma effervescent tablet and preparation method thereof is characterized in that: made by weight by following raw materials of effective components:

Herba Ephedrae 0.5-1.5 Flos Lonicerae 5-15 Semen Armeniacae Amarum 1-9

Radix Isatidis 5-15 Gypsum Fibrosum 10-20 Radix Glycyrrhizae 1-9

Fructus Trichosanthis 1-9;

Preparation method:

Above seven flavor medicine, Herba Ephedrae add 6 times of amount 80% ethanol, reflux, extract, 3 times, each 2 hours, filter merging filtrate, placement is spent the night, and filters filtrate recycling ethanol and to be concentrated into 60 ℃ of relative densities when surveying be 1.05-1.06, add the hydrochloric acid solution of 4 times of amounts 0.1% of medicinal liquid while hot, stir well, cold preservation is spent the night, filter, filtrate is regulated pH value near neutral with ammonia, and cold preservation is spent the night, filter filtrate for later use; Other gets Gypsum Fibrosum, after decocting with water half an hour, add Flos Lonicerae again, Semen Armeniacae Amarum, Radix Isatidis, Fructus Trichosanthis, Radix Glycyrrhizae decocts each 1 hour 3 times, amount of water is 10 times of medical material amount, filter, collecting decoction, relative density is 1.05-1.06 when being concentrated into 60 ℃ of surveys, high speed centrifugation under 150000rpm, it is 1.10-1.12 that centrifugal liquid continues to be concentrated into 60 ℃ of relative densities when surveying, and adds ethanol and makes and contain the alcohol amount and reach 65%, and placement is spent the night, filter, filtrate recycling ethanol and to be concentrated into 60 ℃ of relative densities when surveying be 1.03-1.05 adds the water of 3 times of amounts of medicinal liquid, stirs evenly, cold preservation is spent the night, high speed centrifugation under 150000rpm, the extracting solution of centrifugal liquid and above-mentioned Herba Ephedrae merges, and relative density is the thick paste of 1.20-1.25 when continuing to be concentrated into 60 ℃ of surveys, drying under reduced pressure is ground into fine powder; Get above-mentioned dried cream powder, add the tartaric acid of equivalent and the sodium bicarbonate of equivalent, and Aspartane 30 restrains, xylitol is an amount of, mixing is with dehydrated alcohol granulation, dry, tabletting, promptly.

The present invention has carried out independent extraction with the monarch drug Herba Ephedrae, all the other still adopt decocting, collecting decoction is concentrated into the relative density of regulation, precipitate with ethanol, cold preservation, centrifugal, centrifugal liquid is concentrated into behind the thick paste water precipitating again, improving final preparation clarity, be condensed into after centrifugal and add Herba Ephedrae behind the thick paste and extract extractum, be ground into fine powder behind the vacuum drying, make granule with auxiliary materials and mixing again, drying, tabletting promptly, effervescent is dissolved in hot water but the present invention both has, but effervescent is dissolved in the advantage of directly taking behind the cold water again, be suitable for child administration, simultaneously again because it is a solid preparation, transportation, easy to carry, steady quality, increased content of effective after the process modification, improved curative effect, it is big to have overcome former preparation loss of effective components, the finished product precipitation is many, preserves, carry the shortcoming of inconvenience.

Epheday intermedia of the present invention mainly contains alkaloids composition and volatile oil compositions such as ephedrine, pseudoephedrine, ephedine, L-N methylephedrine, d-N-methyl pseudoephedrine, L-demethyl ephedrine, d-demethyl pseudoephedrine; In addition, also contain compositions such as flavonoid, organic acid, catechu matter; Wherein to be that the main effective ingredient of Herba Ephedrae has analgesic, antiinflammatory, the antitussive effect of relievining asthma for alkaloids composition such as ephedrine and volatile oil composition; Because of volatile oil content is low, be difficult to propose, so extraction process is many to consider alkaloid extraction; The extracting method that Herba Ephedrae alkaloid is commonly used has sour water lixiviate, sour water percolation, alcohol reflux, decocting to boil etc., is the quality of each extraction process relatively, with above-mentioned four kinds of main methods Herba Ephedrae has been carried out extracting relatively respectively, sees Table 1:

Different Extraction Method is extracted the ephedrine tables of data

Extracting method	Paste-forming rate (%)	Ephedrine hydrochloride content (mg/g Herba Ephedrae)
			The sour water lixiviate	????18.77	????9.40
The sour water percolation	????15.50	????8.22
			Alcohol reflux	????16.83	????10.25
Decocting boils	????19.33	????8.35

As shown in Table 2, the highest with the ethanol refluxing process Determination of Ephedrine Hydrochloride, and paste-forming rate is lower.

Other drug:

Flos Lonicerae: main effective ingredient is organic acids such as chlorogenic acid, and water-soluble, Yi Shui carries.

Semen Armeniacae Amarum: mainly contain compositions such as amygdaloside and enzyme, fatty acid, volatile oil, aminoacid; Wherein amygdaloside is the effective ingredient of antitussive and antiasthmatic, and is soluble in water, and suitable decocting extracts.

Gypsum Fibrosum: main component is a hydrous calcium sulfate, still contains Celiang elementses such as titanium, copper, ferrum, aluminum, silicomanganese in addition, and Organic substance, sulfide etc.; The Gypsum Fibrosum decocting liquid causes that to Typhoid Vaccine fever in rabbit has certain antipyretic effect, and tradition is decocted first with Gypsum Fibrosum during clinical practice, reenters other medicines with frying in shallow oil, so should the decocting extraction and be decocted first.

Radix Glycyrrhizae: mainly contain triterpene saponin constituents such as glycyrrhizic acid, enoxolone, and compositions such as flavonoid, alkaloids, polysaccharide, how water-soluble, suitable decocting extracts.

Radix Isatidis: mainly contain indigo, indirubin (but amount is seldom), and some water soluble ingredients.Its decocting liquid has bacteriostasis to staphylococcus aureus, can suppress its proliferation function of the viral infection and the criminal of having system again; So suitable decocting extracts.

Fructus Trichosanthis: mainly contain the triterpene saponin constituents, water-soluble, Yi Shui carries.

In sum, above-mentioned 6 flavor medicines should mix decocting and extract, and wherein Gypsum Fibrosum should be decocted first half an hour.

The preparation stability experiment:

It is 75% calorstat that the effervescent tablet of two aluminum laminated films packing is placed 40 ℃, relative humidity, places 1 month, takes out, and measures appearance character, effervescent time and pH value variation before and after its test, the results are shown in Table 2:

Table 1: comparing result before and after the accelerated test

Sample	Appearance character	The effervescent time	PH value
				Before the test	Brown tablet	5 minutes 15 seconds	4.1
After the test	Brown tablet	5 minutes 08 second	4.0

The result shows: this medicine has no significant change at aspects such as appearance color, physical behavior, effervescent time and pH values before and after the accelerated test, illustrates that this medicine is basicly stable, and moulding process is reasonable.

Acute toxicity test:

With 3.8 crude drugs/ml concentration, 0.4ml/10g volume gastric infusion, 2 times on the one. accumulated dose is 304g crude drug/kg, is equivalent to 238 times of clinical consumption. observed 7 days, mice all survives, and does not see the overt toxicity reaction.

Long term toxicity test:

Rat is irritated stomach respectively and gives infantile asthma effervescent tablet 94.35,47.175,23.5875g/kg (be equivalent to human dosage 74,27,18.5 times), and continuous 90 days, to observe 14 days after the drug withdrawal, rat all survives, and does not see the overt toxicity reaction.

Antivirus test: the big or middle dosage group of infantile asthma effervescent tablet and oral liquid causes that to the influenza virus infecting mouse pneumonia all has the obvious suppression effect, and the lung exponential quantity obviously reduces.

Bacteriostasis: infantile asthma effervescent tablet and oral liquid all have in various degree inhibitory action to six kinds of antibacterial 19 strain bacterial strains such as examination streptococcus pneumoniae.The heavy dose of group of effervescent tablet can make the golden Portugal of infection bacterium mortality of mice obviously reduce, and the effervescent tablet bacteriostasis is better than oral liquid.

Antitussive action: infantile asthma effervescence tablet and oral liquid all can reduce strong aqua ammonia, citric acid causes mice and guinea pig cough's reaction times and prolongs cough latent period, and prompting has antitussive effect.

Phlegm-dispelling functions: infantile asthma effervescence tablet and oral liquid all can increase phenol red output in the mice trachea, and prompting has certain phlegm-dispelling functions.

Antiinflammatory action: infantile asthma effervescence tablet and oral liquid all can suppress HAC and cause the effect that capillary permeability increases, and prompting has antiinflammatory action.

Refrigeration function: infantile asthma effervescence tablet and oral liquid have tangible refrigeration function to yeast pyrogenicity rat.

The present invention has summed up kinds of Diseases and curative effect and following relation was arranged between the course of treatment through clinical practice, sees Table 3, table 4:

Kinds of Diseases and therapeutic effect relationship

Disease	Case load	Recovery from illness	Remarkable result	Invalid	Effective percentage
						Upper respiratory tract infection	100	?80	?20	?0	?100％
Acute bronchitis	80	?50	?26	?4	?95％
						Pneumonia	50	?25	?23	?2	?96％
Cough	50	?27	?21	?2	?96％

Kinds of Diseases and the course of treatment relation

Disease	Case load	Healing time
						One week	Two weeks	Three weeks	All around
		Upper respiratory tract infection	100	?20	?50					?30
Acute bronchitis	80					?5	?20	?40	?11
		Pneumonia	50		?20					?10	?18
Cough	50						?20	?20	?8

Usage and consumption:

Two years old with interior one time 1; Three to four years old one time 1.5; Five to seven years old one time 2; 3-4 time on the one, every 1.5g; Be two weeks 1 course of treatment.

Curative effect judging standard:

Recovery from illness: do not have heating, do not have cough, no expectorant, the symptom of relievining asthma;

Produce effects: heating, cough, expectorant, asthma obviously alleviate.

Invalid: as to continue the symptom that heating arranged, cough, have expectorant, asthma.

The specific embodiment:

Embodiment 1: a kind of infantile asthma effervescent tablet and preparation method thereof, make by following raw materials of effective components: (by the gram number)

Herba Ephedrae 62.5g Flos Lonicerae 625g Semen Armeniacae Amarum 312.5g

Radix Isatidis 625g Gypsum Fibrosum 937.5g Radix Glycyrrhizae 312.5g

Fructus Trichosanthis 312.5g;

Preparation method:

Above seven flavor medicine, Herba Ephedrae add 6 times of amount 80% ethanol, reflux, extract, 3 times, each 2 hours, filter merging filtrate, placement is spent the night, and filters filtrate recycling ethanol and to be concentrated into 60 ℃ of relative densities when surveying be 1.05-1.06, add the hydrochloric acid solution of 4 times of amounts 0.1% of medicinal liquid while hot, stir well, cold preservation is spent the night, filter, filtrate is regulated pH value near neutral with ammonia, and cold preservation is spent the night, filter filtrate for later use; Other gets Gypsum Fibrosum, after decocting with water half an hour, add Flos Lonicerae again, Semen Armeniacae Amarum, Radix Isatidis, Fructus Trichosanthis, Radix Glycyrrhizae decocts each 1 hour 3 times, amount of water is 10 times of medical material amount, filter, collecting decoction, relative density is 1.05-1.06 when being concentrated into 60 ℃ of surveys, high speed centrifugation under 150000rpm, it is 1.10-1.12 that centrifugal liquid continues to be concentrated into 60 ℃ of relative densities when surveying, and adds ethanol and makes and contain the alcohol amount and reach 65%, and placement is spent the night, filter, filtrate recycling ethanol and to be concentrated into 60 ℃ of relative densities when surveying be 1.03-1.05 adds the water of 3 times of amounts of medicinal liquid, stirs evenly, cold preservation is spent the night, high speed centrifugation under 150000rpm, the extracting solution of centrifugal liquid and above-mentioned Herba Ephedrae merges, and relative density is the thick paste of 1.20-1.25 when continuing to be concentrated into 60 ℃ of surveys, drying under reduced pressure is ground into fine powder; Get above-mentioned dried cream powder, add the tartaric acid of equivalent and the sodium bicarbonate of equivalent, and Aspartane 30 restrains, xylitol is an amount of, mixing is with dehydrated alcohol granulation, dry, tabletting, promptly.Make 1000 of effervescent tablets altogether.

Embodiment 2: a kind of infantile asthma effervescent tablet and preparation method thereof, make by following raw materials of effective components: (by the gram number)

Herba Ephedrae 62.5g Flos Lonicerae 500g Semen Armeniacae Amarum 250g

Radix Isatidis 562.5g Gypsum Fibrosum 875g Radix Glycyrrhizae 250g

Fructus Trichosanthis 250g;

Preparation method is with embodiment 1.

Embodiment 3: a kind of infantile asthma effervescent tablet and preparation method thereof, make by following raw materials of effective components: (by the gram number)

Herba Ephedrae 62.5g Flos Lonicerae 438g Semen Armeniacae Amarum 188g

Radix Isatidis 438g Gypsum Fibrosum 750g Radix Glycyrrhizae 188g

Fructus Trichosanthis 188g;

Preparation method is with embodiment 1.

Embodiment 4: a kind of infantile asthma effervescent tablet and preparation method thereof, make by following raw materials of effective components: (by the gram number)

Herba Ephedrae 50g Flos Lonicerae 450g Semen Armeniacae Amarum 200g

Radix Isatidis 450g Gypsum Fibrosum 750g Radix Glycyrrhizae 200g

Fructus Trichosanthis 200g;

Preparation method is with embodiment 1.

Embodiment 5: a kind of infantile asthma effervescent tablet and preparation method thereof, make by following raw materials of effective components: (by the gram number)

Herba Ephedrae 40g Flos Lonicerae 320g Semen Armeniacae Amarum 120g

Radix Isatidis 360g Gypsum Fibrosum 400g Radix Glycyrrhizae 120g

Fructus Trichosanthis 120g;

Preparation method is with embodiment 1.

Claims (1)

1, a kind of infantile asthma effervescent tablet is characterized in that: made by weight by following raw materials of effective components:

Herba Ephedrae 0.5-1.5 Flos Lonicerae 5-15 Semen Armeniacae Amarum 1-9

Radix Isatidis 5-15 Gypsum Fibrosum 10-20 Radix Glycyrrhizae 1-9

Fructus Trichosanthis 1-9;

Preparation method:

Above seven flavor medicine, Herba Ephedrae add 6 times of amount 80% ethanol, reflux, extract, 3 times, each 2 hours, filter merging filtrate, placement is spent the night, and filters filtrate recycling ethanol and to be concentrated into 60 ℃ of relative densities when surveying be 1.05-1.06, add the hydrochloric acid solution of 4 times of amounts 0.1% of medicinal liquid while hot, stir well, cold preservation is spent the night, filter, filtrate is regulated pH value near neutral with ammonia, and cold preservation is spent the night, filter filtrate for later use; Other gets Gypsum Fibrosum, after decocting with water half an hour, add Flos Lonicerae again, Semen Armeniacae Amarum, Radix Isatidis, Fructus Trichosanthis, Radix Glycyrrhizae decocts each 1 hour 3 times, amount of water is 10 times of medical material amount, filter, collecting decoction, relative density is 1.05-1.06 when being concentrated into 60 ℃ of surveys, high speed centrifugation under 150000rpm, it is 1.10-1.12 that centrifugal liquid continues to be concentrated into 60 ℃ of relative densities when surveying, and adds ethanol and makes and contain the alcohol amount and reach 65%, and placement is spent the night, filter, filtrate recycling ethanol and to be concentrated into 60 ℃ of relative densities when surveying be 1.03-1.05 adds the water of 3 times of amounts of medicinal liquid, stirs evenly, cold preservation is spent the night, high speed centrifugation under 150000rpm, the extracting solution of centrifugal liquid and above-mentioned Herba Ephedrae merges, and relative density is the thick paste of 1.20-1.25 when continuing to be concentrated into 60 ℃ of surveys, drying under reduced pressure is ground into fine powder; Get above-mentioned dried cream powder, add the tartaric acid of equivalent and the sodium bicarbonate of equivalent, and Aspartane 30 restrains, xylitol is an amount of, mixing is with dehydrated alcohol granulation, dry, tabletting, promptly.